Table 1 Major characteristics of the 3 INSTIs

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