HIV Drug update -2020
RUKOBIA (fostemsavir) extended-release tablets, for oral use
- Fostemsavir tromethamine – prodrug of temsavir, an HIV-1 gp120-directed attachment inhibitor.
- 3-((4-benzoyl-1-piperazinyl)(oxo)acetyl)-4-ethoxy-7-(3-methyl-1H-1,2,4-triazol-1-yl)-1H-pyrrolo[2,3-c]pyridin-1-yl)methyl dihydrogen phosphate, -amino-2-(hydroxymethyl)-1,3-propanediol (1:1).
- The empirical formula is C25H26N7O8PxC4H11NO3
INDICATIONS AND USAGE
- Given 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.
DOSAGE AND ADMINISTRATION
- Extended-release tablets: 600 mg (equivalent to 725 mg of fostemsavir tromethamine)
- One tablet taken twice daily with or without food.
- Hypersensitivity to fostemsavir or any of the components of the formulation.
- Coadministration with strong cytochrome P450 (CYP)3A inducers (eg: Rifampin, Carbamazepine, phenytoin,Herbal product: St John’s wort etc) as significant decreases in temsavir (the active moiety of fostemsavir) plasma concentrations may occur, which may result in loss of virologic response.
WARNINGS AND PRECAUTIONS
- Immune reconstitution syndrome
- QTc prolongation: Use 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 or C virus co-infection
- The most common adverse reaction (all grades) observed in 5% of subjects was nausea.
- (To report SUSPECTED ADVERSE REACTIONS, contact ViiV Healthcare at 1-877-844-8872 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch )
- When coadministered with OCPs, temsavir increased concentrations of ethinyl estradiol
- Doses of OCPs should not contain more than 30 mcg of ethinyl estradiol per day.
USE IN SPECIFIC POPULATIONS
- Pregnancy Cateogory: Not yet classified (N)
- Lactation: Breastfeeding is not recommended due to the potential for HIV-1 transmission