497223-25-3

Usage

Uses

Used in HIV Treatment:
Cenicriviroc is used as an entry inhibitor for the treatment of HIV infection. It targets the CCR2 and CCR5 receptors, preventing the virus from entering human cells and thus suppressing the infection.
Used in Anti-inflammatory Applications:
Cenicriviroc is used as an anti-inflammatory agent, particularly in the context of non-alcoholic fatty liver disease (NAFLD). It has been shown to reduce serum levels of interleukin-6, C-reactive protein, and fibrinogen, suggesting its potential action on inflammation that may not be reflected by crude histological assessment.
Used in Anti-fibrotic Applications:
Cenicriviroc is used as an anti-fibrotic agent, with preclinical studies suggesting its potential to reduce fibrosis in the liver. In the phase 2b CENTAUR study, cenicriviroc treatment showed improvement in liver fibrosis without worsening of non-alcoholic steatohepatitis (NASH) in 20% of the treatment group, compared to 10% in the placebo group.

Clinical Use

Cenicriviroc is a small molecule inhibitor of both CCR2 and CCR5, and has demonstrated safety in early trials of human patients afflicted with HIV-1, as well as a phase IIb trial (ClinicalTrials.gov NCT01338883). Cenicriviroc has also demonstrated therapeutic potential in animal models of liver fibrosis as well as renal fibrosis. A phase II trial of cenicriviroc in patients with NASH and liver fibrosis is planned to complete in late 2017 and (ClinicalTrials.gov NCT02217475). This trial, also called “CENTAUR: Efficacy and Safety Study of Cenicriviroc for the Treatment of Nonalcoholic Steatohepatitis (NASH) in Adult Subjects With Liver Fibrosis,” is a double-blind, placebo-controlled, randomized multinational study with the primary endpoint being histologic improvement of NASH activity score without worsening of fibrosis in patients with NASH and liver fibrosis. Results of this study are pending. An open label rollover extension study of participants in CENTAUR began in early 2017 and is ongoing (ClinicalTrials. gov NCT03059446). There is evidence that CCRs are important in fibrosis in the liver, lung and kidney. At least one molecule that inhibits CCRs has demonstrable safety in human subjects. As such, blockade of CCRs with molecules such as Cenicriviroc represent another potential therapeutic avenue for the treatment of fibrotic inflammatory bowel disease.