Cenicriviroc (

INN Inns are generally establishments or buildings where travelers can seek lodging, and usually, food and drink. Inns are typically located in the country or along a highway; before the advent of motorized transportation they also provided accommo ...

, code names TAK-652, TBR-652, commonly abbreviated as CVC) is an experimental drug candidate for the treatment of

HIV The human immunodeficiency viruses (HIV) are two species of ''Lentivirus'' (a subgroup of retrovirus) that infect humans. Over time, they cause acquired immunodeficiency syndrome (AIDS), a condition in which progressive failure of the immune ...

infection and in combination with

Tropifexor Tropifexor is an investigational drug which acts as an agonist of the farnesoid X receptor (FXR). It was discovered by researchers from Novartis and Genomics Institute of the Novartis Research Foundation. Its synthesis and pharmacological propert ...

for

non-alcoholic steatohepatitis Non-alcoholic fatty liver disease (NAFLD), also known as metabolic (dysfunction) associated fatty liver disease (MAFLD), is excessive fat build-up in the liver without another clear cause such as alcohol use. There are two types; non-alcoholic ...

. It is being developed by

Takeda is a Japanese family name.1990 Census Name Files< ...

and Tobira Therapeutics. Cenicriviroc is an inhibitor of

CCR2 C-C chemokine receptor type 2 (CCR2 or CD192 ( cluster of differentiation 192) is a protein that in humans is encoded by the ''CCR2'' gene. CCR2 is a CC chemokine receptor. Gene This CCR2 gene is located in the chemokine receptor gene clust ...

and

CCR5 C-C chemokine receptor type 5, also known as CCR5 or CD195, is a protein on the surface of white blood cells that is involved in the immune system as it acts as a receptor for chemokines. In humans, the ''CCR5'' gene that encodes the CCR5 p ...

receptors, allowing it to function as an

entry inhibitor Entry inhibitors, also known as fusion inhibitors, are a class of antiviral drugs that prevent a virus from entering a cell, for example, by blocking a receptor. Entry inhibitors are used to treat conditions such as HIV and hepatitis D. HIV entr ...

which prevents the virus from entering into a human cell. Inhibition of CCR2 may have an anti-inflammatory effect. A double-blind, randomized, placebo-controlled clinical study to assess the antiviral activity, safety, and tolerability of cenicriviroc was conducted in 2010. HIV-infected patients taking cenicriviroc had significant reductions in viral load, with the effect persisting up to two weeks after discontinuation of treatment. Additional Phase II clinical trials are underway. Cenicriviroc is also in two separate clinical trials for

COVID-19 Coronavirus disease 2019 (COVID-19) is a contagious disease caused by a virus, the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). The first known case was identified in Wuhan, China, in December 2019. The disease quickly ...

: the ACTIV-I trial run by the

National Center for Advancing Translational Sciences The National Center for Advancing Translational Sciences (NCATS) was established in 2012 and is located in Bethesda, Maryland. NCATS is one of 27 institutes and centers of the US National Institutes of Health (NIH), an agency of the US Departmen ...

, where it is compared with a number of other immunomodulatory agents, and the Charité Trial of Cenicriviroc at the Charité Hospital in

Berlin Berlin ( , ) is the capital and List of cities in Germany by population, largest city of Germany by both area and population. Its 3.7 million inhabitants make it the European Union's List of cities in the European Union by population within ci ...

. , both trials are recruiting participants, and are expected to complete in September 2021. Phase IIb data presented at the 20th Conference on Retroviruses and Opportunistic Infections (CROI) in March 2013 showed similar viral suppression rates of 76% for patients taking 100 mg cenicriviroc, 73% with 200 mg cenicriviroc, and 71% with efavirenz. Non-response rates were higher with cenicriviroc, however, largely due to greater drop-out of patients. A new tablet formulation with lower pill burden may improve adherence. Looking at immune and inflammatory biomarkers, levels of

MCP-1 ''For the ICAO airport code see Candle Lake Airpark, for the diradical compound see Dichlorocarbene.'' The chemokine (C-C motif) ligand 2 (CCL2) is also referred to as monocyte chemoattractant protein 1 (MCP1) and small inducible cytokine A2. CC ...

increased and soluble

CD14 CD14 (cluster of differentiation 14) is a human protein made mostly by macrophages as part of the innate immune system. It helps to detect bacteria in the body by binding lipopolysaccharide (LPS), a pathogen-associated molecular pattern (PAMP). ...

decreased in the cenicriviroc arms.CROI 2013: CCR5/CCR2 Inhibitor Cenicriviroc Has Both Anti-HIV and Anti-inflammatory Effects
Highleyman, Liz. HIVandHepatitis.com. 7 March 2013.

References

{{Chemokine receptor modulators Benzazocines Entry inhibitors Imidazoles Sulfoxides Experimental drugs

See also

References