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Last update 03 Apr 2026

Cenicriviroc mesylate

Last update 03 Apr 2026

Overview

R&D Status

Clinical Result

Translational Medicine

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

CCR5/CCR2 antagonist, Cenicriviroc, Cenicriviroc mesylate (USAN)

+ [3]

Target

CCR2 x CCR5

Action

antagonists

Mechanism

CCR2 antagonists(C-C chemokine receptor type 2 antagonists), CCR5 antagonists(C-C chemokine receptor type 5 antagonists)

Therapeutic Areas

Endocrinology and Metabolic DiseaseImmune System DiseasesInfectious Diseases+ [4]

Active Indication

ObesityArteritisHIV Infections+ [2]

Inactive Indication

Acquired Immunodeficiency SyndromeAIDS Dementia ComplexCholestasis+ [12]

Originator Organization

Tobira Therapeutics, Inc.

Active Organization

Takeda Pharmaceutical Co., Ltd.

AbbVie, Inc.

Tobira Therapeutics, Inc.

Inactive Organization

Novartis Pharmaceuticals Corp.Allergan UC

Allergan Information Consulting (Shanghai) Co. Ltd.

License Organization

Dong-A ST Co., Ltd.

Quantumleap Healthcare Collaborative

Tobira Therapeutics, Inc.

+ [4]

Drug Highest PhasePhase 3

First Approval Date-

Regulation-

Structure/Sequence

Molecular FormulaC42H56N4O7S2

InChIKeyIXPBPUPDRDCRSY-YLZLUMLXSA-N

CAS Registry497223-28-6

Clinical Trials associated with Cenicriviroc mesylate

NCT05630885

/ CompletedPhase 2IIT

A Limited-Center, Prospective, Double-Blind, Placebo-Controlled Study to Evaluate the Effects of Cenicriviroc Mesylate on Arterial Inflammation in People Living With HIV

The study was conducted to determine if cenicriviroc mesylate (CVC) would decrease vascular inflammation as measured by 18F-fluorodeoxyglucose (FDG)-positron emission tomography (PET)/computed tomography (CT) imaging of the aorta and carotid arteries.

Start Date30 May 2023

Sponsor / Collaborator

National Institute of Allergy & Infectious Diseases

[+1]

NCT04334915

/ WithdrawnPhase 2IIT

A Multicenter, Prospective, Double-Blind, Placebo-Controlled Study to Evaluate the Effects of Cenicriviroc Mesylate on Arterial Inflammation in People Living With HIV

The purpose of this study is to evaluate the effects of cenicriviroc mesylate (CVC) on arterial inflammation in people living with HIV.

Start Date22 Nov 2022

Sponsor / Collaborator

National Institute of Allergy & Infectious Diseases

[+1]

NCT04593940

/ CompletedPhase 3IIT

Randomized Master Protocol for Immune Modulators for Treating COVID-19

ACTIV-1 IM is a master protocol designed to evaluate multiple investigational agents for the treatment of moderately or severely ill patients infected with severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). The research objectives are to evaluate each agent with respect to speed of recovery, mortality, illness severity, and hospital resource utilization. Each agent will be evaluated as add-on therapy to the standard of care (SoC) in use at the local clinics, including remdesivir (provided). The SoC may change during the course of the study based on other research findings. Comparisons of the agents among themselves is not a research objective.
The study population corresponds to moderately and severely ill patients infected with the coronavirus disease 2019 (COVID-19) virus. Recruitment will target patients already hospitalized for treatment of COVID-19 infection as well as patients being treated for COVID-19 infection in Emergency Departments while waiting to be admitted to the hospital. Patients both in and out of the ICU are included in the study population.

