Antimetabolites / Disease-Modifying Antirheumatic Drugs (DMARDs)
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Overview
Antimetabolites are drugs that interfere with normal metabolic processes, particularly nucleic acid synthesis. Methotrexate, originally developed as a cancer chemotherapy agent, is now the anchor DMARD for rheumatoid arthritis treatment and is used at much lower doses for autoimmune conditions than for oncology.
How do antimetabolites / disease-modifying antirheumatic drugs (dmards) work?
Methotrexate competitively inhibits dihydrofolate reductase (DHFR), blocking the conversion of dihydrofolate to tetrahydrofolate. This disrupts purine and pyrimidine synthesis, inhibiting DNA replication and cell division. At the low doses used for rheumatoid arthritis, its anti-inflammatory effects are thought to be primarily mediated through increased adenosine release and inhibition of pro-inflammatory cytokine production.
Drugs in this class
- Methotrexate (Trexall, Otrexup, Rasuvo, Xatmep)