NS-136 / NeuShen Therap - LARVOL DELTA

A first-in-human (FIH) study to assess the safety, tolerability, and pharmacokinetics of NS-136, a novel M4 muscarinic receptor (mAChR) positive allosteric modulator (PAM), in healthy subjects both in Australia and China (NS136HV101) [WITHDRAWN] (Neuroscience 2025) - "NS-136 demonstrated favorable safety and tolerability up to 100 mg, with PK properties suitable for once-daily administration without titration. No major ethnic differences between Australian and Chinese population observed, which supports multi-regional studies in phase 2 or beyond. A Phase 2a proof-of-concept study is under planning in patients with schizophrenia."

Clinical • First-in-human • P1 data • PK/PD data • CNS Disorders • Psychiatry • Schizophrenia • DRD2

Preclinical characterization of M4 muscarinic receptor positive allosteric modulator NS-136 (Neuroscience 2025) - "Additionally, in the Sprague-Dawley rat catalepsy model, NS-136 did not induce extrapyramidal symptoms, indicating a low risk of motor side effects.NS-136 also demonstrated strong brain penetration, as evidenced by high Kp, uu and brain-to-plasma (B/P) ratios across multiple species. These findings suggest efficient central nervous system (CNS) exposure, which may contribute to enhanced therapeutic efficacy in CNS disorders.In summary, NS-136 is a potent and selective M4 PAM with a promising preclinical safety and pharmacokinetic profile, supporting its potential as a next-generation antipsychotic therapy."

Preclinical • CNS Disorders • Psychiatry • Schizophrenia • DRD2

First-into-human Study of NS-136 in Healthy Subjects (clinicaltrials.gov) - P1 | N=60 | Recruiting | Sponsor: NeuShen Therapeutics | Not yet recruiting ➔ Recruiting

Enrollment open

NeuShen Therapeutics Initiates First-in-Human Trial of NS-136, a Novel Selective M4 Receptor Positive Allosteric Modulator for the Treatment of Schizophrenia (PRNewswire) - "NeuShen Therapeutics...announced the dosing of the first healthy volunteer in Australia in the Phase I first-in-human clinical trial of NS-136, a novel selective M4 receptor positive allosteric modulator (M4 PAM) designed for the treatment of schizophrenia and other conditions associated with psychosis."

Trial status • CNS Disorders • Schizophrenia

First-into-human Study of NS-136 in Healthy Subjects (clinicaltrials.gov) - P1 | N=60 | Not yet recruiting | Sponsor: NeuShen Therapeutics

New P1 trial