DHFR inhibitor
Dihydrofolate reductase inhibitor
- No folate reduction, so no thymidine or purine synthesis
- Rapidly dividing tissues bear it: myelosuppression, mucositis
- Hepatotoxicity (chronic fibrosis/steatosis) by a separate, slower route
- Reduced-folate rescue bypasses the block
Drugs with this mechanism (1)
- Methotrexate — Antifolate; low-dose anchor DMARD for rheumatoid arthritis, high-dose chemotherapy.
Self-check
- How does reduced-folate rescue overcome DHFR inhibition?
It bypasses the block. - Which rapidly dividing tissues are vulnerable to DHFR inhibition?
Marrow and mucosa.
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