Darunavir Ethanolate

- Overview
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    Background
    
    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].
    
    [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.
- Properties
  - Alternative Name
    
    (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl ((2S,3R)-4-(4-amino-N-isobutylphenylsulfonamido)-3-hydroxy-1-phenylbutan-2-yl)carbamate compound with ethanol (1:1)
    
    CAS Number
    
    635728-49-3
    
    Molecular Formula
    
    C29H43N3O8S
    
    Molecular Weight
    
    593.73
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≥21 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

Darunavir Ethanolate

Background

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