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Elvitegravir (United States: Not available): Drug information

Elvitegravir (United States: Not available): Drug information
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For additional information see "Elvitegravir (United States: Not available): Patient drug information"

For abbreviations, symbols, and age group definitions show table
Pharmacologic Category
  • Antiretroviral, Integrase Inhibitor (Anti-HIV)
Dosing: Adult

Note: Vitekta has been discontinued in the US for more than 1 year.

HIV-1 infection in antiretroviral treatment-experienced patients

HIV-1 infection in antiretroviral treatment-experienced patients: Oral: Note: Must be administered in combination with a protease inhibitor, ritonavir, and another antiretroviral drug. See individual agents.

Administered with concomitant atazanavir and ritonavir or lopinavir and ritonavir: 85 mg once daily

Administered with concomitant darunavir and ritonavir, fosamprenavir and ritonavir, or tipranavir and ritonavir: 150 mg once daily

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Kidney Impairment: Adult

No dosage adjustment necessary.

Dosing: Hepatic Impairment: Adult

Mild-to-moderate hepatic impairment (Child-Pugh class A or B): No dosage adjustment necessary.

Severe hepatic impairment (Child-Pugh class C): Use is not recommended (has not been studied).

Dosing: Older Adult

Refer to adult dosing.

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Adverse reactions reported with combination therapy in adults.

1% to 10%:

Dermatologic: Skin rash (<2%)

Endocrine & metabolic: Hyperglycemia (grades 3/4: 5%), increased serum cholesterol (grades 3/4: 5%), increased serum triglycerides (grades 3/4: 5%)

Gastrointestinal: Abdominal pain (<2%), diarrhea (7%), dyspepsia (<2%), increased serum amylase (grades 3/4: 6%), nausea (4%), vomiting (<2%)

Genitourinary: Glycosuria (grades 3/4: 4%), hematuria (grades 3/4: 6%)

Hematologic & oncologic: Decreased neutrophils (grades 3/4: 3%)

Hepatic: Increased gamma-glutamyl transferase (grades 3/4: 3%), increased serum alanine aminotransferase (grades 3/4: 2%), increased serum aspartate aminotransferase (grades 3/4: 2%), increased serum bilirubin (grades 3/4: 6%)

Nervous system: Depression (<2%), fatigue (<2%), headache (3%), insomnia (<2%)

Neuromuscular & skeletal: Increased creatine phosphokinase in blood specimen (grades 3/4: 6%)

<1%: Nervous system: Suicidal ideation, suicidal tendencies

Frequency not defined: Gastrointestinal: Increased serum lipase

Postmarketing:

Endocrine & metabolic: Diabetes mellitus (O'Halloran 2022)

Immunologic: Immune reconstitution syndrome (Wijting 2019)

Contraindications

There are no contraindications listed in the manufacturer's labeling.

Warnings/Precautions

Concerns related to adverse effects:

• Immune reconstitution syndrome: Patients may develop immune reconstitution syndrome resulting in the occurrence of an inflammatory response to an indolent or residual opportunistic infection during initial HIV treatment or activation of autoimmune disorders (eg, Graves’ disease, polymyositis, Guillain-Barré syndrome) later in therapy; further evaluation and treatment may be required.

Disease-related concerns:

• Hepatic impairment: No dosage adjustment is required in mild or moderate (Child-Pugh class A or B) hepatic impairment. Use is not recommended in severe hepatic impairment (Child-Pugh class C); has not been studied in this population.

Concurrent drug therapy issues:

• Appropriate use: Not recommended in combination with a protease inhibitor and cobicistat due to lack of dosing recommendations, potential suboptimal plasma concentrations, loss of therapeutic effect, or development of resistance.

• Concurrent therapy: Avoid concurrent use with other elvitegravir-containing products.

Product Availability

Vitekta has been discontinued in the US for more than 1 year.

