Cenicriviroc

Cenicriviroc
Names
IUPAC name
(S,E)-8-(4-(2-Butoxyethoxy)phenyl)-1-isobutyl-N-(4-(((1-propyl-1H-imidazol-5-yl)methyl)sulfinyl)phenyl)-1,2,3,4-tetrahydrobenzo[b]azocine-5-carboxamide
Other names
TAK-652; TBR-652
Identifiers
497223-25-3 Yes
497223-28-6 (mesylate) Yes
ChEMBL ChEMBL2110727 
ChemSpider 9460783 
Jmol-3D images Image
PubChem 11285792
11285792
UNII 15C116UA4Y Yes
Properties
Molecular formula
 C41H52N4O4S
Molar mass 696.94 g·mol−1
Except where noted otherwise, data is given for materials in their standard state (at 25 °C (77 °F), 100 kPa)
  verify (what is: Yes/?)
Infobox references

Cenicriviroc (TAK-652, TBR-652) is an experimental drug candidate for the treatment of HIV infection.[1] It is being developed by Takeda Pharmaceutical and Tobira Therapeutics.

Cenicriviroc is an inhibitor of CCR2 and CCR5 receptors,[2] allowing it to function as an entry inhibitor 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.[3] Additional Phase II clinical trials are underway.[4]

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 increased and soluble CD14 decreased in the cenicriviroc arms.[5]

See also

References

  1. ↑ Klibanov, Olga M.; Williams, Shannon H.; Iler, Cameron A (2010). "Cenicriviroc, an orally active CCR5 antagonist for the potential treatment of HIV infection". Current Opinion in Investigational Drugs 11 (8): 940–950. PMID 20721836.
  2. ↑ Baba, Masanori; Takashima, Katsunori; Miyake, Hiroshi; Kanzaki, Naoyuki; Teshima, Koichiro; Wang, Xin; Shiraishi, Mitsuru; Iizawa, Yuji (2005). "TAK-652 inhibits CCR5-mediated human immunodeficiency virus type 1 infection in vitro and has favorable pharmacokinetics in humans". Antimicrobial Agents and Chemotherapy 49 (11): 4584–4591. doi:10.1128/AAC.49.11.4584-4591.2005. PMC 1280155. PMID 16251299.
  3. ↑ C. Reviriego (2011). Drugs of the Future 36 (7): 511–517. doi:10.1358/dof.2011.36.7.1622066. Missing or empty |title= (help)
  4. ↑ "Tobira Therapeutics Initiates Phase 2b Trial of Cenicriviroc". The Body. July 5, 2011.
  5. ↑ CROI 2013: CCR5/CCR2 Inhibitor Cenicriviroc Has Both Anti-HIV and Anti-inflammatory Effects. Highleyman, Liz. HIVandHepatitis.com. 7 March 2013.