Elvitegravir (Vitekta) is an antiviral medicine that is used in combination with other antiretroviral drugs for the treatment of HIV-1 infection.

Elvitegravir (Vitekta) Uses:

• HIV-1 infection:

  • It is indicated for the treatment of adult patients with HIV-1 infection in patients who have previously been on antiretroviral therapy.
  • It is used in combination with an HIV protease inhibitor coadministered with ritonavir and with other antiretroviral drugs.

• Off Label Use of Elvitegravir in Adults:

  • Treatment of HIV-1 infectiom in antiretroviral-naive patients

Adult dose:

 Note: In the US, Vitekta has been discontinued for more than a year.

Elvitegravir (Vitekta) Dose in HIV-1 infection in antiretroviral treatment-experienced patients: 

Note:

• • Administer the drug in combination with other antiretroviral drugs (a protease inhibitor, ritonavir, or other antiretroviral drugs)

• When administered with concomitant atazanavir and ritonavir or lopinavir and ritonavir:

  • 85 mg orally once a day.

• When administered with concomitant darunavir and ritonavir, fosamprenavir and ritonavir, or tipranavir and ritonavir:

  • 150 mg once a day.

Use in Children: 

Not indicated. 

Elvitegravir (Vitekta) Pregnancy Risk Factor: B

• It is relatively easy for the drug to cross the placental barriers.
• Limited data are available on the drug's teratogenicity.
• Although antiretroviral treatment may increase the risk of preterm birth, information about maternal risk factors like disease severity and other maternal risk factors is contradictory.
• Some studies show an increase in stillbirths, low birth weight, small gestational age, and other risks.
• Antiretroviral treatment for mothers is a good option, as the benefits far outweigh any risks.
• Follow-up should be given to all infants who have been exposed to the drug or antiretroviral treatment. If a child develops significant organ disorder, he or she should be tested for mitochondrial dysfunction.
• Because of low serum levels during pregnancy, Elvitegravir is not recommended for pregnant females with HIV.
• Insufficient pharmacokinetic information makes it impossible to make recommendations for dose adjustment during pregnancy.
• Patients already receiving treatment should be considered to receive a more effective regimen of ART.
• Women who continue the same treatment should be monitored closely, including monitoring for therapeutic drug use.
• Do not administer treatment within two hours after taking calcium- or iron-containing preparations.
• To reduce the risk of HIV virus transmission in perinatal HIV-infected infants, all pregnant women should be treated with antiretroviral medication.
• HIV-positive pregnant patients are more likely to be monitored.
• After delivery, antiretroviral treatment can be continued and may require modification.

Elvitegravir use during breastfeeding:

• It is unknown if the drug will be excreted into breastmilk.
• Postnatal HIV transmission can still be prevented by maternal ART and antiretroviral treatment in infants. There have been instances of infants with multiclass resistance to HIV virus despite receiving maternal ART.
• The risk of developing gastrointestinal or respiratory tract infections in children should be avoided.

Dose in Kidney disease: 

• Adjustment in the dose is not necessary.

Elvitegravir (Vitekta) Dose in Liver disease:

• Mild-to-moderate hepatic impairment (Child-Pugh class A or B):
  • Adjustment in the dose is not necessary.
• Severe hepatic impairment (Child-Pugh class C):
  • Avoid its use (it has not been studied).

Side Effects of Elvitegravir (Vitekta):

• Central Nervous System:

  • Headache
  • Depression
  • Fatigue
  • Insomnia
  • Suicidal Ideation

• Dermatologic:

  • Skin Rash

• Gastrointestinal:

  • Diarrhea
  • Nausea
  • Abdominal Pain
  • Dyspepsia
  • Vomiting

• Immunologic:

  • Immune Reconstitution Syndrome

Contraindications to Elvitegravir (Vitekta):

The manufacturer has not provided any information about contraindications.

Warnings and precautions

• Immune reconstitution syndrome:
  • The immune reconstitution syndrome, which is an exaggerated reaction to indolent or residual opportunistic infections, occurs following the start of antiretroviral therapy.
  • Some patients may be affected by autoimmune disorders like polymysitis or Guillain Barre syndrome.
  • It is important to evaluate the underlying cause of the problem. Some patients may require glucocorticoids, or temporary interruptions to their treatment.

• Hepatic impairment

  • Patients with mild or moderate hepatic dysfunction should not be given a dose adjustment.
  • Treatment with elvitegravir should not be attempted in patients suffering from severe hepatic impairment.

Elvitegravir: Drug Interaction

Note: Drug Interaction Categories:

• Risk Factor C: Monitor When Using Combination
• Risk Factor D: Consider Treatment Modification
• Risk Factor X: Avoid Concomitant Use

Monitoring parameters:

• CBC with differential counts,
• Reticulocyte count,
• CD4 count,
• Plasma levels of HIV RNA
• Liver function tests,
• Prior to treatment (antiretroviral therapy) initiation, test the patient for Hepatitis B infection.

How to administer Elvitegravir (Vitekta)?

• Administer the drug orally once a day with food.

Mechanism of action of Elvitegravir:

It blocks the enzyme integrase, which is necessary for HIV-DNA integration into the host genome. It prevents the spread of the virus through the blocking of HIV-1 provirus formation. It does not interfere with human topoisomerase enzymes. Absorption:

• AUC increases with food

Protein binding:

• 99%

Metabolism:

• It is metabolized in the liver via CYP3A enzymes and also hepatic glucuronidation mediated by UGT1A1/3

Terminal Half-life elimination:

• ~9 hours

Time to peak plasma concentration:

• ~4 hours

Excretion:

• Feces (~95%);
• Urine (~7%)

International Brand Names of Elvitegravir:

• Vitekta

Elvitegravir Brand Names in Pakistan:

• No Brands Available in Pakistan.