ASP-8062
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| Clinical data | |
|---|---|
| Other names | ASP8062 |
| Routes of administration | Oral[1] |
| Drug class | GABAB receptor positive allosteric modulator[2] |
| ATC code |
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| Pharmacokinetic data | |
| Elimination half-life | ~40–50 hours[2] |
| Identifiers | |
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| PubChem CID | |
| Chemical and physical data | |
| Formula | C20H29N3O2S2 |
| Molar mass | 407.59 g·mol−1 |
| 3D model (JSmol) | |
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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]
Pharmacology
[edit]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
[edit]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
[edit]References
[edit]- 1 2 3 4 5 6 "ASP 8062". AdisInsight. 8 June 2023. Retrieved 30 September 2025.
- 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.
- ↑ "Delving into the Latest Updates on ASP-8062 with Synapse". Synapse. 24 May 2025. Retrieved 30 September 2025.
- 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.
- ↑ 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.
- 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.
- ↑ 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.
- 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.
- 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.