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fosmidomycin + azithromycin
- Development stage
- Unknown
- Lead developer
- Astellas Pharma
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
A combination of **fosmidomycin**, a phosphonic acid antibiotic, and **azithromycin**, a macrolide antibiotic, investigated for the treatment of malaria and other infectious diseases. Fosmidomycin inhibits 1-deoxy-D-xylulose 5-phosphate (DOXP) reductoisomerase, a key enzyme in the nonmevalonate (MEP) pathway of isoprenoid biosynthesis found in malaria parasites, resulting in antimalarial activity[1]. Azithromycin acts by binding to the 23S rRNA of the 50S ribosomal subunit, inhibiting protein synthesis in bacteria and the apicoplast organelle of malaria parasites[2][4][6]. Azithromycin also exhibits immunomodulatory and anti-inflammatory effects[4]. The combination was studied for synergistic effects and to reduce the risk of recrudescence observed with fosmidomycin monotherapy[3]. Both agents are orally administered small molecules, though the most effective antimalarial partner with fosmidomycin appears to be clindamycin; the fosmidomycin + azithromycin combination showed an additive, not synergistic, antimalarial effect in vitro[1].
- Brand names
- fosmidomycin + azithromycin
- Other names
- fosmidomycin + azithromycin
02
Targets
Bacterial 50S ribosomal subunitDXR (1-deoxy-D-xylulose-5-phosphate reductoisomerase)
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