Start Date15 Oct 2020

Sponsor / Collaborator

Duke University

[+2]

100 Clinical Results associated with Cenicriviroc mesylate

100 Translational Medicine associated with Cenicriviroc mesylate

100 Patents (Medical) associated with Cenicriviroc mesylate

178

Literatures (Medical) associated with Cenicriviroc mesylate

01 Aug 2025·PATHOLOGY RESEARCH AND PRACTICE

Protective effect of pH-sensitive carvacrol zinc oxide quantum dots on Nrf-2, MAPK and NF-κB pathways and protein-bound carbohydrates in DMBA-induced mammary carcinogenesis

Article

Author: Muthupandian, Saravanan ; Aruchamy, Mohanprasanth ; Srinivasan, Manoj Kumar ; Namasivayam, Nalini

Breast cancer is the most common malignancy among women worldwide, with increasing incidence and significant mortality rates. Conventional treatment strategies, including chemotherapy and radiation, often lead to adverse side effects and may not effectively prevent cancer recurrence or metastasis. pH-sensitive nanoparticles offer a promising alternative, leveraging the acidic tumor microenvironment for targeted drug delivery with minimal systemic toxicity. This study investigates the therapeutic potential of pH-sensitive carvacrol-ZnO quantum dots (CVC-ZnO QDs) in a DMBA-induced mammary cancer model in female Sprague-Dawley rats. The study specifically examines the impact of CVC-ZnO QDs on protein-bound carbohydrate levels and the molecular regulation of Nrf-2, MAPK and NF-κB pathways. Four experimental groups were analyzed: a control group, a DMBA-induced cancer group, a CVC-ZnO QDs-alone treated group and a combined DMBA and CVC-ZnO QDs-treated group. Results revealed that DMBA-induced mammary cancer led to significant elevations in protein-bound carbohydrates, including hexose, hexosamine and sialic acid. CVC-ZnO QDs administration effectively restored these levels to near-normal concentrations. Immunohistochemistry, qRT-PCR and Western blot analyses demonstrated that CVC-ZnO QDs significantly downregulated MAPK and NF-κB expression while upregulating Nrf-2, suggesting enhanced antioxidant defense and suppression of tumor-promoting pathways. Molecular docking confirmed strong binding affinities of CVC to Nrf-2, MAPK and NF-κB, with key hydrogen bonding interactions contributing to the stability of ligand-protein complexes. These findings highlight the potential of CVC-ZnO QDs as a novel therapeutic strategy for breast cancer, offering targeted cytotoxicity with reduced systemic toxicity. Further studies are warranted to explore the clinical translatability of these nanocarriers in breast cancer treatment.

01 Aug 2025·INFLAMMOPHARMACOLOGY

Chemokine receptor type-5: a key regulator of immunity, disease pathogenesis, and emerging therapeutic target

Review

Author: Vanaja, Kenchappa ; Bambal, Vaishali ; Kodihalli Basavaraj, Priyanka

CCR5 (C-C chemokine receptor type 5) is a critical chemokine receptor involved in immune cell migration, signaling, and inflammation. Expressed on T lymphocytes, macrophages, and dendritic cells, it regulates leukocyte recruitment to inflamed sites via ligands such as CCL3, CCL4, and CCL5. Beyond immune regulation, CCR5 is implicated in diseases like rheumatoid arthritis, inflammatory bowel disease, and atherosclerosis, where the CCL5/CCR5 axis exacerbates inflammation and tissue damage. In cancer, CCR5 promotes tumor growth, metastasis, and immune evasion, particularly in aggressive breast cancer subtypes (basal and HER-2 +). It also serves as a co-receptor for HIV entry, with the CCR5Δ32 mutation conferring resistance. With therapeutic inhibition of CCR5 gaining attention, Maraviroc is approved for HIV treatment, while monoclonal antibodies such as leronlimab, genetic strategies (CRISPR), and dual CCR2/CCR5 antagonists such as cenicriviroc are under investigation for broader applications. Blocking CCR5 has shown efficacy in reducing metastasis and improving chemotherapy outcomes, reinforcing its therapeutic potential. Along with CCR5's role in disease pathogenesis, emphasizing its involvement in immune regulation and inflammatory processes, this review explores the multifaceted role of CCR5 in immunity, its contribution to disease pathogenesis, and innovative therapeutic interventions targeting CCR5 to modulate immune responses and treat diseases.

01 Jul 2025·Current Opinion in HIV and AIDS

Understanding residual risk of cardiovascular disease in people with HIV

Review

Author: Stephens, Victoria R. ; Obare, Laventa M. ; Wanjalla, Celestine N.

