Chemical: Drug
gefitinib

PharmGKB contains no prescribing info for this . Contact us to report known genotype-based dosing guidelines, or if you are interested in developing guidelines.


Annotated Labels

  1. FDA Label for gefitinib and EGFR
  2. EMA Label for gefitinib and CYP2D6,CYP3A4,EGFR
  3. PMDA Label for gefitinib and CYP2D6,EGFR
  4. HCSC Label for gefitinib and EGFR

last updated 10/25/2013

1. FDA Label for gefitinib and EGFR

Genetic testing required

Summary

The FDA-approved drug label for gefinitib states that it is indicated for first-line treatment of patients with metastatic non-small cell lung cancer (NSCLC) whose tumors have epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 (L858R) substitution mutations as detected by an FDA-approved test. The label also notes the potential clinical importance of considering CYP2D6 phenotype, though CYP2D6 testing is not mentioned.

There's more of this label. Read more.


last updated 10/25/2013

2. EMA Label for gefitinib and CYP2D6,CYP3A4,EGFR

Genetic testing required

Summary

The EMA European Public Assessment Report (EPAR) contains biomarker information regarding the indication of gefitinib (Iressa) in patients with tumors that have activating EGFR mutations, due to its mechanism of action.

There's more of this label. Read more.


3. PMDA Label for gefitinib and CYP2D6,EGFR

Genetic testing required

Summary

The PMDA package insert for gefitinib (Iressa) states that patients should be tested for EGFR gene mutations prior to administration. It also discusses the role of CYP2D6 is the metabolism of gefitinib.

There's more of this label. Read more.


4. HCSC Label for gefitinib and EGFR

Genetic testing required

Summary

The product monograph for gefitinib (IRESSA) states that it is indicated for patients with activating EGFR mutations, and should not be used in those with EGFR mutation negative tumors.

There's more of this label. Read more.


Clinical Variants that meet the highest level of criteria, manually curated by PharmGKB, are shown below.

To see more Clinical Variants with lower levels of criteria, click the button at the bottom of the page.

Disclaimer: The PharmGKB's clinical annotations reflect expert consensus based on clinical evidence and peer-reviewed literature available at the time they are written and are intended only to assist clinicians in decision-making and to identify questions for further research. New evidence may have emerged since the time an annotation was submitted to the PharmGKB. The annotations are limited in scope and are not applicable to interventions or diseases that are not specifically identified.

The annotations do not account for individual variations among patients, and cannot be considered inclusive of all proper methods of care or exclusive of other treatments. It remains the responsibility of the health-care provider to determine the best course of treatment for a patient. Adherence to any guideline is voluntary, with the ultimate determination regarding its application to be made solely by the clinician and the patient. PharmGKB assumes no responsibility for any injury or damage to persons or property arising out of or related to any use of the PharmGKB clinical annotations, or for any errors or omissions.

? = Mouse-over for quick help

The table below contains information about pharmacogenomic variants on PharmGKB. Please follow the link in the "Variant" column for more information about a particular variant. Each link in the "Variant" column leads to the corresponding PharmGKB Variant Page. The Variant Page contains summary data, including PharmGKB manually curated information about variant-drug pairs based on individual PubMed publications. The PMIDs for these PubMed publications can be found on the Variant Page.

The tags in the first column of the table indicate what type of information can be found on the corresponding Variant Page.

Links in the "Gene" column lead to PharmGKB Gene Pages.

