Drug/Small Molecule:
docetaxel

Overview
Properties
Genetics
Related Genes
Pathways
Related Drugs
Related Diseases
Datasets
Downloads/LinkOuts

Overview

Generic Names:	Docetaxel anhydrous; Docetaxel, Trihydrate; TXL; docetaxel
Trade Names:	Taxotere
PharmGKB Accession Id:	PA449383

Description

Docetaxel is a clinically well established anti-mitotic chemotherapy medication used mainly for the treatment of breast, ovarian, and non-small cell lung cancer. Docetaxel binds to microtubules reversibly with high affinity and has a maximum stoichiometry of 1 mole docetaxel per mole tubulin in microtubules. (source: Drug Bank)

Indication

For the treatment of patients with locally advanced or metastatic breast cancer after failure of prior chemotherapy. Also used as a single agent in the treatment of patients with locally advanced or metastatic non-small cell lung cancer after failure of prior platinum-based chemotherapy. Lastly, for use, in combination with prednisone, in the treatment of patients with androgen independent (hormone refractory) metastatic prostate cancer. (source: Drug Bank)

ATC Therapeutic Category

L01CD:Taxanes

Pharmacology, Interactions, and Contraindications

Mechanism Of Action

Docetaxel interferes with the normal function of microtubule growth. Whereas drugs like colchicine cause the depolymerization of microtubules in vivo, docetaxel arrests their function by having the opposite effect; it hyper-stabilizes their structure. This destroys the cell's ability to use its cytoskeleton in a flexible manner. Specifically, docetaxel binds to the β-subunit of tubulin. Tubulin is the "building block" of mictotubules, and the binding of docetaxel locks these building blocks in place. The resulting microtubule/docetaxel complex does not have the ability to disassemble. This adversely affects cell function because the shortening and lengthening of microtubules (termed dynamic instability) is necessary for their function as a transportation highway for the cell. Chromosomes, for example, rely upon this property of microtubules during mitosis. Further research has indicated that docetaxel induces programmed cell death (apoptosis) in cancer cells by binding to an apoptosis stopping protein called Bcl-2 (B-cell leukemia 2) and thus arresting its function. (source: Drug Bank)

Pharmacology

Docetaxel is a taxoid antineoplastic agent. It promotes the assembly of microtubules from tubulin dimers and stabilizes microtubules by preventing depolymerization. This stability results in the inhibition of the normal dynamic reorganization of the microtubule network that is essential for vital interphase and mitotic cellular functions. In addition, docetaxel induces abnormal arrays or "bundles" of microtubules throughout the cell cycle and multiple asters of microtubules during mitosis. (source: Drug Bank)

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Hepatic. In vitro drug interaction studies revealed that docetaxel is metabolized by the CYP3A4 isoenzyme (1 major, 3 minor metabolites). (source: Drug Bank)

Protein Binding

About 94% protein bound, mainly to a1-acid glycoprotein, albumin, and lipoproteins. (source: Drug Bank)

Toxicity

Oral LD50 in rat is >2000 mg/kg. Anticipated complications of overdosage include: bone marrow suppression, peripheral neurotoxicity, and mucositis. In two reports of overdose, one patient received 150 mg/m2 and the other received 200 mg/m2 as 1-hour infusions. Both patients experienced severe neutropenia, mild asthenia, cutaneous reactions, and mild paresthesia, and recovered without incident. (source: Drug Bank)

Isomeric SMILES Code:

CC1=C2[C@H](C(=O)[C@@]3([C@H](C[C@@H]4[C@]([C@H]3[C@@H]([C@@](C2(C)C)(C[C@@H]1OC(=O)[C@@H]([C@H](c5ccccc5)NC(=O)OC(C)(C)C)O)O)OC(=O)c6ccccc6)(CO4)OC(=O)C)O)C)O (source: Drug Bank)

Curated Annotations ()

rs4646487 at chr1:47051762 in CYP4B1
Risk or phenotype-associated allele: T Phenotype: The CYP4B1:rs4646487 T variant was associated with toxicity in response to docetaxel and thalidomide. Study size: 47 Study population/ethnicity: Patients diagnosed with castration-resistant prostate cancer enrolled in a randomized phase II clinical trial comparing docetaxel to docetaxel with thalidomide. Significance metric(s):p = 0.008 Type of association: CO; TOX

Variant Name:

CYP4B1:rs4646487 C>T; NM_000779.3:c.517C>T; NP_000770.2:p.Arg173Trp

Related Drugs:

docetaxel, thalidomide

Related Diseases:

Prostatic Neoplasms

Evidence:

PMID:20038957
rs2253316 at chr1:91934103 in TGFBR3
Risk or phenotype-associated allele: Not specified. Phenotype: This SNP was associated with clearance of docetaxel. Study size: 31. Study population/ethnicity: Patients with Non-Small-Cell Lung Carcinoma. Significance metric(s): p = 0.0998 (ANOVA); p = 0.2400 (QMIS); p = 0.0021 (KW) Type of association: PK.