Generic Equivalent Available: US

May be product dependent

Pricing: US

Tablets (Vitekta Oral)

85 mg (30): $1445.34

150 mg (30): $1445.34

Disclaimer: The pricing data provide a representative AWP and/or AAWP price from a single manufacturer of the brand and/or generic product, respectively. The pricing data should be used for benchmarking purposes only, and as such should not be used to set or adjudicate any prices for reimbursement or purchasing functions. Pricing data is updated monthly.

Administration: Adult

Oral: Administer once daily with food.

Use: Labeled Indications

HIV-1 infection: In combination with an HIV protease inhibitor coadministered with ritonavir and with other antiretroviral drug(s) for the treatment of HIV-1 infection in antiretroviral treatment-experienced adults

Metabolism/Transport Effects

Substrate of CYP3A4 (major), UGT1A1, UGT1A3; Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential

Drug Interactions

Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the drug interactions program by clicking on the “Launch drug interactions program” link above.

Antacids: May decrease the serum concentration of Elvitegravir. Management: Separate administration of aluminum and magnesium containing antacids and elvitegravir-containing products by at least 2 hours in order to minimize the risk for an interaction. Risk D: Consider therapy modification

Atazanavir: May increase the serum concentration of Elvitegravir. Specifically, atazanavir/ritonavir may increase the concentration of elvitegravir. Management: When elvitegravir is combined with atazanavir/ritonavir, the dose of elvitegravir should be reduced to 85 mg once daily and the dose of atazanavir/ritonavir should be 300 mg/100 mg once daily. Avoid the use of atazanavir/cobicistat and elvitegravir. Risk D: Consider therapy modification

Atidarsagene Autotemcel: Antiretroviral Agents may diminish the therapeutic effect of Atidarsagene Autotemcel. Risk X: Avoid combination

Belumosudil: May increase the serum concentration of UGT1A1 Substrates. Management: Avoid coadministration of belumosudil with substrates of UGT1A1 for which minimal concentration increases can cause serious adverse effects. If coadministration is required, dose reductions of the UGT1A1 substrate may be required. Risk D: Consider therapy modification

CarBAMazepine: May decrease the serum concentration of Elvitegravir. Risk X: Avoid combination

CYP3A4 Inducers (Moderate): May decrease the serum concentration of Elvitegravir. Risk C: Monitor therapy

CYP3A4 Inducers (Strong): May decrease the serum concentration of Elvitegravir. Management: Consider alternatives to this combination when possible. If combined, monitor for reduced elvitegravir efficacy. Risk D: Consider therapy modification

Darunavir: May increase the serum concentration of Elvitegravir. Management: When elvitegravir is combined with darunavir/ritonavir, the dose of elvitegravir should remain 150 mg once daily and the dose of darunavir/ritonavir should be 600 mg/100 mg twice daily. Avoid the combination of darunavir/cobicistat and elvitegravir. Risk D: Consider therapy modification

DexAMETHasone (Systemic): May decrease the serum concentration of Elvitegravir. Management: Consider using an alternative corticosteroid. Monitor patients receiving these agents in combination for diminished antiviral response. Risk D: Consider therapy modification

Efavirenz: May decrease the serum concentration of Elvitegravir. Risk X: Avoid combination

Fosphenytoin-Phenytoin: May decrease the serum concentration of Elvitegravir. Risk X: Avoid combination

Lopinavir: May increase the serum concentration of Elvitegravir. Specifically, lopinavir/ritonavir may increase the concentration of elvitegravir. Management: When elvitegravir is combined with lopinavir/ritonavir, the dose of elvitegravir should be reduced to 85 mg once daily and the dose of lopinavir/ritonavir should be 400 mg/100 mg twice daily. Risk D: Consider therapy modification

Mitapivat: May decrease the serum concentration of UGT1A1 Substrates. Risk C: Monitor therapy

Nevirapine: May decrease the serum concentration of Elvitegravir. Risk X: Avoid combination

Orlistat: May decrease the serum concentration of Antiretroviral Agents. Risk C: Monitor therapy

OXcarbazepine: May decrease the serum concentration of Elvitegravir. Management: For elvitegravir plus a ritonavir-boosted protease inhibitor, use of oxcarbazepine is not recommended; for elvitegravir/cobicistat/emtricitabine/tenofovir combination products, consider using an alternative antiseizure agent when possible. Risk X: Avoid combination

