| Identification | Back Directory | [Name]
Cadazolid | [CAS]
1025097-10-2 | [Synonyms]
CS-2475
Cadazolid
ACT179811
ACT-179811
ACT 179811
Cadazolid (ACT-179811)
ACT-179811; ACT 179811; ACT179811; CADAZOLID.
3-Quinolinecarboxylic acid, 1-cyclopropyl-6-fluoro-7-[4-[[2-fluoro-4-[(5R)-5-(hydroxymethyl)-2-oxo-3-oxazolidinyl]phenoxy]methyl]-4-hydroxy-1-piperidinyl]-1,4-dihydro-4-oxo- | [Molecular Formula]
C29H29F2N3O8 | [MOL File]
1025097-10-2.mol | [Molecular Weight]
585.55 |
| Chemical Properties | Back Directory | [Boiling point ]
832.6±65.0 °C(Predicted) | [density ]
1.539±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO:100.0(Max Conc. mg/mL);170.78(Max Conc. mM) | [form ]
A crystalline solid | [pka]
6.44±0.41(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
Cadazolid (ACT-179811) is a new oxazolidinone antibiotic with potent activity against Clostridium difficile. | [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]. | [IC 50]
Oxazolidinone | [storage]
Store at -20°C | [References]
[1] Baldoni D, et al. Cadazolid, a novel antibiotic with potent activity against Clostridium difficile: safety, tolerability and pharmacokinetics in healthy subjects following single and multiple oral doses. J Antimicrob Chemother. 2014 Mar;69(3):706-14. DOI:10.1093/jac/dkt401
[2] Chilton CH, et al. In vitro activity of cadazolid against clinically relevant Clostridium difficile isolates and in an in vitro gut model of C. difficile infection. J Antimicrob Chemother. 2014 Mar;69(3):697-705. DOI:10.1093/jac/dkt411 |
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