PF-00489791

PF-00489791 is a novel, selective, and long‐acting small molecule inhibitor of phosphodiesterase type 5 (PDE5), developed by Pfizer. It was investigated for the treatment of hypertension, diabetic nephropathies (including overt diabetic nephropathy in type 2 diabetes), Raynaud's disease, pulmonary hypertension, peripheral vascular disease, postherpetic neuralgia, and renal failure. The drug acts by inhibiting PDE5 in vascular smooth muscle cells (VSMCs), leading to increased intracellular cyclic GMP (cGMP) levels. This results in reduced intracellular calcium concentrations and subsequent vasorelaxation of arterial and venous vessels—lowering systemic blood pressure. In diabetic nephropathy models it demonstrated significant reduction of albuminuria when added to standard care therapy. Clinical trials showed that it was generally well tolerated with mild adverse events such as headache and upper gastrointestinal symptoms[1][4][5][7][9].

Other names

UNII 2S27T3DSZ3UNII2S27T3DSZ3UNII-2S27T3DSZ3CAS 853003-48-2CAS853003-48-2CAS-853003-48-2