Darunavir Ethanolate

Darunavir ethanolate is a nonpeptidic HIV protease inhibitor approved for the treatment of HIV infection[1].

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[1].

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%[2].

References:

[1]. 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.

[2]. Bhalekar MR, et al. In-vivo bioavailability and lymphatic uptake evaluation of lipid nanoparticulates of darunavir. Drug Deliv, 2016, 23(7): 2581-2586.