Pharmacokinetics of Coadministered Ritonavir-Boosted Elvitegravir and Zidovudine, Didanosine, Stavudine, or Abacavir

Ramanathan, S.; Shen, Gong; Hinkle, John E.; Enejosa, Jeffrey; Kearney, Brian P.

doi:10.1097/qai.0b013e318151fd9a

Cited by 31 publications

(24 citation statements)

References 10 publications

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“…None of darunavir/ritonavir, fosamprenavir/ ritonavir, or tipranavir/ritonavir alter elvitegravir levels [11,69,70]. Elvitegravir/ritonavir 200/100 mg once daily plus maraviroc 150 mg twice daily, increased maraviroc AUC by 186%, elvitegravir pharmacokinetics were not altered [71]. This increase in maraviroc concentrations is consistent with that seen with ritonavir-boosted protease inhibitors.…”

Section: Elvitegravir (Gs-9137)supporting

confidence: 82%

“…Elvitegravir/ritonavir does not interact with tenofovir disoproxil fumarate, stavudine, or emtricitabine [66,67]. Elvitegravir/ritonavir lowers didanosine, abacavir, and zidovudine AUCs slightly (approximately 15%), but elvitegravir concentrations are not altered by these NRTIs [67].…”

Section: Elvitegravir (Gs-9137)mentioning

confidence: 96%

“…Elvitegravir/ritonavir lowers didanosine, abacavir, and zidovudine AUCs slightly (approximately 15%), but elvitegravir concentrations are not altered by these NRTIs [67]. Elvitegravir AUC is increased about two-fold with atazanavir/ritonavir and lopinavir/ritonavir, but reducing the elvitegravir dose to 85 mg with these protease inhibitors produces a similar exposure to elvitegravir alone [65,68].…”

Section: Elvitegravir (Gs-9137)mentioning

confidence: 99%

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Pharmacologic characteristics of investigational and recently approved agents for the treatment of HIV

Kiser

2008

Current Opinion in HIV and AIDS

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Section: Elvitegravir (Gs-9137)supporting

confidence: 82%

Section: Elvitegravir (Gs-9137)mentioning

confidence: 96%

Section: Elvitegravir (Gs-9137)mentioning

confidence: 99%

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Pharmacologic characteristics of investigational and recently approved agents for the treatment of HIV

Kiser

2008

Current Opinion in HIV and AIDS

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“…Hence, a 100 mg dose of ritonavir was selected for further efficacy studies. Coadministration of EVG with ritonavir did not alter the pharmacokinetics of commonly used nucleoside/nucleotide reverse transcriptase inhibitors including FTC and tenofovir 29. The probable reason for non-interaction is that FTC and tenofovir follow different metabolic and excretory pathways.…”

Section: Metabolism and Pharmacokineticsmentioning

confidence: 92%

Critical appraisal of elvitegravir in the treatment of HIV-1/AIDS

Pandey¹

2014

HIV

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Human immunodeficiency virus type 1 (HIV-1) integrase inhibitors belong to a novel class of antiretroviral drugs with high potency and better tolerability. Elvitegravir (EVG) is the second integrase inhibitor approved by the US Food and Drug Administration when administered in combination with a novel pharmacoenhancer, cobicistat (COBI), and two nucleoside/nucleotide reverse transcriptase inhibitors, emtricitabine (FTC) and tenofovir disoproxil fumarate (TDF). This combination of drugs (EVG/COBI/FTC/TDF) developed and marketed by Gilead Sciences Inc. (Foster City, CA, USA) as STRIBILD®, is the first integrase inhibitor-based single-tablet regimen administered once-daily. In the USA, it has been approved for use in antiretroviral treatment-naïve HIV-1 patients with estimated creatinine clearance of >70 mL/min. The Department of Health and Human Services has approved EVG/COBI/FTC/TDF as one of preferred first-line regimens for HIV-1 treatment. In Europe, the European Medicines Agency has approved STRIBILD in treatment-naïve patients as well as in patients having no resistant mutation to any of the antiviral agents contained in STRIBILD. Its availability as a fixed-dose combination and once-daily dosage makes the adherence highly likely. However, it also discounts the possibility of dosage adjustment if needed.

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“…The overlapping metabolic pathways of both drugs proved in significant and thus no dosage adjustment is warranted when they are given concomitantly. The potential interaction between elvitegravir/ritonavir and commonly used nucleoside reverse transcriptase inhibitors (NRTIs) zidovudine, didanosine, stavudine, abacavir, tenofovir and emtricitabine have also been studied 22,23. No significant change in exposures of these NRTIs or elvitegravir were found.…”

Section: Interactions With Key Drugs In the Management Of Hiv/aidsmentioning

confidence: 99%

Review of the safety, efficacy, and pharmacokinetics of elvitegravir with an emphasis on resource-limited settings

Lee¹,

Calmy²,

Andrieux-Meyer³

et al. 2012

HIV

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Integrase inhibitors represent an important new class of antiretroviral drugs. Elvitegravir, the second available integrase inhibitor to be submitted for regulatory approval appears to be a promising once-daily agent when combined with other antiretroviral drugs. Elvitegravir has demonstrated good efficacy and safety, with minimal side effects and no specific requirements in terms of laboratory monitoring. In addition, elvitegravir is available as a fixed-dose combination. However, the drug requires boosting and this leads to a number of drug–drug interactions and necessary dose adjustment when dosing with certain drugs, including dose reduction in the presence of atazanavir, lopinavir, rifabutin, and ketoconazole, and dose increase for ethinyl estradiol when co-administered with boosted elvitegravir. The main advantage of elvitegravir lies in its potential to be administered as a once-daily, single pill. Limitations include dose adjustment requirements, a relatively low genetic barrier to resistance, high price, and lack of data for use in children. Clinical trials addressing specific challenges encountered in resources-limited settings should be encouraged.

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Pharmacokinetics of Coadministered Ritonavir-Boosted Elvitegravir and Zidovudine, Didanosine, Stavudine, or Abacavir

Abstract: There are no clinically relevant drug interactions between EVG/r and the NRTIs zidovudine, didanosine, stavudine, or abacavir. These agents can be coadministered without dose adjustment.

Cited by 31 publications

References 10 publications

Pharmacologic characteristics of investigational and recently approved agents for the treatment of HIV

Pharmacologic characteristics of investigational and recently approved agents for the treatment of HIV

Critical appraisal of elvitegravir in the treatment of HIV-1/AIDS

Review of the safety, efficacy, and pharmacokinetics of elvitegravir with an emphasis on resource-limited settings

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