List of all variant annotations for gefitinib

Gene ? Variant?
(147)
Alternate Names ? Chemicals ? Alleles ?
(+ chr strand)
Function ? Amino Acid?
Translation
VIP CA VA CYP2D6 *1 N/A N/A N/A
VIP CA VA CYP2D6 *2 N/A N/A N/A
VIP CA VA CYP2D6 *3 N/A N/A N/A
VIP CA VA CYP2D6 *4 N/A N/A N/A
No VIP available CA VA CYP2D6 *4xN N/A N/A N/A
No VIP available CA VA CYP2D6 *5 N/A N/A N/A
VIP CA VA CYP2D6 *6 N/A N/A N/A
VIP No VIP available No VIP available CYP2D6 *9 N/A N/A N/A
VIP CA VA CYP2D6 *10 N/A N/A N/A
No VIP available CA VA CYP2D6 *14 N/A N/A N/A
No VIP available No VIP available VA CYP2D6 *14A N/A N/A N/A
VIP No VIP available No VIP available CYP2D6 *17 N/A N/A N/A
VIP No VIP available No VIP available CYP2D6 *29 N/A N/A N/A
No VIP available No VIP available VA CYP2D6 *36 N/A N/A N/A
VIP CA VA CYP2D6 *41 N/A N/A N/A
No VIP available No VIP available VA CYP3A4 *1 N/A N/A N/A
No VIP available No VIP available VA CYP3A4 *1G N/A N/A N/A
No VIP available No VIP available VA CYP3A5 *1A N/A N/A N/A
No VIP available No VIP available VA CYP3A5 *3A N/A N/A N/A
rs1045642 NC_000007.13:g.87138645A>G, NC_000007.14:g.87509329A>G, NG_011513.1:g.208920T>C, NM_000927.4:c.3435T>C, NP_000918.2:p.Ile1145=, rs10239679, rs11568726, rs117328163, rs17210003, rs2229108, rs386513066, rs60023214, rs9690664
A > G
SNP
I1145I
rs1065852 NC_000022.10:g.42526694G=, NC_000022.10:g.42526694G>A, NC_000022.11:g.42130692G=, NC_000022.11:g.42130692G>A, NG_008376.3:g.4300C=, NG_008376.3:g.4300C>T, NM_000106.5:c.100C=, NM_000106.5:c.100C>T, NM_001025161.2:c.100C=, NM_001025161.2:c.100C>T, NP_000097.3:p.Pro34=, NP_000097.3:p.Pro34Ser, NP_001020332.2:p.Pro34=, NP_001020332.2:p.Pro34Ser, NT_187682.1:g.53033G=, NT_187682.1:g.53033G>A, NW_004504305.1:g.53019A=, NW_004504305.1:g.53019A>G, NW_009646208.1:g.16258A=, NW_009646208.1:g.16258A>G, XM_005278353.1:c.100T=, XM_005278353.1:c.100T>C, XM_005278354.1:c.-1454C>T, XM_005278354.1:c.-1454T>C, XM_005278354.3:c.-1454C>T, XM_005278354.3:c.-1454T>C, XM_011529966.1:c.100C=, XM_011529966.1:c.100C>T, XM_011529967.1:c.100C=, XM_011529967.1:c.100C>T, XM_011529968.1:c.100C=, XM_011529968.1:c.100C>T, XM_011529969.1:c.37+605C>T, XM_011529969.1:c.37+605T>C, XM_011529970.1:c.100C=, XM_011529970.1:c.100C>T, XM_011529971.1:c.37+605C>T, XM_011529971.1:c.37+605T>C, XM_011529972.1:c.100C=, XM_011529972.1:c.100C>T, XM_011547541.1:c.-1454C>T, XM_011547541.1:c.-1454T>C, XM_011547750.1:c.37+605C>T, XM_011547750.1:c.37+605T>C, XM_011547751.1:c.-1114C>T, XM_011547751.1:c.-1114T>C, XM_011547756.1:c.42+469A>G, XM_011547756.1:c.42+469G>A, XM_011548819.1:c.-1454C>T, XM_011548819.1:c.-1454T>C, XP_005278410.1:p.Ser34=, XP_005278410.1:p.Ser34Pro, XP_011528268.1:p.Pro34=, XP_011528268.1:p.Pro34Ser, XP_011528269.1:p.Pro34=, XP_011528269.1:p.Pro34Ser, XP_011528270.1:p.Pro34=, XP_011528270.1:p.Pro34Ser, XP_011528272.1:p.Pro34=, XP_011528272.1:p.Pro34Ser, XP_011528274.1:p.Pro34=, XP_011528274.1:p.Pro34Ser, XR_430455.2:n.328+4A>G, XR_430455.2:n.328+4G>A, XR_952536.1:n.-1751A>G, XR_952536.1:n.-1751G>A, XR_952537.1:n.-1751A>G, XR_952537.1:n.-1751G>A, XR_952538.1:n.-1751A>G, XR_952538.1:n.-1751G>A, XR_952539.1:n.-1462A>G, XR_952539.1:n.-1462G>A, XR_952745.1:n.1257C=, XR_952745.1:n.1257C>T, rs117813846, rs58862176
G > A
SNP
P34S
rs10799754 NC_000001.10:g.22746686T>C, NC_000001.11:g.22420193T>C, XR_947058.1:n.-1255A>G, rs58371367
T > C
SNP
rs1128503 NC_000007.13:g.87179601A>G, NC_000007.14:g.87550285A>G, NG_011513.1:g.167964T>C, NM_000927.4:c.1236T>C, NP_000918.2:p.Gly412=, rs116989428, rs17276907, rs2032587, rs2229105, rs28365046, rs386518005, rs58257317
A > G
SNP
G412G
rs11568315
(CA)16 > (CA)14
(CA)16 > (CA)15
(CA)16 > (CA)17
(CA)16 > (CA)18
(CA)16 > (CA)19
(CA)16 > (CA)20
(CA)16 > (CA)21
(CA)16 > (CA)22
(CA)16 > (CA)23
(CA)16 > (CA)9
microsatellite
rs121434568 NC_000007.13:g.55259515T>G, NC_000007.14:g.55191822T>G, NG_007726.3:g.177791T>G, NM_005228.3:c.2573T>G, NP_005219.2:p.Leu858Arg, XM_005271746.1:c.2438T>G, XM_005271747.1:c.2414T>G, XP_005271803.1:p.Leu813Arg, XP_005271804.1:p.Leu805Arg
T > G
SNP
L858R
rs121434569 NC_000007.13:g.55249071C>T, NC_000007.14:g.55181378C>T, NG_007726.3:g.167347C>T, NM_005228.3:c.2369C>T, NP_005219.2:p.Thr790Met, NR_047551.1:n.1193G>A, XM_005271746.1:c.2234C>T, XM_005271747.1:c.2210C>T, XP_005271803.1:p.Thr745Met, XP_005271804.1:p.Thr737Met
C > T
SNP
T790M
rs12145722 NC_000001.10:g.22742985C>T, NC_000001.11:g.22416492C>T, XR_947058.1:n.811G>A, rs60246279
C > T
SNP
rs16947 NC_000022.10:g.42523943A=, NC_000022.10:g.42523943A>G, NC_000022.11:g.42127941G=, NC_000022.11:g.42127941G>A, NG_008376.3:g.7051C=, NG_008376.3:g.7051C>T, NM_000106.5:c.886C=, NM_000106.5:c.886C>T, NM_001025161.2:c.733C=, NM_001025161.2:c.733C>T, NP_000097.3:p.Arg296=, NP_000097.3:p.Arg296Cys, NP_001020332.2:p.Arg245=, NP_001020332.2:p.Arg245Cys, NT_187682.1:g.50282A=, NT_187682.1:g.50282A>G, NW_004504305.1:g.50268G=, NW_004504305.1:g.50268G>A, NW_009646208.1:g.13507G=, NW_009646208.1:g.13507G>A, XM_005278353.1:c.742C=, XM_005278353.1:c.742C>T, XM_005278354.1:c.586C=, XM_005278354.1:c.586C>T, XM_005278354.3:c.586C=, XM_005278354.3:c.586C>T, XM_011529966.1:c.886C=, XM_011529966.1:c.886C>T, XM_011529967.1:c.886C=, XM_011529967.1:c.886C>T, XM_011529968.1:c.886C=, XM_011529968.1:c.886C>T, XM_011529969.1:c.742C=, XM_011529969.1:c.742C>T, XM_011529970.1:c.733C=, XM_011529970.1:c.733C>T, XM_011529971.1:c.742C=, XM_011529971.1:c.742C>T, XM_011529972.1:c.843+233C>T, XM_011529972.1:c.843+233T>C, XM_011547541.1:c.586C=, XM_011547541.1:c.586C>T, XM_011547750.1:c.742T=, XM_011547750.1:c.742T>C, XM_011547751.1:c.670T=, XM_011547751.1:c.670T>C, XM_011547756.1:c.-2094A>G, XM_011547756.1:c.-2094G>A, XM_011548819.1:c.586C=, XM_011548819.1:c.586C>T, XP_005278410.1:p.Arg248=, XP_005278410.1:p.Arg248Cys, XP_005278411.1:p.Arg196=, XP_005278411.1:p.Arg196Cys, XP_011528268.1:p.Arg296=, XP_011528268.1:p.Arg296Cys, XP_011528269.1:p.Arg296=, XP_011528269.1:p.Arg296Cys, XP_011528270.1:p.Arg296=, XP_011528270.1:p.Arg296Cys, XP_011528271.1:p.Arg248=, XP_011528271.1:p.Arg248Cys, XP_011528272.1:p.Arg245=, XP_011528272.1:p.Arg245Cys, XP_011528273.1:p.Arg248=, XP_011528273.1:p.Arg248Cys, XP_011545843.1:p.Arg196=, XP_011545843.1:p.Arg196Cys, XP_011546052.1:p.Cys248=, XP_011546052.1:p.Cys248Arg, XP_011546053.1:p.Cys224=, XP_011546053.1:p.Cys224Arg, XP_011547121.1:p.Arg196=, XP_011547121.1:p.Arg196Cys, XR_430455.2:n.-1930A>G, XR_430455.2:n.-1930G>A, XR_952745.1:n.2000+233C>T, XR_952745.1:n.2000+233T>C, rs117039205, rs57836231
A > G
SNP
R296C
rs2032582 NC_000007.13:g.87160618A>C, NC_000007.13:g.87160618A>T, NC_000007.14:g.87531302A>C, NC_000007.14:g.87531302A>T, NG_011513.1:g.186947T>A, NG_011513.1:g.186947T>G, NM_000927.4:c.2677T>A, NM_000927.4:c.2677T>G, NP_000918.2:p.Ser893Ala, NP_000918.2:p.Ser893Thr, rs10228331, rs2229106, rs386553610, rs57135550, rs9641018
A > C
A > T
SNP
S893A
rs2231142 NC_000004.11:g.89052323G>T, NC_000004.12:g.88131171G>T, NG_032067.2:g.105152C>A, NM_001257386.1:c.421C>A, NM_004827.2:c.421C>A, NP_001244315.1:p.Gln141Lys, NP_004818.2:p.Gln141Lys, XM_005263354.1:c.421C>A, XM_005263354.2:c.421C>A, XM_005263355.1:c.421C>A, XM_005263355.2:c.421C>A, XM_005263356.1:c.421C>A, XM_005263356.2:c.421C>A, XM_011532420.1:c.421C>A, XP_005263411.1:p.Gln141Lys, XP_005263412.1:p.Gln141Lys, XP_005263413.1:p.Gln141Lys, XP_011530722.1:p.Gln141Lys, rs12721641, rs28365035, rs3736117, rs52809243, rs58973676
G > T
SNP
Q141K
rs2293347 NC_000007.13:g.55268916C>T, NC_000007.14:g.55201223C>T, NG_007726.3:g.187192C>T, NM_005228.3:c.2982C>T, NP_005219.2:p.Asp994=, XM_005271746.1:c.2847C>T, XM_005271747.1:c.2823C>T, XP_005271803.1:p.Asp949=, XP_005271804.1:p.Asp941=, rs10435501, rs17337472, rs386564009, rs56649858, rs61150996
C > T
SNP
D994D
rs2622604 NC_000004.11:g.89078924T>C, NC_000004.12:g.88157772T>C, NG_032067.2:g.78551A>G, NM_001257386.1:c.-19-17758A>G, NM_004827.2:c.-20+614A>G, XM_005263354.1:c.-20+805A>G, XM_005263354.2:c.-20+805A>G, XM_005263355.1:c.-19-17758A>G, XM_005263355.2:c.-19-17758A>G, XM_005263356.1:c.-20+614A>G, XM_005263356.2:c.-20+614A>G, XM_011532420.1:c.-19-17758A>G, rs61481684
T > A
T > C
SNP
rs28371706 NC_000022.10:g.42525772G>A, NC_000022.11:g.42129770G>A, NG_008376.3:g.5222C>T, NM_000106.5:c.320C>T, NM_001025161.2:c.320C>T, NP_000097.3:p.Thr107Ile, NP_001020332.2:p.Thr107Ile, NT_187682.1:g.52111G>A, NW_004504305.1:g.52097G>A, NW_009646208.1:g.15336G>A, XM_005278353.1:c.320C>T, XM_005278354.1:c.-532C>T, XM_005278354.3:c.-532C>T, XM_011529966.1:c.320C>T, XM_011529967.1:c.320C>T, XM_011529968.1:c.320C>T, XM_011529969.1:c.177C>T, XM_011529970.1:c.320C>T, XM_011529971.1:c.177C>T, XM_011529972.1:c.320C>T, XM_011547541.1:c.-532C>T, XM_011547750.1:c.177C>T, XM_011547751.1:c.-192C>T, XM_011547756.1:c.-265G>A, XM_011548819.1:c.-532C>T, XP_005278410.1:p.Thr107Ile, XP_011528268.1:p.Thr107Ile, XP_011528269.1:p.Thr107Ile, XP_011528270.1:p.Thr107Ile, XP_011528271.1:p.His59=, XP_011528272.1:p.Thr107Ile, XP_011528273.1:p.His59=, XP_011528274.1:p.Thr107Ile, XP_011546052.1:p.His59=, XR_430455.2:n.-101G>A, XR_952745.1:n.1477C>T, rs587777915, rs59604033