Purpose of review:

Traditional cardiovascular risk factors, combined with persistent systemic inflammation, contribute to the increased prevalence of atherosclerotic cardiovascular disease (ASCVD) in people with HIV (PWH). This review highlights key findings from the REPRIEVE trial on statin-based primary prevention of major adverse cardiovascular events in PWH. It explores HIV-specific immune mechanisms contributing to residual cardiovascular risk.

Recent findings:

In REPRIEVE, statin therapy used for primary prevention of major adverse cardiovascular events in PWH decreased the plasma lipoprotein-associated phospholipase A2, oxidized low-density lipoprotein, and high-sensitivity C-reactive protein (hs-CRP). However, several inflammatory markers including soluble CD14 (sCD14), sCD163, interleukin (IL)-1β, interleukin (IL)-6, IL-10, and caspase 1 did not change. The HIV reservoir, dysfunctional CD4+ T cells, immunoglobulin G N-glycans, antiapolipoprotein A1 autoantibodies, trained immunity, and clonal hematopoiesis of indeterminate potential may contribute to residual inflammation.

Summary:

Despite antiretroviral and statin therapy, residual ASCVD risk in PWH underscores the need for targeted interventions. Anti-inflammatory therapies, including IL-6 and IL-1β inhibitors, CCR5 antagonists (e.g., maraviroc, cenicriviroc mesylate), and immunomodulatory agents like methotrexate and colchicine, are being explored. Understanding HIV-driven immune dysregulation may lead to novel strategies to mitigate cardiovascular risk in this population.

News (Medical) associated with Cenicriviroc mesylate

10 Jan 2024

·synapse.patsnap.com

What are FXR agonists and how do you quickly get the latest development progress?

FXR, or farnesoid X receptor, is a crucial nuclear receptor found in the human body. It plays a significant role in regulating bile acid metabolism and maintaining overall liver health. FXR is primarily expressed in the liver, intestine, and kidneys, where it controls the synthesis, transport, and excretion of bile acids. By activating FXR, it promotes the production of bile acids, which aid in the digestion and absorption of dietary fats. Additionally, FXR regulates glucose and lipid metabolism, inflammation, and immune responses. Understanding the role of FXR has opened up new avenues for developing therapeutic interventions targeting liver diseases, metabolic disorders, and gastrointestinal disorders. The current competitive landscape of target FXR shows that Intercept Pharmaceuticals, Inc., AbbVie, Inc., and Travere Therapeutics, Inc. are the leading companies with drugs in the highest development phases. These companies have made significant progress in R&D, with drugs in various phases of development. Several drugs under the target FXR have been approved for indications such as Liver Cirrhosis, Biliary; Steatorrhea; Primary Biliary Cholangitis; Inborn error in primary bile acid synthesis; and more. The most rapidly progressing drug types under the target FXR are Small molecule drugs, Chemical drugs, and Fusion protein. Biosimilars do not pose intense competition in this case. Countries/locations such as the United States, China, European Union, and Japan are developing rapidly under the target FXR. China has shown progress in the development of drugs under this target. Overall, the target FXR presents a competitive landscape with multiple companies and drug types in various stages of development. The future development of target FXR holds potential for advancements in the treatment of liver-related indications and offers opportunities for further research and innovation. How do they work?From a biomedical perspective, FXR agonists are a type of drug that activate the farnesoid X receptor (FXR) in the body. The FXR is a nuclear receptor that plays a crucial role in regulating bile acid synthesis, transport, and metabolism. By activating the FXR, these agonists can modulate various metabolic pathways related to cholesterol, bile acid, and glucose homeostasis. FXR agonists have shown potential therapeutic effects in several diseases, particularly in the treatment of liver disorders such as non-alcoholic fatty liver disease (NAFLD) and primary biliary cholangitis (PBC). They can help reduce liver inflammation, improve liver function, and regulate lipid and glucose metabolism. Furthermore, FXR agonists have also demonstrated promising effects in other conditions like metabolic syndrome, diabetes, and inflammatory bowel disease. They work by influencing gene expression and signaling pathways involved in these diseases. Overall, FXR agonists are a class of drugs that target the FXR receptor to modulate various metabolic processes, making them a potential therapeutic option for liver and metabolic disorders. List of FXR AgonistsThe currently marketed FXR agonists include: Obeticholic acidCholic AcidCilofexor tromethamineASC-42Bezafibrate/obeticholic acidCenicriviroc mesylate/TropifexorCilofexor/FirsocostatEDP-305HEC-96719HPG-1860For more information, please click on the image below. What are FXR agonists used for?FXR agonists are commonly used in the treatment of liver disorders such as non-alcoholic fatty liver disease (NAFLD) and primary biliary cholangitis (PBC). For more information, please click on the image below to log in and search. How to obtain the latest development progress of FXR agonists?In the Synapse database, you can keep abreast of the latest research and development advances of FXR agonists anywhere and anytime, daily or weekly, through the "Set Alert" function. Click on the image below to embark on a brand new journey of drug discovery!

