Drug intelligence / Profile preview

linezolid + sulfamethoxazole-trimethoprim

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

Overview

Linezolid + sulfamethoxazole-trimethoprim is a combination of two distinct antibiotics used together in certain clinical scenarios to treat severe or resistant bacterial infections. Linezolid is an oxazolidinone antibiotic that inhibits bacterial protein synthesis by binding to the 50S ribosomal subunit, thereby preventing the formation of a functional 70S initiation complex essential for the bacterial translation process[1][2]. Sulfamethoxazole-trimethoprim (also known as co-trimoxazole or TMP-SMX) is a fixed-dose combination of two antibiotics that act synergistically by inhibiting successive steps in the folate synthesis pathway—sulfamethoxazole inhibits dihydropteroate synthase and trimethoprim inhibits dihydrofolate reductase—resulting in impaired DNA and protein synthesis in susceptible bacteria[5]. This dual therapy may be considered for difficult-to-treat infections such as those caused by Nocardia species or multidrug-resistant Staphylococcus aureus when monotherapy is insufficient or resistance patterns dictate combined use[6]. The combination has been reported effective in case reports and small studies but should be used with caution due to potential drug interactions and overlapping toxicities.

Other names
linezolid + trimethoprim-sulfamethoxazolelinezolid + TMP-SMXlinezolid + co-trimoxazole
02

Targets

DHFR (Dihydrofolate reductase)Bacterial 50S ribosomal subunitDHPS (Dihydropteroate synthase)

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