General Information

Rukobia (fostemsavir) is a human immunodeficiency virus type 1 (HIV-1) gp120-directed attachment inhibitor.

Rukobia is specifically indicated for use in combination with other antiretroviral(s) for the treatment of HIV-1 infection in heavily treatment-experienced adults with multidrug-resistant HIV-1 infection failing their current antiretroviral regimen due to resistance, intolerance, or safety considerations.

Rukobia is supplied as an extended release tablet. The recommended dosage of Rukobia is one 600-mg tablet taken orally twice daily with or without food. Swallow tablets whole. Do not chew, crush, or split tablets.

Mechanism of Action

Rukobia (fostemsavir) is a first-in-class HIV-1 attachment inhibitor. After oral administration, fostemsavir is converted to temsavir, which is then absorbed and exerts antiviral activity by attaching directly to the glycoprotein 120 (gp120) subunit on the surface of the virus, thereby blocking HIV from attaching to host immune system CD4+ T-cells and preventing the virus from infecting those cells and multiplying. As Rukobia is the first antiretroviral therapy to target this step of the viral cycle, there is no demonstrated resistance to other classes of antiretrovirals, which may help patients who have become resistant to most other medicines. 

Side Effects

The most common adverse effect associated with the use of Rukobia is nausea.

Clinical Trial Results

The FDA approval of Rukobia, taken twice daily by mouth, was based on BRIGHTE, a clinical trial of 371 heavily treatment-experienced adults who continued to have high levels of virus (HIV-RNA) in their blood despite being on antiretroviral drugs. Two hundred seventy-two patients were treated in the main trial arm, and an additional 99 patients received Rukobia in a different arm of the trial. Most patients had been treated for HIV for more than 15 years (71 percent), had been exposed to five or more different HIV treatment regimens before entering the trial (85 percent) and/or had a history of AIDS (86 percent). Patients in the main cohort of the trial received either Rukobia or a placebo twice daily for eight days, in addition to their failing antiretroviral regimen. On the eighth day, patients treated with Rukobia had a significantly greater decrease in levels of HIV-RNA in their blood compared to those taking the placebo. After the eighth day, all patients received Rukobia with other antiretroviral drugs. After 24 weeks of Rukobia plus other antiretroviral drugs, 53 percent of patients achieved HIV RNA suppression, where levels of HIV were low enough to be considered undetectable. After 96 weeks, 60 percent of patients continued to have HIV RNA suppression.