Chemistry:ASP-8062

From HandWiki

ASP-8062, or ASP8062, is a GABAB receptor positive allosteric modulator which is under development for the treatment of alcoholism.[1][2][3] 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][4]

Pharmacology

It shows analgesic and antiaddictive effects in animals.[3][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.[4]

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][3][9] The drug is the most advanced GABAB receptor positive allosteric modulator in clinical trials as of 2024.[3][9][6]

See also

References

  1. ↑ 1.0 1.1 1.2 1.3 1.4 "ASP 8062". 8 June 2023. https://adisinsight.springer.com/drugs/800046940. 
  2. ↑ "Delving into the Latest Updates on ASP-8062 with Synapse". 24 May 2025. https://synapse.patsnap.com/drug/3af69c6f1f0f4d00827664dfa6aa75d9. 
  3. ↑ 3.0 3.1 3.2 3.3 "Recent Advances on the Chemistry of GABAB Receptor Allosteric Modulators". GABAB Receptor. The Receptors. Cham: Springer International Publishing. 2024. pp. 169–200. doi:10.1007/978-3-031-67148-7_8. ISBN 978-3-031-67147-0. https://link.springer.com/10.1007/978-3-031-67148-7_8. Retrieved 30 September 2025. 
  4. ↑ 4.0 4.1 Cite error: Invalid <ref> tag; no text was provided for refs named Walzer_2020
  5. ↑ "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. 2024. pp. 239–258. doi:10.1007/978-3-031-67148-7_11. ISBN 978-3-031-67147-0. https://link.springer.com/10.1007/978-3-031-67148-7_11. Retrieved 30 September 2025. 
  6. ↑ 6.0 6.1 "Recent Advances on GABAB Receptor Positive Allosteric Modulators as Potential Pharmacotherapies for Alcohol Use Disorder". GABAB Receptor. The Receptors. Cham: Springer International Publishing. 2024. pp. 259–281. doi:10.1007/978-3-031-67148-7_12. ISBN 978-3-031-67147-0. https://link.springer.com/10.1007/978-3-031-67148-7_12. Retrieved 30 September 2025. 
  7. ↑ "A novel GABAB receptor positive allosteric modulator, ASP8062, exerts analgesic effects in a rat model of fibromyalgia". Eur J Pharmacol 865. December 2019. doi:10.1016/j.ejphar.2019.172750. PMID 31647906. 
  8. ↑ 8.0 8.1 "A randomized phase 1 single-dose polysomnography study of ASP8062, a GABAB receptor positive allosteric modulator". Psychopharmacology (Berl) 238 (3): 867–876. March 2021. doi:10.1007/s00213-020-05738-y. PMID 33433644. 
  9. ↑ 9.0 9.1 "GABAB Receptor Positive Allosteric Modulators: Novel Approaches for Drug Design and Discovery". GABAB Receptor. The Receptors. Cham: Springer International Publishing. 2024. pp. 201–217. doi:10.1007/978-3-031-67148-7_9. ISBN 978-3-031-67147-0. https://link.springer.com/10.1007/978-3-031-67148-7_9. Retrieved 30 September 2025. 


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