Disposition and metabolism of the cathepsin K inhibitor odanacatib in humans

• Published in: Drug metabolism and disposition Vol. 42; no. 5; pp. 818 - 827
• Main Authors: Kassahun, Kelem, McIntosh, Ian, Koeplinger, Kenneth, Sun, Li, Talaty, Jennifer E, Miller, Deborah L, Dixon, Russell, Zajic, Stefan, Stoch, S Aubrey
• Format: Journal Article
• Language: English
• Published: United States 01.05.2014
• Subjects: Adolescent; Adult; Animals; ATP-Binding Cassette, Sub-Family B, Member 1 - metabolism; Biotransformation; Biphenyl Compounds - blood; Biphenyl Compounds - pharmacokinetics; Biphenyl Compounds - urine; Bone Density Conservation Agents - blood; Bone Density Conservation Agents - pharmacokinetics; Bone Density Conservation Agents - urine; Cathepsin K - antagonists & inhibitors; Cells, Cultured; Cytochrome P-450 Enzyme System - metabolism; Feces - chemistry; Hepatocytes - drug effects; Hepatocytes - metabolism; Humans; Male; Microsomes, Liver - drug effects; Microsomes, Liver - enzymology; Microsomes, Liver - metabolism; Middle Aged; Rats; Substrate Specificity; Tissue Distribution; Young Adult

Odanacatib is a selective inhibitor of the cathepsin K enzyme that is expressed in osteoclasts involved in the degradation of bone organic matrix, and is being developed as a novel treatment of osteoporosis. Odanacatib has demonstrated increases in bone mineral density in postmenopausal women and is...