Antineoplastics (topoisomerase I inhibitors)
- Trap topoisomerase-I DNA cleavage complexes
- Replication converts lesions into DNA breaks
- Irinotecan/topotecan are prototypes
- Irinotecan: diarrhea is signature toxicity
- Myelosuppression is common
- UGT1A1 can strongly affect irinotecan toxicity
Class at a glance
- Trap topoisomerase-I DNA cleavage complexes
Safety / monitoring
- Irinotecan/topotecan are prototypes
- Irinotecan: diarrhea is signature toxicity
Practical pearls
- Replication converts lesions into DNA breaks
Safety distinctions
- Myelosuppression is common
- UGT1A1 can strongly affect irinotecan toxicity
Self-check
- What is irinotecan’s signature toxicity?
Diarrhea. - Which enzyme can strongly affect irinotecan toxicity?
UGT1A1.
Drugs in this class (2)
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