Drug intelligence / Profile preview

trimethoprim + sulfamethoxazole + rifampicin

Development stage
Unknown
Lead developer
University Hospital
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

This combination antibiotic regimen consists of trimethoprim-sulfamethoxazole (TMP-SMX) and rifampicin. It was specifically evaluated by researchers at the University Hospital, Geneva, for the treatment of methicillin-resistant Staphylococcus aureus (MRSA) infections. The regimen typically involves oral or intravenous administration of TMP-SMX (160/800 mg) three times daily combined with rifampicin (600 mg) once daily. The mechanism of action is synergistic: TMP-SMX inhibits two consecutive steps in the bacterial biosynthesis of essential nucleic acids and proteins (folate synthesis pathway), while rifampicin inhibits bacterial DNA-dependent RNA polymerase, thereby suppressing RNA synthesis. This combination was studied in a Phase 4 trial (NCT00711854) to provide a cost-effective oral alternative to linezolid or vancomycin for MRSA.

Other names
TMP-SMX + rifampicinco-trimoxazole + rifampicin
02

Targets

DHFR (Dihydrofolate reductase)RNAP (Bacterial dna-dependent RNA polymerase)DHPS (Dihydropteroate synthase)

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