| Clinical data | |
|---|---|
| Other names | VR1065; R-1065; R1065; VMR-003; VMR003 |
| Routes of administration | Unspecified1 |
| Drug class | Serotonin 5-HT2C receptor agonist |
| ATC code |
|
VR-1065 is a serotonin 5-HT2C receptor agonist which was under development for the treatment of obesity but was never marketed.1234 Its pharmacology has not been described.4 The drug was under development by Roche and Vernalis Group.132 It reached phase 1 clinical trials prior to the discontinuation of its development in 2002.132 The drug's development was discontinued due to suboptimal pharmacokinetics in phase 1 trials.1235 The chemical structure of VR-1065 has not been disclosed.143
References
References
- "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.
- Moran N (7 August 2002). "Vernalis, Roche Stop Phase I Study Due To Pharmacokinetics". Bioworld. Retrieved 31 January 2026.