| Indication |
For use in the treatment of the following fungal infections: Candidemia and other forms of Candida
infections (intra-abdominal abscess, and peritonitis), Aspergillus
infections, and esophageal candidiasis. Also considered an alternative
treatment for oropharyngeal canaidiasis. |
| Pharmacodynamics |
Anidulafungin is a semi-synthetic lipopeptide synthesized from a fermentation product of Aspergillus nidulans.
Anidulafungin is an echinocandin, a class of antifungal drugs that
inhibits the synthesis of 1,3-β-D-glucan, an essential component of
fungal cell walls. Anidulafungin is active in vitro against many Candida, as well as some Aspergillus. Like other echinocandins, anidulafungin is not active against Cryptococcus neoformans, Trichosporon, Fusarium, or zygomycetes. |
| Mechanism of action |
Anidulafungin is a semi-synthetic echinocandin with antifungal
activity. Anidulafungin inhibits glucan synthase, an enzyme present in
fungal, but not mammalian cells. This results in inhibition of the
formation of 1,3-β-D-glucan, an essential component of the fungal cell
wall, ultimately leading to osmotic instability and cell death. |
| Absorption |
Not Available |
| Volume of distribution |
|
| Protein binding |
84% |
| Metabolism |
Hepatic metabolism of anidulafungin has not been observed.
Anidulafungin is not a clinically relevant substrate, inducer, or
inhibitor of cytochrome P450 (CYP450) isoenzymes. Anidulafungin
undergoes slow chemical degradation at physiologic temperature and pH to
a ring-opened peptide that lacks antifungal activity. |
| Route of elimination |
Less than 1% of the administered radioactive dose was excreted in the urine. Anidulafungin is not hepatically metabolized. |
| Half life |
40-50 hours |
| Clearance |
|
| Toxicity |
During clinical trials a single 400 mg dose of anidulafungin was
inadvertently administered as a loading dose. No clinical adverse events
were reported. The maximum non-lethal dose of anidulafungin in rats was
50 mg/kg, a dose which is equivalent to 10 times the recommended daily
dose for esophageal candidiasis (50mg/day). |