G > A
SNP
T107I
rs28371725 NC_000022.10:g.42523805C>T, NC_000022.11:g.42127803C>T, NG_008376.3:g.7189G>A, NM_000106.5:c.985+39G>A, NM_001025161.2:c.832+39G>A, NT_187682.1:g.50144C>T, NW_004504305.1:g.50130C>T, NW_009646208.1:g.13369C>T, XM_005278353.1:c.841+39G>A, XM_005278354.1:c.685+39G>A, XM_005278354.3:c.685+39G>A, XM_011529966.1:c.985+39G>A, XM_011529967.1:c.985+39G>A, XM_011529968.1:c.985+39G>A, XM_011529969.1:c.841+39G>A, XM_011529970.1:c.832+39G>A, XM_011529971.1:c.841+39G>A, XM_011529972.1:c.844-169G>A, XM_011547541.1:c.724G>A, XM_011547750.1:c.841+39G>A, XM_011547751.1:c.769+39G>A, XM_011548819.1:c.724G>A, XP_011545843.1:p.Glu242Lys, XP_011547121.1:p.Glu242Lys, XR_952745.1:n.2001-169G>A, rs57124011, rs587777916
C > T
SNP
rs35742686 NC_000022.10:g.42524244delT, NC_000022.11:g.42128242delT, NG_008376.3:g.6750delA, NM_000106.5:c.775delA, NM_001025161.2:c.622delA, NP_000097.3:p.Arg259Glyfs, NP_001020332.2:p.Arg208Glyfs, NT_187682.1:g.50583delT, NW_004504305.1:g.50569delT, NW_009646208.1:g.13808delT, XM_005278353.1:c.631delA, XM_005278354.1:c.475delA, XM_005278354.3:c.475delA, XM_011529966.1:c.775delA, XM_011529967.1:c.775delA, XM_011529968.1:c.775delA, XM_011529969.1:c.631delA, XM_011529970.1:c.622delA, XM_011529971.1:c.631delA, XM_011529972.1:c.775delA, XM_011547541.1:c.475delA, XM_011547750.1:c.631delA, XM_011547751.1:c.559delA, XM_011547756.1:c.-1793delT, XM_011548819.1:c.475delA, XP_005278410.1:p.Arg211Glyfs, XP_005278411.1:p.Arg159Glyfs, XP_011528268.1:p.Arg259Glyfs, XP_011528269.1:p.Arg259Glyfs, XP_011528270.1:p.Arg259Glyfs, XP_011528271.1:p.Arg211Glyfs, XP_011528272.1:p.Arg208Glyfs, XP_011528273.1:p.Arg211Glyfs, XP_011528274.1:p.Arg259Glyfs, XP_011545843.1:p.Arg159Glyfs, XP_011546052.1:p.Arg211Glyfs, XP_011546053.1:p.Arg187Glyfs, XP_011547121.1:p.Arg159Glyfs, XR_430455.2:n.-1629delT, XR_952745.1:n.1932delA, rs45593132, rs60790764
T > -
T > T
indel
R259G
rs3892097 NC_000022.10:g.42524947C=, NC_000022.10:g.42524947C>T, NC_000022.11:g.42128945C=, NC_000022.11:g.42128945C>T, NG_008376.3:g.6047G=, NG_008376.3:g.6047G>A, NM_000106.5:c.506-1A>G, NM_000106.5:c.506-1G>A, NM_001025161.2:c.353-1A>G, NM_001025161.2:c.353-1G>A, NT_187682.1:g.51286C=, NT_187682.1:g.51286C>T, NW_004504305.1:g.51272T=, NW_004504305.1:g.51272T>C, NW_009646208.1:g.14511C=, NW_009646208.1:g.14511C>T, XM_005278353.1:c.363-2A>G, XM_005278353.1:c.363-2G>A, XM_005278354.1:c.207-2A>G, XM_005278354.1:c.207-2G>A, XM_005278354.3:c.207-2A>G, XM_005278354.3:c.207-2G>A, XM_011529966.1:c.506-1A>G, XM_011529966.1:c.506-1G>A, XM_011529967.1:c.506-1A>G, XM_011529967.1:c.506-1G>A, XM_011529968.1:c.506-1A>G, XM_011529968.1:c.506-1G>A, XM_011529969.1:c.363-2A>G, XM_011529969.1:c.363-2G>A, XM_011529970.1:c.353-1A>G, XM_011529970.1:c.353-1G>A, XM_011529971.1:c.363-2A>G, XM_011529971.1:c.363-2G>A, XM_011529972.1:c.506-1A>G, XM_011529972.1:c.506-1G>A, XM_011547541.1:c.207-2A>G, XM_011547541.1:c.207-2G>A, XM_011547750.1:c.363-2A>G, XM_011547750.1:c.363-2G>A, XM_011547751.1:c.290-1A>G, XM_011547751.1:c.290-1G>A, XM_011547756.1:c.-1090C>T, XM_011547756.1:c.-1090T>C, XM_011548819.1:c.207-2A>G, XM_011548819.1:c.207-2G>A, XR_430455.2:n.-926C>T, XR_430455.2:n.-926T>C, XR_952745.1:n.1663-1A>G, XR_952745.1:n.1663-1G>A, rs1800716, rs28371711, rs60082401, rs606231227
C > T
SNP
rs5030655 NC_000022.10:g.42525086delA, NC_000022.11:g.42129084delA, NG_008376.3:g.5908delT, NM_000106.5:c.454delT, NM_001025161.2:c.353-140delT, NP_000097.3:p.Trp152Glyfs, NT_187682.1:g.51425delA, NW_004504305.1:g.51411delA, NW_009646208.1:g.14650delA, XM_005278353.1:c.363-141delT, XM_005278354.1:c.155delT, XM_005278354.3:c.155delT, XM_011529966.1:c.454delT, XM_011529967.1:c.454delT, XM_011529968.1:c.454delT, XM_011529969.1:c.311delT, XM_011529970.1:c.353-140delT, XM_011529971.1:c.311delT, XM_011529972.1:c.454delT, XM_011547541.1:c.155delT, XM_011547750.1:c.311delT, XM_011547751.1:c.238delT, XM_011547756.1:c.-951delA, XM_011548819.1:c.155delT, XP_005278411.1:p.Val52Glyfs, XP_011528268.1:p.Trp152Glyfs, XP_011528269.1:p.Trp152Glyfs, XP_011528270.1:p.Trp152Glyfs, XP_011528271.1:p.Val104Glyfs, XP_011528273.1:p.Val104Glyfs, XP_011528274.1:p.Trp152Glyfs, XP_011545843.1:p.Val52Glyfs, XP_011546052.1:p.Val104Glyfs, XP_011546053.1:p.Trp80Glyfs, XP_011547121.1:p.Val52Glyfs, XR_430455.2:n.-787delA, XR_952745.1:n.1611delT, rs11568727, rs28371709
A > -
A > A
indel
W152G
rs5030656 NC_000022.10:g.42524176_42524178delCTT, NC_000022.11:g.42128174_42128176delCTT, NG_008376.3:g.6816_6818delAAG, NM_000106.5:c.841_843delAAG, NM_001025161.2:c.688_690delAAG, NP_000097.3:p.Lys281del, NP_001020332.2:p.Lys230del, NT_187682.1:g.50515_50517delCTT, NW_004504305.1:g.50501_50503delCTT, NW_009646208.1:g.13740_13742delCTT, XM_005278353.1:c.697_699delAAG, XM_005278354.1:c.541_543delAAG, XM_005278354.3:c.541_543delAAG, XM_011529966.1:c.841_843delAAG, XM_011529967.1:c.841_843delAAG, XM_011529968.1:c.841_843delAAG, XM_011529969.1:c.697_699delAAG, XM_011529970.1:c.688_690delAAG, XM_011529971.1:c.697_699delAAG, XM_011529972.1:c.841_843delAAG, XM_011547541.1:c.541_543delAAG, XM_011547750.1:c.697_699delAAG, XM_011547751.1:c.625_627delAAG, XM_011547756.1:c.-1861_-1859del, XM_011548819.1:c.541_543delAAG, XP_005278410.1:p.Lys233del, XP_005278411.1:p.Lys181del, XP_011528268.1:p.Lys281del, XP_011528269.1:p.Lys281del, XP_011528270.1:p.Lys281del, XP_011528271.1:p.Lys233del, XP_011528272.1:p.Lys230del, XP_011528273.1:p.Lys233del, XP_011528274.1:p.Lys281del, XP_011545843.1:p.Lys181del, XP_011546052.1:p.Lys233del, XP_011546053.1:p.Lys209del, XP_011547121.1:p.Lys181del, XR_430455.2:n.-1697_-1695del, XR_952745.1:n.1998_2000delAAG, rs587777919
CTT > -
CTT > CTT
indel
rs59421388 NC_000022.10:g.42523610C>T, NC_000022.11:g.42127608C>T, NG_008376.3:g.7384G>A, NM_000106.5:c.1012G>A, NM_001025161.2:c.859G>A, NP_000097.3:p.Val338Met, NP_001020332.2:p.Val287Met, NT_187682.1:g.49949C>T, NW_004504305.1:g.49935C>T, NW_009646208.1:g.13174C>T, XM_005278353.1:c.868G>A, XM_005278354.1:c.712G>A, XM_005278354.3:c.712G>A, XM_011529966.1:c.1012G>A, XM_011529967.1:c.1012G>A, XM_011529968.1:c.1012G>A, XM_011529969.1:c.868G>A, XM_011529970.1:c.859G>A, XM_011529971.1:c.868G>A, XM_011529972.1:c.870G>A, XM_011547541.1:c.*118G>A, XM_011547750.1:c.868G>A, XM_011547751.1:c.796G>A, XM_011548819.1:c.*118G>A, XP_005278410.1:p.Val290Met, XP_005278411.1:p.Val238Met, XP_011528268.1:p.Val338Met, XP_011528269.1:p.Val338Met, XP_011528270.1:p.Val338Met, XP_011528271.1:p.Val290Met, XP_011528272.1:p.Val287Met, XP_011528273.1:p.Val290Met, XP_011528274.1:p.Thr290=, XP_011546052.1:p.Val290Met, XP_011546053.1:p.Val266Met, XR_952745.1:n.2027G>A
C > T
SNP
V338M
rs61736512 NC_000022.10:g.42525134C>T, NC_000022.11:g.42129132C>T, NG_008376.3:g.5860G>A, NM_000106.5:c.406G>A, NM_001025161.2:c.353-188G>A, NP_000097.3:p.Val136Met, NT_187682.1:g.51473C>T, NW_004504305.1:g.51459C>T, NW_009646208.1:g.14698C>T, XM_005278353.1:c.363-189G>A, XM_005278354.1:c.107G>A, XM_005278354.3:c.107G>A, XM_011529966.1:c.406G>A, XM_011529967.1:c.406G>A, XM_011529968.1:c.406G>A, XM_011529969.1:c.263G>A, XM_011529970.1:c.353-188G>A, XM_011529971.1:c.263G>A, XM_011529972.1:c.406G>A, XM_011547541.1:c.107G>A, XM_011547750.1:c.263G>A, XM_011547751.1:c.190G>A, XM_011547756.1:c.-903C>T, XM_011548819.1:c.107G>A, XP_005278411.1:p.Arg36His, XP_011528268.1:p.Val136Met, XP_011528269.1:p.Val136Met, XP_011528270.1:p.Val136Met, XP_011528271.1:p.Arg88His, XP_011528273.1:p.Arg88His, XP_011528274.1:p.Val136Met, XP_011545843.1:p.Arg36His, XP_011546052.1:p.Arg88His, XP_011546053.1:p.Val64Ile, XP_011547121.1:p.Arg36His, XR_430455.2:n.-739C>T, XR_952745.1:n.1563G>A
C > T
SNP
V136M
rs712829 NC_000007.13:g.55086755G>T, NC_000007.14:g.55019062G>T, NG_007726.3:g.5031G>T, NM_005228.3:c.-216G>T, NM_201282.1:c.-216G>T, NM_201283.1:c.-216G>T, NM_201284.1:c.-216G>T, XM_005271746.1:c.-216G>T, XM_005271748.1:c.-216G>T, rs17288931
G > T
SNP
rs72552713 NC_000004.11:g.89052957G>A, NC_000004.12:g.88131805G>A, NG_032067.2:g.104518C>T, NM_001257386.1:c.376C>T, NM_004827.2:c.376C>T, NP_001244315.1:p.Gln126Ter, NP_004818.2:p.Gln126Ter, XM_005263354.1:c.376C>T, XM_005263354.2:c.376C>T, XM_005263355.1:c.376C>T, XM_005263355.2:c.376C>T, XM_005263356.1:c.376C>T, XM_005263356.2:c.376C>T, XM_011532420.1:c.376C>T, XP_005263411.1:p.Gln126Ter, XP_005263412.1:p.Gln126Ter, XP_005263413.1:p.Gln126Ter, XP_011530722.1:p.Gln126Ter
G > A
SNP
Q126*
rs726501 NC_000005.10:g.56832039G>A, NC_000005.9:g.56127866G>A, NG_031884.1:g.21967G>A, NM_005921.1:c.482+15984G>A, XM_005248519.1:c.71+11223G>A, XM_005248519.3:c.104+11223G>A, XM_005248520.1:c.-8+14923G>A, XM_011543406.1:c.227+15704G>A, XM_011543407.1:c.482+15984G>A, XM_011543408.1:c.482+15984G>A, rs57031684
G > A
SNP
Alleles, Functions, and Amino Acid Translations are all sourced from dbSNP 147

