Drug intelligence / Profile preview

trimetrexate glucuronate + dapsone

Development stage
Unknown
Lead developer
U.S. Bioscience
Modality
Small Molecules
Administration
Intravenous, Oral
01

Overview

**Trimetrexate glucuronate + dapsone** is a combination of two pharmaceutical agents used primarily in the treatment of moderate to severe Pneumocystis carinii (jirovecii) pneumonia (PCP) in patients with AIDS. Trimetrexate glucuronate is a non-classical folate antagonist that competitively inhibits dihydrofolate reductase (DHFR), interfering with DNA, RNA, and protein synthesis[2][6][8]. Dapsone is a sulfone antibiotic that inhibits bacterial and protozoal dihydropteroate synthase (DHPS), disrupting folic acid synthesis, and also has anti-inflammatory properties[4]. Both are administered alongside leucovorin calcium (folinic acid) rescue to reduce toxicity to host cells[3]. The combination exploits their complementary mechanisms for anti-protozoal efficacy with manageable safety profiles[1][5].

02

Targets

DHFR (Dihydrofolate reductase)PDF (Peptide deformylase, mitochondrial)DHPS (Dihydropteroate synthase)

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