VR-1065
Pharmaceutical compound
From Wikipedia, the free encyclopedia
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]
Other namesVR1065; R-1065; R1065; VMR-003; VMR003
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"R 1065". AdisInsight. 1 August 2002. Retrieved 31 January 2026. Heal DJ, Gosden J, Smith SL (January 2013). "A review of late-stage CNS drug candidates for the treatment of obesity". International Journal of Obesity. 37 (1): 107–117. 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.
Bishop MJ, Nilsson BM (2003). "New 5-HT2C receptor agonists". Expert Opinion on Therapeutic Patents. 13 (11): 1691–1705. doi:10.1517/13543776.13.11.1691. ISSN 1354-3776. 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.
Smith BM, Thomsen WJ, Grottick AJ (March 2006). "The potential use of selective 5-HT2C agonists in treating obesity". Expert Opinion on Investigational Drugs. 15 (3): 257–266. 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.