Variant Name:

rs2253316 A/T TGFBR3

Related Drugs:

docetaxel

Evidence:

PMID:20157331
rs2234922 at chr1:224093029 in EPHX1
Risk or phenotype-associated allele: A. Phenotype: The AA homozygote was associated with higher clearance of docetaxel. Study size: 31. Study population/ethnicity: Patients with Non-Small-Cell Lung Carcinoma. Significance metric(s): Type of association: PK.

Variant Name:

2234922 A/G EPHX1

Related Drugs:

docetaxel

Evidence:

PMID:20157331
rs1056836 at chr2:38151707 in CYP1B1
In clinical studies of prostate cancer patients treated with docetaxel, CYP1B1*3 was associated with patient survival.

Variant Name:

CYP1B1*3;CYP1B1:4326 C>G; CYP1B1:L432V

Related Drugs:

docetaxel

Related Diseases:

Prostatic Neoplasms

Evidence:

PMID:18187806
rs2236930 at chr2:101992312 in IL1R2
Risk or phenotype-associated allele: Not specified. Phenotype: This SNP was associated with clearance of docetaxel. Study size: 31. Study population/ethnicity: Patients with Non-Small-Cell Lung Carcinoma. Significance metric(s): p = 0.0045 (ANOVA); p = 0.052 (QMIS); p = 0.0004 (KW) Type of association: PK.

Variant Name:

rs2236930 A/T IL1R2

Related Drugs:

docetaxel

Evidence:

PMID:20157331
rs1402467 at chr2:108361240 in SULT1C4
Risk or phenotype-associated allele: G Phenotype: The SULT1C2: rs1402467 G variant was associated with positive clincial response (partial or complete response) to treatment. Study size: 47 Study population/ethnicity: Patients diagnosed with castration-resistant prostate cancer enrolled in a randomized phase II clinical trial comparing docetaxel to docetaxel with thalidomide. Significance metric(s): p = 0.0083 Type of association: PD; CO

Variant Name:

SULT1C2:rs1402467 C>G; NM_006588.2:c.15C>G; NP_006579.2:p.Asp5Glu

Related Drugs:

docetaxel, thalidomide

Related Diseases:

Prostatic Neoplasms

Evidence:

PMID:20038957
rs2228001 at chr3:14162450 in TMEM43, XPC
Risk or phenotype-associated allele: Not specified. Phenotype: This SNP was associated with clearance of docetaxel. Study size: 31. Study population/ethnicity: Patients with Non-Small-Cell Lung Carcinoma. Significance metric(s): p = 0.0045 (ANOVA); p = 0.052 (QMIS); p = 0.0004 (KW) Type of association: PK.

Variant Name:

rs2228001 A/C XPC

Related Drugs:

docetaxel

Evidence:

PMID:20157331
rs2607737 at chr3:14168169 in XPC
Risk or phenotype-associated allele: Not specified. Phenotype: This SNP was associated with clearance of docetaxel. Study size: 31. Study population/ethnicity: Patients with Non-Small-Cell Lung Carcinoma. Significance metric(s): p = 0.3743 (ANOVA); p = 0.6323 (QMIS); p < 0.000001 (KW) Type of association: PK.

Variant Name:

rs2607737 T/C XPC

Related Drugs:

docetaxel

Evidence:

PMID:20157331
rs1078985 at chr3:30665915 in TGFBR2
Risk or phenotype-associated allele: Not specified. Phenotype: This SNP was associated with clearance of docetaxel. Study size: 31. Study population/ethnicity: Patients with Non-Small-Cell Lung Carcinoma. Significance metric(s): p = 0.0355 (ANOVA); p = 0.1156 (QMIS); p = 0.0830 (KW) Type of association: PK.

