Darunavir Ethanolate is an inhibitor of HIV protease. 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 mutations to PIs.
|Source||AAPS PharmSciTech (2017). Figure 7.Darunavir Ethanolate|
|Cell Lines||Wistar rats|
|Incubation Time||0.5, 1, 2, 4, 8, and 24 h|
|Results||The plasma concentration of darunavir in rats after oral administration of SLNs and peptide-grafted SLNs showed no significant difference (P > 0.5).|
|Source||AAPS PharmSciTech (2017). Figure 4.Darunavir Ethanolate|
|Method||Identification of Internalization Pathway|
|Cell Lines||Caco-2 cell line|
|Incubation Time||0.5, 1, 2, 3, and 4 h|
|Results||The relative uptake efficiency of darunavir in presence of endocytic inhibitors is graphically depicted in Fig. 4.|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Solubility||DMSO ≥ 50 mg/mL|
The fate of ritonavir in the presence of darunavir.
Nguyen DN, et al. Int J Pharm. 2014 Nov 20;475(1-2):214-26. PMID: 25180992.
Hepatobiliary and intestinal elimination of darunavir in an integrated preclinical rat model.
Stappaerts J, et al. Xenobiotica. 2014 Jun;44(6):489-97. PMID: 24274355.
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