fazamorexant (YZJ-1139) / WuXi AppTec, Yangtze River Pharmaceutical Group - LARVOL DELTA

Drug-drug interaction between ticagrelor and fazamorexant: pharmacokinetic alterations in healthy subjects from a phase I, open-label, fixed-sequence study. (PubMed, BMC Pharmacol Toxicol) - P1 | "Overall, co-administration of CYP3A4 weak inhibitors with fazamorexant is not expected to result in clinically significant drug interactions, and no dosage adjustment is required when these agents are used concomitantly."

Journal • PK/PD data • CNS Disorders • Insomnia • Sleep Disorder

A Clinical Study to Evaluate the Drug Interaction Between YZJ-1139 Tablets and Escitalopram Oxalate Tablets (clinicaltrials.gov) - P1 | N=0 | Completed | Sponsor: Shanghai Haiyan Pharmaceutical Technology Co., Ltd. | Active, not recruiting ➔ Completed

Trial completion • CNS Disorders • Insomnia • Sleep Disorder

A Drug-drug Interaction Study of YZJ-1139 Tablets and Ticagrelor Tablets in Healthy Subjects (clinicaltrials.gov) - P1 | N=0 | Completed | Sponsor: Shanghai Haiyan Pharmaceutical Technology Co., Ltd. | Active, not recruiting ➔ Completed

Trial completion • CNS Disorders • Insomnia • Sleep Disorder

A Drug-drug Interaction Study of YZJ-1139 Tablets and Ticagrelor Tablets in Healthy Subjects (clinicaltrials.gov) - P1 | N=27 | Completed | Sponsor: Shanghai Haiyan Pharmaceutical Technology Co., Ltd. | Active, not recruiting ➔ Completed

Trial completion • CNS Disorders • Insomnia • Sleep Disorder

A Clinical Study to Evaluate the Drug Interaction Between YZJ-1139 Tablets and Escitalopram Oxalate Tablets (clinicaltrials.gov) - P1 | N=24 | Completed | Sponsor: Shanghai Haiyan Pharmaceutical Technology Co., Ltd. | Active, not recruiting ➔ Completed

Trial completion • CNS Disorders • Insomnia • Sleep Disorder

Safety and Efficacy Study of YZJ-1139 in Insomnia Disorder (clinicaltrials.gov) - P3 | N=1037 | Completed | Sponsor: Shanghai Haiyan Pharmaceutical Technology Co., Ltd. | Recruiting ➔ Completed

Trial completion • CNS Disorders • Insomnia • Sleep Disorder

YZJ-1139-1-12: Pharmacokinetics and Safety Study of YZJ-1139 in Subjects With Severe Renal Impairment and Normal Renal Impairment (clinicaltrials.gov) - P1 | N=16 | Completed | Sponsor: Shanghai Haiyan Pharmaceutical Technology Co., Ltd. | Active, not recruiting ➔ Completed

Trial completion • CNS Disorders • Insomnia • Renal Disease • Sleep Disorder

Safety and Efficacy Study of YZJ-1139 Tablets in Insomnia Disorder (clinicaltrials.gov) - P3 | N=61 | Completed | Sponsor: Shanghai Haiyan Pharmaceutical Technology Co., Ltd. | Recruiting ➔ Completed

Trial completion • CNS Disorders • Insomnia • Sleep Disorder

Single-dose pharmacokinetics, tolerability, and physiologically based pharmacokinetic modeling of Fazamorexant in Chinese patients with hepatic impairment and in healthy controls. (PubMed, Front Pharmacol) - "Fazamorexant was generally well tolerated. Fazamorexant showed good safety and minimal impact of hepatic impairment on Cmax, but AUC increased by approximately 50% in patients with mild or moderate hepatic impairment."

Journal • PK/PD data • CNS Disorders • Hepatology • Insomnia • Sleep Disorder

Hypnotic doses of fazamorexant induced less impairment on balance and cognition than zolpidem in healthy younger and elderly individualse. (PubMed, Br J Clin Pharmacol) - "Clinically hypnotic doses of fazamorexant induced less balance, judgement and memory impairment in healthy adults and elderly volunteers compared to the comprehensive suppression of zolpidem on the neurological system. These preliminary results suggest that fazamorexant is a potentially safer drug for insomnia. No age-related pharmacokinetic difference was identified with fazamorexant."

Clinical • Journal • Alzheimer's Disease • CNS Disorders • Insomnia • Sleep Disorder

The Phase III pivotal clinical trial results of Fazamorexant, a first-class innovative anti-insomnia drug independently developed by Yangtze River Pharmaceutical Group,were globally unveiled for the first time at the World Sleep Congress 2025 combined with the annual meeting of the Asian Society of Sleep Medicine (ASSM 2025). (The Manila Times) - "The results show that Fazamorexant, as an dual orexin receptor antagonist (DORA), demonstrates rapid efficacy and a favorable safety profile in adult patients with insomnia...In terms of improved sleep efficiency, shortened period of falling asleep, and decreased nighttime awakening are significantly greater compared to the publicly available clinical data of other DORAs...the company has officially submitted the new drug application (NDA) for Fazamorexant to the Center for Drug Evaluation (CDE) of the National Medical Products Administration (NMPA)."

