& 2 CYH j H 0 comparable to that of our clinical candidate enalkiren (ICs0= 14 nM), 2 which, although not orally bioavailable, was active intravenously. From our extensive clinical investigation of this compound, we realized that a viable drug candidate must not only be well and predictably absorbed from the gastrointestinal tract into the systemic circulation, but it must possess significantly greater in vitro activity than enalkiren. Thus the second phase ...
