Chemistry:VR-1065

From HandWiki

VR-1065 is a serotonin 5-HT2C receptor agonist which was under development for the treatment of obesity but was never marketed.[1][2][3][4] Its pharmacology has not been described.[4] The drug was under development by Roche and Vernalis Group.[1][3][2] It reached phase 1 clinical trials prior to the discontinuation of its development in 2002.[1][3][2] The drug's development was discontinued due to suboptimal pharmacokinetics in phase 1 trials.[1][2][3][5] The chemical structure of VR-1065 has not been disclosed.[1][4][3]

See also

  • Serotonin 5-HT2C receptor agonist

References

  1. ↑ 1.0 1.1 1.2 1.3 1.4 "R 1065". 1 August 2002. https://adisinsight.springer.com/drugs/800017316. 
  2. ↑ 2.0 2.1 2.2 2.3 "A review of late-stage CNS drug candidates for the treatment of obesity". International Journal of Obesity 37 (1): 107–117. January 2013. doi:10.1038/ijo.2012.26. PMID 22410963. "The 5-HT2C agonists that have undergone preclinical or clinical evaluation include Ro 60-0175, VR 1065 and VER-8775 (Vernalis, Winnersh, UK/Roche, Basel, Switzerland), LY 448100 (Lilly, Indianapolis, IN, USA) and lorcaserin (Arena Pharmaceuticals). [...] Although VR 1065 progressed into phase 1 clinical development, its pharmacokinetic profile was not acceptable. There is no public information to indicate whether its successor, VER-8775, was evaluated in humans.". 
  3. ↑ 3.0 3.1 3.2 3.3 3.4 "New 5-HT2C receptor agonists". Expert Opinion on Therapeutic Patents 13 (11): 1691–1705. 2003. doi:10.1517/13543776.13.11.1691. ISSN 1354-3776. http://www.tandfonline.com/doi/full/10.1517/13543776.13.11.1691. Retrieved 31 January 2026. "The Hoffmann-La Roche/Vernalis compound, VR-1065 (structure undisclosed), was discontinued after Phase I trials. Company press releases indicated that progress was halted due to a suboptimal pharmacokinetic profile in humans and that the two companies are actively trying to progress a more suitable compound into the clinic.". 
  4. ↑ 4.0 4.1 4.2 "The potential use of selective 5-HT2C agonists in treating obesity". Expert Opinion on Investigational Drugs 15 (3): 257–266. March 2006. doi:10.1517/13543784.15.3.257. PMID 16503763. "One compound of undisclosed structure, VR1065, advanced into clinical trials but was discontinued early during Phase I studies. No details are available concerning the reasons for discontinuing with development, nor has data on receptor selectivity, pharmacokinetics, metabolism or other possible challenges been published to date.". 
  5. ↑ "Vernalis, Roche Stop Phase I Study Due To Pharmacokinetics". 7 August 2002. https://www.bioworld.com/articles/391713-vernalis-roche-stop-phase-i-study-due-to-pharmacokinetics?v=preview. 



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