for Health Care Providers
Etravirine Interactions with Other Antiretrovirals
| Interacting ARV | Pharmacokinetic Effects | Recommendations and Comments |
|---|---|---|
Abbreviations: AUC = area under the plasma concentration-time curve; BID = twice daily; Cmax = maximal plasma concentration; Cmin = minimal plasma concentration; ETV = etravirine; PI = protease inhibitor Color code:
| ||
| Nucleoside/Nucleotide Analogues | ||
| Didanosine (ddI) | ddI: no significant change in levels ETV: ↑ AUC 11% |  Not clinically significant |
| Tenofovir (TDF) | TDF: ↑ Cmin 19%; ETV: ↓ Cmin 18%; | Not thought to be clinically significant |
| Nonnucleoside Reverse Transcriptase Inhibitors | ||
| Delavirdine (DLV) | ETV: anticipate ↑ levels |  Do not administer with ETV |
| Efavirenz (EFV) | EFV: anticipate ↓ levels ETV: ↓ AUC 41% | Do not administer with ETV |
| Nevirapine (NVP) | NVP: anticipate ↓ levels ETV: ↓ AUC 55% | Do not administer with ETV |
| Protease Inhibitors (Unboosted) | ||
| Atazanavir (ATV) | ATV: ↓ Cmin 47%; ETV: ↑ Cmin 58%; | ETV should not be used with unboosted PIs |
| Fosamprenavir (FPV) | Not studied; significant ↑ in FPV levels expected | |
| Indinavir (IDV) | IDV: ↓ AUC 46% ETV: ↑ AUC 51% | |
| Nelfinavir (NFV) | Not studied; ↑ NFV levels expected | |
| Ritonavir (RTV) (600 mg BID) | ETV: ↓ AUC 46% | |
| Saquinavir (SQV) | SQV: ↓ AUC 52% | |
| Protease Inhibitors (Ritonavir Boosted) | ||
| Atazanavir (ATV)-r | ATV: ↓ Cmin 38%; ETV: ↑ AUC 30%; | Do not administer with ETV |
| Darunavir (DRV)-r | DRV: no significant change in levels ETV: ↓ Cmin 49%; |  Pharmacokinetic studies of ETV 200 mg + DRV-r versus ETV 200 mg alone have not been conducted; it is not known whether dosage adjustment of ETV is necessary In clinical studies, regimens containing DRV-r + ETV were more effective than those containing DRV-r without ETV |
| Fosamprenavir (FPV)-r | FPV: ↑ Cmin 77%; ↑ AUC 69%; ↑ Cmax 62% | Dosage adjustment not established; do not administer with ETV |
| Indinavir (IDV)-r | Not studied | Do not administer with ETV |
| Lopinavir (LPV)-r (Kaletra) | LPV: ↓ Cmin 8%; ETV: ↑ Cmin 23%; | No dosage adjustment appears to be necessary |
| Saquinavir (SQV)-r | SQV: ↓ Cmin 29%; ETV: ↓ Cmin 29%; | Clinical significance of decreased SQV and ETV levels is unknown; dosage adjustment not established |
| Tipiranavir (TPV)-r | TPV: ↑ Cmin 24%; ETV: ↓ Cmin 82%; | Do not administer with ETV |
| Fusion Inhibitors | ||
| Enfuvirtide (ENF) | Anticipate no significant change in ENF or ETV levels | No dosage adjustment required |
| Chemokine Coreceptor Antagonists | ||
| Maraviroc (MVC) | MVC: ↓ Cmin 29%; ETV: no significant change in levels | Dosage adjustment required: ↑ MVC dosage to 600 mg BID (if ETV is given with MVC + DRV-r or other compatible RTV-boosted PI, ↓ MVC dosage to 150 mg BID) |
| Integrase Inhibitors | ||
| Raltegravir (RAL) | RAL: ↓ Cmin 34%; ETV: no significant change in levels | Clinical significance of decreased RAL levels is not clear; no information available on dosage adjustment |
From Etravirine: ARV Interactions
HIV Meds Quarterly Research Brief
Spring 2008