China filing • P3 data • Insomnia

Efficacy and Safety of Fazamorexant in Adults with Insomnia: A Phase 3 Randomized Controlled Trial of a Rapid-Onset, Short-Acting DORA (WSS 2025) - P3 | "Fazamorexant (FAZ; YZJ-1139) is a DORA characterized by rapid absorption (Tmax: 0.63~1.25 hours) and short elimination half-life (t1/2 : 1.91-3 .68 hours), potentially enabling fast sleep onset and minimal next-morning effects... Fazamorexant significantly improves sleep onset and maintenance in adults with insomnia, with sustained efficacy over 6 months and a favorable safety profile. Its rapid-onset and short half-life profile make it an unique DORA for insomnia."

Clinical • P3 data • CNS Disorders • Dyslipidemia • Excessive Daytime Sleepiness • Hematological Disorders • Insomnia • Leukopenia • Sleep Disorder

Safety and Efficacy Study of YZJ-1139 Tablets in Insomnia Disorder (clinicaltrials.gov) - P3 | N=60 | Recruiting | Sponsor: Shanghai Haiyan Pharmaceutical Technology Co., Ltd.

New P3 trial • CNS Disorders • Insomnia • Sleep Disorder

PK/PD Study of YZJ-1139 (clinicaltrials.gov) - P1 | N=20 | Completed | Sponsor: Shanghai Haiyan Pharmaceutical Technology Co., Ltd.

New P1 trial • CNS Disorders • Insomnia • Sleep Disorder

Safety and Efficacy Study of YZJ-1139 in Primary Chronic Insomnia Disorder (clinicaltrials.gov) - P2 | N=300 | Completed | Sponsor: Shanghai Haiyan Pharmaceutical Technology Co., Ltd.

New P2 trial • CNS Disorders • Insomnia • Sleep Disorder

A Clinical Study to Evaluate the Drug Interaction Between YZJ-1139 Tablets and Escitalopram Oxalate Tablets (clinicaltrials.gov) - P1 | N=24 | Active, not recruiting | Sponsor: Shanghai Haiyan Pharmaceutical Technology Co., Ltd.

New P1 trial • CNS Disorders • Insomnia • Sleep Disorder

A Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of Single and Multiple Doses of YZJ-1139 in Healthy Participants (clinicaltrials.gov) - P1 | N=104 | Completed | Sponsor: Shanghai Haiyan Pharmaceutical Technology Co., Ltd.

New P1 trial • CNS Disorders • Insomnia • Sleep Disorder

A Drug-drug Interaction Study of YZJ-1139 Tablets and Ticagrelor Tablets in Healthy Subjects (clinicaltrials.gov) - P1 | N=27 | Active, not recruiting | Sponsor: Shanghai Haiyan Pharmaceutical Technology Co., Ltd.

New P1 trial • CNS Disorders • Insomnia • Sleep Disorder

Pharmacokinetics and Safety Study of YZJ-1139 in Subjects With Severe Renal Impairment and Normal Renal Impairment (clinicaltrials.gov) - P1 | N=16 | Active, not recruiting | Sponsor: Shanghai Haiyan Pharmaceutical Technology Co., Ltd.

New P1 trial • CNS Disorders • Insomnia • Renal Disease • Sleep Disorder

Pharmacokinetics and Safety Study of YZJ-1139 in Subjects With Mild, Moderate and Normal Hepatic Impairment (clinicaltrials.gov) - P1 | N=24 | Completed | Sponsor: Shanghai Haiyan Pharmaceutical Technology Co., Ltd.

New P1 trial • CNS Disorders • Hepatology • Insomnia • Sleep Disorder

A Interaction Study of YZJ-1139 and Ticagrelor (ChiCTR) - P1 | N=24 | Not yet recruiting | Sponsor: shulan(hangzhou)hospital; Shanghai Haiyan Pharmaceutical Technology Co., Ltd

New P1 trial • CNS Disorders • Insomnia • Sleep Disorder

A clinical study evaluating the drug interaction of YZJ-1139 tablets with Escitalopram oxalate tablets (ChiCTR) - P1 | N=24 | Not yet recruiting | Sponsor: Second Affiliated Hospital of Guangzhou Medical University; Second Affiliated Hospital of Guangzhou Medical University

New P1 trial

Safety and Efficacy Study of YZJ-1139 in Insomnia Disorder (clinicaltrials.gov) - P3 | N=1041 | Recruiting | Sponsor: Shanghai Haiyan Pharmaceutical Technology Co., Ltd. | Trial completion date: Jun 2024 ➔ Dec 2024 | Trial primary completion date: Dec 2023 ➔ Dec 2024

Trial completion date • Trial primary completion date • CNS Disorders • Insomnia • Sleep Disorder

Safety and Efficacy Study of YZJ-1139 in Insomnia Disorder (clinicaltrials.gov) - P3 | N=1041 | Recruiting | Sponsor: Shanghai Haiyan Pharmaceutical Technology Co., Ltd.

New P3 trial • CNS Disorders • Insomnia • Sleep Disorder

Asymmetric Synthesis of Nortropanes via Rh-Catalyzed Allylic Arylation. (PubMed, ACS Catal) - "The method was applied in a highly stereoselective formal synthesis of YZJ-1139(1), a potential insomnia treatment that recently completed Phase II clinical trials. Our report represents an asymmetric catalytic method for the synthesis of YZJ-1139(1) and related compounds."

Journal • CNS Disorders • Insomnia • Sleep Disorder