ASP-8062

Last updated

ASP-8062
ASP-8062.svg
Clinical data
Other namesASP8062
Routes of
administration 		Oral [1]
Drug class GABAB receptor positive allosteric modulator [2]
ATC code
  • None
Pharmacokinetic data
Elimination half-life ~40–50 hours [2]
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
Formula C20H29N3O2S2
Molar mass 407.59 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. [1] [3] [4] 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. [1] [2]

Contents

Pharmacology

It shows analgesic and antiaddictive effects in animals. [4] [5] [6] [7] 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. [1] [4] [9] The drug is the most advanced GABAB receptor positive allosteric modulator in clinical trials as of 2024. [4] [9] [6]

See also

References

  1. 1 2 3 4 5 6 "ASP 8062". AdisInsight. 8 June 2023. Retrieved 30 September 2025.
  2. 1 2 3 4 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. 1 2 3 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. 1 2 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. 1 2 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. 1 2 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.


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