PF-04991532 + cyclosporine

PF-04991532 is a hepatoselective glucokinase activator developed to treat hyperglycemia, particularly in diabetes. It works by activating glucokinase in the liver, thereby enhancing glucose metabolism and lowering blood sugar levels without causing hepatic steatosis. Cyclosporine is an immunosuppressant used primarily to prevent organ transplant rejection and to treat severe psoriasis or rheumatoid arthritis. When administered together, cyclosporine significantly increases the plasma exposure of PF-04991532 by inhibiting hepatic organic anion‐transporting polypeptides (OATP1B1/1B3), which are responsible for the hepatic uptake of PF‑04991532[3][4][5]. This combination has been studied in healthy volunteers to assess drug-drug interactions.

Other names

(S)-6-(3-Cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acidcyclosporin A