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Severe toxicity is commonly observed in cancer patients receiving irinotecan. Studies, have explored the relationships between irinotecan pharmacokinetics and side effects and allelic variants of genes coding for drug metabolising enzymes and transporters of putative relevance for irinotecan. Patients can be genotyped for variants in the genes encoding MDR1 P-glycoprotein (ABCB1), multidrug resistance-associated proteins MRP-1 (ABCC1) and MRP-2 (ABCC2), breast cancer resistance protein (ABCG2), carboxylesterases (CES1, CES2), cytochrome P450 isozymes (CYP3A4, CYP3A5), UDP glucuronosyltransferases (UGT1A1 and UGT1A9), the hepatic transcription factor TCF1 and a DNA-repair enzyme (XRCC1).
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