Variant Name:

rs1078985 T/C TGFBR2

Related Drugs:

docetaxel

Evidence:

PMID:20157331
rs701992 at chr3:121805089 in NDUFB4
Risk or phenotype-associated allele: Not specified. Phenotype: This SNP was associated with clearance of docetaxel. Study size: 31. Study population/ethnicity: Patients with Non-Small-Cell Lung Carcinoma. Significance metric(s): p = 0.0114 (ANOVA); p = 0.0341 (QMIS); p = 0.0294 (KW) Type of association: PK.

Variant Name:

rs701992 A/T NDUFB4

Related Drugs:

docetaxel

Evidence:

PMID:20157331
rs870995 at chr3:180395700 in PIK3CA
Risk or phenotype-associated allele: C. Phenotype: This variant was associated with higher clearance of docetaxel. Study size: 31. Study population/ethnicity: Patients with Non-Small-Cell Lung Carcinoma. Significance metric(s): Type of association: PK.

Variant Name:

870995 A/C in PIK3CA

Related Drugs:

docetaxel

Evidence:

PMID:20157331
rs1382368 at chr5:82486831 in XRCC4
Risk or phenotype-associated allele: A. Phenotype: This variant was associated with higher clearance of docetaxel. Study size: 31. Study population/ethnicity: Patients with Non-Small-Cell Lung Carcinoma. Significance metric(s): Type of association: PK.

Variant Name:

1382368 G/A in XRCC4

Related Drugs:

docetaxel

Evidence:

PMID:20157331
rs2842951 at chr6:18243662 in TPMT
Risk or phenotype-associated allele: Not specified. Phenotype: This SNP was associated with clearance of docetaxel. Study size: 31. Study population/ethnicity: Patients with Non-Small-Cell Lung Carcinoma. Significance metric(s): p = 0.1013 (ANOVA); p = 0.0159 (QMIS); p = 0.0178 (KW) Type of association: PK.

Variant Name:

rs2842951 C/T TPMT

Related Drugs:

docetaxel

Evidence:

PMID:20157331
rs6922548 at chr6:35461501 in PPARD
Risk or phenotype-associated allele: G Phenotype: The PPAR delta SNP rs6922548 A>G was associated with positive clincial response (partial or complete response) to treatment. Study size: 47 Study population/ethnicity: Patients diagnosed with castration-resistant prostate cancer enrolled in a randomized phase II clinical trial comparing docetaxel to docetaxel with thalidomide. Significance metric(s): p = 0.0011 Type of association: PD; CO

Variant Name:

PPARD:rs6922548 A>G;

Related Drugs:

docetaxel, thalidomide

Related Diseases:

Prostatic Neoplasms

Evidence:

PMID:20038957
rs7769719 at chr6:35470503 in PPARD
Risk or phenotype-associated allele: G Phenotype: The PPAR delta SNP rs7769719 A>G was associated with positive clincial response (partial or complete response) to treatment. Study size: 47 Study population/ethnicity: Patients diagnosed with castration-resistant prostate cancer enrolled in a randomized phase II clinical trial comparing docetaxel to docetaxel with thalidomide. Significance metric(s): p = 0.0055 Type of association: PD; CO

Variant Name:

PPARD:rs7769719 A>G

Related Drugs:

docetaxel, thalidomide

Related Diseases:

Prostatic Neoplasms

Evidence:

PMID:20038957
rs1883322 at chr6:35477784 in PPARD
Risk or phenotype-associated allele: G Phenotype: The PPAR delta SNP rs1883322 A>G was associated with positive clincial response (partial or complete response) to treatment. Study size: 47 Study population/ethnicity: Patients diagnosed with castration-resistant prostate cancer enrolled in a randomized phase II clinical trial comparing docetaxel to docetaxel with thalidomide. Significance metric(s): p = 0.0061 Type of association: PD; CO

Variant Name:

PPARD:rs1883322 A>G

Related Drugs:

docetaxel, thalidomide

Related Diseases:

Prostatic Neoplasms

Evidence:

PMID:20038957
rs2016520 at chr6:35486756 in PPARD
Risk or phenotype-associated allele: G Phenotype: The PPAR delta SNP rs2016520 A>G was associated with positive clincial response (partial or complete response) to treatment. Study size: 47 Study population/ethnicity: Patients diagnosed with castration-resistant prostate cancer enrolled in a randomized phase II clinical trial comparing docetaxel to docetaxel with thalidomide. Significance metric(s): p = 0.0056 Type of association: PD; CO

