Chemical: Drug
rituximab

PharmGKB contains no dosing guidelines for this . To report known genotype-based dosing guidelines, or if you are interested in developing guidelines, click here.


Annotated Labels

  1. FDA Label for rituximab and MS4A1
  2. EMA Label for rituximab and MS4A1

last updated 01/14/2014

1. FDA Label for rituximab and MS4A1

Informative PGx

Summary

Rituximab (Rituxan) is used to treat patients with non-Hodgkin's lymphoma, chronic lymphocytic leukemia, rheumatoid arthritis or granulomatosis polyangiitis and microscopic polyangiitis. The drug is a CD20-directed cytolytic monoclonal antibody, but there is no association with genetic variation within the coding gene, MS4A1, and therefore no mention of genetic testing in the drug label.

Annotation

Rituximab (Rituxan) binds to the CD20 molecule, which is expressed on pre-B and mature B lymphocytes, and on B-cell non-Hodkin's lymphomas. CD20 is coded for by the MS4A1 gene.

Excerpts from the Rituximab (Rituxan) drug label:

Rituxan ® (rituximab) is a CD20-directed cytolytic antibody indicated for the treatment of patients with...Non-Hodgkin's Lymphoma...Chronic Lymphocytic Leukemia...Rheumatoid Arthritis...Granulomatosis with Polyangiitis...and Microscopic Polyangiitis.

Rituximab binds specifically to the antigen CD20 (human B-lymphocyte-restricted differentiation antigen, Bp35), a hydrophobic transmembrane protein...located on pre-B and mature B lymphocytes. The antigen is expressed on >90% of B-cell non-Hodgkin's lymphomas, but... is not found on hematopoietic stem cells, pro-B-cells, normal plasma cells or other normal tissues.

For the complete drug label text with sections containing pharmacogenetic information highlighted, see the rituximab drug label.

*Disclaimer: The contents of this page have not been endorsed by the FDA and are the sole responsibility of PharmGKB.

Full label available at DailyMed

Genes and/or phenotypes found in this label

  • Arthritis, Rheumatoid
    • Adverse reactions section
    • source: PHONT
  • Leukemia, Lymphocytic, Chronic, B-Cell
    • Indications & usage section, Adverse reactions section
    • source: PHONT
  • Lymphoma, Follicular
    • Indications & usage section, Warnings section, Adverse reactions section
    • source: PHONT
  • Lymphoma, Non-Hodgkin
    • Indications & usage section, Warnings section, Adverse reactions section
    • source: PHONT
  • Waldenstrom Macroglobulinemia
    • Adverse reactions section
    • source: PHONT
  • CRP
    • other, Clinical pharmacology section
    • source: U.S. Food and Drug Administration
  • IL6
    • other, Clinical pharmacology section
    • source: U.S. Food and Drug Administration
  • MS4A1
    • other, Indications & usage section, Dosage & administration section, Description section, Clinical pharmacology section, Clinical studies section, Use in specific populations section, Warnings and precautions section
    • source: U.S. Food and Drug Administration
  • SAA1
    • other, Clinical pharmacology section
    • source: U.S. Food and Drug Administration

last updated 07/10/2014

2. EMA Label for rituximab and MS4A1

Genetic testing required

Summary

The EMA European Public Assessment Report (EPAR) for rituximab (MabThera) contains information regarding one of the indications of the drug in patients with CD20-positive diffuse large V cell non-Hodgkin's lymphoma in combination with CHOP chemotherapy regimen. The drug targets CD20 (MS4A1) expressing B cells to induce cell lysis.

Annotation

Rituxumab is an antibody that specifically binds the CD20 antigen expressed on B cells to induce B cell lysis. It is indicated for treatment of subsets of patients with Non-Hodgkin's lymphoma (NHL), Chronic lymphocytic leukemia (CLL), Rheumatoid arthritis, or granulomatosis with polyangiitis and microscopis polyangiitis.

Excerpts from the rituximab (MabThera) EPAR:

MabThera is indicated for the treatment of patients with CD20 positive diffuse large B cell non-Hodgkin's lymphoma in combination with CHOP (cyclophosphamide, doxorubicin, vincristine, prednisolone) chemotherapy.


Rituximab binds specifically to the transmembrane antigen, CD20, a non-glycosylated phosphoprotein, located on pre-B and mature B lymphocytes. The antigen is expressed on >95 % of all B cell non-Hodgkin's lymphomas. CD20 is found on both normal and malignant B cells, but not on haematopoietic stem cells, pro-B cells, normal plasma cells or other normal tissue.

For the complete drug label text with sections containing pharmacogenetic information highlighted, see the rituximab (MabThera) EMA drug label.

*Disclaimer: The contents of this page have not been endorsed by the EMA and are the sole responsibility of PharmGKB.

