Bictegravir, cabotegravir, dolutegravir, elvitegravir, and raltegravir are 
members of the latest class of antiretrovirals available to treat human 
immunodeficiency virus (HIV) infection, the integrase strand transfer 
inhibitors. Integrase strand transfer inhibitors are potent inhibitors of the 
HIV integrase enzyme with IC90/95 values in the low nanogram per milliliter 
range and they retain antiviral activity against strains of HIV with acquired 
resistance to other classes of antiretrovirals. Each of the integrase strand 
transfer inhibitors have unique pharmacokinetic/pharmacodynamic properties, 
influencing their role in clinical use in specific subsets of patients. 
Cabotegravir, approved for use in Canada but not yet by the US Food and Drug 
Administration, is formulated in both oral and intramuscular formulations; the 
latter of which has shown efficacy as a long-acting extended-release 
formulation. Cabotegravir, raltegravir, and dolutegravir have minimal drug-drug 
interaction profiles, as their metabolism has minimal cytochrome P450 
involvement. Conversely, elvitegravir metabolism occurs primarily via cytochrome 
P450 3A4 and requires pharmacokinetic boosting to achieve systemic exposures 
amenable to once-daily dosing. Bictegravir metabolism has similar contributions 
from both cytochrome P450 3A4 and uridine 5'-diphospho-glucuronosyltransferase 
1A1. Bictegravir, dolutegravir, and raltegravir are recommended components of 
initial regimens for most people with HIV in the US adult and adolescent HIV 
treatment guidelines. This review summarizes and compares the pharmacokinetics 
and pharmacodynamics of the integrase strand transfer inhibitor agents, and 
describes specific pharmacokinetic considerations for persons with hepatic 
impairment, renal dysfunction, pregnancy, and co-infections.