4-[4-[(2-Hydroxybenzoyl) amino] phenyl] butyric acid as a novel oral delivery agent for recombinant human growth hormone

…, C Lercara, S Milstein, D O'Toole…

Index: Leone-Bay, Andrea; Ho, Koc-Kan; Agarwal, Rajesh; Baughman, Robert A.; Chaudhary, Kiran; DeMorin, Frenel; Genoble, Lise; McInnes, Campbell; Lercara, Christine; Milstein, Sam; O'Toole, Doris; Sarubbi, Donald; Variano, Bruce; Paton, Duncan R. Journal of Medicinal Chemistry, 1996 , vol. 39, # 13 p. 2571 - 2578

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Citation Number: 122

Abstract

A series of N-acetylated, non-α, aromatic amino acids was prepared and shown to promote the absorption of recombinant human growth hormone (rhGH) from the gastrointestinal tract. Seventy compounds in this family were tested in vivo in rats. Of the compounds tested, 4-[4- [(2-hydroxybenzoyl) amino] phenyl] butyric acid was identified as a preclinical candidate and was used to demonstrate the oral delivery of rhGH in primates. A significant positive ...