01 Jan 2024

·www.labiotech.eu

Viscient Bio discovers first drug using 3D bioprinted tissue model

"*" indicates required fields Viscient Bio, Inc. has announced it has identified the world’s first drug candidate discovered primarily using 3D bioprinted tissue models of disease formed from human cells. The company said it expects to develop the drug to treat non-alcoholic steatohepatitis (NASH), a growing epidemic disease that is believed to affect more than 10% of the U.S. population. NASH can often lead to hepatocellular carcinoma or liver failure. Due to the devastating effects of NASH on patients and its wide prevalence, analysis has projected future pharma industry revenues for the drug in the tens of billions of dollars per year. Viscient Bio’s lead compound is an orally-delivered small molecule designed to hit a novel target identified in 3D bioprinted and other 3D tissue models of disease. In preclinical studies, the drug has proven to be well tolerated. In Viscient Bio’s models of disease, the compound shows reduction of fibrosis as measured by histological evidence similar to that used for human liver biopsy. Using the same model, fibrosis reduction is also seen for obeticholic acid and resmetirom, while no fibrosis reduction is seen for drugs such as cenicriviroc, selonsertib, and elafibranor. The newly discovered target is predominantly expressed in liver tissue. “It is long past time to displace the model of drug development reliant on proof of activity in animals,” said Viscient Bio chief executive officer Keith Murphy. “Viscient’s trailblazing work has resulted in 3D cellular human models of disease in which the performance of previously tested compounds has matched clinical results. Failed NASH drugs never would have been put in humans based on what can be clearly seen in these models. Our novel compound shows fibrosis reduction in these models, as do NASH drugs known to work in phase 3, and we are excited to move this lead program forward.” The lead compound’s clear reduction of fibrosis in Viscient Bio’s NASH models is promising because Viscient Bio’s 3D models of NASH have shown extremely high correlation with clinical results in patients. The model demonstrates fibrosis reduction for known clinical compounds tested by pharma companies that have that effect in humans, while revealing lack of fibrosis reduction for compounds that failed in phase 2 or phase 3 for NASH. The model is accurate in predicting both successes and failures among clinical compounds tested to date. The gene expression of Viscient Bio’s models is also well correlated with that seen in disease samples from patients. Though tested post-hoc, the results are not backfit, as the model was finalized before testing of any clinical compounds was conducted. According to the Biotechnology Innovation Organization’s 2021 report, only 7.9% of drugs that enter clinical trials are approved for human use. Viscient Biosciences said it believes it can achieve a significantly better clinical translation rate using more relevant 3D human tissue models of disease, leading to more successes and lower drug development costs per approved drug. Viscient Biosciences’ lead compound is expected to enter the clinic in 2024.

