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PRX-00933

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PRX-00933
Clinical data
Other namesPRX00933; PRX-933; PRX933; ALT-933; ALT933; BVT933; GW-876167; GW876167; GW-876,167
Routes of
administration
Oral[1]
Drug classSerotonin 5-HT2C receptor agonist; Appetite suppressant; Anti-obesity drug
ATC code
  • None
Identifiers
  • 2-[(2R)-2-methylpiperazin-1-yl]-3-(2-pyridin-3-yloxyethoxy)pyrazine
CAS Number
PubChem CID
ChemSpider
UNII
Chemical and physical data
FormulaC16H21N5O2
Molar mass315.377 g·mol−1
3D model (JSmol)
  • C[C@@H]1CNCCN1C2=NC=CN=C2OCCOC3=CN=CC=C3
  • InChI=1S/C16H21N5O2/c1-13-11-18-7-8-21(13)15-16(20-6-5-19-15)23-10-9-22-14-3-2-4-17-12-14/h2-6,12-13,18H,7-11H2,1H3/t13-/m1/s1
  • Key:DNZVDSXVCHUOFL-CYBMUJFWSA-N

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]

References

[edit]
  1. ^ a b c d e f "PRX 00933". AdisInsight. 28 May 2018. Retrieved 28 January 2026.
  2. ^ "Delving into the Latest Updates on GW-876167 with Synapse". Synapse. 24 January 2026. Retrieved 28 January 2026.
  3. ^ a b c d Lee J, Jung ME, Lee J (November 2010). "5-HT2C receptor modulators: a patent survey". Expert Opinion on Therapeutic Patents. 20 (11): 1429–1455. 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. ^ a b Jensen NH, Cremers TI, Sotty F (September 2010). "Therapeutic potential of 5-HT2C receptor ligands". TheScientificWorldJournal. 10: 1870–1885. doi:10.1100/tsw.2010.180. PMC 5763985. 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. ^ a b c Filip M, Spampinato U, McCreary AC, Przegaliński E (October 2012). "Pharmacological and genetic interventions in serotonin (5-HT)(2C) receptors to alter drug abuse and dependence processes". Brain Research. 1476: 132–153. doi:10.1016/j.brainres.2012.03.035. PMID 22494568. 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. ^ Vickers SP, Jackson HC, Cheetham SC (2015). "Chapter 6. New Drug Design and Therapeutic Development for Weight Reduction: Preclinical Studies and Clinical Trials". Drug Discovery. Cambridge: Royal Society of Chemistry. pp. 90–116. doi:10.1039/9781782622390-00090. ISBN 978-1-78262-046-4. Retrieved 28 January 2026.