Overview

Generic Names
  • ZD-1839
  • ZD1839
Trade Names
  • Iressa
  • Irressat
Brand Mixture Names

PharmGKB Accession Id

PA131301952

Type(s):

Drug

Description

Gefitinib (originally coded ZD1839) is a drug used in the treatment of certain types of cancer. Acting in a similar manner to erlotinib (marketed as Tarceva), gefitinib selectively targets the mutant proteins in malignant cells. It is marketed by AstraZeneca under the trade name Iressa. [Wikipedia]

Source: Drug Bank

Pharmacogenetics

There are two kinds of mutations in EGFR that influence efficacy of gefitinib:

Mutations that increase drug sensitivity such as L858R (rs121434568) and exon 19 deletions. These are somatic gain-of-function mutations that are cancer-driving and activate EGFR, making it more sensitive to tyrosine kinase inhibitors, TKIs, such as gefitinib. These are discussed further in the EGFR VIP gene summary.

Secondary mutations that result in aquired resistance to TKIs including T790M (rs121434569) [Article:15737014]. These are also discussed further in the EGFR VIP gene summary.

Source: PharmGKB [Article:23962910] [Article:15737014]

Indication

For the continued treatment of patients with locally advanced or metastatic non-small cell lung cancer after failure of either platinum-based or docetaxel chemotherapies.

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

Mechanism of Action

Gefitinib inhibits the epidermal growth factor receptor (EGFR) tyrosine kinase by binding to the adenosine triphosphate (ATP)-binding site of the enzyme. Thus the function of the EGFR tyrosine kinase in activating the Ras signal transduction cascade is inhibited; and malignant cells are inhibited. Gefitinib is the first selective inhibitor of the EGFR tyrosine kinase which is also referred to as Her1 or ErbB-1. EGFR is overexpressed in the cells of certain types of human carcinomas - for example in lung and breast cancers. Overexpression leads to inappropriate activation of the apoptotic Ras signal transduction cascade, eventually leading to uncontrolled cell proliferation.

Source: Drug Bank

Pharmacology

Gefitinib inhibits the intracellular phosphorylation of numerous tyrosine kinases associated with transmembrane cell surface receptors, including the tyrosine kinases associated with the epidermal growth factor receptor (EGFR-TK). EGFR is expressed on the cell surface of many normal cells and cancer cells.

Source: Drug Bank

Food Interaction

Avoid fresh grapefruit and its juice during therapy as grapefruit may increase serum product levels.|Take without regard to meals.

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Primarily hepatic via CYP3A4. Three sites of biotransformation have been identified: metabolism of the N-propoxymorpholino-group, demethylation of the methoxy-substituent on the quinazoline, and oxidative defluorination of the halogenated phenyl group.

Source: Drug Bank

Protein Binding

90% primarily to serum albumin and alpha 1-acid glycoproteins.

Source: Drug Bank

Absorption

Absorbed slowly after oral administration with mean bioavailability of 60%.

Source: Drug Bank

Half-Life

48 hours

Source: Drug Bank

Toxicity

The acute toxicity of gefitinib up to 500 mg in clinical studies has been low. In non-clinical studies, a single dose of 12,000 mg/m ^2^ (about 80 times the recommended clinical dose on a mg/m ^2^ basis) was lethal to rats. Half this dose caused no mortality in mice. Symptoms of overdose include diarrhea and skin rash.

Source: Drug Bank

Clearance

* 595 mL/min

Source: Drug Bank

Route of Elimination

Elimination is by metabolism (primarily CYP3A4) and excretion in feces. Excretion is predominantly via the feces (86%), with renal elimination of drug and metabolites accounting for less than 4% of the administered dose.

