Tadalafil

Tadalafil is a potent long-acting and selective inhibitor of the cGMP specific phosphodiesterase 5 (PDE5; IC50 = 1.2 nM). It is selective for PDE5 over PDE1-4 and 7-10 (IC50s = 9.2-280 μM), however, it does also inhibit PDE11 (IC50 = 11 nM). In vivo, tadalafil (10 mg/kg) decreases production of the proinflammatory cytokines TNF-α, IL-1β, and IL-6 and improves renal function in a rat model of ischemia/reperfusion injury. Formulations containing tadalafil have been used to treat erectile dysfunction, pulmonary arterial hypertension, benign prostatic hyperplasia (BPH) and lower urinary tract dysfunction. Also delays tumor growth in a mouse model via inhibition of MDSC-mediated immunosuppression.