. Author manuscript; available in PMC: 2015 Nov 5.

Published in final edited form as: Nat Rev Gastroenterol Hepatol. 2013 Jul 2;10(10):596–606. doi: 10.1038/nrgastro.2013.106

Table 1.

Pharmacology and interaction potential of currently approved and investigational DAAs in late-phase clinical development

Drugs	Route of metabolism or excretion	CYP effects	Transporter substrate	Transporter effects	Comments
*Protease inhibitors*

ABT450/ ritonavir	CYP3A¹⁰⁸	CYP3A inhibition by ritonavir	ND	Inhibits OATP1B1¹⁰⁹	NA

Asunaprevir	ND	Moderate inhibitor of CYP2D6; weak inducer of CYP3A4¹¹⁰	OATP1B1/2B1¹¹¹	Weak P-gp and OATP1B1/1B3¹¹¹ inhibitor	NA

Boceprevir¹⁰	CYP3A, AKR	Moderate CYP3A inhibitor	P-gp	Weak P-gp inhibitor¹¹²	NA

Danoprevir/ ritonavir	CYP3A	CYP3A inhibition by ritonavir	ND	ND	A study with midazolam (CYP3A probe) and warfarin (CYP2C9 probe) showed that danoprevir did not change the effect of ritonavir on these probes (midazolam increased, warfarin decreased)¹¹³

Faldaprevir	CYP3A	Moderate inhibitor of hepatic and intestinal CYP3A; weak inhibitor of CYP2C9;⁴⁰ inhibitor of UGT1A1⁴¹	P-gp, MRP2⁴²	Inhibits OATP1B1, OATP1B3, OATP2B1⁴²	NA

Simeprevir	CYP3A	Mild inhibitor of CYP1A2 and intestinal CYP3A³⁷	ND	OATP1B1 and MRP2 inhibitor³⁸	NA

Telaprevir¹¹	CYP3A	Strong CYP3A inhibitor	P-gp	Moderate P-gp inhibitor	NA

*NS5A inhibitors*

ABT267	ND	ND	ND	ND	AUC and C_max increased 62% and 67%, respectively, by ritonavir¹¹⁴

Daclatasvir	CYP3A⁴⁴	ND	P-gp⁴⁴	Moderate P-gp and OATP1B1 inhibitor⁴⁶	NA

Ledipasvir⁴⁹	ND	Not a CYP inhibitor or inducer	P-gp	Weak inhibitor of P-gp, BCRP, OATP1B1, OATP1B3	NA

*Nucleos(t)ide polymerase inhibitors*

Mericitabine	Renal¹¹⁵	ND	ND	ND	Cytidine and uridine analogue

Sofosbuvir	Renal⁵⁰	ND	P-gp	ND	Uridine analogue¹¹⁶

*Non-nucleoside polymerase inhibitors*

ABT333	CYP2C8, CYP3A4 and CYP2D6 contribute approximately 60%, 30%, and 10% to ABT-333 metabolism, respectively¹¹⁷	ND	ND	ND	NA

BI 207127	ND	ND	P-gp, BCRP, OATP1B1, OATP1B3⁴²	ND	NA

Abbreviations: AKR, aldoketoreductase; BCRP, breast cancer resistance protein; CYP, cytochrome P450; DAA, direct-acting antiviral agent; MRP, multidrug resistance protein; NA, not applicable; ND, no data; OATP1, organic anion transporting polypeptide; P-gp, P-glycoprotein; UGT, uridine glucuronyl transferase.