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Other Names: CVC, TAK-652, TBR-652, cenicriviroc mesylate Drug Class: CCR5 Antagonist Molecular Formula: C41 H52 N4 O4 S Registry Number: 497223-25-3 (ChemID) Chemical Name: (5E)-8-[4-(2-butoxyethoxy)phenyl]-1-isobutyl-N-[4-[(S)-(3-propylimidazol-4-yl)methylsulfinyl]phenyl]-3,4-dihydro-2H-1-benzazocine-5-carboxamide Chemical Class: Benzazepines Organization: Allergan, Takeda, Tobira Therapeutics Phase of Development: Cenicriviroc is in Phase IIb development as a treatment for HIV.

(Compound details obtained from ChemIDplus Advanced,1 NIAID Therapeutics Database,2 Allergan press release,3 ClinicalTrials.gov,4 and Antimicrobial Agents and Chemotherapy article5)

What is cenicriviroc?

What is cenicriviroc?

Cenicriviroc is an investigational HIV drug that is being studied to treat HIV infection and HIV-associated neurocognitive disorders (HAND). (HAND ranges from mild problems with memory, language, and reasoning to the more severe HIV-associated dementia [HAD].) Cenicriviroc is also being studied to treat a liver disease called nonalcoholic steatohepatitis (NASH).4,6

Cenicriviroc belongs to a group of HIV drugs called CCR5 antagonists.2,5 A CCR5 antagonist blocks HIV from getting into and infecting certain cells of the immune system. This prevents HIV from multiplying and can reduce the amount of HIV in the body.

Cenicriviroc also appears to block a receptor known as CCR2. The CCR2 receptor is associated with inflammatory diseases. The potential benefits of blocking the CCR2 receptor in people with HIV are being studied.7,8

To learn about how investigational drugs are tested during clinical trials, read the AIDSinfo What is an Investigational HIV Drug? and HIV/AIDS Clinical Trials fact sheets.

Which clinical trials are studying cenicriviroc?

Which clinical trials are studying cenicriviroc?

Study Names: TBR-652-2-202 (Study 202); NCT01338883
Phase: IIb
Status: This study has been completed.
Location: United States and Puerto Rico
Purpose: The purpose of this study was to compare the safety and efficacy of 2 different doses of cenicriviroc versus the FDA-approved non-nucleoside reverse transcriptase inhibitor (NNRTI) efavirenz (brand name: Sustiva) in adults with HIV who had never taken HIV medicines before.4,9

Study Name: NCT02128828
Phase: II
Status: This study has been completed.
Location: United States
Purpose: The purpose of this study was to evaluate cenicriviroc’s ability to improve learning, memory, and other cognitive abilities in participants with HIV who had cognitive impairment.6,10,11

For more details on the studies listed above, see the Health Professional version of this drug summary.

The company that was previously developing cenicriviroc had at one point been planning Phase III clinical trials to investigate a fixed-dose combination (FDC) tablet containing cenicriviroc plus the FDA-approved medicine lamivudine (brand name: Epivir). However, study of the FDC tablet has not occurred.12,13

What side effects might cenicriviroc cause?

What side effects might cenicriviroc cause?

One goal of HIV research is to identify new drugs that have fewer side effects. The following side effects were observed in the studies of cenicriviroc listed above.

Study 202 (NCT01338883):

In this study, the most common side effects associated with cenicriviroc were nausea, headache, diarrhea, and abnormal dreams. One participant receiving cenicriviroc had a severe, symptomless elevation in a liver enzyme level, but it was temporary.4,10

Treatment-related side effects occurred in participants across all study groups, but a smaller percentage of cenicriviroc-treated participants experienced these side effects than efavirenz-treated participants. Participants receiving cenicriviroc saw a drop in total cholesterol levels and in the levels of one specific type of cholesterol. More participants in the efavirenz group dropped out of the study because of side effects than in the cenicriviroc group.14,15


In this study, most side effects reported were mild or moderate in intensity. Some of the moderate side effects included loose stools, nausea, abdominal cramps, and fatigue. One participant withdrew from the study due to mild nausea. Severely high lipase levels in the blood were reported on two separate occasions; however, it’s unknown whether this side effect was related to treatment with cenicriviroc.11

Because cenicriviroc is still being studied, information on possible side effects of the drug is not complete. As testing of cenicriviroc continues, additional information on possible side effects will be gathered.

Where can I get more information about clinical trials studying cenicriviroc?

Where can I get more information about clinical trials studying cenicriviroc?

More information about cenicriviroc-related research studies is available from ClinicalTrials.gov.



