title: Efavirenz/emtricitabine/tenofovir disoproxil fumarate: triple combination tablet.
abstract: A new formulation combining fixed doses of the nucleoside reverse transcriptase inhibitors emtricitabine (200mg) and tenofovir disoproxil fumarate (tenofovir DF; 300 mg) with the non-nucleoside reverse transcriptase inhibitor efavirenz (600 mg) represents the first once-daily, one-tablet antiretroviral regimen. Co-formulated efavirenz/emtricitabine/tenofovir DF demonstrated bioequivalence to concomitant administration of the individual agents in a pharmacokinetic trial in healthy volunteers (n = 48). Co-formulated efavirenz/emtricitabine/tenofovir DF has not been evaluated in clinical trials. However, a once-daily regimen of efavirenz, emtricitabine and tenofovir DF (administered as individual agents) was superior to once-daily efavirenz plus twice-daily co-formulated lamivudine/zidovudine in terms of virological suppression, immunological recovery and adverse events resulting in discontinuation of the study medications in a randomised, multicentre, noninferiority study in treatment-naive patients with HIV infection (n = 517). Both regimens are currently recommended as initial antiretroviral therapy. Preliminary data suggest that co-formulated efavirenz/emtricitabine/tenofovir DF, like the individual agents in combination with other antiretroviral drugs, is generally well tolerated. CNS adverse events, primarily headache and dizziness, were the most common treatment-emergent, drug-related adverse events in the pharmacokinetic study involving the co-formulation.
authors.affiliation: Adis International Limited, Mairangi Bay, Auckland, New Zealand. demail@adis.co.nz
authors.forename: James E
authors.initials: JE
authors.lastname: Frampton
authors.forename: Katherine F
authors.initials: KF
authors.lastname: Croom
mesh_terms: D000225:Adenine / Q000008:administration & dosage / Q000009:adverse effects / Q000031:analogs & derivatives* / Q000493:pharmacokinetics / Q000627:therapeutic use; D000480:Alkynes; D048588:Benzoxazines; D002986:Clinical Trials as Topic; D003521:Cyclopropanes; D003841:Deoxycytidine / Q000008:administration & dosage / Q000009:adverse effects / Q000031:analogs & derivatives* / Q000493:pharmacokinetics / Q000627:therapeutic use; D004338:Drug Combinations; D000068679:Emtricitabine; D015658:HIV Infections / Q000188:drug therapy*; D006801:Humans; D063065:Organophosphonates / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D010078:Oxazines / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D018894:Reverse Transcriptase Inhibitors / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D000068698:Tenofovir; D016896:Treatment Outcome
chemical_list: D000480:Alkynes; D048588:Benzoxazines; D003521:Cyclopropanes; D004338:Drug Combinations; D063065:Organophosphonates; D010078:Oxazines; D018894:Reverse Transcriptase Inhibitors; D003841:Deoxycytidine; D000068698:Tenofovir; D000068679:Emtricitabine; D000225:Adenine; C098320:efavirenz