Chemistry:PRX-00933

From HandWiki

PRX-00933, also known as ALT-933, BVT-933, and GW-876167, is a serotonin 5-HT2C receptor agonist which was under development for the treatment of obesity and glaucoma but was never marketed.[1][2][3][4][5][6] It is taken orally.[1] The drug was found to reduce appetite and promote weight loss in both animals and humans.[3][4] PRX-00933 was originated by Biovitrum and was under development by Proximagen, Altacor, and GlaxoSmithKline.[1][3][5] It reached phase 2 clinical trials for obesity by 2002 prior to the discontinuation of its development.[1][3] No recent development was reported by 2012.[1][5]

See also

  • Serotonin 5-HT2C receptor agonist

References

  1. 1.0 1.1 1.2 1.3 1.4 "PRX 00933". 28 May 2018. https://adisinsight.springer.com/drugs/800016233. 
  2. "Delving into the Latest Updates on GW-876167 with Synapse". 24 January 2026. https://synapse.patsnap.com/drug/b2a5dbf2457d4d66a777439d79727b76. 
  3. 3.0 3.1 3.2 3.3 "5-HT2C receptor modulators: a patent survey". Expert Opinion on Therapeutic Patents 20 (11): 1429–1455. November 2010. doi:10.1517/13543776.2010.518956. PMID 20849206. "3.8 Swedish Orphan Biovitrum AB 3.8.1 PRX-00933: structure not disclosed Proximagen, under license from Swedish Orphan Biovitrum is developing a series of 5-HT2C agonists, including PRX-00933 (previously BVT-933) for the potential treatment of obesity. Biovitrum and GlaxoSmithKline were developing BVT-933, the lead in the series of 5-HT2C receptor agonists. By October 2002, the compound had reached Phase IIb trials. However, in June 2007, GlaxoSmithKline discontinued development of the agonists and returned the rights of the program to Biovitrum. Regarding preclinical studies, the compound (PRX-00933) was reported to be effective in reducing food intake in ob/ob mice with a mechanism indicating increased satiety as revealed by meal pattern analysis (prolongation of the intermeal interval without affecting the size of individual meals). Moreover, continuous s.c. infusion of this compound via osmotic minipump in DIO rats over 14 days produced a dose-dependent reduction of food intake and body weight throughout the study duration [139]. Interestingly, the preclinical finding regarding body weight was consistent with a study in humans. According to data disclosed in February 2002, 154 obese individuals were enrolled in a double-blind, placebo-controlled, Phase IIa study, receiving BVT-933 or placebo in two dose groups over 4 weeks. Patients in both dose groups receiving BVT-933 achieved a significant and clinically relevant weight reduction compared to placebo [140].". 
  4. 4.0 4.1 "Therapeutic potential of 5-HT2C receptor ligands". TheScientificWorldJournal 10: 1870–1885. September 2010. doi:10.1100/tsw.2010.180. PMID 20852829. "TABLE 1 Pharmacology of 5-HT2C Receptors [...] BVT-933 (now PRX-00933), another 5-HT2C receptor agonist, was reported to induce significant weight reduction in a phase II trial. [...]". 
  5. 5.0 5.1 5.2 "Pharmacological and genetic interventions in serotonin (5-HT)(2C) receptors to alter drug abuse and dependence processes". Brain Research 1476: 132–153. October 2012. doi:10.1016/j.brainres.2012.03.035. PMID 22494568. https://ruj.uj.edu.pl/xmlui/handle/item/251126. "In the last decade other 5-HT2C receptor ligands such as BVT-933 (PRX-00933), trans-PAT and YM-348 have been reported, but these drugs either show weak 5-HT2C receptor selectivity (Table 1) or have limited binding and/or limited activity information. [...] Biovitrium disclosed BVT-933 and the company entered into a co-licensing agreement with GSK, subsequently entering phase IIb clinical trials. However, this may now have been discontinued (Lee et al., 2010).". 
  6. "Chapter 6. New Drug Design and Therapeutic Development for Weight Reduction: Preclinical Studies and Clinical Trials". Drug Discovery. Cambridge: Royal Society of Chemistry. 2015. pp. 90–116. doi:10.1039/9781782622390-00090. ISBN 978-1-78262-046-4. https://books.rsc.org/books/monograph/532/chapter-abstract/176769/. Retrieved 28 January 2026.