  1. United States National Library of Medicine. ChemIDplus Advanced: Cenicriviroc. https://chem.nlm.nih.gov/chemidplus/rn/497223-25-3. Accessed October 24, 2018.
  2. National Institute of Allergy and Infectious Diseases (NIAID). NIAID ChemDB, HIV Drugs in Development. https://chemdb.niaid.nih.gov/DrugDevelopmentHIV.aspx. Accessed October 24, 2018.
  3. Allergan: Press Release, dated September 20, 2016. Allergan to acquire Tobira Therapeutics expanding global GI R&D pipeline and taking a leading R&D position in NASH. https://www.allergan.com/news/news/thomson-reuters/allergan-to-acquire-tobira-therapeutics-expanding. Accessed October 24, 2018.
  4. Tobira Therapeutics, Inc. A Phase 2b randomized, double-blind, double-dummy trial of 100 or 200 mg once-daily doses of cenicriviroc (CVC, TBR 652) or once-daily EFV, each with open-label FTC/TDF, in HIV 1-infected, antiretroviral treatment-naive, adult patients with only CCR5-tropic virus. In: ClinicalTrials.gov. Bethesda (MD): National Library of Medicine (US). Registered on April 18, 2011. NLM Identifier: NCT01338883. https://clinicaltrials.gov/ct2/show/NCT01338883. Accessed October 24, 2018.
  5. Baba M, Takashima K, Miyake H, et al. TAK-652 inhibits CCR5-mediated human immunodeficiency virus type 1 infection in vitro and has favorable pharmacokinetics in humans. Antimicrob Agents Chemother. 2005;49(11):4584-4591.
  6. University of Hawaii. Randomized, placebo-controlled, double-blind, pilot study of CCR5/CCR2 inhibitor cenicriviroc (CVC) for HIV associated neurocognitive disorder (HAND). In: ClinicalTrials.gov. Bethesda (MD): National Library of Medicine (US). Registered on September 4, 2013. NLM Identifier: NCT02128828. https://clinicaltrials.gov/ct2/show/NCT02128828. Accessed October 24, 2018.
  7. Marier J-F, Trinh M, Pheng LH, Palleja SM, Martin DE. Pharmacokinetics and pharmacodynamics of TBR-652, a novel CCR5 antagonist, in HIV-1-infected, antiretroviral treatment-experienced, CCR5 antagonist-naive patients. Antimicrob Agents Chemother. 2011;55(6):2768-2774.
  8. Klibanov OM, Williams SH, Iler CA. Cenicriviroc, an orally active CCR5 antagonist for the potential treatment of HIV infection. Curr Opin Investig Drugs. 2010;11(8):940-950.
  9. Thompson M, Saag M, DeJesus E, et al. A 48-week randomized phase 2b study evaluating cenicriviroc versus efavirenz in treatment-naive HIV-infected adults with C-C chemokine receptor type 5-tropic virus. AIDS. 2016;30(6):869-878.
  10. D'Antoni ML, Paul RH, Mitchell BI, et al. Improved cognitive performance and reduced monocyte activation in virally suppressed chronic HIV after dual CCR2 and CCR5 antagonism. J Acquir Immune Defic Syndr. 2018;79(1):108-116. doi:10.1097/QAI.0000000000001752
  11. Ndhlovu L, D’Antoni M, Paul R, et al. Cencriviroc improves neurocognition and reduces monocyte activation in treated HIV. Abstract presented at: Conference on Retroviruses and Opportunistic Infections (CROI); February 13–16, 2017; Seattle, WA. Abstract 381. http://www.croiconference.org/sites/default/files/posters-2017/381_DAntoni.pdf. Accessed October 24, 2018.
  12. Tobira Therapeutics: Press Release, dated October 17, 2013. Tobira Therapeutics presents positive 48-week data from Phase 2b trial of cenicriviroc in treatment-naive HIV infection at the 14th European AIDS Conference. http://files.shareholder.com/downloads/AMDA-2VQ912/2836889662x0x770942/A350DD2A-7061-40A6-BDD1-8B6E4986A158/770942.pdf. Accessed October 24, 2018.
  13. Clayden P, Collins S, Frick M, et al. HIV i-BASE/Treatment Action Group. 2015 pipeline report. July 2015. http://www.pipelinereport.org/sites/default/files/201509/2015%20Pipeline%20Report%20Full.pdf. Accessed October 24, 2018.
  14. Feinberg J, Thompson M, Cade J, et al. Final Week 48 analysis of cenicriviroc (CVC) compared to efavirenz (EFV), in combination with emtricitabine/tenofovir (FTC/TDF), in treatment-naive HIV-1-infected adults with CCR5-tropic virus (study 652-2-202; NCT01338883). European AIDS Conference; October 16-19, 2013; Brussels, Belgium. Levin: Conference Reports for National AIDS Treatment Advocacy Project (NATAP); 2013. http://www.natap.org/2013/EACS/EACS_10.htm. Accessed October 24, 2018.
  15. Feinberg J, Thompson M, Cade J, et al. Final Week 48 analysis of cenicriviroc (CVC) compared to efavirenz (EFV), in combination with emtricitabine/tenofovir (FTC/TDF), in treatment-naive HIV-1-infected adults with CCR5-tropic virus. Abstract presented at: European AIDS Conference; October 16-19, 2013; Brussels, Belgium. Abstract PS4/1. http://www.professionalabstracts.com/eacs2013/planner/index.php?go=abstract&action=abstract_iplanner&print=0&lprID=142&highlight=cenicriviroc&PSID=AOLYUNDFJHCSEFPDLAAC. Accessed October 24, 2018.

Last Reviewed: January 15, 2019