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. Author manuscript; available in PMC: 2016 Sep 6.
Published in final edited form as: JAMA. 2016 Jul 12;316(2):191–210. doi: 10.1001/jama.2016.8900

Table 4.

Advantages and Disadvantages of Currently Available Integrase Strand Transfer Inhibitors

Dolutegravir Elvitegravir Raltegravir
Year of US Food and
Drug Administration
approval
2013 2012 2007
Advantages Superior to efavirenz and ritonavir-boosted
darunavir in comparative clinical trials36,37
Once-daily dosing
Coformulated with abacavir/lamivudine as part
of a complete initial regimen
Dolutegravir (not coformulated) pill size is small
Lowest risk of resistance with virologic failure36,37,40,43
Relatively few drug interactions
Can be taken with or without food
Superior to raltegravir in treatment-experienced patients
Superior to ritonavir-boosted atazanavir
in comparative clinical trial
in HIV-infected women38
Once-daily dosing
Coformulated with tenofovir disoproxil
fumarate/emtricitabine or tenofovir
alafenamide/emtricitabine as
a complete regimen
Superior to ritonavir-boosted
atazanavir and
ritonavir-boosted darunavir
in comparative clinical trial39
Longest safety record
Fewest drug interactions
Can be taken with or
without food
Disadvantages Only available coformulation is with abacavir/lamivudine
Raises serum creatinine owing to inhibition
of tubular secretion of creatinine
Higher rates of insomnia and headache than comparators
in some studies36,37
Largest tablet among coformulated
single-pill regimens
Requires pharmacokinetic boosting with
cobicistat or ritonavir for once-daily
dosing
Most drug interactions
Cobicistat raises serum creatinine owing
to inhibition of tubular secretion
of creatinine
Should be taken with food
Currently must be taken twice
daily (formulation consisting
of 2 pills given once daily
in development)
Not coformulated as part
of a complete regimen