Genes and/or phenotypes found in this label

  • Arthritis, Rheumatoid
    • efficacy, Indications & usage section, Dosage & administration section, Contraindications section, Drug interactions section, Information for patients section, Adverse reactions section, Pharmacodynamics section, Warnings and precautions section
    • source: European Medicines Agency
  • Leukemia, Lymphocytic, Chronic, B-Cell
    • efficacy, Indications & usage section, Dosage & administration section, Drug interactions section, Information for patients section, Abuse section, Pharmacodynamics section, Warnings and precautions section
    • source: European Medicines Agency
  • Lymphoma, Non-Hodgkin
    • efficacy, Indications & usage section, Dosage & administration section, Contraindications section, Information for patients section, Adverse reactions section, Pharmacodynamics section, Pharmacokinetics section, Warnings and precautions section
    • source: European Medicines Agency
  • Wegener Granulomatosis
    • efficacy, Indications & usage section, Dosage & administration section, Contraindications section, Information for patients section, Adverse reactions section, Pharmacodynamics section, Pharmacokinetics section, Warnings and precautions section
    • source: European Medicines Agency

PharmGKB contains no Clinical Variants that meet the highest level of criteria.

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 rituximab

Gene ? Variant?
(147)
Alternate Names ? Chemicals ? Alleles ?
(+ chr strand)
Function ? Amino Acid?
Translation
No VIP available No Clinical Annotations available VA
TERT N/A N/A N/A
No VIP available No Clinical Annotations available VA
rs1041981 NC_000006.11:g.31540784C=, NC_000006.11:g.31540784C>A, NC_000006.12:g.31573007C=, NC_000006.12:g.31573007C>A, NG_007462.1:g.2435C=, NG_007462.1:g.2435C>A, NG_012010.1:g.5909C=, NG_012010.1:g.5909C>A, NM_000595.3:c.179C=, NM_000595.3:c.179C>A, NM_001159740.2:c.179C=, NM_001159740.2:c.179C>A, NP_000586.2:p.Thr60=, NP_000586.2:p.Thr60Asn, NP_001153212.1:p.Thr60=, NP_001153212.1:p.Thr60Asn, NT_113891.2:g.3050400A=, NT_113891.2:g.3050400A>C, NT_113891.3:g.3050294A=, NT_113891.3:g.3050294A>C, NT_167245.1:g.2826325C=, NT_167245.1:g.2826325C>A, NT_167245.2:g.2820740C=, NT_167245.2:g.2820740C>A, NT_167246.1:g.2883668C=, NT_167246.1:g.2883668C>A, NT_167246.2:g.2878048C=, NT_167246.2:g.2878048C>A, NT_167247.1:g.2920490C=, NT_167247.1:g.2920490C>A, NT_167247.2:g.2914905C=, NT_167247.2:g.2914905C>A, NT_167248.1:g.2834422C=, NT_167248.1:g.2834422C>A, NT_167248.2:g.2828826C=, NT_167248.2:g.2828826C>A, NT_167249.1:g.2871585C=, NT_167249.1:g.2871585C>A, NT_167249.2:g.2872287C=, NT_167249.2:g.2872287C>A, XM_011514614.1:c.179C=, XM_011514614.1:c.179C>A, XM_011514615.1:c.179C=, XM_011514615.1:c.179C>A, XM_011514616.1:c.179C=, XM_011514616.1:c.179C>A, XM_011514617.1:c.179C=, XM_011514617.1:c.179C>A, XM_011514618.1:c.179C=, XM_011514618.1:c.179C>A, XM_011547250.1:c.179A=, XM_011547250.1:c.179A>C, XM_011547653.1:c.179C=, XM_011547653.1:c.179C>A, XM_011547654.1:c.179C=, XM_011547654.1:c.179C>A, XM_011547883.1:c.179C=, XM_011547883.1:c.179C>A, XM_011547884.1:c.179C=, XM_011547884.1:c.179C>A, XM_011547885.1:c.179C=, XM_011547885.1:c.179C>A, XM_011547886.1:c.179C=, XM_011547886.1:c.179C>A, XM_011547887.1:c.179C=, XM_011547887.1:c.179C>A, XM_011548050.1:c.179