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Elvitegravir

Medically reviewed by Drugs.com. Last updated on Jul 7, 2020.

Pronunciation

(el vi TEG ra vir)

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Tablet, Oral:

Vitekta: 85 mg [DSC], 150 mg [DSC] [contains fd&c blue #2 aluminum lake]

Brand Names: U.S.

  • Vitekta [DSC]

Pharmacologic Category

  • Antiretroviral, Integrase Inhibitor (Anti-HIV)

Pharmacology

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.

Absorption

AUC increases with food

Metabolism

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

Excretion

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

Time to Peak

Plasma: ~4 hours

Half-Life Elimination

Terminal: ~9 hours

Protein Binding

99%

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

Contraindications

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

Dosing: Adult

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

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: Geriatric

Refer to adult dosing.

Administration

Oral: Administer once daily with food.

Dietary Considerations

Take with food.

Storage

Store below 30°C (86°F). Dispense only in original container.

Drug Interactions

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. Exceptions: Potassium Bicarbonate; Sodium Bicarbonate. 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. Consider therapy modification

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

CYP3A4 Inducers (Moderate): May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

CYP3A4 Inducers (Strong): May increase the metabolism of CYP3A4 Substrates (High risk with Inducers). Management: Consider an alternative for one of the interacting drugs. Some combinations may be specifically contraindicated. Consult appropriate manufacturer labeling. Consider therapy modification

Dabrafenib: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Seek alternatives to the CYP3A4 substrate when possible. If concomitant therapy cannot be avoided, monitor clinical effects of the substrate closely (particularly therapeutic effects). 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. Consider therapy modification

Deferasirox: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

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. Consider therapy modification

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

Enzalutamide: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Concurrent use of enzalutamide with CYP3A4 substrates that have a narrow therapeutic index should be avoided. Use of enzalutamide and any other CYP3A4 substrate should be performed with caution and close monitoring. Consider therapy modification

Erdafitinib: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

Estrogen Derivatives (Contraceptive): Elvitegravir may decrease the serum concentration of Estrogen Derivatives (Contraceptive). Management: Consider the use of an alternative, non-hormone-based contraceptive, in patients who are being treated with elvitegravir-containing products. Consider therapy modification

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

Itraconazole: May increase the serum concentration of Elvitegravir. Management: Limit itraconazole to a maximum dose of 200 mg/day in patients who are being treated with the elvitegravir-containing products. Monitor for evidence of itraconazole or elvitegravir toxicity in patients receiving this combination. Consider therapy modification

Ivosidenib: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

Ketoconazole (Systemic): May increase the serum concentration of Elvitegravir. Management: Limit ketoconazole to a maximum dose of 200 mg/day in patients who are being treated with an elvitegravir-containing product. Monitor for ketoconazole or elvitegravir toxicity in patients receiving this combination. Consider therapy modification

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. Consider therapy modification

Mitotane: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Doses of CYP3A4 substrates may need to be adjusted substantially when used in patients being treated with mitotane. Consider therapy modification

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

Orlistat: May decrease the serum concentration of Antiretroviral Agents. 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 antiepileptic when possible. Avoid combination

PHENobarbital: May decrease the serum concentration of Elvitegravir. 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. Exceptions: Almagate; Aluminum Hydroxide; Calcium Carbonate; Diomagnite; Magaldrate; Magnesium Carbonate; Magnesium Hydroxide; Magnesium Trisilicate. Consider therapy modification

Rifabutin: Elvitegravir may increase serum concentrations of the active metabolite(s) of Rifabutin. Rifabutin may decrease the serum concentration of Elvitegravir. Management: For single-agent elvitegravir, a rifabutin dose reduction of at least 75% is required (ie, reduction to adult dose of 150 mg every other day or three times/week). Use of elvitegravir combination products with rifabutin is not recommended. Avoid combination

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

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

Sarilumab: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

Siltuximab: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

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

Tocilizumab: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

Voriconazole: May increase the serum concentration of Elvitegravir. Management: Careful consideration of the risk/benefit ratio for voriconazole use is recommended prior to its use in patients treated with elvitegravir-containing products. Consider therapy modification

Adverse Reactions

Percentages are reported for antiretroviral treatment experienced adults.

1% to 10%:

Central nervous system: Headache (3%), depression (<2%), fatigue (<2%), insomnia (<2%), suicidal ideation (<2%)

Dermatologic: Skin rash (<2%)

Gastrointestinal: Diarrhea (7%), nausea (4%), abdominal pain (<2%), dyspepsia (<2%), vomiting (<2%)

Immunologic: Immune reconstitution syndrome

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.

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.

Reproductive Considerations

The Health and Human Services perinatal HIV guidelines do not recommend an elvitegravir-containing regimen for females living with HIV who are not yet pregnant but are trying to conceive (HHS [perinatal] 2019).

For males and females living with HIV and planning a pregnancy, maximum viral suppression below the limits of detection with antiretroviral therapy (ART), modification of therapy (if needed), optimization of the woman’s health, and a discussion of the potential risks and benefits of ART therapy during pregnancy is recommended prior to conception (HHS [perinatal] 2019).

Pregnancy Risk Factor

B

Pregnancy Considerations

Elvitegravir has a high level of transfer across the placenta.

Data collected by the antiretroviral pregnancy registry are insufficient to evaluate teratogenic risk. Maternal antiretroviral therapy (ART) may be associated with adverse pregnancy outcomes including preterm delivery, stillbirth, 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 without HIV but who were exposed to ART in utero and develop significant organ system abnormalities of unknown etiology (particularly of the CNS or heart) should be evaluated for potential mitochondrial dysfunction.

The Health and Human Services perinatal HIV guidelines do not recommend an elvitegravir-containing regimen in pregnant females living with HIV due to inadequate serum concentrations observed during pregnancy. Pharmacokinetic data are insufficient to make dosing recommendations during pregnancy. If pregnancy occurs during therapy, consideration should be given to changing to a more effective regimen. If continued, close monitoring, including more frequent therapeutic drug monitoring if available, is recommended. Do not administer within 2 hours of iron or calcium containing preparations, including prenatal vitamins.

In general, ART is recommended for all pregnant females living with HIV to keep the viral load below the limit of detection and reduce the risk of perinatal transmission. Therapy should be individualized following a discussion of the potential risks and benefits of treatment during pregnancy. Monitoring of pregnant females is more frequent than in nonpregnant adults. ART should be continued postpartum for all females living with HIV and can be modified after delivery.

Health care providers are encouraged to enroll pregnant females exposed to antiretroviral medications as early in pregnancy as possible in the Antiretroviral Pregnancy Registry (1-800-258-4263 or http://www.APRegistry.com). Health care providers caring for pregnant females living with HIV and their infants may contact the National Perinatal HIV Hotline (888-448-8765) for clinical consultation (HHS [perinatal] 2019).

Patient Education

What is this drug used for?

• It is used to treat HIV infection.

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

• Diarrhea

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Infection

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.

Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.

Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a limited summary of general information about the medicine's uses from the patient education leaflet and is not intended to be comprehensive. This limited summary does NOT include all information available about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not intended to provide medical advice, diagnosis or treatment and does not replace information you receive from the healthcare provider. For a more detailed summary of information about the risks and benefits of using this medicine, please speak with your healthcare provider and review the entire patient education leaflet.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

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