Elvitegravir

In this article, we will discuss about Elvitegravir (Overview). So, let’s get started.


Elvitegravir is an HIV-1 integrase strand transfer inhibitor. The chemical name of elvitegravir is 6-(3-chloro-2-fluorobenzyl)-1-[(2S)-1-
hydroxy-3-methylbutan-2-yl)-7-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid.

It has a molecular formula of C23H23CIFNO5, and a molecular weight of 447.88.

Elvitegravir is a white to pale yellow powder with a solubility of less than 0.3 micrograms per mL in water at 20°C.

Mechanism of Action

Elvitegravir inhibits the strand transfer activity of HIV-1 integrase (integrase strand transfer inhibitor, INSTI), 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.

Dosage

Elvitegravir, Cobicistat, Emtricitabine, and Tenofovir Alafenamide (GENVOYA) is a four-drug fixed dose combination product containing 150 mg of elvitegravir, 150 mg of cobicistat, 200 mg of emtricitabine, and 10 mg of tenofovir alafenamide (TAF). The recommended dosage of GENVOYA is one tablet taken orally once daily with food in adults and pediatric patients 12 years of age and older with body weight at least 35 kg and creatinine clearance greater than or equal to 30 mL per minute.

Warnings and Precautions

• Risk of adverse reactions or loss of virologic response due to drug
interactions: The concomitant use of Elvitegravir, Cobicistat, Emtricitabine, and Tenofovir Alafenamide (GENVOYA) and other drugs may result in known or potentially significant drug interactions, some of which may lead to loss of therapeutic effect of GENVOYA and possible development of resistance, and possible clinically significant adverse reactions from greater exposures of concomitant drugs.
• Redistribution/accumulation of body fat: Observed in patients receiving antiretroviral therapy.
• Immune reconstitution syndrome: May necessitate further evaluation and treatment.
• New onset or worsening renal impairment: Assessment of serum
creatinine, serum phosphorus, estimated creatinine clearance, urine glucose, and urine protein is recommended before initiating GENVOYA therapy and during therapy as clinically appropriate.

Adverse Reactions

The following adverse drug reactions are observed:

• Lactic Acidosis/Severe Hepatomegaly with Steatosis
• Severe Acute Exacerbations of Hepatitis B
• Immune Reconstitution Syndrome
• New Onset or Worsening Renal Impairment

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