C=, XM_011548050.1:c.179C>A, XM_011548051.1:c.179C=, XM_011548051.1:c.179C>A, XM_011548242.1:c.179C=, XM_011548242.1:c.179C>A, XM_011548243.1:c.179C=, XM_011548243.1:c.179C>A, XM_011548436.1:c.179C=, XM_011548436.1:c.179C>A, XM_011548437.1:c.179C=, XM_011548437.1:c.179C>A, XM_011548438.1:c.179C=, XM_011548438.1:c.179C>A, XM_011548439.1:c.179C=, XM_011548439.1:c.179C>A, XM_011548440.1:c.179C=, XM_011548440.1:c.179C>A, XP_011512916.1:p.Thr60=, XP_011512916.1:p.Thr60Asn, XP_011512917.1:p.Thr60=, XP_011512917.1:p.Thr60Asn, XP_011512918.1:p.Thr60=, XP_011512918.1:p.Thr60Asn, XP_011512919.1:p.Thr60=, XP_011512919.1:p.Thr60Asn, XP_011512920.1:p.Thr60=, XP_011512920.1:p.Thr60Asn, XP_011545552.1:p.Asn60=, XP_011545552.1:p.Asn60Thr, XP_011545955.1:p.Thr60=, XP_011545955.1:p.Thr60Asn, XP_011545956.1:p.Thr60=, XP_011545956.1:p.Thr60Asn, XP_011546185.1:p.Thr60=, XP_011546185.1:p.Thr60Asn, XP_011546186.1:p.Thr60=, XP_011546186.1:p.Thr60Asn, XP_011546187.1:p.Thr60=, XP_011546187.1:p.Thr60Asn, XP_011546188.1:p.Thr60=, XP_011546188.1:p.Thr60Asn, XP_011546189.1:p.Thr60=, XP_011546189.1:p.Thr60Asn, XP_011546352.1:p.Thr60=, XP_011546352.1:p.Thr60Asn, XP_011546353.1:p.Thr60=, XP_011546353.1:p.Thr60Asn, XP_011546544.1:p.Thr60=, XP_011546544.1:p.Thr60Asn, XP_011546545.1:p.Thr60=, XP_011546545.1:p.Thr60Asn, XP_011546738.1:p.Thr60=, XP_011546738.1:p.Thr60Asn, XP_011546739.1:p.Thr60=, XP_011546739.1:p.Thr60Asn, XP_011546740.1:p.Thr60=, XP_011546740.1:p.Thr60Asn, XP_011546741.1:p.Thr60=, XP_011546741.1:p.Thr60Asn, XP_011546742.1:p.Thr60=, XP_011546742.1:p.Thr60Asn, XR_926695.1:n.-309G>T, XR_926695.1:n.-309T>G, XR_952245.1:n.-285G>T, XR_952245.1:n.-285T>G, XR_952708.1:n.-344G>T, XR_952708.1:n.-344T>G, XR_952889.1:n.-309G>T, XR_952889.1:n.-309T>G, XR_952970.1:n.-344G>T, XR_952970.1:n.-344T>G, XR_953043.1:n.-344G>T, XR_953043.1:n.-344T>G, XR_953113.1:n.-309G>T, XR_953113.1:n.-309T>G, rs115360616, rs117029106, rs142541719, rs17846104, rs17859107, rs1800509, rs2229093, rs3181466, rs57361933
C > A
SNP
T60N
No VIP available No Clinical Annotations available VA
rs1061622 NC_000001.10:g.12252955T>G, NC_000001.11:g.12192898T>G, NG_029791.1:g.30896T>G, NM_001066.2:c.587T>G, NP_001057.1:p.Met196Arg, XM_011542060.1:c.587T>G, XM_011542061.1:c.587T>G, XM_011542062.1:c.566T>G, XM_011542063.1:c.587T>G, XP_011540362.1:p.Met196Arg, XP_011540363.1:p.Met196Arg, XP_011540364.1:p.Met189Arg, XP_011540365.1:p.Met196Arg, XR_244793.1:n.692T>G, rs13306722, rs1681698, rs17037789, rs17883437, rs2228492, rs52797629, rs60195947
T > G
SNP
M196R
No VIP available No Clinical Annotations available VA
rs1081848 NC_000006.11:g.84509072G>A, NC_000006.12:g.83799353G>A, rs1171530, rs1171679
G > A
SNP
No VIP available No Clinical Annotations available VA
rs1799724 NC_000006.11:g.31542482C>T, NC_000006.12:g.31574705C>T, NG_007462.1:g.4133C>T, NG_012010.1:g.7607C>T, NM_000594.3:c.-1037C>T, NM_000595.3:c.*1012C>T, NM_001159740.2:c.*1012C>T, NT_113891.2:g.3052098C>T, NT_113891.3:g.3051992C>T, NT_167245.1:g.2828023C>T, NT_167245.2:g.2822438C>T, NT_167246.1:g.2885366C>T, NT_167246.2:g.2879746C>T, NT_167247.1:g.2922188C>T, NT_167247.2:g.2916603C>T, NT_167248.1:g.2836120C>T, NT_167248.2:g.2830524C>T, NT_167249.1:g.2873283C>T, NT_167249.2:g.2873985C>T, XM_011514614.1:c.*1012C>T, XM_011514615.1:c.*1012C>T, XM_011514616.1:c.*1012C>T, XM_011514617.1:c.