Dosing and uses of Vitekta (elvitegravir)
Adult dosage forms and strengths
tablet
- 85mg
- 150mg
HIV Infection
For use in combination with an HIV protease inhibitor coadministered with ritonavir and with other antiretroviral drug(s) indicated for the treatment of HIV-1 infection in antiretroviral treatment-experienced adults
Elvitegravir 85-mg dose
- 85 mg PO qDay plus atazanavir 300 mg qDay plus ritonavir 100 mg qDay
- 85 mg PO qDay plus lopinavir 400 mg PO BID plus ritonavir 100 mg BID
Elvitegravir 150-mg dose
- 150 mg PO qDay plus darunavir 600 mg PO BID plus ritonavir 100 mg BID
- 150 mg PO qDay plus fosamprenavir 700 mg PO BID plus ritonavir 100 mg BID
- 150 mg PO qDay plus tipranavir 500 mg PO BID plus ritonavir 200 mg BID
Dosage modifications
Coadministration with rifabutin: Decrease rifabutin dose by ~75%; (eg, rifabutin 300 mg/day reduced to 150 mg every other day or 3 times per week)
Dosing Considerations
Limitation of use
- No comparative pharmacokinetic or clinical data exist evaluating elvitegravir with cobicistat as single entities compared with Stribild
- Elvitegravir coadministered with protease inhibitors and cobicistat is not recommended
- Coadministration of elvitegravir with dosage regimens or HIV-1 protease inhibitors other than those listed above is not recommended
Administration
Must be taken with food
Elvitegravir plasma concentrations are lower with antacids, owing to the formation of ionic complexes in the GI tract and not to changes in gastric pH; separate elvitegravir and antacid administration by at least 2 hr
Pediatric dosage forms and strengths
Safety and efficacy not established
Vitekta (elvitegravir) adverse (side) effects
2-10%
Diarrhea (7%)
Total bilirubin, >2.5 x ULN (6%)
Hematuria, >75 RBC/HPF (6%)
Serum amylase, >2 x ULN (6%)
Creatine kinase, ≥10 x ULN (6%)
Total cholesterol, >300 mg/dL (5%)
Total triglycerides, >250 mg/dL (5%)
Hyperglycemia, >250 mg/dL (5%)
Urine glucose, +4 (4%)
Nausea (4%)
Headache (3%) GGT, >5 x ULN (3%)
Neutrophils, <750/mm³ (3%)
ALT or AST, >5 x ULN (2%)
<2%
Gastrointestinal disorders: Abdominal pain, dyspepsia, vomiting
General disorders and administration site conditions: Fatigue
Psychiatric disorders: Depression, insomnia, suicidal ideation and suicide attempt (<1%, most in subjects with a preexisting history of depression or psychiatric illness)
Skin and subcutaneous tissue disorders: Rash
Warnings
Contraindications
None for elvitegravir; consult prescribing information for ritonavir and coadministered protease inhibitor
Immune reconstitution syndrome reported with combination ARTs, consisting of anti-inflammatory response to indolent or residual opportunistic infections (eg, Mycobacterium avium infection, CMV, Pneumocystis jirovecii pneumonia [PCP], tuberculosis)
Autoimmune disorders (eg, Graves disease, polymyositis, and Guillain-Barré syndrome) have also been reported to occur with immune reconstitution syndrome
Pregnancy and lactation
Pregnancy category: B
Antiretroviral Pregnancy Registry: 1-800-258-4263
Lactation: Unknown whether distributed in breast milk
In the United States, the CDC recommends that HIV-infected mothers not breastfeed their infants, to avoid risking postnatal transmission of HIV
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Vitekta (elvitegravir)
Mechanism of action
Integrase strand transfer inhibitor (INSTI)
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
Absorption
Peak plasma time: 4 hr
Peak plasma concentration: 1.2-1.5 mcg/mL
Trough plasma concentration: 0.35-0.42 mcg/mL
AUC: 18 mcg•h/mL
Food increases mean systemic exposure of elvitegravir by 34%
A high fat meal (~800 kcal, 50% fat) increases mean systemic exposure of elvitegravir by 87%
Distribution
Protein bound: 98-99%
Metabolism
Metabolized by CYP3A4
Also undergoes glucuronidation via UGT1A1/3 enzymes
Elimination
Half-life: 8.7 hr (administered with ritonavir)
Excretion: 94.8% feces, 6.7% urine