Variant Name:

PPARD:rs2016520 A>G; NM_006238.3:c.-87C>T

Related Drugs:

docetaxel, thalidomide

Related Diseases:

Prostatic Neoplasms

Evidence:

PMID:20038957
rs3734254 at chr6:35502988 in PPARD
Risk or phenotype-associated allele: T Phenotype: The PPAR delta SNP rs3734254 C>T was associated with positive clincial response (partial or complete response) to treatment. Study size: 47 Study population/ethnicity: Patients diagnosed with castration-resistant prostate cancer enrolled in a randomized phase II clinical trial comparing docetaxel to docetaxel with thalidomide. Significance metric(s): p = 0.0089 Type of association: PD; CO

Variant Name:

PPARD:rs3734254 C>T

Related Drugs:

docetaxel, thalidomide

Related Diseases:

Prostatic Neoplasms

Evidence:

PMID:20038957
rs1032419 at chr6:52942801
Risk or phenotype-associated allele: Not specified. Phenotype: This SNP was associated with clearance of docetaxel. Study size: 31. Study population/ethnicity: Patients with Non-Small-Cell Lung Carcinoma. Significance metric(s): p = 0.1495 (ANOVA); p = 0.2805 (QMIS); p = 0.0126 (KW) Type of association: PK.

Variant Name:

rs1032419 A/G GSTA4

Related Drugs:

docetaxel

Evidence:

PMID:20157331
rs2032582 at chr7:86998554 in ABCB1
Patients with epithelial ovarian cancer, with this variant, have been associated with response to taxane- and platinum-based therapy and gastrointestinal toxicity.

Variant Name:

ABCB1: 2677G>T/A

Related Drugs:

carboplatin, cisplatin, docetaxel, paclitaxel, taxanes

Related Diseases:

Ovarian Neoplasms

Evidence:

PMID:19203783
rs2740574 at chr7:99220032 in CYP3A, CYP3A4
Patients with CYP3A4*1B (vs ref) had greater clearance of docetaxel

Variant Name:

CYP3A4*1B; CYP3A4:-392A>G

Related Drugs:

docetaxel

Evidence:

PMID:18509327
rs1799931 at chr8:18302650 in NAT2
Risk or phenotype-associated allele: G Phenotype: The NAT2:rs1799931 G variant was associated with toxicity in response to docetaxel and thalidomide. Study size: 47 Study population/ethnicity: Patients diagnosed with castration-resistant prostate cancer enrolled in a randomized phase II clinical trial comparing docetaxel to docetaxel with thalidomide. Significance metric(s): p = 0.003 Type of association: CO; TOX

Variant Name:

NAT2:rs1799931 A>G; NM_000015.2:c.857G>A; NP_000006.2:p.Gly286Glu

Related Drugs:

docetaxel, thalidomide

Related Diseases:

Prostatic Neoplasms

Evidence:

PMID:20038957
rs4148943 at chr10:73439513 in CHST3
Risk or phenotype-associated allele: C Phenotype: The CHST3:rs4148943 C variant was associated with positive clincial response (partial or complete response) to treatment. Study size: 47 Study population/ethnicity: Patients diagnosed with castration-resistant prostate cancer enrolled in a randomized phase II clinical trial comparing docetaxel to docetaxel with thalidomide. Significance metric(s): p = 0.0001 Type of association: PD; CO

Variant Name:

CHST3:rs4148943 C>T; NM_004273.3:c.*1278C>T

Related Drugs:

docetaxel, thalidomide

Related Diseases:

Prostatic Neoplasms

Evidence:

PMID:20038957
rs4148945 at chr10:73439596 in CHST3
Risk or phenotype-associated allele: C Phenotype: The CHST3:rs4148945 C variant was associated with positive clincial response (partial or complete response) to treatment and toxicity to docetaxel and thalidomide. Study size: 47 Study population/ethnicity: Patients diagnosed with castration-resistant prostate cancer enrolled in a randomized phase II clinical trial comparing docetaxel to docetaxel with thalidomide. Significance metric(s): p = 0.011 (response); p = 0.010 (TOX) Type of association: PD; CO; TOX

Variant Name:

CHST3:rs4148945 C>T; NM_004273.3:c.*1361C>T

Related Drugs:

docetaxel, thalidomide

Related Diseases:

Prostatic Neoplasms

Evidence:

PMID:20038957
rs4148947 at chr10:73440123 in CHST3
Risk or phenotype-associated allele: C Phenotype: The CHST3:rs4148947 C variant was associated with positive clincial response (partial or complete response) to treatment. Study size: 47 Study population/ethnicity: Patients diagnosed with castration-resistant prostate cancer enrolled in a randomized phase II clinical trial comparing docetaxel to docetaxel with thalidomide. Significance metric(s): p = 0.0023 Type of association: PD; CO

Variant Name:

CHST3:rs4148947 C>T; NM_004273.3:c.*1888T>C

Related Drugs:

docetaxel, thalidomide

Related Diseases:

Prostatic Neoplasms

Evidence:

PMID:20038957
rs4148950 at chr10:73441712 in CHST3
Risk or phenotype-associated allele: A Phenotype: The CHST3:rs4148950 A variant was associated with positive clincial response (partial or complete response) to treatment and toxicity to docetaxel and thalidomide. Study size: 47 Study population/ethnicity: Patients diagnosed with castration-resistant prostate cancer enrolled in a randomized phase II clinical trial comparing docetaxel to docetaxel with thalidomide. Significance metric(s):p = 0.024 (response); p = 0.006 (TOX) Type of association: PD; CO; TOX

Variant Name:

CHST3:rs4148950 A>G; NM_004273.3:c.*3477G>A

Related Drugs:

docetaxel, thalidomide

Related Diseases:

Prostatic Neoplasms

Evidence:

PMID:20038957
rs1871450 at chr10:73442020 in CHST3
Risk or phenotype-associated allele: A Phenotype: The CHST3:rs1871450 A variant was associated with positive clincial response (partial or complete response) to treatment and toxicity to docetaxel and thalidomide. Study size: 47 Study population/ethnicity: Patients diagnosed with castration-resistant prostate cancer enrolled in a randomized phase II clinical trial comparing docetaxel to docetaxel with thalidomide. Significance metric(s): p = 0.048 (response); p = 0.006 (TOX) Type of association: PD; CO; TOX

Variant Name:

CHST3:rs1871450 A>G; NM_004273.3:c.*3785G>A

Related Drugs:

docetaxel, thalidomide

Related Diseases:

Prostatic Neoplasms

Evidence:

PMID:20038957
rs730720 at chr10:73442768 in CHST3
Risk or phenotype-associated allele: A Phenotype: The CHST3:rs730720 A variant was associated with positive clincial response (partial or complete response) to treatment. Study size: 47 Study population/ethnicity: Patients diagnosed with castration-resistant prostate cancer enrolled in a randomized phase II clinical trial comparing docetaxel to docetaxel with thalidomide. Significance metric(s): p = 0.0034 Type of association: PD; CO

Variant Name:

CHST3:rs730720 A>G; NM_004273.3:c.*4533C>T

Related Drugs:

docetaxel, thalidomide

Related Diseases:

Prostatic Neoplasms

Evidence:

PMID:20038957
rs12418 at chr10:73443020 in CHST3
Risk or phenotype-associated allele: A Phenotype: The CHST3:rs12418 A variant was associated with positive clincial response (partial or complete response) to treatment. Study size: 47 Study population/ethnicity: Patients diagnosed with castration-resistant prostate cancer enrolled in a randomized phase II clinical trial comparing docetaxel to docetaxel with thalidomide. Significance metric(s): p = 0.0005 Type of association: PD; CO

Variant Name:

CHST3:rs12418 A>G; NM_004273.3:c.*4785G>A

Related Drugs:

docetaxel, thalidomide

Related Diseases:

Prostatic Neoplasms

Evidence:

PMID:20038957
rs1341164 at chr10:96790863 in CYP2C8
Risk or phenotype-associated allele: Not specified. Phenotype: This SNP was associated with clearance of docetaxel. Study size: 31. Study population/ethnicity: Patients with Non-Small-Cell Lung Carcinoma. Significance metric(s): p = 0.0097 (ANOVA); p = 0.0013 (QMIS); p = 0.0040 (KW) Type of association: PK.

Variant Name:

rs1341164 T/C CYP2C8

Related Drugs:

docetaxel

Evidence:

PMID:20157331
rs12762549 at chr10:101610761
A case-control association study in 84 patients who received docetaxel chemotherapy found a significant association of rs12762549 in ABCC2 with docetaxel-induced leukopenia/neutropenia.

