GS 9137
GS 9137 Uses, Dosage, Side Effects, Food Interaction and all others data.
GS 9137 is a human immunodeficiency virus type 1 (HIV-1) integrase strand transfer inhibitor (INSTI) used for the treatment of HIV-1 infection in antiretroviral treatment-experienced adults. Because integrase is necessary for viral replication, inhibition prevents the integration of HIV-1 DNA into the host genome and thereby blocks the formation of the HIV-1 provirus and resulting propagation of the viral infection. Although available as a single dose tablet, elvitegravir must be used in combination with an HIV protease inhibitor coadministered with ritonavir and another antiretroviral drug.
GS 9137 was first licensed from Japan Tobacco in 2008 and developed by Gilead Sciences. It was FDA approved on August 27, 2012. On September 24, 2014, the FDA approved the single pill form of elvitegravir.
| Trade Name | GS 9137 |
| Availability | Prescription only |
| Generic | Elvitegravir |
| Elvitegravir Other Names | elvitégravir, Elvitegravir, GS 9137 |
| Related Drugs | Biktarvy, Truvada, tenofovir, ritonavir, Complera, Atripla, Stribild |
| Type | |
| Formula | C23H23ClFNO5 |
| Weight | Average: 447.884 Monoisotopic: 447.124878763 |
| Protein binding | Elvitegravir is 98–99% bound to human plasma proteins |
| Groups | Approved |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
GS 9137 is an antiretroviral agent used in combination with other antiretrovirals for the treatment of HIV-1 infection in antiretroviral treatment-experienced adults.
GS 9137 in combination with an HIV protease inhibitor coadministered with ritonavir and with other antiretroviral drug(s) is indicated for the treatment of HIV-1 infection in antiretroviral treatment-experienced adults.
GS 9137 is also used to associated treatment for these conditions: Human Immunodeficiency Virus Type 1 (HIV-1) Infection
How GS 9137 works
GS 9137 is an HIV-1 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. GS 9137 does not inhibit human topoisomerases I or II.
Toxicity
The most common adverse reactions reported for elvitegravir use during clinical trials include nausea, vomiting, and diarrhea. Less common side effects occurring in <2% of patients, include abdominal pain, dyspepsia, fatigue, insomnia, rash, depression, suicidal ideation, and suicidal attempt.
Food Interaction
- Avoid St. John's Wort. This herb induces the CYP3A metabolism of elvitegravir. Therefore, it may reduce the serum concentration of elvitegravir and its effectiveness.
- Take separate from antacids. Take at least 2 hours before or after antacids.
- Take with food.
[Moderate] ADJUST DOSING INTERVAL: Food enhances the oral bioavailabilities of both elvitegravir and tenofovir.
When a single dose of cobicistat When administered with a high-fat meal (approximately 800 kcal; 50% fat), the mean AUC of elvitegravir and tenofovir increased by 87% and 23%, respectively, relative to fasting conditions. The alterations in mean AUCs of cobicistat and emtricitabine were not clinically significant with either the light or high-fat meal. GS 9137 as a single-ingredient preparation should also be administered once daily with food.
MANAGEMENT: Cobicistat
GS 9137 Drug Interaction
Unknown: aspirin, testosterone, sulfamethoxazole / trimethoprim, ubiquinone, copper gluconate, ethanol, glycerin, heparin, insulin lispro, arginine, levocarnitine, cysteine, lithium, bioflavonoids, vitamin a topical, bioflavonoids, sotalol, tramadol, triamcinolone ophthalmic, valproic acid
GS 9137 Disease Interaction
Elimination Route
Following oral administration of elvitegravir and ritonavir with food, in HIV-1 infected subjects, peak elvitegravir plasma concentrations were observed approximately 4 hours post-dose.
Half Life
The median terminal plasma half-life following administration of elvitegravir and ritonavir was approximately 8.7 hours.
Elimination Route
Following oral administration of [14C]elvitegravir/ritonavir, 94.8% of the dose was recovered in feces, while 6.7% was recovered in urine as metabolites.
Innovators Monograph
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