ASP-8062

ASP-8062, or ASP8062, is a GABA_B 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]

ASP-8062

Clinical data
Other names	ASP8062
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
IUPAC name 4-{{#parsoidfragment:2}}6-(4,4-dimethylcyclohexyl)-2-methylthieno[2,3-d]pyrimidin-4-yl]methyl]-1,4-thiazinane 1,1-dioxide
PubChem CID	91754521
Chemical and physical data
Formula	C20H29N3O2S2
Molar mass	407.59 g·mol−1
3D model (JSmol)	Interactive image
SMILES CC1=NC(=C2C=C(SC2=N1)C3CCC(CC3)(C)C)CN4CCS(=O)(=O)CC4
InChI 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

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 GABA_B receptor positive allosteric modulator in clinical trials as of 2024.^[4][9][6]

See also

• ADX-71441
• CGP-7930