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Irinotecan (Camptosar)

Raw research findings for this medication. Mostly single studies, not curated or confirmed robust.

About Irinotecan

What it is

Irinotecan is a topoisomerase I inhibitor: it traps the enzyme that relieves tension in DNA as it is copied, so breaks build up and cancer cells die. It is given by drip for advanced bowel cancer, often in FOLFIRI or FOLFIRINOX, and in a liposomal form for pancreatic cancer. Diarrhoea and low white cell counts are its main side effects. It is sold as Camptosar, among other names.

How genes come into it

Irinotecan is turned into SN-38, its active and toxic form, and the liver enzyme UGT1A1 inactivates SN-38. People with two low-activity copies, *28/*28 (the Gilbert's syndrome genotype, about 1 in 10 people of European ancestry) or *6, more common in East Asian populations, clear SN-38 slowly and are more likely to have severe neutropenia and diarrhoea. DPWG has published a guideline on UGT1A1 and irinotecan, and the US label discusses UGT1A1*28. Studies have also looked at SLCO1B1, ABCC2 and ABCG2, with weaker evidence.

Published guidelines

Clinical guidelines that name a gene for Irinotecan. They sort people into groups by the gene copies they carry.

DPWG guideline: UGT1A1. Normal Metabolizer · Intermediate Metabolizer · Poor Metabolizer · Indeterminate · *28/*28 · *1/*28 · *1/*80+*28 · *80+*28/*80+*28. 2023.

US FDA: UGT1A1. *28/*28 · *80+*28/*80+*28 · *6/*6 · *6/*28 · *1/*80+*28 · *1/*6 · *1/*28. 2024.

US FDA: UGT1A1. Intermediate Metabolizer · Poor Metabolizer. Data that Support Therapeutic Management Recommendations.

What research found

Every published finding on gene variants and Irinotecan. Upload your DNA file to see which of these rows apply to you.

Rated evidence (54 rated variants)

PharmGKB weighs all studies of a variant and rates how strong the evidence is, from 1A (strongest) to 4.

UGT1A1 UGT1A1*1, UGT1A1*28: Level 1A · replicated. Toxicity: Neutropenia. 33.

UGT1A1 UGT1A1*1, UGT1A1*28: Level 1A · replicated. Dosage. 10.

UGT1A1 UGT1A1*1, UGT1A1*6, UGT1A1*28: Level 1B · replicated. Toxicity: Diarrhea. 24.

UGT1A1 UGT1A1*1, UGT1A1*6: Level 1B · replicated. Toxicity: Neutropenia. 15.

Metabolism (6 findings)

Studies of how quickly the body processes this medication.

ABCC2 rs2273697: Genotypes AA + AG are associated with increased metabolism of irinotecan in people with Colorectal Neoplasms as compared to genotype GG.

VDR rs11574077: Genotype TT is associated with increased metabolism of irinotecan in people with Colorectal Neoplasms as compared to genotype CT.

HNF4A rs6031587: Allele T is not associated with metabolism of irinotecan in people with Colorectal Neoplasms as compared to allele C.

RXRG rs3767344: Allele G is not associated with metabolism of irinotecan in people with Colorectal Neoplasms as compared to allele C.

Response (55 findings)

Studies of how well it worked in people carrying a variant.

CYP2A6 CYP2A6*1, CYP2A6*4, CYP2A6*7, CYP2A6*9: CYP2A6 *4 + *7 + *9 are associated with decreased response to irinotecan, oxaliplatin and tegafur / gimeracil / oteracil in people with Colorectal Neoplasms as compared to CYP2A6 *1/*1.

RALBP1 rs329007: Genotype GG is associated with decreased response to bevacizumab, fluorouracil, irinotecan and leucovorin in people with Colorectal Neoplasms as compared to genotypes AA + AG.

RGS5 rs1056515: Genotype TT is associated with increased response to bevacizumab, fluorouracil, irinotecan and leucovorin in people with Colorectal Neoplasms as compared to genotypes GG + GT.

SHMT1 rs1979277: Allele A is associated with increased response to bevacizumab, fluorouracil, irinotecan and leucovorin in people with Colorectal Neoplasms as compared to allele G.

Dosing (16 findings)

Studies of how much of the drug people needed or tolerated.

UGT1A1 UGT1A1*1, UGT1A1*28: UGT1A1 *1/*28 + *28/*28 are associated with decreased dose of irinotecan in people with Colorectal Neoplasms as compared to UGT1A1 *1/*1.

UGT1A1 UGT1A1*1, UGT1A1*28, UGT1A1*60: UGT1A1 *28 + *60 is associated with decreased dose of FOLFIRI or irinotecan in people with Colorectal Neoplasms as compared to UGT1A1 *1/*1.

UGT1A1 UGT1A1*1, UGT1A1*6, UGT1A1*28: UGT1A1 *6/*6 + *28/*28 + *6/*28 is associated with decreased dose of irinotecan in people with Neoplasms as compared to UGT1A1 *1/*28 + *1/*6.

UGT1A1 UGT1A1*1, UGT1A1*28: UGT1A1 *28/*28 is associated with decreased dose of irinotecan in people with Colorectal Neoplasms as compared to UGT1A1 *1/*1 + *1/*28.

Side effects (1 finding)

Studies of side effects in people carrying a variant.

NR1I2 rs10934498: Genotype AA is associated with decreased exposure to irinotecan in people with Colonic Neoplasms as compared to genotypes AG + GG.

Study findings and evidence levels: PharmGKB (CC BY-SA 4.0). Guidelines: CPIC and DPWG, as bundled in PharmCAT. Most studies were done mainly in people of European ancestry.

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More drugs from the same category

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Not a prescribing recommendation. This page is educational information about pharmacogenomic research and clinical guidelines - it is not medical or dosing advice, and not a prediction of how any medication will work for you. Never start, stop, or change a medication or dose based on it; talk to your doctor or pharmacist, who can order clinical-grade testing if appropriate.

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Content updated September 2026.

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