Drug updates

Fostemsavir(FTR)

Fostemsavir(FTR)

  HIV Drug update -2020

RUKOBIA (fostemsavir) extended-release tablets, for oral use


DESCRIPTION

  •  Fostemsavir tromethamine – prodrug of temsavir, an HIV-1 gp120-directed attachment inhibitor.

CHEMICAL NAME

  • 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

Capture
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.

CONTRAINDICATIONS

  • 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

ADVERSE REACTIONS

  • 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 )

DRUG INTERACTIONS

  • 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

Reference : https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212950s000lbl.pdf

11
About Author

Dermacademy.in

Leave a Reply