Human pharmacokinetics prediction with an in vitro-in vivo correction factor approach and in vitro drug-drug interaction profile of bictegravir, a potent integrase-strand transfer inhibitor component in approved biktarvy® for the treatment of HIV-1 infection

• Published in: Xenobiotica Vol. 52; no. 12; pp. 1020 - 1030
• Main Authors: Subramanian, Raju, Wang, Jianhong, Murray, Bernard, Custodio, Joseph, Hao, Jia, Lazerwith, Scott, MacLennan Staiger, Kelly, Mwangi, Judy, Sun, Hailing, Tang, Jennifer, Wang, Kelly, Rhodes, Gerry, Wijaya, Samantha, Zhang, Heather, Smith, Bill J.
• Format: Journal Article
• Language: English
• Published: England Taylor & Francis 02.12.2022
• Subjects: Amides; Bictegravir; Drug Interactions; drug-drug interaction potential; Heterocyclic Compounds, 3-Ring - pharmacokinetics; HIV Infections - drug therapy; HIV Integrase Inhibitors - pharmacokinetics; HIV-1; human pharmacokinetics prediction; Humans; in vitro-in vivo correction factor; Pyridones; single-tablet combination regimen; HIV-1; in vitro–in vivo correction factor; drug-drug interaction potential; single-tablet combination regimen; Bictegravir; human pharmacokinetics prediction

Bictegravir (BIC) is a potent small-molecule integrase strand-transfer inhibitor (INSTI) and a component of Biktarvy ® , a single-tablet combination regimen that is currently approved for the treatment of human immunodeficiency virus type 1 (HIV-1) infection. The in vitro properties, pharmacokinetic...