eGS 14824A: ACE inhibitor displayspotent activity

The haemodynamic and pharmacodynamic effectsof the ACE inhibitor CGS 14824A (CGS-14831 ; Ciba­Geigy] were examined in 11 healthy male volunteers.CGS 14824A administered orally reduced the pressorresponse to exogenous angiotens in I to 50% (5mgCGS 14824A) and 25% (1Omg) of control with in 1hour, and the response lasted 4 hours.

Plasma angiotensin convert ing enzyme activitywas less than 10% of control 1 hour after CGS14824A5, 10 or 20mg and less than 10% of control 2hours after 2mg of the drug (control activity was 106nmol/ml/min). Recovery of enzyme activity was slow,being still below control 72 hours after administration.

After only 2mg of CGS 14824A, plasmaangiotensin II and aldosterone had fallen significantlyat 1 hour, and plasma renin activity and angiotensin Ihad risen significantly by 8 hours. These effects wereincreased in magnitude. and prolonged . by increasingthe dose. All doses were well tolerated and no sideeffects were reported.

'In conclusion, CGS 14824A is a very potent, orallyactive angiotensin converting enzyme inhibitor with apharmacological profile similar to that of somepreviously tested, potent, long acting agents.'Schaller. M.D.: Nussberger. J : Waeber. B.; Bussien, J.P.: Tunni, G.A. elet. European Journal of Clinical Pharmacology 28: 267272 (No 3. 1985)

6 INPHARMA'" 22 Jun 1985 0156-2703 /85/0622-0006/0$01.00/0 © ADIS Press