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. Author manuscript; available in PMC: 2012 Sep 1.
Published in final edited form as: Lancet Oncol. 2011 May 12;12(9):905–912. doi: 10.1016/S1470-2045(11)70056-0

Table 1. Drug Interaction Potential of HAART.

Drug Route of Elimination (Substrate) Effect on CYP450/Transporters Potential for Clinically Significant Pharmacokinetic Drug Interactions Ref.
Effect on ARVs (substrate) Effect on Cancer Drugs (due to enzyme or transporter induction or inhibition)
Nucleoside reverse-transcriptase inhibitors (NRTIs)
Abacavir Renal excretion, ALDH, UGT1 None known Unlikely Unlikely 9-11
Didanosine Renal excretion, purine nucleoside phosphorylase None known Unlikely Unlikely 12
Emtricitabine Renal excretion None known Unlikely Unlikely 13
Lamivudine Renal excretion None known Unlikely Unlikely 14
Stavudine Renal excretion None known Unlikely Unlikely 15
Zidovudine UGT2B7 None known Possible Unlikely 16,17
Nucleotide reverse-transcriptase inhibitors (NtRTIs)
Tenofovir Renal excretion Weak inhibitor: CYP1A2 Unlikely Possible 18
Non-nucleoside reverse-transcriptase inhibitor (NNRTIs)
Delavirdine CYP2D6, CYP3A4 Inhibitor: CYP2C9/2C19, CYP2D6, CYP3A4 Possible Possible (inhibitor) 19,20
Efavirenz CYP2B6>CYP3A, UGT2B7 Inducer: CYP2B6, CYP3A4
Inhibitor: CYP2C9/2C19. CYP3A4		 Possible Highly likely (inducer) 21-24
Etravirine CYP2C9/2C19, CYP3A4, UGT1 Weak inducer: CYP2B6, CYP3A4
Weak inhibitor: CYP2C9/2C19, ABCB1		 Possible Highly likely (inducer) 25,26
Nevirapine CYP2B6, CYP3A4, UGT1 Potent inducer: CYP2B6, CYP3A4 Possible Highly likely (inducer) 26-28
Ritonavir or ritonavir–boosted HIV-1 protease inhibitors (PI)
Amprenavir CYP3A4>CYP2D6, CYP2C9, ABCB1, UGT1 Strong to weak inhibitor: CYP3A
Inducer: CYP3A4, ABCB1		 Possible Definite (inhibitor)2 29-33
Darunavir CYP3A4 Inhibitor: CYP3A4 Possible Definite (inhibitor)2 34
Fosamprenavir (prodrug) Hydrolyzed to amprenavir See amprenavir Possible Definite (inhibitor)2 29,35
Indinavir CYP3A4, ABCB1, ABCC2, UGT1 Strong to weak inhibitor: CYP3A>CYP2D6, UGT1A1 Possible Definite (inhibitor)2 29,32,36-41
Lopinavir CYP3A, ABCC2 Strong to weak inhibitor: CYP3A4>UGT1A1 Possible Definite (inhibitor)2 41-44
Ritonavir CYP3A4 >CYP2D6, ABCB1, ABCC2 Inducer: CYP2B6, CYP2C9/2C19, CYP3A4, UGT1
Inhibitor: CYP3A>CYP2D6>CYP2C9		 Possible Definite (inhibitor or inducer) 29,32,36, 38,39,45-49
Saquinavir CYP3A4, ABCB1, ABCC2 Weak inhibitor: CYP3A, CYP2C9>CYP2D6, UGT1A1, ABCB1, ABCC2 Possible Definite (inhibitor)2 29,32,36, 38,39,41, 44
Tipranavir CYP3A4, UGT1, ABCB1 Inducer: CYP3A4, ABCB1
Inhibitor: CYP1A2, CYP2C9/2C19, CYP2D6		 Possible Definite (inhibitor or inducer)2 50-52
Non-ritonavir boosted HIV-1 protease inhibitors (PI)
Atazanavir CYP3A4, ABCB1 Inhibitor: CYP3A4>CYP2C8, UGT1A1, ABCC2 Possible Possible (inhibitor) 41,44,53-56
Nelfinavir CYP2C19> CYP3A4 CYP2D6, CYP2C9 Inducer: CYP2C9, CYP3A4, ABCB1
Inhibitor: CYP3A>CYP2D6		 Possible Possible (inhibitor or inducer) 29,31,36, 38,57-59
Integrase strand transfer inhibitors
Raltegravir UGT1A1 None known Possible Unlikely 60
Fusion inhibitors
Enfuvirtide Catabolism None known Unlikely Unlikely 61
Entry inhibitors (Chemokine receptor antagonists)
Maraviroc CYP3A4, ABCB1 None known Possible Unlikely 62-65

Abbreviations: ABCB1, ATP-binding cassette sub-family B member 1 (a.k.a., P-glycoprotein); ABCC2, ATP-binding cassette sub-family C member 2 (a.k.a., CMOAT, MRP2); ALDH, alcohol dehydrogenase; ARV, antiretroviral; CYP, cytochrome P450; UGT, Uridine 5′-diphospho-glucuronosyltransferase

1

Isozyme not specified.

2

When used as a ritonavir-boosted PI.