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Table 1 Major characteristics of the 3 INSTIs

From: Multiple choices for HIV therapy with integrase strand transfer inhibitors

Characteristic RAL EVG/cobi DTG
Dosing 400 mg bid 150/150 mg qd 50 mg qd in INSTI-naive and 50 mg bid in INSTI-experienced patients
STR No Yes (TDF/FTC/EVG/cobi) Together with abacavir(ABC) and 3TC
To be taken with food No Yes No
In vitro activity* 33 nM (IC95) 45 ng/mL (IC95) 0.064 μg/mL (0.15 μM) (IC90)
Protein binding 83% 98 % 99.3%
Terminal half-life 9 h 12.9 h/3.5 h 15 h
Drug-drug interactions with inducers of UGT1A1 (rifampin) Presence of a strong CYP3A inhibitor such as cobicistat creates the potentialfor an increase in systemic exposure of CYP3A substrates with inducers of UGT1A1 (rifampin)
Interaction with proton pump inhibitors and antacids No No No
Major resistance mutations [summarized in 3] E92Q T66I/A/K None (accumulation of multiple mutations required to confer resistance)
  Y143C/H/R E92Q/G  
  Q148H/K/R T97A  
  N155H S147G  
   Q148H/R/K  
   N155H  
  1. RAL = raltegravir ; EVG/cobi = elvitegravir/cobicistat ; DTG = dolutegravir ; bid = twice-daily ; qd = once-daily ; TDF/FTC = tenofovir/emtricitabine ; ABC/3TC = abacavir/lamivudine.
  2. * in vitro protein-adjusted inhibitory concentration.