Table 1. Main characteristics of the integrase inhibitors used in clinical practice or in clinical trials in humans.

Generic Name	FDA/EMA status	Dosing Recommendations	Serum Half-life	Route of Metabolisation	Major Adverse Events
Raltegravir	FDA/EMA approved for therapy-naive and experienced patients	400 mg BD - no food restrictions	∼9 hrs	UGT1A1- mediated glucuronidation	nausea and diarrhea - skin rash with fever (rare) - CPK elevation, muscle weakness, rhabdomyolysis - transient elevation of serum transaminase levels - hypersensitivity reactions, hepatitis
Elvitegravir	FDA approved for therapy-naive patients as part of single tablet regimen	150 mg QD, + booster (100 mg ritonavir or cobicistat) - to be taken with meals	∼9,5 hrs if boosted	Predominantly cytochrome P450 (CYP3A4) metabolized, minor pathways via UGT1A1/3 glucuronidation and oxidative metabolism	nausea and diarrhea - headache, insomnia - eGFR decrease when combined with cobicistat (inhibition of tubular secretion of creatinine)
Dolutegravir	Phase III studies ongoing	50 mg QD in INI- naive patients, 50 mg BD in INI-experienced patients - no food restrictions	∼15 hrs	Predominantly UGT1A1- mediated glucuronidation, cytochrome P450 (CYP3A4) metabolisation as minor pathway	nausea and diarrhea - transient low-level increases in serum creatinine - eGFR decrease (inhibition of tubular secretion of creatinine) - hypersensitivity reactions, hepatitis

FDA (Food and Drug Administration) and EMA (European Medicines Agency) status , dosing recommendations, serum-half-life, main route of metabolization and currently reported major adverse events are indicated.

BD = twice-daily; QD = once-daily.