FORMULATION FOR ORAL ADMINISTRATION OF APOPTOSIS PROMOTER

• Main Authors: CATRON NATHANIEL, SANZGIRI YESHWANT D, LAFOUNTAINE JUSTIN S, SHI YI, GOKHALE RAJEEV, STEIGER NORBERT, MARSH KENNAN, PACKHAEUSER CLAUDIA, ZHOU DELIANG, HILL DAVID, HEEMSTRA KATHERINE, TONG PING, WU HUAILIANG, KNOBLOCH MARTIN, LIEPOLD BERND, SCHMITT ERIC A, MILLER JONATHAN M, FISCHER CRISTINA M, LI YANXIA, ZHANG GEOFF G.Z, HAIGHT ANTHONY R, KOSTELAC DRAZEN, FICKES MICHAEL G
• Format: Patent
• Language: English
• Published: 25.11.2010
• Subjects: HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

An orally deliverable pharmaceutical composition comprises as a sole or first active ingredient a compound of Formula I defined herein or a pharmaceutically acceptable salt thereof, for example ABT-263 free base or ABT-263 bis-HCl salt, dispersed, in a free base equivalent amount of at least about 2.5% by weight of the composition, in a pharmaceutically acceptable carrier; wherein said active ingredient is in solid-state form and/or the composition further comprises, dispersed in the carrier, a pharmaceutically acceptable heavier-chalcogen antioxidant in an amount effective to inhibit oxidation of the active ingredient at a thioether linkage thereof. The composition is suitable for oral administration to a subject in need thereof for treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer.