Ivacaftor-d 9 is a potent CFTR modulator and exhibits an EC 50 value of 255 nM for CFTR potentiation in G551D/F508del HBE Cells. Ivacaftor-D9 acts as an orally active and improved deuterated Ivacaftor analog for cystic fibrosis research [1].
In Vivo, In PK study, CTP-656 (oral gavage; 10 mg/kg; single dose) shows a superior pharmacokinetic profile, The plasma levels of compound were measured over 72 hours,exhibits the parameters Cmax, AUC0-24 hr, C24hr and t1/2 of 1970 ng/ml (15%), 24,260 hr*ng/ml(17%), 413 ng/ml (19%) and 13.9 hours, respectively in Male Sprague-Dawley rats. CTP-656 (oral gavage; 3 mg/kg; single dose) exhibits the parameters Cmax, AUC0-24 hr, C24hr and t1/2 of 3643 ng/ml (9%), 49,782 hr*ng/ml(31%), 1418 ng/ml (31%) and 22.8 hours, respectively in Male Beagle Dogs (3.0 mg/kg).
References:
[1]. Scott L Harbeson, et al. Altering Metabolic Profiles of Drugs by Precision Deuteration 2: Discovery of a Deuterated Analog of Ivacaftor with Differentiated Pharmacokinetics for Clinical Development. J Pharmacol Exp Ther. 2017 Aug;362(2):359-367.
In Vivo, In PK study, CTP-656 (oral gavage; 10 mg/kg; single dose) shows a superior pharmacokinetic profile, The plasma levels of compound were measured over 72 hours,exhibits the parameters Cmax, AUC0-24 hr, C24hr and t1/2 of 1970 ng/ml (15%), 24,260 hr*ng/ml(17%), 413 ng/ml (19%) and 13.9 hours, respectively in Male Sprague-Dawley rats. CTP-656 (oral gavage; 3 mg/kg; single dose) exhibits the parameters Cmax, AUC0-24 hr, C24hr and t1/2 of 3643 ng/ml (9%), 49,782 hr*ng/ml(31%), 1418 ng/ml (31%) and 22.8 hours, respectively in Male Beagle Dogs (3.0 mg/kg).
References:
[1]. Scott L Harbeson, et al. Altering Metabolic Profiles of Drugs by Precision Deuteration 2: Discovery of a Deuterated Analog of Ivacaftor with Differentiated Pharmacokinetics for Clinical Development. J Pharmacol Exp Ther. 2017 Aug;362(2):359-367.