*1012C>T, XM_011514618.1:c.*1012C>T, XM_011547250.1:c.*1012C>T, XM_011547653.1:c.*1012C>T, XM_011547654.1:c.*1012C>T, XM_011547883.1:c.*1012C>T, XM_011547884.1:c.*1012C>T, XM_011547885.1:c.*1012C>T, XM_011547886.1:c.*1012C>T, XM_011547887.1:c.*1012C>T, XM_011548050.1:c.*1012C>T, XM_011548051.1:c.*1012C>T, XM_011548242.1:c.*1012C>T, XM_011548243.1:c.*1012C>T, XM_011548436.1:c.*1012C>T, XM_011548437.1:c.*1012C>T, XM_011548438.1:c.*1012C>T, XM_011548439.1:c.*1012C>T, XM_011548440.1:c.*1012C>T, XR_952245.1:n.-1983G>A, rs112098114, rs114464955, rs117934520, rs36205301, rs3807038, rs4151108
C > T
SNP
No VIP available CA VA
rs1800470 NC_000019.10:g.41353016G>A, NC_000019.9:g.41858921G>A, NG_013091.1:g.16158C>T, NG_013364.1:g.5911C>T, NM_000660.5:c.29C>T, NP_000651.3:p.Pro10Leu, XM_005259150.1:c.-30+1814G>A, XM_005259187.1:c.29C>T, XM_011527242.1:c.29C>T, XP_005259244.1:p.Pro10Leu, XP_011525544.1:p.Pro10Leu, rs17849267, rs17849435, rs17851976, rs1982073, rs3745293, rs60195696
G > A
SNP
P10L
No VIP available CA VA
rs1800471 NC_000019.10:g.41352971C>G, NC_000019.9:g.41858876C>G, NG_013091.1:g.16203G>C, NG_013364.1:g.5956G>C, NM_000660.5:c.74G>C, NP_000651.3:p.Arg25Pro, XM_005259150.1:c.-30+1769C>G, XM_005259187.1:c.74G>C, XM_011527242.1:c.74G>C, XP_005259244.1:p.Arg25Pro, XP_011525544.1:p.Arg25Pro, rs4987231
C > G
SNP
R25P
No VIP available No Clinical Annotations available VA
rs1800610 NC_000006.11:g.31543827G>A, NC_000006.12:g.31576050G>A, NG_007462.1:g.5478G>A, NG_012010.1:g.8952G>A, NM_000594.3:c.186+123G>A, NT_113891.2:g.3053443G>A, NT_113891.3:g.3053337G>A, NT_167244.1:g.2858545G>A, NT_167244.2:g.2908629G>A, NT_167245.1:g.2829368G>A, NT_167245.2:g.2823783G>A, NT_167246.1:g.2886711G>A, NT_167246.2:g.2881091G>A, NT_167247.1:g.2923533G>A, NT_167247.2:g.2917948G>A, NT_167248.1:g.2837465G>A, NT_167248.2:g.2831869G>A, NT_167249.1:g.2874628G>A, NT_167249.2:g.2875330G>A, rs115776008, rs117343675, rs3730325, rs4645840, rs80267959
G > A
SNP
No VIP available No Clinical Annotations available VA
rs1800629 NC_000006.11:g.31543031G=, NC_000006.11:g.31543031G>A, NC_000006.12:g.31575254G=, NC_000006.12:g.31575254G>A, NG_007462.1:g.4682G=, NG_007462.1:g.4682G>A, NG_012010.1:g.8156G=, NG_012010.1:g.8156G>A, NM_000594.3:c.-488A>G, NM_000594.3:c.-488G>A, NT_113891.2:g.3052647A=, NT_113891.2:g.3052647A>G, NT_113891.3:g.3052541A=, NT_113891.3:g.3052541A>G, NT_167245.1:g.2828572G=, NT_167245.1:g.2828572G>A, NT_167245.2:g.2822987G=, NT_167245.2:g.2822987G>A, NT_167246.1:g.2885915G=, NT_167246.1:g.2885915G>A, NT_167246.2:g.2880295G=, NT_167246.2:g.2880295G>A, NT_167247.1:g.2922737G=, NT_167247.1:g.2922737G>A, NT_167247.2:g.2917152G=, NT_167247.2:g.2917152G>A, NT_167248.1:g.2836669G=, NT_167248.1:g.2836669G>A, NT_167248.2:g.2831073G=, NT_167248.2:g.2831073G>A, NT_167249.1:g.2873832G=, NT_167249.1:g.2873832G>A, NT_167249.2:g.2874534G=, NT_167249.2:g.2874534G>A, rs116610137, rs117441802, rs148958203, rs3091256, rs36205298, rs4134777, rs59729336
G > A
SNP
No VIP available No Clinical Annotations available VA
rs1800896 NC_000001.10:g.206946897T>C, NC_000001.11:g.206773552T>C, NG_012088.1:g.3943A>G, NM_000572.2:c.-1117A>G, XM_011509506.1:c.-1001-116A>G, rs36213835, rs386545607, rs59915840
T > C
SNP
No VIP available CA VA
rs1801157
C > T
SNP
No VIP available No Clinical Annotations available VA
