trimetrexate (neutrexin) Report issue

Small molecule Orphan Drug FDA Approved FDA Priority Review FDA
AACT ChEMBL DrugBank Drug Central Drugs@FDA KEGG MeSH PubChem repoDB

Active Ingredient History

NOW
  • Now
Trimetrexate, a second-generation folate antagonist which was used under brand name NEUTREXIN with concurrent leucovorin administration (leucovorin protection) was indicated 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). Nevertheless, this product was discontinued. In present time, trimetrexate with a different combinations is in the phase II of clinical trial for the treatment the following cancer diseases: pancreatic cancer and colorectal cancer (in combination with fluorouracil and leucovorin) and to treat a refractory acute leukemia in combination with leucovorin. 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 purine biosynthesis. The result is disruption of DNA, RNA, and protein synthesis, with consequent cell death.   NCATS

Chemistry

More Chemistry

Pharmacology

  • Mechanism of Action:
  • Multi-specific: Missing data
  • Black Box: No
  • Availability: Discontinued
  • Delivery Methods: Parenteral
  • Pro Drug: No

Alternative names

ci-898 | jb-11 | neutrexin | nsc 352122 | nsc-352122 | trimetrexate | trimetrexate glucuronate | trimetrexate glucuronic acid combination | trimetrexate hydrate | trimetrexato | trimetrexatum

Organizations (8)

Research & Development (7)

Organization Org Type FDA approvals Clinical Trials involvement Org ID Force Sort

Marketing (2)

Organization Org Type FDA approvals Clinical Trials involvement Org ID Force Sort

Indications (8)

Approved Indications (1)


 

Pneumonia, Pneumocystis (approved 1993)

Experimental Indications - Clinical Trial Phases 1-4 (8)


 

Colorectal Neoplasms (Phase 2)

HIV Infections (Phase 3)

Leukemia (Phase 2)

Leukemia, Myeloid, Acute (Phase 2)

Lymphoma (Phase 2)

Pancreatic Neoplasms (Phase 2)

Pneumonia, Pneumocystis (Phase 3)

Sarcoma (Phase 2)

Overview

  • Highest Phase: Phase 3
  • # of Trials: 17
  • # of Trial Organizations: 7

Trials by Phase

Trial Phase Start Date Organizations Indications

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