ATHX-105

ATHX-105
Clinical data
Other namesATHX105
Routes of
administration		Oral[1]
Drug classSerotonin 5-HT2C receptor agonist; Appetite suppressant; Anti-obesity drug
ATC code
  • None

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

References

  1. ^ a b c d e f "ATHX 105". AdisInsight. 17 August 2011. Retrieved 26 January 2026.
  2. ^ a b c "Delving into the Latest Updates on ATHX-105 with Synapse". Synapse. 24 January 2026. Retrieved 26 January 2026.
  3. ^ a b c d e 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. 3.7 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. ^ Miller KJ, Wacker DA (December 2010). "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. 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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