Article · Wikipedia archive · Last revised Jul 26, 2026

ASP-8062

ASP-8062, or ASP8062, is a GABAB receptor positive allosteric modulator which is under development for the treatment of alcoholism. It was also under development for the treatment of fibromyalgia and opioid-related disorders, but development for these indications was discontinued. The drug is taken orally.

Last revised
Jul 26, 2026
Read time
≈ 2 min
Length
479 w
Citations
23
Source
Wikipedia ↗
ASP-8062
Clinical data
Other namesASP8062
Routes of
administration		Oral1
Drug classGABAB receptor positive allosteric modulator2
ATC code
  • None
Pharmacokinetic data
Elimination half-life~40–50 hours2
Identifiers
  • 4-[[6-(4,4-dimethylcyclohexyl)-2-methylthieno[2,3-d]pyrimidin-4-yl]methyl]-1,4-thiazinane 1,1-dioxide
PubChem CID
Chemical and physical data
FormulaC20H29N3O2S2
Molar mass407.59 g·mol−1
3D model (JSmol)
  • CC1=NC(=C2C=C(SC2=N1)C3CCC(CC3)(C)C)CN4CCS(=O)(=O)CC4
  • InChI=1S/C20H29N3O2S2/c1-14-21-17(13-23-8-10-27(24,25)11-9-23)16-12-18(26-19(16)22-14)15-4-6-20(2,3)7-5-15/h12,15H,4-11,13H2,1-3H3
  • Key:USFNNXLOYXNESM-UHFFFAOYSA-N

ASP-8062, or ASP8062, is a GABAB receptor positive allosteric modulator which is under development for the treatment of alcoholism.134 It was also under development for the treatment of fibromyalgia and opioid-related disorders, but development for these indications was discontinued.1 The drug is taken orally.12

Pharmacology

It shows analgesic and antiaddictive effects in animals.4567 In a polysomnography study, ASP-8062 dose-dependently enhanced slow wave sleep (SWS; deep sleep) without affecting REM sleep in humans.8 It also dose-dependently increased growth hormone (GH) release.8 The time to peak levels of ASP-8062 in humans is 1 to 4 hours and its elimination half-life is approximately 40 to 50 hours.2

Development

ASP-8062 is under development by Astellas Pharma in collaboration with the National Institute on Alcohol Abuse and Alcoholism (NIAAA).1 As of June 2023, it is in phase 2 clinical trials for alcoholism.149 The drug is the most advanced GABAB receptor positive allosteric modulator in clinical trials as of 2024.496

See also

See also

References

References

  1. "ASP 8062". AdisInsight. 8 June 2023. Retrieved 30 September 2025.
  2. Walzer M, Marek GJ, Wu R, Nagata M, Han D (April 2020). "Single- and Multiple-Dose Safety, Tolerability, and Pharmacokinetic Profiles of ASP8062: Results From 2 Phase 1 Studies". Clin Pharmacol Drug Dev. 9 (3): 297–306. doi:10.1002/cpdd.766. PMID 31926000.
  3. "Delving into the Latest Updates on ASP-8062 with Synapse". Synapse. 24 May 2025. Retrieved 30 September 2025.
  4. Mugnaini C, Corelli F (2024). "Recent Advances on the Chemistry of GABAB Receptor Allosteric Modulators". GABAB Receptor. The Receptors. Cham: Springer International Publishing. pp. 169–200. doi:10.1007/978-3-031-67148-7_8. ISBN 978-3-031-67147-0. Retrieved 30 September 2025.
  5. Wydra K, Frankowska M, Filip M (2024). "Recent Advances on GABAB Receptor Positive Allosteric Modulators as Potential Pharmacotherapies for Substance Use Disorder and Food Addiction". GABAB Receptor. The Receptors. Cham: Springer International Publishing. pp. 239–258. doi:10.1007/978-3-031-67148-7_11. ISBN 978-3-031-67147-0. Retrieved 30 September 2025.
  6. Maccioni P, Colombo G (2024). "Recent Advances on GABAB Receptor Positive Allosteric Modulators as Potential Pharmacotherapies for Alcohol Use Disorder". GABAB Receptor. The Receptors. Cham: Springer International Publishing. pp. 259–281. doi:10.1007/978-3-031-67148-7_12. ISBN 978-3-031-67147-0. Retrieved 30 September 2025.
  7. Murai N, Kondo Y, Akuzawa S, Mihara T, Shiraishi N, Kakimoto S, et al. (December 2019). "A novel GABAB receptor positive allosteric modulator, ASP8062, exerts analgesic effects in a rat model of fibromyalgia". Eur J Pharmacol. 865 172750. doi:10.1016/j.ejphar.2019.172750. PMID 31647906.
  8. Walzer M, Wu R, Ahmad M, Freeman J, Zammit G, Marek GJ (March 2021). "A randomized phase 1 single-dose polysomnography study of ASP8062, a GABAB receptor positive allosteric modulator". Psychopharmacology (Berl). 238 (3): 867–876. doi:10.1007/s00213-020-05738-y. PMC 7914186. PMID 33433644.
  9. Evenseth LS (2024). "GABAB Receptor Positive Allosteric Modulators: Novel Approaches for Drug Design and Discovery". GABAB Receptor. The Receptors. Cham: Springer International Publishing. pp. 201–217. doi:10.1007/978-3-031-67148-7_9. ISBN 978-3-031-67147-0. Retrieved 30 September 2025.