Avanafil and its intermediates

Avanafil and Its Intermediates 330784-47-9
Product Name: Avanafil
Specification/Brand: 25kg/drum
Detailed Description: Avanafil
Avanafil English Name: Avanafil
Avanafil Chemical Name: 4-[(3-Chloro-4-methoxybenzyl)amino]-2-[2-(hydroxymethyl)-1-pyrrolidinyl]-N-(2-pyrimidinylmethyl)-5-pyrimidinecarboxamide
Molecular Formula: C₂₃H₂₆ClN₇O₃
Molecular Weight: 483.95
CAS Number: 330784-47-9
Structural Formula:

Density: 1.372
Appearance: White or off-white powder
Melting Point: 160-165°C
Avanafil (TA 1790) is a phosphodiesterase type 5 inhibitor under development for the treatment of male sexual dysfunction. It has completed Phase II clinical trials in the United States, the European Union, and Japan, with Phase III clinical trials about to commence. This product is being developed by Japan's Tanabe Seiyaku Co., Ltd. and VIVUS Inc. In addition to the oral formulation, VIVUS is also developing a urethral administration form of Avanafil for patients who do not respond to the oral formulation. Avanafil is a potent and highly selective phosphodiesterase type 5 inhibitor; in vitro studies have found it to have stronger selectivity for phosphodiesterase type 5 compared to sildenafil. The compound has weak affinity for other phosphodiesterases and reduced effects on adenosine receptors, indicating that Avanafil's cardiovascular effects should be weaker than those of sildenafil. Preclinical studies have confirmed that when Avanafil is co-administered with organic nitrates, the reduction in blood pressure is significantly less than when sildenafil is taken with nitrates. Furthermore, Avanafil has a weak inhibitory effect on phosphodiesterase type 6, the inhibition of which may be related to visual disturbances caused by other phosphodiesterase type 5 inhibitors.