Celsentri

Celsentri - General Information

Celsentri (brand-named Selzentry, or Celsentri outside the U.S.) is a chemokine receptor antagonist drug developed by the drug company Pfizer that is designed to act against HIV by interfering with the interaction between HIV and CCR5. It was originally labelled as UK-427857 during development but was assigned the Celsentri name as it entered trials. It was approved for use by the FDA in August, 2007.

Pharmacology of Celsentri

Celsentri is a chemokine receptor antagonist drug developed by the drug company Pfizer that is designed to act against HIV by interfering with the interaction between HIV and CCR5.

Additional information about Celsentri

Celsentri Indication: For treatment-experienced adult patients infected with only CCR5-tropic HIV-1 detectable, who have evidence of viral replication and HIV-1 strains resistant to multiple antiretroviral agents.
Mechanism Of Action: Celsentri is an entry inhibitor and works by blocking HIV from entering human cells. Specifically maraviroc is a selective, slowly reversible, small molecule antagonist of the interaction between human CCR5 and HIV-1 gp120. Celsentri selectively binds to the human chemokine receptor CCR5 present on the membrane of CD4 cells (T-cells), preventing the interaction of HIV-1 gp120 and CCR5 necessary for CCR5-tropic HIV-1 to enter cells.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Maraviroc
Synonyms: Not Available
Drug Category: Anti-HIV Agents
Drug Type: Small Molecule; Approved; Investigational

Other Brand Names containing Maraviroc: Selzentry; Celsentri;
Absorption: The absolute oral bioavailability of a 100 mg dose is 23% and is predicted to be 33% at 300 mg. Coadministration of a 300mg tablet with a high fat breakfast reduced maraviroc Cmax and AUC by 33% in healthy volunteers.
Toxicity (Overdose): Not Available
Protein Binding: Approximately 76% bound to human plasma proteins, with moderate affinity for albumin and alpha-1 acid glycoprotein.
Biotransformation: In vitro studies indicate that CYP3A is the major enzyme responsible for maraviroc metabolism.
Half Life: 14-18 hours
Dosage Forms of Celsentri: Tablet, film coated Oral
Chemical IUPAC Name: 4,4-difluoro-N-[(1S)-3-[(1R,5S)-3-(3-methyl-5-propan-2-yl-1,2,4-triazol-4-yl)-8-azabicyclo[3.2.1]octan-8-yl]-1-phenylpropyl]cyclohexane-1-carboxamide
Chemical Formula: C29H41F2N5O
Maraviroc on Wikipedia: https://en.wikipedia.org/wiki/Maraviroc
Organisms Affected: Human Immunodeficiency Virus