Chemotherapy

Chemotherapy agents and pharmacogenetics

Also known as: Cancer medications, Oncology drugs

12 medications 17 brand products DPYDTPMTUGT1A1

Why pharmacogenetics matter for chemotherapy agents

Pharmacogenetic testing in oncology is the most well-established and consequential part of clinical pharmacogenetics. Several chemotherapy drugs have mandatory or strongly recommended pre-treatment genetic testing because the toxicity difference between a normal metabolizer and a deficient metabolizer can be the difference between a typical treatment course and severe, sometimes fatal, toxicity.^[1]^[2]

DPYD testing before fluoropyrimidines (capecitabine, 5-FU) is standard of care at most major cancer centers.^[3] TPMT and NUDT15 testing before thiopurines (mercaptopurine, thioguanine) is similarly well-established. UGT1A1 guides irinotecan and nilotinib dosing.^[4]

Key genes in this class

DPYD

Dihydropyrimidine Dehydrogenase

DPYD breaks down fluoropyrimidine chemotherapy drugs (5-FU, capecitabine). A small percentage of people carry reduced-function variants that cause the drug to accumulate to toxic levels. This is one of the …

TPMT

Thiopurine S-Methyltransferase

TPMT inactivates thiopurine drugs like azathioprine, mercaptopurine, and thioguanine. About 1 in 300 people of European descent has essentially no TPMT activity, and standard doses can cause life-threatening bone marrow …

UGT1A1

UDP Glucuronosyltransferase Family 1 Member A1

UGT1A1 clears bilirubin (the molecule that builds up in jaundice) and several drugs including irinotecan and nilotinib. A variant called *28, common in people of all ancestries, reduces UGT1A1 activity. …

Medications in this class with pharmacogenetic guidelines

Each link goes to the drug's full pharmacogenetics page with CPIC and FDA phenotype recommendations.

Belinostat UGT1A1 Belzutifan CYP2C19 Capecitabine DPYD Erdafitinib CYP2C9 Fluorouracil DPYD Gefitinib CYP2D6 Irinotecan UGT1A1 Mercaptopurine NUDT15 / TPMT Nilotinib UGT1A1 Pazopanib UGT1A1 Sacituzumab Govitecan Hziy UGT1A1 Thioguanine NUDT15 / TPMT

Brand products in the Chemotherapy class

Combined products and brand names for the medications above. Each links to a pharmacogenetic breakdown.

sacituzumab govitecan-hziy

References

CPIC. CPIC Guideline for Fluoropyrimidines and DPYD (2017). cpicpgx.org
CPIC. CPIC Guideline for Thiopurines and TPMT and NUDT15 (2018). cpicpgx.org
U.S. Food and Drug Administration. Table of Pharmacogenomic Biomarkers in Drug Labeling (2024). fda.gov
PharmGKB / Stanford University. PharmGKB: The Pharmacogenomics Knowledge Base. pharmgkb.org

Which chemotherapy is right for your genetics?

This page covers the pharmacogenetics of chemotherapy agents in general. A Gene2Rx report tells you how your personal genotype interacts with every drug on this page.

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Informational only, not medical advice. Pharmacogenetic guidelines describe population-level patterns that inform prescribing decisions. Never start, stop, or change a medication without talking to your prescribing clinician.