Pharmacokinetics of Temsavir, the Active Moiety of the HIV-1 Attachment Inhibitor Prodrug, Fostemsavir, Coadministered with Cobicistat, Etravirine, Darunavir/Cobicistat, or Darunavir/Ritonavir with or without Etravirine in Healthy Participants
Katy Moore, Nilay Thakkar, Mindy Magee, Heather Sevinsky, Blisse Vakkalagadda, Susan Lubin, Cyril Llamoso, Peter Ackerman
Abstract
by 79%, 97%, and 124%, respectively. Fostemsavir with all combinations was generally well tolerated. No dose adjustment is required for fostemsavir when coadministered with strong CYP3A inhibitors, P-glycoprotein inhibitors, and modest inducers, including regimens with DRV/r, DRV/c, cobicistat, etravirine, and DRV/r plus etravirine based on the therapeutic margin for temsavir (ClinicalTrials.gov registration no. NCT02063360 and NCT02277600).
Topics & Concepts
EtravirineDarunavirCobicistatCmaxRitonavirPharmacologyCminPharmacokineticsChemistryMaravirocMedicineViral loadVirologyHuman immunodeficiency virus (HIV)Antiretroviral therapyHIV/AIDS drug development and treatmentHIV Research and TreatmentHIV/AIDS Research and Interventions