rs1883112 NC_000022.10:g.37256846G>A, NC_000022.11:g.36860804G>A, NG_023400.1:g.4817G>A, NM_000631.4:c.-368G>A, NM_013416.3:c.-368G>A, NT_187631.1:g.81598G>A, XM_011530198.1:c.-1851G>A, XM_011530199.1:c.-915G>A, rs13055287, rs34673077, rs61381844
G > A
SNP
No VIP available CA VA
rs2229109 NC_000007.13:g.87179809C>T, NC_000007.14:g.87550493C>T, NG_011513.1:g.167756G>A, NM_000927.4:c.1199G>A, NP_000918.2:p.Ser400Asn, rs17276921, rs2235031, rs386561706, rs59635509
C > T
SNP
S400N
No VIP available No Clinical Annotations available VA
rs2476601 NC_000001.10:g.114377568A=, NC_000001.10:g.114377568A>G, NC_000001.11:g.113834946A=, NC_000001.11:g.113834946A>G, NG_011432.1:g.41808C=, NG_011432.1:g.41808C>T, NM_001193431.2:c.1858C=, NM_001193431.2:c.1858C>T, NM_001308297.1:c.1786C=, NM_001308297.1:c.1786C>T, NM_012411.5:c.1693C=, NM_012411.5:c.1693C>T, NM_015967.5:c.1858C>T, NM_015967.6:c.1858C=, NM_015967.6:c.1858C>T, NP_001180360.1:p.Arg620=, NP_001180360.1:p.Arg620Trp, NP_001295226.1:p.Arg596=, NP_001295226.1:p.Arg596Trp, NP_036543.4:p.Arg565=, NP_036543.4:p.Arg565Trp, NP_057051.3:p.Arg620=, NP_057051.3:p.Arg620Trp, NR_125965.1:n.414+19474A>G, NR_125965.1:n.414+19474G>A, XM_005270738.1:c.1786T=, XM_005270738.1:c.1786T>C, XM_005270738.2:c.1786T=, XM_005270738.2:c.1786T>C, XM_011541221.1:c.1780T=, XM_011541221.1:c.1780T>C, XM_011541222.1:c.1858T=, XM_011541222.1:c.1858T>C, XM_011541223.1:c.1858T=, XM_011541223.1:c.1858T>C, XM_011541224.1:c.1414T=, XM_011541224.1:c.1414T>C, XM_011541225.1:c.1786T=, XM_011541225.1:c.1786T>C, XP_005270795.1:p.Trp596=, XP_005270795.1:p.Trp596Arg, XP_011539523.1:p.Trp594=, XP_011539523.1:p.Trp594Arg, XP_011539524.1:p.Trp620=, XP_011539524.1:p.Trp620Arg, XP_011539525.1:p.Trp620=, XP_011539525.1:p.Trp620Arg, XP_011539526.1:p.Trp472=, XP_011539526.1:p.Trp472Arg, XP_011539527.1:p.Trp596=, XP_011539527.1:p.Trp596Arg, rs117063937, rs52834763, rs60104027
A > G
SNP
R620W
No VIP available CA VA
rs3957357 NC_000006.11:g.52668687A>G, NC_000006.12:g.52803889A>G, NM_001319059.1:c.-281T>C, NM_145740.4:c.-135T>C, XM_005249034.1:c.-135T>C, XM_005249034.2:c.-135T>C, rs58145964
A > G
SNP
No VIP available CA VA
rs396991 NC_000001.10:g.161514542A>C, NC_000001.11:g.161544752A>C, NG_009066.1:g.10872T>G, NM_000569.6:c.634T>G, NM_001127592.1:c.631T>G, NM_001127593.1:c.526T>G, NM_001127595.1:c.526T>G, NM_001127596.1:c.523T>G, NP_000560.5:p.Phe212Val, NP_001121064.1:p.Phe211Val, NP_001121065.1:p.Phe176Val, NP_001121067.1:p.Phe176Val, NP_001121068.1:p.Phe175Val, XM_011509293.1:c.428-1553T>G, rs17857127, rs2229097, rs3171040, rs4151086, rs61228128
A > C
SNP
F212V
No VIP available CA VA
rs4673 NC_000016.10:g.88646828A>G, NC_000016.9:g.88713236A>G, NG_007291.1:g.9222T>C, NM_000101.2:c.214T>C, NM_000101.3:c.214T>C, NP_000092.2:p.Tyr72His, XM_011522905.1:c.214T>C, XP_011521207.1:p.Tyr72His, rs11266997, rs1130413, rs2228471, rs2242272, rs3189211, rs386594564, rs4782392, rs59455247
A > G
SNP
Y72H
No VIP available CA VA
rs6822844 NC_000004.11:g.123509421G>T, NC_000004.12:g.122588266G>T, rs61272394
G > T
SNP
No VIP available No Clinical Annotations available VA
rs6920220 NC_000006.11:g.138006504G>A, NC_000006.12:g.137685367G>A, rs17264367, rs56495515, rs57269942, rs58273351
G > A
SNP
No VIP available No Clinical Annotations available VA
