TABLE 2

Inhibition of human ATP-binding cassette transporters and solute carriers by DTG

Transporter	IC₅₀	Substrate	[I₁]/IC₅₀^{^a}	[I₂]/IC₅₀^{^b}
	μM
Pgp	>100	[³H]Digoxin	<0.08	<5
BCRP	>30	[¹⁴C]Cimetidine	<0.26*	<16**
OATP1B1	>100	[³H]Estradiol 17β-d-glucuronide	<0.08	n/a^{^d}
OATP1B3	>100	[³H]Estradiol 17β-d-glucuronide	<0.08	n/a
MRP2	>100	[³H]Estradiol 17β-d-glucuronide	<0.08	<5
OCT1	NC^{^c}	[¹⁴C]Metformin	NC	NC
OCT2	1.9 (0.29)^{^d}	[¹⁴C]Metformin	4.2*	n/a

↵^a [I₁] = 8 μM with DTG clinical daily dose of 50mg (Song et al., 2010); *possible DDI risk based on [I₁] > 0.1 assuming [I₁] = total plasma concentration as described in (Zhang et al., 2008; Giacomini et al., 2010).
↵^b [I₂] = 477 μM using 250 ml gastrointestinal volume. **Possible DDI risk based on [I₂] > 10 as described in (Zhang et al., 2008; Giacomini et al., 2010).
↵^c Not calculated; DTG at a concentration of 10 μM inhibited OCT1 by 22%.
↵^d n/a = not applicable; transporter not (highly) expressed in the gastrointestinal tract (Hilgendorf et al., 2007).