loxo-783 + cholestyramine

LOXO-783 + cholestyramine is a **combination of LOXO-783, an investigational oral small molecule inhibitor targeting phosphoinositide 3-kinase alpha (PI3Kα) with high selectivity for the H1047R mutant, and cholestyramine, a commercially available bile acid sequestrant.** LOXO-783 is designed to treat cancers, especially breast cancer and other solid tumors, characterized by the PIK3CA H1047R mutation. LOXO-783 is an allosteric, brain-penetrant PI3Kα inhibitor that demonstrates selectivity for the mutant over the wild-type enzyme, producing tumor regression and minimizing hyperglycemia commonly associated with other PI3K inhibitors. Cholestyramine binds bile acids in the gastrointestinal tract and is primarily used for hypercholesterolemia, but also sometimes for pruritus from bile acid retention; it may alter absorption of concomitantly administered oral agents by binding them in the gut. No data currently supports a specific efficacy or safety synergetic effect of this combination in oncology or any other disease, and no clinical trials or preclinical research on this particular combination have been published. LOXO-783 is developed and manufactured by Eli Lilly (via Loxo Oncology), while cholestyramine is available from multiple generics manufacturers.

Other names

colestyramine