PHENobarbital: May decrease the serum concentration of Elvitegravir. Risk X: Avoid combination

Polyvalent Cation Containing Products: May decrease the serum concentration of Elvitegravir. Management: Administer elvitegravir 2 hours before or 6 hours after the administration of polyvalent cation containing products. Risk D: Consider therapy modification

Primidone: May decrease the serum concentration of Elvitegravir. Risk X: Avoid combination

RifAMPin: May decrease the serum concentration of Elvitegravir. Risk X: Avoid combination

Rifapentine: May decrease the serum concentration of Elvitegravir. Risk X: Avoid combination

St John's Wort: May decrease the serum concentration of Elvitegravir. Risk X: Avoid combination

Reproductive Considerations

Contraception is not required to initiate or continue antiretroviral therapy (ART).

The Health and Human Services (HHS) perinatal HIV guidelines do not recommend an elvitegravir-containing regimen for patients with HIV who are not yet pregnant but are trying to conceive.

Maximum viral suppression sustained below the limits of detection prior to conception is recommended for all persons with HIV who are planning a pregnancy. Optimization of the health of the person who will become pregnant is recommended. Selection of or changes to a specific antiretroviral regimen prior to pregnancy should be done as part of a shared decision-making process. In most cases, recommendations from the HHS perinatal HIV guidelines (based on data obtained from cisgender women) can be applied to transgender and gender diverse people assigned female sex at birth.

Health care providers caring for couples planning a pregnancy when one or both partners are diagnosed with HIV may contact the National Perinatal HIV Hotline (1-888-448-8765) for clinical consultation (HHS [perinatal] 2023).

Pregnancy Considerations

Elvitegravir has a high level of transfer across the placenta.

No increased risk of overall teratogenic effects has been observed following first trimester exposure according to data collected by the antiretroviral pregnancy registry. Maternal antiretroviral therapy (ART) may be associated with adverse pregnancy outcomes including preterm birth, low birth-weight, and small-for-gestational-age infants. Actual risks may be influenced by maternal factors such as disease severity, gestational age at initiation of therapy, and specific ART regimen, therefore close fetal monitoring is recommended. Because there is clear benefit to appropriate treatment, maternal ART should not be withheld due to concerns for adverse neonatal outcomes. Long-term follow-up is recommended for all infants exposed to antiretroviral medications; children not diagnosed with HIV but who were exposed to ART in utero or as a neonate and develop significant organ system abnormalities of unknown etiology (particularly of the CNS or heart) should be evaluated for potential metabolic dysfunction.

The Health and Human Services (HHS) perinatal HIV guidelines do not recommend an elvitegravir-containing regimen in pregnant patients with HIV due to inadequate serum concentrations observed during pregnancy. If pregnancy occurs during therapy, consideration should be given to changing to a preferred or alternative regimen. If continued in patients who are virologically suppressed, frequent viral load monitoring is recommended.

The pharmacokinetics of elvitegravir are significantly changed by pregnancy; data are insufficient to make dosing recommendations and use is not recommended during pregnancy. Do not administer within 2 hours of iron or calcium containing preparations, including prenatal vitamins.

ART is recommended for all pregnant people with HIV to maximize their health, maintain the viral load below the limit of detection, and reduce the risk of perinatal transmission. Selection of or changes to a specific antiretroviral regimen during pregnancy should be done as part of a shared decision-making process. Patients on fully suppressive regimens prior to pregnancy generally may continue the same regimen considering known pregnancy outcomes and pharmacokinetic data. Monitoring of patients who are pregnant is more frequent than in patients who are not pregnant. ART initiated during pregnancy can be modified after delivery. In most cases, recommendations from the HHS perinatal HIV guidelines (based on data obtained from cisgender women) can be applied to transgender and gender diverse people assigned female sex at birth.

Data collection to monitor pregnancy and infant outcomes following exposure to ART is ongoing. Health care providers should enroll all patients exposed to antiretroviral medications during pregnancy in the Antiretroviral Pregnancy Registry (1-800-258-4263). Enrollment should be done as early in pregnancy as possible.

