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.