Cadazolid

Cadazolid (ACT-179811) is a new oxazolidinone antibiotic with potent activity against Clostridium difficile. In Vitro:Cadazolid is an antibiotic in development for the treatment of Clostridium difficile-associated diarrhea^[1].
Cadazolid is active against all (including linezolid- and moxifloxacin-resistant) Clostridium difficile strains (MIC₉₀ 0.125, range 0.03-0.25 mg/L)^[2]. In Vivo:Cadazolid is well tolerated up to 3000 mg given twice daily for 10 days. The most common adverse event is headache, with no observed relationship between dose or treatment duration and adverse events. Plasma concentrations of cadazolid are low. No plasma concentrations >3.3 ng/mL are observed after single doses or >6.9 ng/mL after 10 days of multiple doses. Food increased the mean Cmax from 0.73 to 1.87 ng/mL and mean AUC0–t from 3.13 to 15.69 ng·h/mL after a single 300 mg dose. The increase in systemic exposure to cadazolid across doses is less than dose-proportional. The mean cumulative faecal recovery is 81.0%–93.5%. Urinary recovery of unchanged compound is less than 0.015%^[1].