trimetrexate glucuronate + leucovorin calcium

This drug is a **combination therapy** comprised of trimetrexate glucuronate and leucovorin calcium, administered together as an alternative treatment for moderate-to-severe **Pneumocystis carinii (jirovecii) pneumonia (PCP)** in immunocompromised patients, especially those with AIDS who are intolerant of, or refractory to, trimethoprim-sulfamethoxazole. Trimetrexate glucuronate is a **non-classical folate antagonist** and a synthetic small molecule that **inhibits dihydrofolate reductase (DHFR)**, thereby blocking folate metabolism and impairing DNA, RNA, and protein synthesis, primarily affecting rapidly dividing cells. Leucovorin calcium (folinic acid) is a reduced folate that protects mammalian host cells from the toxic effects of DHFR inhibition by bypassing the DHFR enzyme and supplying tetrahydrofolate needed for nucleotide synthesis, mitigating toxicity such as myelosuppression and mucosal damage. Both components are administered as intravenous infusions: trimetrexate glucuronate once daily and leucovorin calcium every 6 hours, with leucovorin continued 72 hours past the last trimetrexate dose[1][3][5][6].

Brand names

Neutrexin (for trimetrexate glucuronate)

Other names

trimetrexate plus leucovorin calciumtrimetrexate + leucovorin