Trimetrexate is a folate antagonist used for the treatment of moderate-to-severe Pneumocystis carinii pneumonia (PCP) in immunocompromised patients as an alternative therapy in combination with leucovorin. A nonclassical folic acid inhibitor through its inhibition of the enzyme dihydrofolate reductase.
- Mechanism
- Curator reviewed
In vitro studies have shown that trimetrexate is a competitive inhibitor of dihydrofolate reductase (DHFR) from bacterial, protozoan, and mammalian sources. DHFR catalyzes the reduction of intracellular dihydrofolate to the active coenzyme tetrahydrofolate. Inhibition of DHFR results in the depletion of this coenzyme, leading directly to interference with thymidylate biosynthesis, as well as inhibition of folate-dependent formyltransferases, and indirectly to inhibition of p.r.n. biosynthesis. The end result is disruption of DNA, RNA, and protein synthesis, with consequent cell death.
- Primary indication
- For use, with concurrent leucovorin administration (leucovorin protection), as an alternative therapy for the treatment of moderate-to-severe Pneumocystis carinii pneumonia (PCP) in immunocompromised patients, including patients with the acquired immunodeficiency syndrome (AIDS).Curator reviewed · 2 structured indications
- Formula / weight
- C19H23N5O3 · 369.4176 g/mol (avg)
- First approval
- Canada, 2000 · United States, 2006
- Brand names
Resolves to
NOYPYLRCIDNJJB-UHFFFAOYSA-NSMILESCOC1=CC(NCC2=C(C)C3=C(C=C2)N=C(N)N=C3N)=CC(OC)=C1OCWhat you can answer from here — as of September 23, 2026
Which drugs share a target with Trimetrexate, and which of those have an active Phase 3 trial?
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