Related Drugs:

docetaxel

Related Diseases:

Leukopenia, Neutropenia

Evidence:

PMID:18294295
rs12762549 at chr10:101610761
In a case control study using samples from BioBank Japan, the G allele of rs12762549 was associated with docetaxel-induced leukopenia/neutropenia.

Related Drugs:

docetaxel

Related Diseases:

Leukopenia, Neutropenia

Evidence:

PMID:18294295
rs2230949 at chr11:2110764 in IGF2, IGF2AS, INS-IGF2
Risk or phenotype-associated allele: Not specified. Phenotype: This SNP was associated with clearance of docetaxel. Study size: 31. Study population/ethnicity: Patients with Non-Small-Cell Lung Carcinoma. Significance metric(s): p = 0.0043 (ANOVA); p = 0.0261 (QMIS); p = 0.0622 (KW) Type of association: PK.

Variant Name:

rs2230949 C/T IGF2

Related Drugs:

docetaxel

Evidence:

PMID:20157331
rs11045585 at chr12:20936961 in SLCO1B3
A case-control association study in 84 patients who received docetaxel chemotherapy found a significant association of rs11045585 in SLCO1B3 with docetaxel-induced leukopenia/neutropenia.

Related Drugs:

docetaxel

Related Diseases:

Leukopenia, Neutropenia

Evidence:

PMID:18294295
rs2301159 at chr13:102495729 in SLC10A2
Risk or phenotype-associated allele: T Phenotype: The SLC10A2:rs2301159 T variant was associated with toxicity in response to docetaxel and thalidomide. Study size: 47 Study population/ethnicity: Patients diagnosed with castration-resistant prostate cancer enrolled in a randomized phase II clinical trial comparing docetaxel to docetaxel with thalidomide. Significance metric(s): p = 0.01 Type of association: CO; TOX

Variant Name:

SLC10A2:rs2301159 C>T; NM_000452.2:c.*755C>T

Related Drugs:

docetaxel, thalidomide

Related Diseases:

Prostatic Neoplasms

Evidence:

PMID:20038957
rs2238472 at chr16:16159100 in ABCC6
Risk or phenotype-associated allele: G Phenotype: The ABCC6 rs2238472 G variant was associated with toxicity in response to docetaxel and thalidomide. Study size: 47 Study population/ethnicity: Patients diagnosed with castration-resistant prostate cancer enrolled in a randomized phase II clinical trial comparing docetaxel to docetaxel with thalidomide. Significance metric(s): p = 0.006 Type of association: CO; TOX

Variant Name:

ABCC6:rs2238472 A>G; NM_001171.5:c.3803G>A; NP_001162.4:p.Arg1268Gln

Related Drugs:

docetaxel, thalidomide

Related Diseases:

Prostatic Neoplasms

Evidence:

PMID:20038957
rs2292954 at chr16:88140624 in SPG7
Risk or phenotype-associated allele: T Phenotype: The SPG7:rs2292954 T variant was associated with toxicity in response to docetaxel and thalidomide. Study size: 47 Study population/ethnicity: Patients diagnosed with castration-resistant prostate cancer enrolled in a randomized phase II clinical trial comparing docetaxel to docetaxel with thalidomide. Significance metric(s): p = 0.0004 Type of association: CO; TOX

Variant Name:

SPG7:rs2292954 C>T; NM_003119.2:c.1507A>G; NP_003110.1:p.Thr503Ala

Related Drugs:

docetaxel, thalidomide

Related Diseases:

Prostatic Neoplasms

Evidence:

PMID:20038957
rs12960 at chr16:88147829 in RPL13, SNORD68, SPG7
Risk or phenotype-associated allele: G Phenotype: The SPG7:rs12960 G variant was associated with toxicity in response to docetaxel and thalidomide. Study size: 47 Study population/ethnicity: Patients diagnosed with castration-resistant prostate cancer enrolled in a randomized phase II clinical trial comparing docetaxel to docetaxel with thalidomide. Significance metric(s): p = 0.004 Type of association: CO; TOX

Variant Name:

SPG7:rs12960 A>G; NM_003119.2:c.2063G>A; NP_003110.1:p.Arg688Gln

Related Drugs:

docetaxel, thalidomide

Related Diseases:

Prostatic Neoplasms

Evidence:

PMID:20038957
rs1042865 at chr17:19227198 in MAPK7, MFAP4
Risk or phenotype-associated allele: Not specified. Phenotype: This SNP was associated with clearance of docetaxel. Study size: 31. Study population/ethnicity: Patients with Non-Small-Cell Lung Carcinoma. Significance metric(s): p = 0.0240 (ANOVA); p = 0.0084 (QMIS); p = 0.0534 (KW) Type of association: PK.

