Fusidic Acid is a bacteriostatic, tetracyclic, steroid antibiotic which targets protein synthesis in Gram-positive bacteria. It was first isolated in 1960 from Fusidium coccineum and later developed by Leo Pharma (Denmark). It targets Gram-positive bacteria.
| Mechanism of Action | Fusidic acid inhibits protein synthesis by preventing translocation by inhibiting ribosomal elongation factor G (EF-G). It prevents preventing the turnover of EF-G from the ribosome. |
| Spectrum | Fusidic Acid targets Gram-positive bacteria such as Staphylococcus, Streptococcus, and Corynebacterium species. |
| Microbiology Applications | The most studied mechanism of Fusidic Acid resistance is via development of point mutations in fusA, the gene that codes for EF-G. The mutation alters EF-G so that Fusidic Acid is no longer able to bind to it.[26][27] Resistance is acquired when Fusidic Acid is used alone, thus when used in combination with other agents, this results in less resistance emergence. |
| Related Substances | ≤ 2.0% |
| Impurity Profile | Impurity A| ent-(24SR,17Z)-16a-(acetoxy)-3b,11b,24,25-tetrahydroxy-4b,8,14-trimethyl-18-nor-5b,10a-cholest-17(20)-en-21-oic acid (24,25-dihydroxyfusidic acid)|||| Impurity C| ent-(17Z) -3b,11b-dihydroxy-17-[(6S)-6-(1-Hydroxy-1-methylethyl)-2-oxodihydro-2H-pyran-3(4H)-ylidene]-4b,8,14-trimethyl-18-nor-5b,10a-androstan-16a-yl acetate ((24R)-24,25-dihydroxyfusidic acid 21,24-lactone)|||| Impurity D| ent-(17Z) -3b,11b-dihydroxy-17-[(6R)-6-(1-hydroxy-1-methylethyl)-2-oxodihydro-2H-pyran-3(4H)-ylidene]-4b,8,14-trimethyl-18-nor-5b,10a-androstan-16a-yl acetate ((24S)-24,25-dihydroxyfusidic acid 21,24-lactone|||| Impurity E| ent-(17Z) -16a-(acetyloxy)-3b,11b,27-trihydroxy-4b,8,14-trimethyl-18-nor-5b,10a-cholesta-17(20),24-dien-21-oic acid (27-hydroxyfusidic acid)|||| Impurity F| ent-(17Z) -16a-(acetyloxy)-3b,11b,27-trihydroxy-4b,8,14-trimethyl-18-nor-5b,10a-cholesta-17(20),24-dien-21-oic acid (27-hydroxyfusidic acid)|||| Impurity K| ent-(17Z) -3b,11b,16a-trihydroxy-4b,8,14-trimethyl-18-nor-5b,10a-cholesta-17(20),24-dien-21,16-lactone(16-deacetylfusidic acid 21,16-lactone)|||| Impurity UN1| Fusidate Sodium|||| |
| Microbiology Applications | Fusidic Acid is commonly used in clinical in vitro microbiological antimicrobial susceptibility tests (panels, discs, and MIC strips) against Gram-positive microbial isolates. Medical microbiologists use AST results to recommend antibiotic treatment options. Representative MIC values include:
For a representative list of Fusidic Acid MIC values, click here.
The most studied mechanism of Fusidic Acid resistance is due to the development of point mutations in fusA, the gene that codes for EF-G. Individual amino acid exchanges within EF-G are responsible for the generation of Fusidic Acid resistance in S. aureus (Besier et al, 2003). The mutation alters EF-G so that Fusidic Acid is no longer able to bind to it. Resistance is acquired when Fusidic Acid is used alone, thus it is often used in combination.
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| References |
Collignon P and Turnidge J (1999) Fusidic Acid in vitro activity. Int. J. Antimicrob.Agents 11(2):45-58 Turnidge J, Collignon P. Resistance to fusidic acid. Int J Antimicrob Agents. 1999 Aug;12 Suppl 2:S35-44. doi: 10.1016/s0924-8579(98)00072-7. PMID: 10528785 Besier S, Ludwig A, Brade V, Wichelhaus TA. Molecular analysis of fusidic acid resistance in Staphylococcus aureus. Mol Microbiol. 2003 Jan;47(2):463-9. doi: 10.1046/j.1365-2958.2003.03307.x. PMID: 12519196. |