ispronicline (AZD3480) / Gyre Therapeutics, AstraZeneca - LARVOL DELTA

Nicotinic aspects of the discriminative stimulus effects of arecoline. (PubMed, Behav Pharmacol) - "However, both nicotine itself and two nicotine agonists with selective affinity for the α4β2* receptor (ispronicline and metanicotine) produced full arecoline-like discriminative stimulus effects in these rats. These data indicate a selective α4β2* nicotine receptor component to the behavioral effects of arecoline. Although the nicotinic aspects of arecoline's behavior effects could suggest that abuse of arecoline-containing material (e.g. betel nut chewing) is mediated through nicotinic rather than muscarinic actions, further research, specifically on the reinforcing effects of arecoline, is necessary before this conclusion can be supported."

Journal

Nicotine-like discriminative and aversive effects of two α4β2-selective nicotine agonists, ispronicline and metanicotine. (PubMed, Behav Pharmacol) - "Both ispronicline and metanicotine as well as nicotine were avoided in the drug + food vs. food choice situation. The receptor-selective nature of ispronicline and metanicotine was hereby confirmed in a behavioral assay, as were earlier reports that the discriminative stimulus effects of relatively small doses of nicotine are likely mediated by activity at the α4β2* nicotine receptor."

Journal

Efficacy, Safety, & Tolerability of AZD3480 Patients With Mild to Moderate Dementia of the Alzheimer's Type (AD) (clinicaltrials.gov) - P2; N=386; Completed; Sponsor: Targacept Inc.; Active, not recruiting -> Completed ; N=300 -> 386

Enrollment change • Trial completion • Alzheimer's Disease • Biosimilar

Targacept and AstraZeneca amend collaboration (Businesswire) - "Targacept...announced that its collaboration with AstraZeneca has been restructured. Targacept now has the right to pursue development and commercialization of any alpha7 NNR modulator in any therapeutic area...without obligation to AstraZeneca. AstraZeneca now has the right to develop and commercialize the alpha4beta2 NNR modulators...including AZD1446, in any therapeutic area. AstraZeneca will return to Targacept all rights to the alpha4beta2 modulator TC-1734 (also known as AZD3480)...mild to moderate Alzheimer’s disease. TC-5619...top-line results from this study are expected by the end of 2013."

Anticipated P2 data • Licensing / partnership • Alzheimer's Disease • Schizophrenia

Development pipeline update (AstraZeneca Press Release) - AZD1446 discontinued for Alzheimer’s disease due to safety / efficacy reasons. AZD3480 discontinued for Alzheimer’s disease due to safety / efficacy reasons.

Discontinued • Alzheimer's Disease