celsentri

celsentri Uses, Dosage, Side Effects, Food Interaction and all others data.

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.

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.

celsentri
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	celsentri
Availability	Prescription only
Generic	Maraviroc
Maraviroc Other Names	Maraviroc, Maravirocum
Related Drugs	Biktarvy, Truvada, tenofovir, ritonavir, Complera, Atripla, Stribild
Weight	150mg, 300mg,
Type	Film-coated Tablet, Tablet
Formula	C₂₉H₄₁F₂N₅O
Weight	Average: 513.6655 Monoisotopic: 513.327917369
Protein binding	Approximately 76% bound to human plasma proteins, with moderate affinity for albumin and alpha-1 acid glycoprotein.
Groups	Approved, Investigational
Therapeutic Class
Manufacturer	Glaxosmithkline (gsk), Viiv Healthcare Uk Ltd
Available Country	Saudi Arabia, Australia, Canada, United Kingdom, United States, France, Italy, Netherlands, Portugal, Spain, Switzerland,
Last Updated:	September 19, 2023 at 7:00 am

Uses

celsentri is a CCR5 co-receptor antagonist used with other antiretroviral medications to treat CCR5-tropic HIV-1 infection.

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.

celsentri is also used to associated treatment for these conditions: Human Immunodeficiency Virus Type 1 (HIV-1) Infection

How celsentri works

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.

Food Interaction

Avoid St. John's Wort. This herb induces CYP3A metabolism and may reduce serum levels of maraviroc.
Take with or without food.

[Minor] Administration with food may reduce the bioavailability of maraviroc.

According to the product labeling, coadministration of a 300 mg dose of maraviroc with a high-fat breakfast reduced maraviroc peak plasma concentration (Cmax) and systemic exposure (AUC) by 33% in healthy volunteers.

However, no food restrictions were used in the clinical studies that demonstrated the safety and efficacy of maraviroc.

Therefore, maraviroc can be taken with or without food at the recommended dosage.

celsentri Drug Interaction

Major: ritonavir, ritonavirUnknown: contained in alcoholic beverages , contained in alcoholic beverages , lorazepam, lorazepam, diphenhydramine, diphenhydramine, loratadine, loratadine, cyclobenzaprine, cyclobenzaprine, ascorbic acid, ascorbic acid, cholecalciferol, cholecalciferol, alprazolam, alprazolam, zinc sulfate, zinc sulfate

celsentri Disease Interaction

Major: hepatotoxicity/liver impairment, renal impairmentModerate: cardiovascular disease

Volume of Distribution

194 L

Elimination Route

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.