Source: Drug Bank

Volume of Distribution

* 1400 L

Source: Drug Bank

Chemical Properties

Chemical Formula

C22H24ClFN4O3

Source: Drug Bank

Isomeric SMILES

COc1cc2c(cc1OCCCN3CCOCC3)c(ncn2)Nc4ccc(c(c4)Cl)F

Source: OpenEye

Canonical SMILES

COC1=C(OCCCN2CCOCC2)C=C2C(NC3=CC(Cl)=C(F)C=C3)=NC=NC2=C1

Source: Drug Bank

Average Molecular Weight

446.902

Source: Drug Bank

Monoisotopic Molecular Weight

446.152096566

Source: Drug Bank

SMILES

COC1=C(OCCCN2CCOCC2)C=C2C(NC3=CC(Cl)=C(F)C=C3)=NC=NC2=C1

Source: Drug Bank

InChI String

InChI=1S/C22H24ClFN4O3/c1-29-20-13-19-16(12-21(20)31-8-2-5-28-6-9-30-10-7-28)22(26-14-25-19)27-15-3-4-18(24)17(23)11-15/h3-4,11-14H,2,5-10H2,1H3,(H,25,26,27)

Source: Drug Bank

PharmGKB Curated Pathways

Pathways created internally by PharmGKB based primarily on literature evidence.

  1. EGFR Inhibitor Pathway, Pharmacodynamics
    Model non-tissue specific cancer cell displaying genes that may be involved in the treatment using epidermal growth factor receptor specific tyrosine kinase inhibitors or monoclonal antibodies.
  1. Gefitinib Pathway, Pharmacokinetics
    Representation of the candidate genes involved in the transportation and metabolism of gefitinib.

Genes that are associated with this drug in PharmGKB's database based on (1) variant annotations, (2) literature review, (3) pathways or (4) information automatically retrieved from DrugBank, depending on the "evidence" and "source" listed below.

Curated Information ?

Drug Targets

Gene Description
EGFR (source: Drug Bank )

Drug Interactions

Interaction Description
carbamazepine - gefitinib This CYP3A4 inducer may reduce gefitinib plasma concentrations and pharmacological effects (source: Drug Bank )
carbamazepine - gefitinib The CYP3A4 inducer, carbamazepine, may decrease the serum concentration and therapeutic effects of gefitinib. (source: Drug Bank )
clarithromycin - gefitinib This CYP3A4 inhibitor increases levels/toxicity of gefitinib (source: Drug Bank )
clarithromycin - gefitinib This CYP3A4 inhibitor increases levels/toxicity of gefitinib (source: Drug Bank )
erythromycin - gefitinib This CYP3A4 inhibitor increases levels/toxicity of gefitinib (source: Drug Bank )
erythromycin - gefitinib This CYP3A4 inhibitor increases levels/toxicity of gefitinib (source: Drug Bank )
fosphenytoin - gefitinib The CYP3A4 inducer, fosphenytoin, may decrease the serum concentration and therapeutic effects of gefitinib. (source: Drug Bank )
gefitinib - acenocoumarol Gefitinib increases the anticoagulant effect (source: Drug Bank )
gefitinib - acenocoumarol Gefitinib may increase the anticoagulant effect of acenocoumarol. (source: Drug Bank )
gefitinib - amobarbital This CYP3A4 inducer may reduce gefitinib concentrations and pharmacological effects (source: Drug Bank )
gefitinib - amobarbital The CYP3A4 inducer, amobarbital, may decrease the serum concentration and therapeutic effects of gefitinib. (source: Drug Bank )
gefitinib - anisindione Gefitinib may increase the anticoagulant effect of anisindione. (source: Drug Bank )
gefitinib - aprobarbital The CYP3A4 inducer, aprobarbital, may decrease the serum concentration and therapeutic effects of gefitinib. (source: Drug Bank )
gefitinib - butabarbital The CYP3A4 inducer, butabarbital, may decrease the serum concentration and therapeutic effects of gefitinib. (source: Drug Bank )
gefitinib - butalbital This CYP3A4 inducer may reduce gefitinib concentrations and pharmacological effects (source: Drug Bank )
gefitinib - butalbital The CYP3A4 inducer, butalbital, may decrease the serum concentration and therapeutic effects of gefitinib. (source: Drug Bank )
gefitinib - butethal The CYP3A4 inducer, butethal, may decrease the serum concentration and therapeutic effects of gefitinib. (source: Drug Bank )
gefitinib - carbamazepine This CYP3A4 inducer may reduce gefitinib concentrations and pharmacological effects (source: Drug Bank )
gefitinib - carbamazepine The CYP3A4 inducer, carbamazepine, may decrease the serum concentration and therapeutic effects of gefitinib. (source: Drug Bank )
gefitinib - clarithromycin This CYP3A4 inhibitor increases levels/toxicity of gefitinib (source: Drug Bank )
gefitinib - clarithromycin This CYP3A4 inhibitor increases levels/toxicity of gefitinib (source: Drug Bank )
gefitinib - dicumarol Gefitinib increases the anticoagulant effect (source: Drug Bank )
gefitinib - dicumarol Gefitinib may increase the anticoagulant effect of dicumarol. (source: Drug Bank )
gefitinib - erythromycin This CYP3A4 inhibitor increases levels/toxicity of gefitinib (source: Drug Bank )
gefitinib - erythromycin This CYP3A4 inhibitor increases levels/toxicity of gefitinib (source: Drug Bank )
gefitinib - ethotoin The CYP3A4 inducer, ethotoin, may decrease the serum concentration and therapeutic effects of gefitinib. (source: Drug Bank )
gefitinib - fosphenytoin The CYP3A4 inducer, fosphenytoin, may decrease the serum concentration and therapeutic effects of gefitinib. (source: Drug Bank )
gefitinib - heptabarbital The CYP3A4 inducer, heptabarbital, may decrease the serum concentration and therapeutic effects of gefitinib. (source: Drug Bank )
gefitinib - hexobarbital This CYP3A4 inducer may reduce gefitinib concentrations and pharmacological effects (source: Drug Bank )
gefitinib - hexobarbital The CYP3A4 inducer, hexobarbital, may decrease the serum concentration and therapeutic effects of gefitinib. (source: Drug Bank )
gefitinib - itraconazole This CYP3A4 inhibitor increases levels/toxicity of gefitinib (source: Drug Bank )
gefitinib - itraconazole This CYP3A4 inhibitor increases levels/toxicity of gefitinib (source: Drug Bank )
gefitinib - ketoconazole This CYP3A4 inhibitor increases levels/toxicity of gefitinib (source: Drug Bank )
gefitinib - ketoconazole This CYP3A4 inhibitor increases levels/toxicity of gefitinib (source: Drug Bank )
gefitinib - mephenytoin This CYP3A4 inducer may reduce gefitinib concentrations and pharmacological effects (source: Drug Bank )
gefitinib - mephenytoin The CYP3A4 inducer, mephenytoin, may decrease the serum concentration and therapeutic effects of gefitinib. (source: Drug Bank )
gefitinib - methohexital The CYP3A4 inducer, methohexital, may decrease the serum concentration and therapeutic effects of gefitinib. (source: Drug Bank )
gefitinib - methylphenobarbital This CYP3A4 inducer may reduce gefitinib concentrations and pharmacological effects (source: Drug Bank )
gefitinib - methylphenobarbital The CYP3A4 inducer, methylphenobarbital, may decrease the serum concentration and therapeutic effects of gefitinib. (source: Drug Bank )
gefitinib - pentobarbital This CYP3A4 inducer may reduce gefitinib concentrations and pharmacological effects (source: Drug Bank )
gefitinib - pentobarbital The CYP3A4 inducer, pentobarbital, may decrease the serum concentration and therapeutic effects of gefitinib. (source: Drug Bank )
gefitinib - phenobarbital This CYP3A4 inducer may reduce gefitinib concentrations and pharmacological effects (source: Drug Bank )
gefitinib - phenobarbital The CYP3A4 inducer, phenobarbital, may decrease the serum concentration and therapeutic effects of gefitinib. (source: Drug Bank )
gefitinib - phenytoin This CYP3A4 inducer may reduce gefitinib concentrations and pharmacological effects (source: Drug Bank )
gefitinib - phenytoin The CYP3A4 inducer, phenytoin, may decrease the serum concentration and therapeutic effects of gefitinib. (source: Drug Bank )
gefitinib - primidone This CYP3A4 inducer may reduce gefitinib concentrations and pharmacological effects (source: Drug Bank )
gefitinib - primidone The CYP3A4 inducer, primidone, may decrease the serum concentration and therapeutic effects of gefitinib. (source: Drug Bank )
gefitinib - quinidine The CYP3A4 inducer, quinidine barbiturate, may decrease the serum concentration and therapeutic effects of gefitinib. (source: Drug Bank )
gefitinib - rifampin Rifampin reduces levels and efficacy of gefitinib (source: Drug Bank )
gefitinib - rifampin Rifampin reduces levels and efficacy of gefitinib (source: Drug Bank )
gefitinib - ritonavir This CYP3A4 inhibitor increases levels/toxicity of gefitinib (source: Drug Bank )
gefitinib - ritonavir This CYP3A4 inhibitor increases levels/toxicity of gefitinib (source: Drug Bank )
gefitinib - secobarbital The CYP3A4 inducer, secobarbital, may decrease the serum concentration and therapeutic effects of gefitinib. (source: Drug Bank )
gefitinib - talbutal The CYP3A4 inducer, talbutal, may decrease the serum concentration and therapeutic effects of gefitinib. (source: Drug Bank )
gefitinib - warfarin Gefitinib increases the anticoagulant effect (source: Drug Bank )
gefitinib - warfarin Gefitinib may increase the anticoagulant effect of warfarin. (source: Drug Bank )
itraconazole - gefitinib This potent CYP3A4 inhibitor increases levels/toxicity of gefitinib (source: Drug Bank )
itraconazole - gefitinib This potent CYP3A4 inhibitor increases levels/toxicity of gefitinib (source: Drug Bank )
ketoconazole - gefitinib This CYP3A4 inhibitor increases levels/toxicity of gefitinib (source: Drug Bank )
ketoconazole - gefitinib This CYP3A4 inhibitor increases levels/toxicity of gefitinib (source: Drug Bank )
phenobarbital - gefitinib This CYP3A4 inducer may reduce gefitinib plasma concentrations and pharmacological effects (source: Drug Bank )
phenobarbital - gefitinib The CYP3A4 inducer, phenobarbital, may decrease the serum concentration and therapeutic effects of gefitinib. (source: Drug Bank )
phenytoin - gefitinib This CYP3A4 inducer may reduce gefitinib plasma concentrations and pharmacological effects (source: Drug Bank )
phenytoin - gefitinib The CYP3A4 inducer, phenytoin, may decrease the serum concentration and therapeutic effects of gefitinib. (source: Drug Bank )
primidone - gefitinib This CYP3A4 inducer may reduce gefitinib plasma concentrations and pharmacological effects (source: Drug Bank )
primidone - gefitinib The CYP3A4 inducer, primidone, may decrease the serum concentration and therapeutic effects of gefitinib. (source: Drug Bank )
rifampin - gefitinib Rifampin reduces levels and efficacy of gefitinib (source: Drug Bank )
rifampin - gefitinib Rifampin reduces levels and efficacy of gefitinib (source: Drug Bank )
telithromycin - gefitinib Telithromycin may reduce clearance of Gefitinib. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Gefitinib if Telithromycin is initiated, discontinued or dose changed. (source: Drug Bank )
topotecan - gefitinib The BCRP/ABCG2 inhibitor, Gefitnib, may increase the bioavailability and serum concentration of oral Topotecan. Monitor for change in the therapeutic and adverse effects of Topotecan if Gefitinib is initiated, discontinued or dose changed. (source: Drug Bank )
trastuzumab - gefitinib Trastuzumab may increase the risk of neutropenia and anemia. Monitor closely for signs and symptoms of adverse events. (source: Drug Bank )
voriconazole - gefitinib Voriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of gefitinib by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of gefitinib if voriconazole is initiated, discontinued or dose changed. (source: Drug Bank )

