Elvitegravir
 |
|
 |
|
| Clinical data | |
|---|---|
| Trade names | Vitekta; Stribild (fixed-dose combination) |
| Pregnancy category |
|
| Routes of administration |
oral |
| ATC code | |
| Pharmacokinetic data | |
| Protein binding | 98% |
| Metabolism | liver, via CYP3A |
| Biological half-life | 12.9 (8.7–13.7) hours |
| Excretion | liver 93%, renal 7% |
| Identifiers | |
|
|
| Synonyms | GS-9137 |
| CAS Number | |
| PubChem CID | |
| DrugBank | |
| ChemSpider | |
| UNII | |
| KEGG | |
| ChEBI | |
| ChEMBL | |
| NIAID ChemDB | |
| Chemical and physical data | |
| Formula | C23H23ClFNO5 |
| Molar mass | 447.883 g/mol |
| 3D model (Jmol) | |
|
|
|
|
  (what is this?)
|
|
Elvitegravir (EVG) is an integrase inhibitor used to treat HIV infection. It was developed by the pharmaceutical company Gilead Sciences, which licensed EVG from Japan Tobacco in March 2008. The drug gained approval by the U.S. Food and Drug Administration on August 27, 2012 for use in adult patients starting HIV treatment for the first time as part of the fixed dose combination known as Stribild. On September 24, 2014 the FDA approved Elvitegravir as a single pill formulation under the trade name Vitekta. On November 5, 2015 the FDA approved the drug for use in patients affected with HIV-1 as a part of a second fixed dose combination pill known as Genvoya.
According to the results of the phase II clinical trial, patients taking once-daily elvitegravir boosted by ritonavir had greater reductions in viral load after 24 weeks compared to individuals randomized to receive a ritonavir-boosted protease inhibitor.
In the United States, elvitegravir can be obtained either as part of the combination pill Stribild or as the single pill formulation Vitekta.
Vitekta is FDA approved to be used for the treatment of HIV-1 infection in adults who have previous treatment experience with antiretroviral therapy. It must be used in combination with a protease inhibitor that is coadministered with ritonavir as well as additional antiretroviral drug(s).
The most common side effects of taking elvitegravir are diarrhea (in 7% of patients) and nausea (4%). Other side effects that occurred in more than 1% of people are headache, tiredness, rashes, and vomiting.
Elvitegravir is metabolised via the liver enzyme CYP3A. Substances that induce this enzyme can reduce elvitegravir concentrations in the body, potentially triggering the development of resistant virus strains. Consequently, co-administration of strong CYP3A inducers is contraindicated; examples are rifampicin, the anticonvulsants carbamazepine, phenobarbital and phenytoin, as well as St John's wort.
...
Wikipedia