Pharmacist Medication Insights: Fostemsavir (Rukobia) for HIV

Fostemsavir (Rukobia) has been approved by the FDA for the treatment of HIV-1 infection. The medication is indicated in combination with other antiretroviral medications in heavily treatment-experienced (HTE) adults with multidrug-resistant HIV-1 infection failing their antiretroviral regimen due to intolerance, resistance, or safety considerations. HTE patients comprise approximately 6% of patients with HIV-1 using treatment.

Rukobia is a glycoprotein 120-directed attachment inhibitor. It is a prodrug that is hydrolyzed to its active moiety, temsavir. Temsavir binds directly to the glycoprotein 120 subunit of the HIV-1 envelope and selectively inhibits the interaction between the virus and cellular CD4 receptors. In addition, temsavir can inhibit glycoprotein 120-dependent post-attachment steps that are required for viral entry into host cells.

Temsavir reaches maximum plasma concentrations 2 hours after oral administration and displays an elimination half-life of 11 hours. Age, ethnicity, race, and sex do not affect its pharmacokinetics.