Variant Name:

rs1042865 C/T MAPK7

Related Drugs:

docetaxel

Evidence:

PMID:20157331
rs518329 at chrX:23605157 in PRDX4
Risk or phenotype-associated allele: A. Phenotype: The AA homozygote was associated with lower clearance of docetaxel. Study size: 31. Study population/ethnicity: Patients with Non-Small-Cell Lung Carcinoma. Significance metric(s): Type of association: PK.

Variant Name:

518329 A/G PRDX4

Related Drugs:

docetaxel

Evidence:

PMID:20157331
rs795491 at chrX:23608784 in PRDX4
Risk or phenotype-associated allele: Not specified. Phenotype: This SNP was associated with clearance of docetaxel. Study size: 31. Study population/ethnicity: Patients with Non-Small-Cell Lung Carcinoma. Significance metric(s): p = 0.0203 (ANOVA); p = 0.0552 (QMIS); p = 0.0003 (KW) Type of association: PK.

Variant Name:

rs795491 T/A PRDX4

Related Drugs:

docetaxel

Evidence:

PMID:20157331
rs2227291 at chrX:77155158 in ATP7A
Risk or phenotype-associated allele: G Phenotype: The ATP7A:rs2227291 G variant was associated with toxicity in response to docetaxel and thalidomide. Study size: 47 Study population/ethnicity: Patients diagnosed with castration-resistant prostate cancer enrolled in a randomized phase II clinical trial comparing docetaxel to docetaxel with thalidomide. Significance metric(s): p = 0.006 Type of association: CO; TOX

Variant Name:

ATP7A:rs2227291 C>G; NM_000052.4:c.2299G>C; NP_000043.3:p.Val767Leu

Related Drugs:

docetaxel, thalidomide

Related Diseases:

Prostatic Neoplasms

Evidence:

PMID:20038957

Variant names are different names that have been used in the literature and other resources to refer to the same variant.

The following genes are in curated knowledge about this drug.

view legend

Gene	Relationship	Evidence
ABCB1	CO PK FA GN	Publications, Variants
ABCC1	CO PK GN	Publications
ABCC2	CO PK GN	Publications
ABCC5	FA	Publications
ABCC6	CO PK GN	Publications, Variants
ABCC8	FA	Publications
ABCG2	CO PK GN	Publications
APAF1	FA	Publications
ATP7A	CO PK GN	Publications, Variants
ATP7B	FA	Publications
BCL2	CO PD PK FA GN	Publications
BCL2L1	FA	Publications
BRCA2	CO	Publications
CDKN1A	CO FA GN	Publications
CDKN1B	FA	Publications
CHST3	CO PD PK GN	Publications, Variants
CYP1B1	CO PD PK FA GN	Publications, Variants
CYP2A6	CO GN	Publications
CYP2B6	PK GN	Publications
CYP2C18	PK GN	Publications
CYP2C19	PK GN	Publications
CYP2C8	CO PK GN	Publications, Variants
CYP2C9	PK GN	Publications
CYP2D6	CO PK GN	Publications
CYP2E1	PK GN	Publications
CYP2F1	PK GN	Publications
CYP3A	PK GN	Publications, Variants
CYP3A4	CO PK GN	Publications, Variants
CYP3A5	CO PK GN	Publications
CYP3A7	PK GN	Publications
CYP4B1	CO PK GN	Publications, Variants
DPYD	PK GN	Publications
EGF	PK GN	Publications
EGFR	PK GN	Publications
EPHX1	PK GN	Publications, Variants
EPHX2	PK GN	Publications
ERBB2	CO FA	Publications
ERCC4	CO FA	Publications
GSTA2	PK GN	Publications
GSTA3	PK GN	Publications
GSTA4	PK GN	Publications
GSTM1	PK GN	Publications
GSTM5	PK GN	Publications
GSTP1	PK FA GN	Publications
GSTT2	PK GN	Publications
IGF2	PK GN	Publications, Variants
IGF2AS		Variants
IGFBP1	FA	Publications
IGFBP2	FA	Publications
IL1R2	PK GN	Publications, Variants
INS-IGF2		Variants
MAPK7	PK GN	Publications, Variants
MAPT	CO GN	Publications
MFAP4		Variants
MLH1	FA	Publications
MTHFR	CO FA	Publications
NAT2	CO PK GN	Publications, Variants
NDUFB4	PK GN	Publications, Variants
NR1I2	FA	Publications
PIK3CA	PK GN	Publications, Variants
PPARD	CO PD GN	Publications, Variants
PRDX4	PK GN	Publications, Variants
PTEN	FA	Publications
RPL13		Variants
RPN2	CO FA	Publications
SLC10A2	CO PK GN	Publications, Variants
SLCO1B3	CO FA GN	Publications, Variants
SNORD68		Variants
SPG7	CO PK GN	Publications, Variants
SULT1C2	CO PD GN	Publications
SULT1C4		Variants
TGFBR2	PK GN	Publications, Variants
TGFBR3	PK GN	Publications, Variants
TMEM43		Variants
TNFAIP2	PK GN	Publications
TP53	CO FA GN	Publications
TPMT	PK GN	Publications, Variants
TUBB	CO PD	Publications
WDR7	CO FA	Publications
XPC	PK GN	Publications, Variants
XRCC4	PK GN	Publications, Variants