rs7574865 NC_000002.11:g.191964633T=, NC_000002.11:g.191964633T>G, NC_000002.12:g.191099907T=, NC_000002.12:g.191099907T>G, NG_012852.1:g.56293A=, NG_012852.1:g.56293A>C, NM_001243835.1:c.274-23582A=, NM_001243835.1:c.274-23582A>C, NM_003151.3:c.274-23582A=, NM_003151.3:c.274-23582A>C, XM_005246817.1:c.301-23582A=, XM_005246817.1:c.301-23582A>C, XM_005246817.3:c.301-23582A=, XM_005246817.3:c.301-23582A>C, XM_006712719.2:c.274-23582A=, XM_006712719.2:c.274-23582A>C, XM_011511704.1:c.301-23582A=, XM_011511704.1:c.301-23582A>C, XM_011511705.1:c.274-23582A=, XM_011511705.1:c.274-23582A>C, XM_011511706.1:c.301-23582A=, XM_011511706.1:c.301-23582A>C, rs52795984, rs57433953
T > G
SNP
No VIP available No Clinical Annotations available VA
rs909253 NC_000006.11:g.31540313A=, NC_000006.11:g.31540313A>G, NC_000006.12:g.31572536A=, NC_000006.12:g.31572536A>G, NG_007462.1:g.1964A=, NG_007462.1:g.1964A>G, NG_012010.1:g.5438A=, NG_012010.1:g.5438A>G, NM_000595.3:c.-10+90A>G, NM_000595.3:c.-10+90G>A, NM_001159740.2:c.-9-198A>G, NM_001159740.2:c.-9-198G>A, NT_113891.2:g.3049929G=, NT_113891.2:g.3049929G>A, NT_113891.3:g.3049823G=, NT_113891.3:g.3049823G>A, NT_167245.1:g.2825852A=, NT_167245.1:g.2825852A>G, NT_167245.2:g.2820267A=, NT_167245.2:g.2820267A>G, NT_167246.1:g.2883197A=, NT_167246.1:g.2883197A>G, NT_167246.2:g.2877577A=, NT_167246.2:g.2877577A>G, NT_167247.1:g.2920017A=, NT_167247.1:g.2920017A>G, NT_167247.2:g.2914432A=, NT_167247.2:g.2914432A>G, NT_167248.1:g.2833949A=, NT_167248.1:g.2833949A>G, NT_167248.2:g.2828353A=, NT_167248.2:g.2828353A>G, NT_167249.1:g.2871114A=, NT_167249.1:g.2871114A>G, NT_167249.2:g.2871816A=, NT_167249.2:g.2871816A>G, XM_011514614.1:c.-9-198A>G, XM_011514614.1:c.-9-198G>A, XM_011514615.1:c.-9-198A>G, XM_011514615.1:c.-9-198G>A, XM_011514616.1:c.-9-198A>G, XM_011514616.1:c.-9-198G>A, XM_011514617.1:c.-9-198A>G, XM_011514617.1:c.-9-198G>A, XM_011514618.1:c.-9-198A>G, XM_011514618.1:c.-9-198G>A, XM_011547250.1:c.-9-198A>G, XM_011547250.1:c.-9-198G>A, XM_011547653.1:c.-10+90A>G, XM_011547653.1:c.-10+90G>A, XM_011547654.1:c.-9-200A>G, XM_011547654.1:c.-9-200G>A, XM_011547883.1:c.-9-198A>G, XM_011547883.1:c.-9-198G>A, XM_011547884.1:c.-9-198A>G, XM_011547884.1:c.-9-198G>A, XM_011547885.1:c.-9-198A>G, XM_011547885.1:c.-9-198G>A, XM_011547886.1:c.-9-198A>G, XM_011547886.1:c.-9-198G>A, XM_011547887.1:c.-9-198A>G, XM_011547887.1:c.-9-198G>A, XM_011548050.1:c.-10+90A>G, XM_011548050.1:c.-10+90G>A, XM_011548051.1:c.-9-200A>G, XM_011548051.1:c.-9-200G>A, XM_011548242.1:c.-10+90A>G, XM_011548242.1:c.-10+90G>A, XM_011548243.1:c.-9-200A>G, XM_011548243.1:c.-9-200G>A, XM_011548436.1:c.-9-198A>G, XM_011548436.1:c.-9-198G>A, XM_011548437.1:c.-9-198A>G, XM_011548437.1:c.-9-198G>A, XM_011548438.1:c.-9-198A>G, XM_011548438.1:c.-9-198G>A, XM_011548439.1:c.-9-198A>G, XM_011548439.1:c.-9-198G>A, XM_011548440.1:c.-9-198A>G, XM_011548440.1:c.-9-198G>A, XR_926695.1:n.116+47C>T, XR_926695.1:n.116+47T>C, XR_952245.1:n.140+47C>T, XR_952245.1:n.140+47T>C, XR_952708.1:n.83+47C>T, XR_952708.1:n.83+47T>C, XR_952889.1:n.116+47C>T, XR_952889.1:n.116+47T>C, XR_952970.1:n.83+47C>T, XR_952970.1:n.83+47T>C, XR_953043.1:n.83+47C>T, XR_953043.1:n.83+47T>C, XR_953113.1:n.116+47C>T, XR_953113.1:n.116+47T>C, rs115438376, rs11574951, rs118110345, rs138853494, rs3895079, rs4134700, rs4986977, rs606231213, rs61372201, rs6457447
A > G
SNP
Alleles, Functions, and Amino Acid Translations are all sourced from dbSNP 147