Phase 3Phase 2

11 Jul 2023

·www.pharmaceutical-technology.com

Covid-19: Anti-inflammatory drugs do not lead to a swifter hospital exit

Robert Barrie There were still over 6,000 hospitalisations due to Covid-19 in the past week in the US. Unvaccinated adults are fives times more likely to die from the disease. Image credit: Shutterstock/Gorodenkoff Anti-inflammatory drugs may reduce deaths due to Covid-19, but they do not help speed up the recovery for those in hospital, according to a recent study. Results from the study , published in The Journal of the American Medical Association , demonstrated that giving abatacept , cenicriviroc, or Johnson and Johnson’s Remicade (infliximab) in addition to standard of care did not decrease time to recovery for patients hospitalised with Covid-19 pneumonia. The standard of care included in this study involved Gilead Sciences’ Veklury (remdesivir) and the corticosteroid dexamethasone. Recommended Reports Reports Artificial Intelligence in Healthcare: Non-Invasive Physiological Monitoring GlobalData Reports Nitric Oxide Synthase (NO Synthase or NOS or EC 1.14.13.39) Drugs in Development by Therapy Areas... GlobalData View all Companies Intelligence SOC Co., Ltd Roche S.A. Genentech, Inc. JAMA Sp. z o.o. View all Patients who took either one of the three drugs recovered after a similar number of days compared to those who were on placebo. The investigators also measured mortality across the sub-studies by day 28 – which did show slight differences, though not statistically significant. Abatacept and Remicade led to a narrow decrease in patient deaths – a 4.1% and 4.4% difference respectively, whilst the cenicriviroc group’s mortality rose by 1.9%. A limitation with the latter group was adherence, however, as cenicriviroc is orally administered, unlike abatacept and Remicade which are infused intravenously. Though the study did not meet any endpoints, the authors note that “expanding treatment armament” is important as SARS-CoV-2 variants may always emerge that may evade antiviral treatments. Although the World Health Organization (WHO) declared an end to the Covid-19 public health emergency, there were still over 6,000 hospitalisations due to the disease in the past week in the US. Based on statistics from March 2023, the Centers for Disease Control and Prevention state that unvaccinated adults are around five times more likely to die from Covid-19. The JAMA trial remains a helpful scaffold with the investigators saying that other previous large-scale Covid-19 studies have not concurrently evaluated multiple agents whilst simultaneously providing a shared placebo group. Still, the study was a randomised, double-masked, placebo-controlled clinical trial (NCT04593940) that enrolled almost 2,000 patients, in comparison to other smaller open-label studies that explored similar questions. However, a limitation of this study itself was that it took place before the SARS-CoV-2 Omicron variant became prevalent. During the pandemic, Covid-19 patients were prescribed the corticosteroid dexamethasone, with research showing that the drug reduces mortality for patients on respiratory support. There was interest in whether giving additional, targeted anti-inflammatory agents could complement steroid action. Tocilizumab, marketed as Actemra by Roche subsidiary Genentech, was given emergency authorisation by the US Food and Drug Administration (FDA) for treating hospitalised Covid-19 patients receiving systemic corticosteroids. “One of the fundamental questions of early Covid-19 research was whether we could dampen the inflammatory process using existing anti-inflammatory drugs,” said Dr. William G. Powderly, national principal investigator of the trial. “Our data suggest that two of the drugs we studied can be given to reduce mortality in severely ill patients. We hope this study will be helpful in revising guidelines for best practices in treating patients hospitalized with Covid-19.”

Clinical StudyClinical ResultDrug Approval

100 Deals associated with Cenicriviroc mesylate

External Link

KEGG	Wiki	ATC	Drug Bank
D09879	Cenicriviroc mesylate	-	DB11758

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Fibrosis, Liver	Phase 3	United States	Tobira Therapeutics, Inc.	05 Apr 2017
Fibrosis, Liver	Phase 3	Australia	Tobira Therapeutics, Inc.	05 Apr 2017
Fibrosis, Liver	Phase 3	Austria	Tobira Therapeutics, Inc.	05 Apr 2017
Fibrosis, Liver	Phase 3	Belgium	Tobira Therapeutics, Inc.	05 Apr 2017
Fibrosis, Liver	Phase 3	Brazil	Tobira Therapeutics, Inc.	05 Apr 2017
Fibrosis, Liver	Phase 3	Canada	Tobira Therapeutics, Inc.	05 Apr 2017
Fibrosis, Liver	Phase 3	Chile	Tobira Therapeutics, Inc.	05 Apr 2017
Fibrosis, Liver	Phase 3	France	Tobira Therapeutics, Inc.	05 Apr 2017
Fibrosis, Liver	Phase 3	Germany	Tobira Therapeutics, Inc.	05 Apr 2017
Fibrosis, Liver	Phase 3	Greece	Tobira Therapeutics, Inc.	05 Apr 2017