A list of non-curated publications that mention this drug along with other genes is available.

Drug Targets

Gene		Description
BCL2		(source: Drug Bank)
TUBB1		(source: Drug Bank)

PharmGKB Curated Pathways

Taxane Pathway

The following drugs are in curated knowledge about this drug.

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Drug	Relationship	Evidence
cyclosporine	PK	Publications
ketoconazole	PK	Publications
ritonavir	PK	Publications

A list of non-curated publications that mention this drug along with other drugs is available.

Drug Interactions

Drug		Description
erythromycin		The agent increases the serum levels and toxicity of docetaxel (source: Drug Bank)
ketoconazole		The agent increases the serum levels and toxicity of docetaxel (source: Drug Bank)
midazolam		The agent increases the serum levels and toxicity of docetaxel (source: Drug Bank)
orphenadrine		The agent increases the serum levels and toxicity of docetaxel (source: Drug Bank)
testosterone		The agent increases the serum levels and toxicity of docetaxel (source: Drug Bank)

Curated Information

The following diseases are in curated knowledge about this drug.

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Disease	Relationship	Evidence
Breast Neoplasms	CO PD FA GN	Publications
Carcinoma, Non-Small-Cell Lung	PK FA GN	Publications
Head and Neck Neoplasms	CO	Publications
Leukopenia	CO GN	Publications, Variants
Lung Neoplasms	CO PK FA GN	Publications
Neoplasms	CO PK GN	Publications
Ovarian Neoplasms	CO FA	Publications, Variants
Prostatic Neoplasms	CO PD PK FA GN	Publications, Variants
Stomach Neoplasms	CO GN	Publications

Non-Curated Information

A list of non-curated publications that mention this drug along with other diseases is available.

Curated Phenotype Datasets

These datasets are sorted alphabetically by title.

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Cytotoxicity of docetaxel in the CEPH population
- FA
Submitted by Howard McLeod, PharmD involving docetaxel
Midazolam and docetaxel clearance
- PK
Submitted by Mary Relling, PharmD involving ABCB1, CYP3A4, CYP3A5, docetaxel, midazolam, and Neoplastic Processes

Additional Datasets

These datasets are minimally curated and are sorted alphabetically by title.

Downloads

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LinkOuts

Web Resource:: Wikipedia
DrugBank:: DB01248
KEGG Compound ID:: C11231
PubChem Compound ID:: 148124
PubChem Substance ID:: 13410

Common Searches

Search PubMed
Search Medline Plus
Search PubChem
Search CTD

Non-Curated Publications

A list of non-curated publications that mention this drug is available.

PharmGKB integrates drug information from different sources: DrugBank, Open Eye Scientific Software.

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Drug/Small Molecule: docetaxel

Overview

Description

Indication

ATC Therapeutic Category

Pharmacology, Interactions, and Contraindications

Mechanism Of Action

Pharmacology

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Protein Binding

Toxicity

Isomeric SMILES Code:

Curated Annotations ()

Drug Targets

PharmGKB Curated Pathways

Drug Interactions

Curated Information

Non-Curated Information

Curated Phenotype Datasets

Additional Datasets

Downloads

LinkOuts

Common Searches

Non-Curated Publications

Drug/Small Molecule:
docetaxel