Steps of identification, design and validation of candesartan cilexetil

Candesartan (CV-11974) is the active compound of the prodrug candesartan cilexetil (TCV-116) used in treatment of hypertension by selective blockade of Angiotensin II receptors and thus inhibits the effect of renin-angiotensin-aldosteron system. Chemical modification of the hit compound (CV-11194) yielded the lead compound (CV-11974) which passed through series of in vitro and in vivo studies successfully. The preclinical studies of CV-11974 and its prodrug shown that it was safe and did not cause serious adverse effects therefore TCV-116 was eligible for clinical trials which was firstly done in healthy individuals then involved wider group of patients with different cardiovascular conditions.