Cabotegravir, also known as S/GSK1265744 or GSK744, is potent HIV integrase inhibitor. Cabotegravir is an inhibitor of OAT1 (IC50 0.81 μM) and OAT3 (IC50 0.41 μM).
|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 14 mg/mL|
The promise and pitfalls of long-acting injectable agents for HIV prevention
Raphael J Landovitz, et al. Curr Opin HIV AIDS. 2016 Jan;11(1):122-8. PMID: 26633643.
Disposition and metabolism of cabotegravir: a comparison of biotransformation and excretion between different species and routes of administration in humans
Gary David Bowers, et al. Xenobiotica. 2016;46(2):147-62. PMID: 26134155.
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|Apelin-36(rat, mouse) TFA
Apelin-36(rat, mouse) TFA is an endogenous orphan G protein-coupled receptor APJ agonist.
|HIV-1 TAT Peptide TFA
TAT TFA is a cell-penetrating peptide which derived from the transactivator of transcription (TAT) of human immunodeficiency virus (HIV-1).
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