Table of contents

  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Unlabeled Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Genes that may be involved
  • Drug Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Drug combinations


Trimetrexate Glucuronate: C~19~H~23~N~5~O~3~ C~6~H~10~O~7~. Mw: 563.56. (1) 2,4-Quinazolinediamine, 5-methyl-6-[[(3,4,5-trimethoxyphenyl)amino]methyl]-, mono-D-glucuronate; (2) 2,4-Diamino-5-methyl-6-[(3,4,5-trimethoxyanilino)methyl]quinazoline mono-D-glucuronate. CAS-82952-64-5 (1988).

Pharmacologic Category

Miscellanous Antiprotozoals. (ATC-Code: P01AX07).

Mechanism of action

A folate antimetabolite which inhibits DNA synthesis by inhibition of dihydrofolate reductase (DHFR). DHFR inhibition reduces formation of reduced folates and thymidylate synthetase, resulting in inhibition of purine and thymidylic acid synthesis.

Therapeutic use

Alternative therapy for treatment of moderate-to-severe Pneumocystis jiroveci pneumonia in immunocompromised patients, including patients with acquired immunodeficiency syndrome, who are intolerant of, or are refractory to, sulfamethoxazole/trimethoprim therapy or for whom sulfamethoxazole/trimethoprim and pentamidine are contraindicated.

Pregnancy and lactiation implications

May cause fetal harm when administered to pregnant women. Women of childbearing potential should avoid becoming pregnant while receiving treatment.

Unlabeled use

Treatment of non-small cell lung cancer, metastatic colorectal cancer, metastatic head and neck cancer, pancreatic adenocarcinoma, cutaneous T-cell lymphoma.


Hypersensitivity to trimetrexate, methotrexate, leucovorin, or any component of the formulation. Severe existing myelosuppression. Pregnancy.

Warnings and precautions

Use with caution in patients on previously extensive myelosuppressive therapies. Hypersensitivity/allergic-type reactions reported, primarily when given as bolus infusion, at higher than recommended doses for Pneumocystis jiroveci pneumonitis, or in combination with fluorouracil or leucovorin. May cause anaphylactoid reactions (rarely) including acute hypotension and loss of consciousness. Use with caution in mild myelosuppression. Must be administered with concurrent leucovorin to avoid potentially serious or life-threatening toxicities. Use with caution in hepatic and renal impairment. Withhold zidovudine during trimetrexate treatment. Use with caution in hypoalbuminemia or hypoproteinemia.



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