Product Information
Registration Status: ActiveCELSENTRI FILM-COATED TABLET 300MG is approved to be sold in Singapore with effective from 2009-04-30. It is marketed by GLAXOSMITHKLINE PTE LTD, with the registration number of SIN13641P.
This product contains Maraviroc 300mg in the form of TABLET, FILM-COATED. It is approved for ORAL use.
This product is manufactured by Pfizer Manufacturing Deutschland GmbH in GERMANY.
It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.
Description
Maraviroc (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 Maraviroc name as it entered trials. It was approved for use by the FDA in August, 2007.
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
Maraviroc 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. Maraviroc 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.
Pharmacokinetics
- 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.
- Distribution
- * 194 L
- Metabolism
- In vitro studies indicate that CYP3A is the major enzyme responsible for maraviroc metabolism.
- Elimination
Active Ingredient/Synonyms
Maraviroc | Maraviroc |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.