Health care providers caring for pregnant patients with HIV and their infants may contact the National Perinatal HIV Hotline (1-888-448-8765) for clinical consultation (HHS [perinatal] 2023).

Breastfeeding Considerations

It is not known if elvitegravir is present in breast milk.

Maintaining maximum viral suppression during pregnancy and postpartum decreases but does not eliminate the risk of HIV transmission via breast milk. In addition, multiclass-resistant virus has been detected in breastfeeding infants who acquire HIV despite maternal therapy. In the United States, where formula is usually accessible, affordable, safe, and sustainable, and the risk of infant mortality due to diarrhea and respiratory infections is low, the Health and Human Services perinatal HIV guidelines do not recommend breastfeeding for patients with HIV when safer infant feeding options are available. Persons with HIV who maintain an undetectable viral load while taking antiretroviral therapy (ART) should evaluate infant feeding options (formula, banked donor milk, or breastfeeding) as part of a shared decision-making process (if breastfeeding is being considered, see guidelines for measures to reduce the risk of HIV transmission). When the HIV status at delivery is not known, breastmilk may be expressed and stored until a negative test is available. If HIV infection is diagnosed after breastfeeding has been initiated, breastfeeding should be discontinued immediately. Breastfeeding is not recommended for persons with HIV who are not taking ART and/or who do not have sustained viral suppression.

Information is available for counseling and managing patients with HIV who are considering breastfeeding (1-888-448-8765). In most cases, recommendations from the HHS perinatal HIV guidelines (based on data obtained from cisgender women) can be applied to transgender and gender diverse people assigned female sex at birth (HHS [perinatal] 2023).

Dietary Considerations

Take with food.

Monitoring Parameters

CBC with differential, reticulocyte count, CD4 count, HIV RNA plasma levels, hepatic function tests, testing for HBV is recommended prior to the initiation of antiretroviral therapy.

Mechanism of Action

Integrase is an HIV-1 encoded enzyme that is required for viral replication. Inhibition of integrase prevents the integration of HIV-1 DNA into host genomic DNA, blocking the formation of the HIV-1 provirus and propagation of the viral infection. Elvitegravir does not inhibit human topoisomerases I or II.

Pharmacokinetics (Adult Data Unless Noted)

Absorption: AUC increases with food

Protein binding: 99%

Metabolism: Hepatic via CYP3A enzymes and also hepatic glucuronidation mediated by UGT1A1/3

Half-life elimination: Terminal: ~9 hours

Time to peak, plasma: ~4 hours

Excretion: Feces (~95%); urine (~7%)

Brand Names: International
International Brand Names by Country
For country code abbreviations (show table)

  • (AT) Austria: Vitekta;
  • (GB) United Kingdom: Vitekta;
  • (PR) Puerto Rico: Vitekta;
  • (RO) Romania: Vitekta;
  • (SE) Sweden: Vitekta
  1. O'Halloran JA, Sahrmann J, Parra-Rodriguez L, et al. Integrase strand transfer inhibitors are associated with incident diabetes mellitus in people with HIV. Clin Infect Dis. 2022;ciac355. doi:10.1093/cid/ciac355 [PubMed 35521785]
  2. US Department of Health and Human Services (HHS) Panel on Treatment of HIV During Pregnancy and Prevention of Perinatal Transmission. Recommendations for the use of antiretroviral drugs during pregnancy and interventions to reduce perinatal HIV transmission in the United States. https://clinicalinfo.hiv.gov/en/guidelines/perinatal/whats-new. Updated January 31, 2023. Accessed February 23, 2023.
  3. Vitekta (elvitegravir) [prescribing information]. Foster City, CA: Gilead Sciences; July 2015.
  4. Wijting IEA, Wit FWNM, Rokx C, et al. Immune reconstitution inflammatory syndrome in HIV infected late presenters starting integrase inhibitor containing antiretroviral therapy. EClinicalMedicine. 2019;17:100210. doi:10.1016/j.eclinm.2019.11.003 [PubMed 31891143]
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