Curated Information ?

EvidenceDisease
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Adenocarcinoma
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Arrhythmias, Cardiac
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Arthritis, Rheumatoid
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Atrial Fibrillation
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Attention Deficit Disorder with Hyperactivity
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Bipolar Disorder
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Breast Neoplasms
No Dosing Guideline available DL CA VA No VIP available No VIP available
Carcinoma, Non-Small-Cell Lung
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Carcinoma, Renal Cell
No Dosing Guideline available DL No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Carcinoma, Small Cell
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Colonic Neoplasms
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Colorectal Neoplasms
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Crohn Disease
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Cystic Fibrosis
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Depression
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Diabetes Mellitus, Type 2
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Diarrhea
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Drug Hypersensitivity
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Drug Resistance
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Drug Toxicity
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Epilepsy
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Esophagitis
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Exanthema
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Gastrointestinal Stromal Tumors
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Glioblastoma
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Glioma
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Graft vs Host Disease
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Heart Failure
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Hemorrhage
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Hepatitis
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HIV Infections
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Hypercholesterolemia
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Hypereosinophilic Syndrome
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Hyperlipoproteinemia Type II
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Hypersensitivity
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Hypertension
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Inflammatory Bowel Diseases
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Kidney Transplantation
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Leukemia
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Leukemia, Lymphocytic, Chronic, B-Cell
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Leukemia, Myelogenous, Chronic, BCR-ABL Positive
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Leukemia, Myeloid
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Leukemia, Myeloid, Acute
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Leukemia, Nonlymphocytic, Acute
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Leukemia, Promyelocytic, Acute
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Lung Diseases, Interstitial
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Lung Neoplasms
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Lymphoma
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Lymphoma, Large-Cell, Anaplastic
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Lymphoma, Non-Hodgkin
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Malaria
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Melanoma
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Muscular Diseases
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Mycoses
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Myelodysplastic Syndromes
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Myocardial Infarction
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Neoplasm Metastasis
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Neoplasms
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nephrotoxicity
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Ocular Hypertension
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Ovarian Neoplasms
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Pain
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Pancreatic Neoplasms
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Peripheral Vascular Diseases
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Precursor Cell Lymphoblastic Leukemia-Lymphoma
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Pulmonary Disease, Chronic Obstructive
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Pulmonary Fibrosis
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Schizophrenia
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Sjogren's Syndrome
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Stevens-Johnson Syndrome
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Stomach Neoplasms
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Stroke
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Thromboembolism
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Thrombosis
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Thyroid Neoplasms
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Toxic liver disease
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Tuberculosis, Pulmonary
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Tumor Lysis Syndrome
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Urinary Incontinence

Relationships from National Drug File - Reference Terminology (NDF-RT)