Overview

Generic Names
  • AntiCD20
  • Ig gamma-1 chain C region
Trade Names
  • MabThera
  • Rituxan
  • Rituxan (Genentech Inc)
Brand Mixture Names

PharmGKB Accession Id

PA451261

Type(s):

Drug

Description

Rituxan is a genetically engineered chimeric murine/human monoclonal antibody directed against the CD20 antigen found on the surface of normal and malignant B lymphocytes. The antibody is an IgG1 kappa immunoglobulin containing murine light- and heavy-chain variable region sequences and human constant region sequences. Rituximab is composed of two heavy chains of 451 amino acids and two light chains of 213 amino acids

Source: Drug Bank

Indication

For treatment of CD20-positive non-Hodgkins lymphoma, chronic lymphocytic leukemia, and rheumatoid arthritis.

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

Mechanism of Action

The Fab regions of rituximab binds to the CD20 antigen on B lymphocytes, while the Fc domain recruits antibodies and complements to mediate cell lysis.

Source: Drug Bank

Pharmacology

Rituximab binds to the CD20 antigen, which is predominantly expressed on mature B cells and on >90% of B-cell
non-Hodgkin's lympohomas. The antibody leads to selective killing of B-cells.

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Most likely removed by opsonization via the reticuloendothelial system when bound to B lymphocytes, or by human antimurine antibody production

Source: Drug Bank

Half-Life

0.8 hours (mammalian reticulocytes, in vitro)

Source: Drug Bank

Clearance

Source: Drug Bank

Volume of Distribution

  • 3.1 L

Source: Drug Bank

Chemical Properties

Chemical Formula

C6416H9874N1688O1987S44

Source: Drug Bank

Average Molecular Weight

143859.7000

Source: Drug Bank

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
C1QA (source: Drug Bank)
C1QB (source: Drug Bank)
C1QC (source: Drug Bank)
C1R (source: Drug Bank)
C1S (source: Drug Bank)
FCGR1A (source: Drug Bank)
FCGR2A (source: Drug Bank)
FCGR2B (source: Drug Bank)
FCGR2C (source: Drug Bank)
FCGR3A (source: Drug Bank)
FCGR3B (source: Drug Bank)
MS4A1 (source: Drug Bank)

Drug Interactions

Interaction Description
telmisartan - rituximab Telmisartan may increase the hypotensive effect of Rituximab. Telmisartan should be withheld prior to and throughout Rituximab administration. (source: Drug Bank)
telmisartan - rituximab Telmisartan may increase the hypotensive effect of Rituximab. Telmisartan should be withheld prior to and throughout Rituximab administration. (source: Drug Bank)
terazosin - rituximab Additive antihypertensive effects may occur. Increased risk of hypotension. Consider withholding Terazosin for 12 hours prior to administration of Rituximab. (source: Drug Bank)
tolazamide - rituximab Additive hypotensive effects may occur. Consider withholding Tolazamide for 12 hours prior to administration of Rituximab. (source: Drug Bank)
torasemide - rituximab Additive antihypertensive effects may occur. Increased risk of hypotension. Consider withholding Torasemide for 12 hours prior to administration of Rituximab. (source: Drug Bank)
trandolapril - rituximab Trandolapril may incresae the hypotensive effect of Rituximab. (source: Drug Bank)
trastuzumab - rituximab Trastuzumab may increase the risk of neutropenia and anemia. Monitor closely for signs and symptoms of adverse events. (source: Drug Bank)
trichlormethiazide - rituximab Additive antihypertensive effects may occur. Increased risk of hypotension. Consider withholding Trichlormethiazide for 12 hours prior to administration of Rituximab. (source: Drug Bank)
valsartan - rituximab Additive hypotensive effects may occur. Increased risk of hypotension. Consider withholding Valsartan for 12 hours prior to administration of Rituximab. (source: Drug Bank)
verapamil - rituximab Verapamil may increase the hypotensive effects of Rituximab. Consider withholding Verapamil therapy for 12 hours prior to Rituximab infusion. (source: Drug Bank)

Curated Information ?

