Darunavir ethanolate

The Uses of Darunavir ethanolate

Darunavir Ethanolate(Prezista) is an inhibitor of HIV protease. [1] Darunavir was designed to form robust interactions with the protease enzyme from many strains of HIV, including strains from treatment-experienced patients with multiple resistance mutati

The Uses of Darunavir ethanolate

Darunavir Ethanolate (Prezista) is an HIV protease inhibitor. Derivative of Darunavir (D193500), a second generation HIV-1-protease inhibitor; structurally similar to amprenavir. Antiviral. It is a COVID19-related research product.

Biological Activity

darunavir ethanolate is a nonpeptidic hiv protease inhibitor approved for the treatment of hiv infection.transepithelial transport of darunavir in caco-2 cell monolayers is 2-fold greater in the basal-to-apical direction compared to that in the opposite direction. in l-mdr1 cell, darunavir (121 mm) inhibits p-glycoprotein-mediated efflux of calcein-acetoxymethyl ester.darunavir is effective against wild-type and pi-resistant hiv, and has a low oral bioavailability (37%). when used in combination with ritonavir, bioavailability can be increased to 82%.fujimoto h, higuchi m, watanabe h, et al. p-glycoprotein mediates efflux transport of darunavir in human intestinal caco-2 and abcb1 gene-transfected renal llc-pk1 cell lines. biological & pharmaceutical bulletin, 2009, 32(9): 1588-1593. bhalekar mr, et al. in-vivo bioavailability and lymphatic uptake evaluation of lipid nanoparticulates of darunavir. drug deliv, 2016, 23(7): 2581-2586.

Chemical properties

Darunavir ethanolate is a white to off-white powder with a solubility of approximately 0.15 mg/mL in water at 20°C.

Mechanism of action

Darunavir ethanolate is an inhibitor of the HIV-1 protease. It selectively inhibits the cleavage of HIV encoded Gag-Pol polyproteins in infected cells, thereby preventing the formation of mature virus particles.