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT05630885 (CTgov)	Phase 2	Arteritis \| HIV Infections	110	CVC 300 mg (CVC Arm (Arm A))	giyucjvzpx(mszlzddvca) = orvxbunbbe ouaykskrea (ksccdquilu, vrbveepgxf - yodixerdht) View more	-	16 Jul 2025
				Placebo for CVC 300 mg (Placebo for CVC Arm (Arm B))	giyucjvzpx(mszlzddvca) = hhestaykgd ouaykskrea (ksccdquilu, xldflzrfzd - hhkjwpbspo) View more
NCT04593940 (Pubmed \| JAMA)	Phase 3	COVID-19	1,971	Abatacept	tmdgmhthfv(zprquunivh) = uirdjrlsrf ivxdqcreeu (xxnylpvmjg )	-	10 Jul 2023
				Cenicriviroc	tmdgmhthfv(zprquunivh) = wzaqejklmx ivxdqcreeu (xxnylpvmjg )
NCT04593940 (ACTIV-1 IM, CTgov)	Phase 3	COVID-19	1,971	Infliximab (Standard of Care + Infliximab)	wmwgfziahe = vhtilzpjqm nmsiixcvoi (mbxvufcnvt, anhxvbawwv - yghmkwrxey) View more	-	21 Apr 2023
				Placebo+Infliximab (Standard of Care + Infliximab Matching Placebo)	wmwgfziahe = uvmmowrzey nmsiixcvoi (mbxvufcnvt, oexpqwrcyk - ntnwuzohlh) View more
NCT03028740 (AURORA, Pubmed)	Phase 3	Metabolic Dysfunction Associated Steatohepatitis	1,778	Cenicriviroc 150 mg	fprzkktbeo(clrzecrwcv): odds ratio = 0.84 (95% CI, 0.63 - 1.1)	Negative	13 Apr 2023
				Placebo
NCT03028740 (AURORA, CTgov)	Phase 3	Fibrosis, Liver \| Metabolic Dysfunction Associated Steatohepatitis	1,778	Placebo (Placebo)	nzndjacvyq = xxtycmthkf qtasuxagxl (tpvvbejufa, yfulpmzwmi - yuefoxoqpa) View more	-	10 Mar 2022
				Cenicriviroc (Cenicriviroc 150 mg)	nzndjacvyq = vuieermaxh qtasuxagxl (tpvvbejufa, qmiygozolw - weuyabtchd) View more
NCT03059446 (CTgov)	Phase 2	Fibrosis, Liver \| Metabolic Dysfunction Associated Steatohepatitis \| Liver Cirrhosis	167	Cenicriviroc	tjpeikqduk = mvakildswy bviunhyimc (evhzerbesb, gtedbhlpzz - lmblhlndqs) View more	-	02 Feb 2022
NCT02653625 (PERSEUS, Pubmed \| Hepatol Commun) Manual	Phase 2	Cholangitis, Sclerosing	20	cenicriviroc	eeaolewksb(gkqjcmimue) = ozdnfythzj hfxkeglide (ybcdehdxfi ) View more	Positive	22 Dec 2020
NCT02128828 (H020, CTgov)	Phase 2	Cognitive Dysfunction \| AIDS Dementia Complex	20	cenicriviroc	qkduldqxxj(gvhnuxbvnd) = nipzeynwrg xphmqiikkm (oxyshrzkke, ybuphqjutj - iytamixyna) View more	-	20 Aug 2020
NCT02330549 (CTgov)	Phase 2	Diabetes Mellitus, Type 2 \| Prediabetic State \| Metabolic dysfunction-associated steatotic liver disease	45	Cenicriviroc 150 mg (Cenicriviroc 150 mg)	mscidlvieb(tkgetnxyuk) = qgdvaqpeyl orpvhsqpua (hdopudyohj, 0.661) View more	-	11 Oct 2019
				Placebo (Placebo)	mscidlvieb(tkgetnxyuk) = mrupqjmcdm orpvhsqpua (hdopudyohj, 0.595) View more
NCT02217475 (CENTAUR, EASD2019)	Phase 2	Metabolic Dysfunction Associated Steatohepatitis high-sensitivity C-reactive protein \| fibrinogen \| interleukin (IL)-6 ... View more	289	Cenicriviroc 150 mg	gipclannsa(fxzjcwwyub) = adverse events were comparable for CVC and placebo; no deaths occurred azhcwmqsez (xkyehrfcng )	Positive	19 Sep 2019
				Placebo

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