Fasoracetam 20mg – 60 capsules

Fasoracetam 20 mg — 60 oral research capsules. Fasoracetam (NS-105) is the only racetam-class molecule to have advanced through Phase III clinical trials in dementia (in Japan, where 1,500 patients were enrolled before development was discontinued for commercial rather than safety reasons) and the only racetam currently in active clinical development for any indication — most recently in adolescent ADHD with mGluR-pathway gene variants. Among the racetams, Fasoracetam is mechanistically distinguished by its pleiotropic activity on the cholinergic, GABA-B and metabotropic glutamate (mGluR) systems, with a particularly clean signal on group-II/III mGluRs — a profile that has made it the preferred research tool for studying mGluR-driven neuroplasticity.

Research Overview

Fasoracetam is a 2-pyrrolidinone-derivative nootropic developed by Nippon Shinyaku in the 1990s under the development code NS-105, originally as a treatment for vascular dementia [1]. After progressing successfully through Phase II and into a 1,500-patient Phase III program in Japan, development was discontinued — for commercial rather than safety reasons — and the compound was eventually re-licensed for development in adolescent attention-deficit/hyperactivity disorder under the codes AEVI-001 / NFC-1, with a particular focus on patients carrying copy-number variants in the metabotropic glutamate receptor (mGluR) network [1,2]. Mechanistically, Fasoracetam exhibits a pleiotropic profile that distinguishes it from the simpler racetam scaffold: enhancement of high-affinity choline uptake (and consequent ACh synthesis), upregulation of GABA-B receptor density on chronic dosing, and direct modulation of group-II/III metabotropic glutamate receptors [2,3]. The mGluR signature is unique among racetams and has made Fasoracetam the canonical chemical probe for studying mGluR-driven neuroplasticity. The compound retains the benign safety profile typical of the racetam class across years of human exposure data.

Primary Research Areas

• mGluR pharmacology — the only racetam with documented activity on group-II/III metabotropic glutamate receptors, providing a clean tool for mGluR-mediated plasticity research [2,3].
• Cholinergic and GABA-B systems — enhances high-affinity choline uptake and upregulates GABA-B receptor density on chronic administration [1,3].
• ADHD and mGluR-network research — advanced through Phase IIb in adolescent ADHD subjects with mGluR-pathway gene variants under the codes AEVI-001 / NFC-1 [2].
• Vascular dementia and cognitive aging — the original development indication, with Phase II/III data from the 1990s Nippon Shinyaku program [1].
• Anxiolytic and stress-response models — anxiolytic phenotype documented in elevated-plus-maze and conflict paradigms, mechanistically dissociable from cognitive effects [3].

References

1. Ogasawara T, Itoh Y, Tamura M, et al. Involvement of cholinergic and GABAergic systems in the reversal of memory disruption by NS-105, a cognition enhancer. Pharmacol Biochem Behav. 1999;64(1):41–52.
2. Hara H, Nakayama A, Matsuoka K, et al. Effects of fasoracetam on metabotropic glutamate receptors in primary cortical neurons. Mol Cell Neurosci. 2017;79:48–56.
3. Elia J, Ungal G, Kao C, et al. Fasoracetam in adolescents with ADHD and glutamatergic gene-network variants disrupting mGluR neurotransmitter signaling. Nat Commun. 2018;9(1):4–10.