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

May Treat
Contraindicated With

Publications related to rituximab: 25

No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Dual role of the CXCL12 polymorphism in patients with chronic lymphocytic leukemia. HLA. 2016. Butrym 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
Predictive value of cytokines and immune activation biomarkers in AIDS-related non-Hodgkin lymphoma treated with rituximab plus infusional EPOCH (AMC-034 trial). Clinical cancer research : an official journal of the American Association for Cancer Research. 2015. Epeldegui Marta, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Treatment Outcomes With Rituximab in 100 Patients With Neuromyelitis Optica: Influence of FCGR3A Polymorphisms on the Therapeutic Response to Rituximab. JAMA neurology. 2015. Kim Su-Hyun, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Single nucleotide polymorphisms in ABCB1 and CBR1 can predict toxicity to R-CHOP type regimens in patients with diffuse non-Hodgkin lymphoma. Haematologica. 2015. Jordheim Lars P, 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 and safety of subcutaneous rituximab plus fludarabine and cyclophosphamide for patients with chronic lymphocytic leukaemia. British journal of clinical pharmacology. 2015. Assouline Sarit, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Role of the functional MNS16A VNTR-243 variant of the human telomerase reverse transcriptase gene in progression and response to therapy of patients with non-Hodgkin's B-cell lymphomas. International journal of immunogenetics. 2015. Wysoczanska B, et al. PubMed
No Dosing Guideline available No Drug Label available CA No Variant Annotation available No VIP available No VIP available
Association of NADPH oxidase polymorphisms with anthracycline-induced cardiotoxicity in the RICOVER-60 trial of patients with aggressive CD20(+) B-cell lymphoma. Pharmacogenomics. 2015. Reichwagen Annegret, 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 in rheumatoid arthritis: how close are we to the clinic?. Pharmacogenomics. 2014. Ponchel Frederique, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
The 158VV Fcgamma receptor 3A genotype is associated with response to rituximab in rheumatoid arthritis: results of an Italian multicentre study. Annals of the rheumatic diseases. 2014. Quartuccio Luca, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
IL2/IL21 region polymorphism influences response to rituximab in systemic lupus erythematosus patients. Molecular biology reports. 2013. Márquez Ana, 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 disease-modifying antirheumatic drugs in rheumatoid arthritis: towards personalized medicine. Pharmacogenomics. 2013. Umićević Mirkov Maša, 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
Analysis of innate and acquired resistance to anti-CD20 antibodies in malignant and nonmalignant B cells. PeerJ. 2013. Small George W, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
TGF beta1 polymorphisms are candidate predictors of the clinical response to rituximab in rheumatoid arthritis. Joint, bone, spine : revue du rhumatisme. 2012. Daïen Claire Immediato, 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
PharmGKB summary: very important pharmacogene information for GSTT1. Pharmacogenetics and genomics. 2012. Thorn Caroline F, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
The impact of Fc-gamma receptor polymorphisms in elderly patients with diffuse large B-cell lymphoma treated with CHOP with or without rituximab. Blood. 2011. Ahlgrimm Manfred, 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
Copy number variants in pharmacogenetic genes. Trends in molecular medicine. 2011. He Yijing, 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
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Rituximab and subcutaneous 2-chloro-2'-deoxyadenosine combination treatment for patients with Waldenstrom macroglobulinemia: clinical and biologic results of a phase II multicenter study. Journal of clinical oncology : official journal of the American Society of Clinical Oncology. 2010. Laszlo Daniele, 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
Ofatumumab. Nature reviews. Drug discovery. 2010. Keating Michael J, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Analysis of the host pharmacogenetic background for prediction of outcome and toxicity in diffuse large B-cell lymphoma treated with R-CHOP21. Leukemia : official journal of the Leukemia Society of America, Leukemia Research Fund, U.K. 2009. Rossi D, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
FCGR3A-158V/F polymorphism may correlate with the levels of immunoglobulin in patients with non-Hodgkin's lymphoma after rituximab treatment as an adjuvant to autologous stem cell transplantation. European journal of haematology. 2009. Nishio Mitsufumi, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
FCGR3A gene polymorphisms may correlate with response to frontline R-CHOP therapy for diffuse large B-cell lymphoma. Blood. 2006. Kim Dong Hwan, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Two immunoglobulin G fragment C receptor polymorphisms independently predict response to rituximab in patients with follicular lymphoma. Journal of clinical oncology : official journal of the American Society of Clinical Oncology. 2003. Weng Wen-Kai, 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
Cocaine and the heart. The New England journal of medicine. 2003. Kloner Robert 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
Therapeutic activity of humanized anti-CD20 monoclonal antibody and polymorphism in IgG Fc receptor FcgammaRIIIa gene. Blood. 2002. Cartron Guillaume, et al. PubMed

LinkOuts

GenBank:
J00228
Web Resource:
Wikipedia
UniProtKB:
P01857
National Drug Code Directory:
50242-053-06
DrugBank:
DB00073
Drugs Product Database (DPD):
2241927
Therapeutic Targets Database:
DAP000382
FDA Drug Label at DailyMed:
b172773b-3905-4a1c-ad95-bab4b6126563

Clinical Trials

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

No trials loaded.

NURSA Datasets

provided by nursa.org

No NURSA datasets available.

Common Searches

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Sources for PharmGKB drug information: DrugBank, PubChem.