May Treat
Contraindicated With

Publications related to gefitinib: 98

No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Determinants of Gefitinib toxicity in advanced non-small cell lung cancer (NSCLC): a pharmacogenomic study of metabolic enzymes and transporters. The pharmacogenomics journal. 2016. Ma Y, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Association of pharmacokinetics and pharmacogenomics with safety and efficacy of gefitinib in patients with EGFR mutation positive advanced non-small cell lung cancer. Lung cancer (Amsterdam, Netherlands). 2016. Hirose Takashi, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Impact of single nucleotide polymorphisms on severe hepatotoxicity induced by EGFR tyrosine kinase inhibitors in patients with non-small cell lung cancer harboring EGFR mutations. Lung cancer (Amsterdam, Netherlands). 2015. Sugiyama Eri, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Comparison of clinical outcomes of patients with non-small-cell lung cancer harbouring epidermal growth factor receptor exon 19 or exon 21 mutations after tyrosine kinase inhibitors treatment: a meta-analysis. European journal of clinical pharmacology. 2015. Sheng Miaomiao, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Relationship Among Gefitinib Exposure, Polymorphisms of Its Metabolizing Enzymes and Transporters, and Side Effects in Japanese Patients With Non-Small-Cell Lung Cancer. Clinical lung cancer. 2015. Kobayashi Hiroyuki, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
In vitro assessment of time-dependent inhibitory effects on CYP2C8 and CYP3A activity by fourteen protein kinase inhibitors. Drug metabolism and disposition: the biological fate of chemicals. 2014. Filppula Anne M, et al. PubMed
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EMA Initiatives and Perspectives on Pharmacogenomics. British journal of clinical pharmacology. 2014. Ehmann Falk, et al. PubMed
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Polymorphisms of CYP2D6 gene and gefitinib-induced hepatotoxicity. Clinical lung cancer. 2013. Takimoto Takayuki, et al. PubMed
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Emerging landscape of oncogenic signatures across human cancers. Nature genetics. 2013. Ciriello Giovanni, et al. PubMed
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PharmGKB summary: very important pharmacogene information for the epidermal growth factor receptor. Pharmacogenetics and genomics. 2013. Hodoglugil Ugur, et al. PubMed
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Challenges in pharmacogenetics. European journal of clinical pharmacology. 2013. Cascorbi Ingolf, et al. PubMed
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Efficacy of EGFR tyrosine kinase inhibitors for non-adenocarcinoma NSCLC patients with EGFR mutation. Cancer chemotherapy and pharmacology. 2012. Cho Su-Hee, et al. PubMed
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Pharmacogenetics and pharmacogenomics: role of mutational analysis in anti-cancer targeted therapy. The pharmacogenomics journal. 2012. Savonarola A, et al. PubMed
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First-SIGNAL: first-line single-agent iressa versus gemcitabine and cisplatin trial in never-smokers with adenocarcinoma of the lung. Journal of clinical oncology : official journal of the American Society of Clinical Oncology. 2012. Han Ji-Youn, et al. PubMed
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Pretreatment epidermal growth factor receptor (EGFR) T790M mutation predicts shorter EGFR tyrosine kinase inhibitor response duration in patients with non-small-cell lung cancer. Journal of clinical oncology : official journal of the American Society of Clinical Oncology. 2012. Su Kang-Yi, et al. PubMed
No Dosing Guideline available No Drug Label available CA No Variant Annotation available No VIP available No VIP available
Pharmacogenetic analysis of BR.21, a placebo-controlled randomized phase III clinical trial of erlotinib in advanced non-small cell lung cancer. Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer. 2012. Liu Geoffrey, et al. PubMed
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Epidermal growth factor receptor mutation status in circulating free DNA in serum: from IPASS, a phase III study of gefitinib or carboplatin/paclitaxel in non-small cell lung cancer. Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer. 2012. Goto Koichi, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Reduced CYP2D6 function is associated with gefitinib-induced rash in patients with non-small cell lung cancer. BMC cancer. 2012. Suzumura Tomohiro, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Quality of life with gefitinib in patients with EGFR-mutated non-small cell lung cancer: quality of life analysis of North East Japan Study Group 002 Trial. The oncologist. 2012. Oizumi Satoshi, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Pharmacogenetic predictors for EGFR-inhibitor-associated skin toxicity. The pharmacogenomics journal. 2011. Parmar S, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
A noninvasive system for monitoring resistance to epidermal growth factor receptor tyrosine kinase inhibitors with plasma DNA. Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer. 2011. Nakamura Tomomi, et al. PubMed
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Safe and successful treatment with erlotinib after gefitinib-induced hepatotoxicity: difference in metabolism as a possible mechanism. Journal of clinical oncology : official journal of the American Society of Clinical Oncology. 2011. Kijima Takashi, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Interstitial lung disease in gefitinib-treated Japanese patients with non-small-cell lung cancer: genome-wide analysis of genetic data. Pharmacogenomics. 2011. Nyberg Fredrik, et al. PubMed
No Dosing Guideline available No Drug Label available CA No Variant Annotation available No VIP available No VIP available
Genetic variations in multiple drug action pathways and survival in advanced stage non-small cell lung cancer treated with chemotherapy. Clinical cancer research : an official journal of the American Association for Cancer Research. 2011. Li Yafei, et al. PubMed
No Dosing Guideline available No Drug Label available CA No Variant Annotation available No VIP available No VIP available
Pretreatment EGFR T790M mutation and BRCA1 mRNA expression in erlotinib-treated advanced non-small-cell lung cancer patients with EGFR mutations. Clinical cancer research : an official journal of the American Association for Cancer Research. 2011. Rosell Rafael, et al. PubMed
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Rebiopsy of lung cancer patients with acquired resistance to EGFR inhibitors and enhanced detection of the T790M mutation using a locked nucleic acid-based assay. Clinical cancer research : an official journal of the American Association for Cancer Research. 2011. Arcila Maria E, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Very important pharmacogene summary: ABCB1 (MDR1, P-glycoprotein). Pharmacogenetics and genomics. 2011. Hodges Laura M, et al. PubMed
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Genotypic and histological evolution of lung cancers acquiring resistance to EGFR inhibitors. Science translational medicine. 2011. Sequist Lecia V, et al. PubMed
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Genomics and drug response. The New England journal of medicine. 2011. Wang Liewei, et al. PubMed
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Impact of ABCG2 polymorphisms on the clinical outcome and toxicity of gefitinib in non-small-cell lung cancer patients. Pharmacogenomics. 2011. Lemos Clara, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Practical recommendations for pharmacogenomics-based prescription: 2010 ESF-UB Conference on Pharmacogenetics and Pharmacogenomics. Pharmacogenomics. 2011. Becquemont Laurent, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Pharmacogenetic tests in cancer chemotherapy: what physicians should know for clinical application. The Journal of pathology. 2011. Lee Soo-Youn, et al. PubMed
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Systematic review of pharmacoeconomic studies of pharmacogenomic tests. Pharmacogenomics. 2010. Beaulieu Mathieu, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Impact of functional ABCG2 polymorphisms on the adverse effects of gefitinib in Japanese patients with non-small-cell lung cancer. Cancer chemotherapy and pharmacology. 2010. Akasaka Keiichi, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Gefitinib or chemotherapy for non-small-cell lung cancer with mutated EGFR. The New England journal of medicine. 2010. Maemondo Makoto, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Targeted cancer therapies in the twenty-first century: lessons from imatinib. Clinical pharmacology and therapeutics. 2010. Stegmeier F, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Acquired resistance to gefitinib: the contribution of mechanisms other than the T790M, MET, and HGF status. Lung cancer (Amsterdam, Netherlands). 2010. Onitsuka Takamitsu, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Pharmacogenomics of membrane transporters: past, present and future. Pharmacogenomics. 2010. Yee Sook Wah, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Effective global drug development strategy for obtaining regulatory approval in Japan in the context of ethnicity-related drug response factors. Clinical pharmacology and therapeutics. 2010. Ichimaru K, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Predictors of gefitinib outcomes in advanced non-small cell lung cancer (NSCLC): study of a comprehensive panel of molecular markers. Lung cancer (Amsterdam, Netherlands). 2010. Tiseo Marcello, et al. PubMed
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Molecular predictors of outcome with gefitinib and docetaxel in previously treated non-small-cell lung cancer: data from the randomized phase III INTEREST trial. Journal of clinical oncology : official journal of the American Society of Clinical Oncology. 2010. Douillard Jean-Yves, et al. PubMed
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Gefitinib versus cisplatin plus docetaxel in patients with non-small-cell lung cancer harbouring mutations of the epidermal growth factor receptor (WJTOG3405): an open label, randomised phase 3 trial. The lancet oncology. 2010. Mitsudomi Tetsuya, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Preexistence and clonal selection of MET amplification in EGFR mutant NSCLC. Cancer cell. 2010. Turke Alexa B, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Comparison of the drug-drug interactions potential of erlotinib and gefitinib via inhibition of UDP-glucuronosyltransferases. Drug metabolism and disposition: the biological fate of chemicals. 2010. Liu Yong, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Clinicopathologic and molecular features of epidermal growth factor receptor T790M mutation and c-MET amplification in tyrosine kinase inhibitor-resistant Chinese non-small cell lung cancer. Pathology oncology research : POR. 2009. Chen Hua-Jun, et al. PubMed
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Polymorphisms of EGFR predict clinical outcome in advanced non-small-cell lung cancer patients treated with Gefitinib. Lung cancer (Amsterdam, Netherlands). 2009. Ma Fei, et al. PubMed
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Gefitinib or carboplatin-paclitaxel in pulmonary adenocarcinoma. The New England journal of medicine. 2009. Mok Tony S, et al. PubMed
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Cytochrome P450 2D6. Pharmacogenetics and genomics. 2009. Owen Ryan P, et al. PubMed
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Prospective phase II study of gefitinib in non-small cell lung cancer with epidermal growth factor receptor gene mutations. Lung cancer (Amsterdam, Netherlands). 2009. Sugio Kenji, et al. PubMed
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Effects of erlotinib in EGFR mutated non-small cell lung cancers with resistance to gefitinib. Clinical cancer research : an official journal of the American Association for Cancer Research. 2008. Costa Daniel B, et al. PubMed
