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Trimethoprim and sulfamethoxazole

National Institute of Allergy and Infectious Diseases (NIAID) · FDA-approved active Small molecule

Trimethoprim and sulfamethoxazole is a fixed-dose combination antibiotic that inhibits bacterial folate synthesis by blocking two sequential enzymes in the pathway.

Trimethoprim and sulfamethoxazole is a fixed-dose combination antibiotic that inhibits bacterial folate synthesis by blocking two sequential enzymes in the pathway. Used for Urinary tract infections, Pneumocystis jirovecii pneumonia (PCP) prophylaxis and treatment, Acute otitis media.

At a glance

Generic nameTrimethoprim and sulfamethoxazole
Also known asSeptra®)
SponsorNational Institute of Allergy and Infectious Diseases (NIAID)
Drug classSulfonamide antibiotic combination
TargetDihydropteroate synthase and dihydrofolate reductase
ModalitySmall molecule
Therapeutic areaInfectious Disease
PhaseFDA-approved

Mechanism of action

Sulfamethoxazole inhibits bacterial dihydropteroate synthase, while trimethoprim inhibits dihydrofolate reductase. Together, they sequentially block the synthesis of dihydrofolate and tetrahydrofolate, which are essential cofactors for bacterial nucleotide synthesis. This synergistic dual inhibition is bactericidal against a broad spectrum of gram-positive and gram-negative bacteria.

Approved indications

Common side effects

Key clinical trials

Primary sources

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SourceUsed for
ClinicalTrials.govTrial enrolment, design, endpoints, results

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