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
- Blocks folate reduction — impaired DNA synthesis
- Myelosuppression, mucositis; hepatotoxicity by a separate, slower route
- Reversed by supplying reduced folate
Drugs with this mechanism (1)
- Methotrexate — Antifolate; low-dose anchor DMARD for rheumatoid arthritis, high-dose chemotherapy.
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