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Detection of mutations in EGFR in circulating lung-cancer cells. The New England journal of medicine. 2008. Maheswaran Shyamala, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
CYP450 pharmacogenetics for personalizing cancer therapy. Drug resistance updates : reviews and commentaries in antimicrobial and anticancer chemotherapy. 2008. van Schaik Ron H N. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
First-line gefitinib in patients with advanced non-small-cell lung cancer harboring somatic EGFR mutations. Journal of clinical oncology : official journal of the American Society of Clinical Oncology. 2008. Sequist Lecia V, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Tumor suppressor FUS1 signaling pathway. Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer. 2008. Ji Lin, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Epidermal growth factor receptor polymorphisms and clinical outcomes in non-small-cell lung cancer patients treated with gefitinib. The pharmacogenomics journal. 2008. Liu G, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
The effects of CYP3A4 inhibition on erlotinib pharmacokinetics: computer-based simulation (SimCYP) predicts in vivo metabolic inhibition. European journal of clinical pharmacology. 2008. Rakhit Ashok, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Pharmacogenetics of EGFR and VEGF inhibition. Drug discovery today. 2007. Pander Jan, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
MET amplification occurs with or without T790M mutations in EGFR mutant lung tumors with acquired resistance to gefitinib or erlotinib. Proceedings of the National Academy of Sciences of the United States of America. 2007. Bean James, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Evaluation of epidermal growth factor receptor mutation status in serum DNA as a predictor of response to gefitinib (IRESSA). British journal of cancer. 2007. Kimura H, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
The epidermal growth factor receptor intron1 (CA) n microsatellite polymorphism is a potential predictor of treatment outcome in patients with advanced lung cancer treated with Gefitinib. European journal of pharmacology. 2007. Nie Qiang, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Epidermal growth factor receptor mutations and their correlation with gefitinib therapy in patients with non-small cell lung cancer: a meta-analysis based on updated individual patient data from six medical centers in mainland China. Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer. 2007. Wu Yi-Long, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Intron 1 CA dinucleotide repeat polymorphism and mutations of epidermal growth factor receptor and gefitinib responsiveness in non-small-cell lung cancer. Pharmacogenetics and genomics. 2007. Han Sae-Won, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
MET amplification leads to gefitinib resistance in lung cancer by activating ERBB3 signaling. Science (New York, N.Y.). 2007. Engelman Jeffrey A, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Combination of EGFR gene copy number and protein expression predicts outcome for advanced non-small-cell lung cancer patients treated with gefitinib. Annals of oncology : official journal of the European Society for Medical Oncology / ESMO. 2007. Hirsch F R, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Predictive factors associated with prolonged survival in patients with advanced non-small-cell lung cancer (NSCLC) treated with gefitinib. British journal of cancer. 2007. Satouchi M, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
A phase II and pharmacodynamic study of gefitinib in patients with refractory or recurrent epithelial ovarian cancer. Cancer. 2007. Posadas Edwin M, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Association of variant ABCG2 and the pharmacokinetics of epidermal growth factor receptor tyrosine kinase inhibitors in cancer patients. Cancer biology & therapy. 2007. Li Jing, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
The impact of epidermal growth factor receptor gene status on gefitinib-treated Japanese patients with non-small-cell lung cancer. International journal of cancer. Journal international du cancer. 2007. Ichihara Shuji, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Response to treatment and survival of patients with non-small cell lung cancer undergoing somatic EGFR mutation testing. The oncologist. 2007. Sequist Lecia V, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Gefitinib for non-small-cell lung cancer patients with epidermal growth factor receptor gene mutations screened by peptide nucleic acid-locked nucleic acid PCR clamp. British journal of cancer. 2006. Sutani A, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Liver toxicity after treatment with gefitinib and anastrozole: drug-drug interactions through cytochrome p450?. Journal of clinical oncology : official journal of the American Society of Clinical Oncology. 2006. Carlini Paolo, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Pharmacogenetics of ABCG2 and adverse reactions to gefitinib. Journal of the National Cancer Institute. 2006. Cusatis George, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Novel D761Y and common secondary T790M mutations in epidermal growth factor receptor-mutant lung adenocarcinomas with acquired resistance to kinase inhibitors. Clinical cancer research : an official journal of the American Association for Cancer Research. 2006. Balak Marissa N, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Clinical predictors versus epidermal growth factor receptor mutation in gefitinib-treated non-small-cell lung cancer patients. Lung cancer (Amsterdam, Netherlands). 2006. Han Sae-Won, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Novel heteroduplex method using small cytology specimens with a remarkably high success rate for analysing EGFR gene mutations with a significant correlation to gefitinib efficacy in non-small-cell lung cancer. British journal of cancer. 2006. Oshita F, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Analysis of epidermal growth factor receptor gene mutation in patients with non-small cell lung cancer and acquired resistance to gefitinib. Clinical cancer research : an official journal of the American Association for Cancer Research. 2006. Kosaka Takayuki, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Evaluation of the epidermal growth factor receptor gene mutation and copy number in non-small cell lung cancer with gefitinib therapy. Oncology reports. 2006. Endo Katsuhiko, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Presence of epidermal growth factor receptor gene T790M mutation as a minor clone in non-small cell lung cancer. Cancer research. 2006. Inukai Michio, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Gefitinib modulates the function of multiple ATP-binding cassette transporters in vivo. Cancer research. 2006. Leggas Markos, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Exploring the relationship between expression of cytochrome P450 enzymes and gefitinib pharmacokinetics. Clinical pharmacokinetics. 2006. Swaisland Helen C, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Inherited susceptibility to lung cancer may be associated with the T790M drug resistance mutation in EGFR. Nature genetics. 2005. Bell Daphne W, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Epidermal growth factor receptor mutations and gene amplification in non-small-cell lung cancer: molecular analysis of the IDEAL/INTACT gefitinib trials. Journal of clinical oncology : official journal of the American Society of Clinical Oncology. 2005. Bell Daphne W, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Side effects related to cancer treatment: CASE 1. Hepatitis following treatment with gefitinib. Journal of clinical oncology : official journal of the American Society of Clinical Oncology. 2005. Ho Cheryl, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Clinicopathologic significance of the mutations of the epidermal growth factor receptor gene in patients with non-small cell lung cancer. Clinical cancer research : an official journal of the American Association for Cancer Research. 2005. Tomizawa Yoshio, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Activating mutations in the tyrosine kinase domain of the epidermal growth factor receptor are associated with improved survival in gefitinib-treated chemorefractory lung adenocarcinomas. Clinical cancer research : an official journal of the American Association for Cancer Research. 2005. Taron Miguel, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Epithelial membrane protein-1 is a biomarker of gefitinib resistance. Proceedings of the National Academy of Sciences of the United States of America. 2005. Jain Anjali, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Mutation in the tyrosine kinase domain of epidermal growth factor receptor is a predictive and prognostic factor for gefitinib treatment in patients with non-small cell lung cancer. Clinical cancer research : an official journal of the American Association for Cancer Research. 2005. Chou Teh-Ying, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Acquired resistance of lung adenocarcinomas to gefitinib or erlotinib is associated with a second mutation in the EGFR kinase domain. PLoS medicine. 2005. Pao William, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Cytochrome P450-dependent metabolism of gefitinib. Xenobiotica; the fate of foreign compounds in biological systems. 2005. McKillop D, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Pharmacokinetic drug interactions of gefitinib with rifampicin, itraconazole and metoprolol. Clinical pharmacokinetics. 2005. Swaisland Helen C, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Gefitinib enhances the antitumor activity and oral bioavailability of irinotecan in mice. Cancer research. 2004. Stewart Clinton F, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Pharmacokinetics of gefitinib, an epidermal growth factor receptor tyrosine kinase inhibitor, in rat and dog. Xenobiotica; the fate of foreign compounds in biological systems. 2004. McKillop D, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
EGF receptor gene mutations are common in lung cancers from "never smokers" and are associated with sensitivity of tumors to gefitinib and erlotinib. Proceedings of the National Academy of Sciences of the United States of America. 2004. Pao William, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
High-affinity interaction of tyrosine kinase inhibitors with the ABCG2 multidrug transporter. Molecular pharmacology. 2004. Ozvegy-Laczka Csilla, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
EGFR mutations in lung cancer: correlation with clinical response to gefitinib therapy. Science (New York, N.Y.). 2004. Paez J Guillermo, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Activating mutations in the epidermal growth factor receptor underlying responsiveness of non-small-cell lung cancer to gefitinib. The New England journal of medicine. 2004. Lynch Thomas J, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
United States Food and Drug Administration Drug Approval summary: Gefitinib (ZD1839; Iressa) tablets. Clinical cancer research : an official journal of the American Association for Cancer Research. 2004. Cohen Martin H, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Targeting the epidermal growth factor receptor in non-small cell lung cancer. Clinical cancer research : an official journal of the American Association for Cancer Research. 2003. Herbst Roy S, et al. PubMed

LinkOuts

Web Resource:
Wikipedia
National Drug Code Directory:
0310-0482-30
DrugBank:
DB00317
PDB:
IRE
ChEBI:
49668
KEGG Drug:
D01977
PubChem Compound:
123631
PubChem Substance:
46508649
7849039
Drugs Product Database (DPD):
2248676
BindingDB:
5447
ChemSpider:
110217
HET:
IRE
Therapeutic Targets Database:
DAP000657
FDA Drug Label at DailyMed:
827d60e8-7e07-41b7-c28b-49ef1c4a5a41

Clinical Trials

These are trials that mention gefitinib and are related to either pharmacogenetics or pharmacogenomics.

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NURSA Datasets

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No NURSA datasets available.

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Sources for PharmGKB drug information: DrugBank, PubChem.