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Rukobia Generic Name & Formulations
Legal Class
Rx
General Description
Fostemsavir 600mg; ext-rel tabs.
Pharmacological Class
HIV-1 gp120-directed attachment inhibitor.
How Supplied
Ext-rel tabs—60
Manufacturer
Generic Availability
NO
Mechanism of Action
Fostemsavir is a prodrug without significant biochemical or antiviral activity that is hydrolyzed to the active moiety, temsavir, which is an HIV-1 attachment inhibitor. Temsavir binds directly to the gp120 subunit within the HIV-1 envelope glycoprotein gp160 and selectively inhibits the interaction between the virus and cellular CD4 receptors, thereby preventing attachment. Additionally, temsavir can inhibit gp120-dependent post-attachment steps required for viral entry into host cells.
Rukobia Indications
Indications
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.
Rukobia Dosage and Administration
Adult
Swallow whole. 600mg twice daily.
Children
Not established.
Rukobia Contraindications
Contraindications
Concomitant strong CYP3A4 inducers (eg, enzalutamide, carbamazepine, phenytoin, rifampin, mitotane, St. John's wort).
Rukobia Boxed Warnings
Not Applicable
Rukobia Warnings/Precautions
Warnings/Precautions
History of QTc interval prolongation. Preexisting cardiac disease. Immune reconstitution syndrome. Monitor LFTs in those with hepatitis B and/or C coinfection. Elderly. Pregnancy. Nursing mothers.
Rukobia Pharmacokinetics
Absorption
Absolute bioavailability: 26.9%. Time to maximum concentration: 2 hours.
Distribution
Volume of distribution (at steady-state): 29.5 L. Plasma protein bound: 88.4%.
Elimination
Renal (51%), fecal (33%). Half-life: 11 hours. Clearance: 17.9 L/h.
Rukobia Interactions
Interactions
See Contraindications. May be antagonized by strong CYP3A4 inducers. May potentiate HCV direct-acting antivirals (eg, grazoprevir, voxilaprevir), statins drugs (eg, rosuvastatin, atorvastatin, fluvastatin, pitavastatin, simvastatin), ethinyl estradiol. Caution when concomitant drugs with a known risk for Torsade de Pointes.
Rukobia Adverse Reactions
Adverse Reactions
Nausea, diarrhea, headache, abdominal pain, dyspepsia, fatigue, rash, sleep disturbance; elevated transaminases.
Rukobia Clinical Trials
See Literature
Rukobia Note
Not Applicable
Rukobia Patient Counseling
See Literature
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