Fostemsavir

RUKOBIA, in combination with other antiretroviral(s), is indicated for the treatment of human immunodeficiency virus type 1 (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, a human immunodeficiency virus type 1 (HIV-1) gp120-directed attachment inhibitor, in combination with other antiretroviral(s), is indicated 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 an HIV-1 antiretroviral agent.

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. One tablet taken twice daily with or without food.

RUKOBIA is contraindicated in patients: • with previous hypersensitivity to fostemsavir or any of the components of RUKOBIA. • coadministered strong cytochrome P450 (CYP)3A inducers, as significant decreases in temsavir (the active moiety of fostemsavir) plasma concentrations may occur which may result in loss of virologic response. These drugs include, but are not limited to: o Androgen receptor inhibitor: Enzalutamide o Anticonvulsants: Carbamazepine, phenytoin o Antimycobacterial: Rifampin o Antineoplastic: Mitotane o Herbal product: St John’s wort ( Hypericum perforatum ) • Hypersensitivity to fostemsavir or any of the components of the formulation.

• Immune reconstitution syndrome has been reported in patients treated with combination antiretroviral therapies. • QTc prolongation: Use RUKOBIA with caution in patients with a history of QTc prolongation or with relevant pre-existing cardiac disease or who are taking drugs with a known risk of Torsade de Pointes. • Elevations in hepatic transaminases in patients with hepatitis B (HBV) or C (HCV) virus co-infection: Elevations in hepatic transaminases were observed in a greater proportion of subjects with HBV and/or HCV co-infection compared with those with HIV mono-infection.

The following adverse reactions are discussed in greater detail in other sections of the labeling: • Immune reconstitution syndrome. • QTc prolongation. • Elevations in hepatic transaminases in patients with hepatitis B or C virus co-infection. The most common adverse reaction (all grades) observed in ≥5% of subjects was nausea.

• See full prescribing information for complete list of significant drug interactions. • Doses of oral contraceptives should not contain more than 30 mcg of ethinyl estradiol per day.

Store at 20°C to 25°C (68°F to 77°F), excursions permitted between 15°C and 30°C (59°F and 86°F).