Chemistry:ATHX-105

From HandWiki

ATHX-105 is a highly selective serotonin 5-HT2C receptor agonist which was under development for the treatment of obesity but was never marketed.[1][2][3] It is taken orally.[1] The drug has been found to reduce food intake and produce weight loss in animals.[3] ATHX-105 was developed by Athersys.[1][2][3] It reached and completed several phase 1 clinical trials and was preparing to enter phase 2 trials prior to the discontinuation of its development due to safety concerns in March 2009.[1][2][3][4] The chemical structure of ATHX-105 does not appear to have been disclosed.[1][3]

See also

  • Serotonin 5-HT2C receptor agonist

References

  1. ↑ 1.0 1.1 1.2 1.3 1.4 "ATHX 105". 17 August 2011. https://adisinsight.springer.com/drugs/800024939. 
  2. ↑ 2.0 2.1 2.2 "Delving into the Latest Updates on ATHX-105 with Synapse". 24 January 2026. https://synapse.patsnap.com/drug/5526307b02b94d8fab1c16f6331a9a89. 
  3. ↑ 3.0 3.1 3.2 3.3 3.4 "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. "3.7 Athersys, Inc. 3.7.1 ATHX-105: structure not disclosed Athersys is developing ATHX-105 (structure not disclosed), the lead from a series of 5-HT2C receptor agonists for the potential oral treatment of obesity. Athersys completed several Phase I clinical trials for ATHX-105, demonstrating positive data. In September 2008, the FDA placed a partial hold on the Phase II trial and requested further information [128]. In March 2009, Athersys believed that continued development of the program would be ‘challenging’ and suspended further development of the drug and was focusing on the development of next generation candidates [129,130]. ATHX-105 has a low nano-molar activity and was highly selective for 5-HT2A or 5-HT2B. It has a good selectivity against CYP450 enzymes (CYP1A2 IC50 = 1.8 µM, other isoforms IC50 > 10 µM). It has a brain:plasma ratio of 37, t1/2 of 1.1 and 3.7 h in rats and dogs, respectively, and 30% oral bioavailability. In Zucker rats, ATHX-105 (2.5 -- 40 mg/kg) decreased food intake (maximal 57% reduction) and chronic dosing gave 10% weight loss. Doses of 0.1 and 1 mg/ kg decreased food intake in dogs [131]. Top-line data from the 107-subject Phase I clinical trial were reported in February 2008. Drug exposure and maximum drug concentrations were dose-dependent and in the fed-fasted cohorts, food consumption had no effects on drug exposure [132]. As described before, development of ATHX-105 for the treatment of obesity was suspended since March 2009.". 
  4. ↑ "Discovery and development of 5-HT(₂C) receptor agonists for obesity: is there light at the end of the tunnel?". Future Medicinal Chemistry 2 (12): 1761–1775. December 2010. doi:10.4155/fmc.10.261. PMID 21428799. "Athersys Pharmaceuticals also had a selective 5-HT2C agonist advance through multiple PhaseI studies, ATHX-105. The compound was put on clinical hold, however, due to the potential for safety issues and the company has suspended all further development activities [202].". 



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