sunobinop (IMB-115) / Shionogi, Knoa Pharma - LARVOL DELTA

Design, Synthesis, and Pharmacological Characterization of Substituted Quinoxalines as NOP Receptor Ligands. (PubMed, Curr Med Chem) - "The discovery of sunobinop (compound 5), a NOP partial agonist highly selective for NOP in vitro, was significant. Compound 5 produced antihyperalgesic efficacy in rodents and has progressed to clinical trials."

Journal • Neuralgia • Pain

Study of Sunobinop on Alcohol Consumption in Alcohol Use Disorder (clinicaltrials.gov) - P2 | N=209 | Completed | Sponsor: Imbrium Therapeutics | Active, not recruiting ➔ Completed

Trial completion • Addiction (Opioid and Alcohol)

A Randomized, Double-Blind, Placebo-Controlled, Crossover Study to Evaluate the Safety, Tolerability, Pharmacokinetic, and Pharmacodynamic Interactions Between Alcohol and Sunobinop in Healthy Participants. (PubMed, J Clin Psychopharmacol) - "A single oral dose of sunobinop was safe and tolerated alone and in combination with alcohol. No pharmacokinetic interaction between sunobinop and alcohol was observed. An additive or greater-than-additive effect was observed for psychomotor/cognitive measures consistent with sunobinop's sleep-promoting effect, and would peak and resolve during a typical night's sleep."

Clinical • Journal • PK/PD data

Human Abuse Potential of Single Oral Doses of Sunobinop, a Novel, Highly Potent, and Selective Partial Agonist for Nociceptin/Orphanin-FQ Peptide (NOP) Receptors. (PubMed, J Clin Psychopharmacol) - "Drug-liking following sunobinop at a potential therapeutic dose was not different from placebo and was significantly lower compared with triazolam at a recommended dose. In addition, its good tolerability profile suggests sunobinop may be a useful new treatment option, particularly in at-risk populations."

Clinical • Journal • Addiction (Opioid and Alcohol) • CNS Disorders • Insomnia • Sleep Disorder

Study of Sunobinop on Alcohol Consumption in Alcohol Use Disorder (clinicaltrials.gov) - P2 | N=200 | Active, not recruiting | Sponsor: Imbrium Therapeutics | Recruiting ➔ Active, not recruiting

Enrollment closed • Addiction (Opioid and Alcohol)

Efficacy and safety of a selective partial agonist for nociception/orphanin-FQ peptide (NOP) receptors in patients with insomnia disorder. (PubMed, Br J Clin Pharmacol) - "In this Phase 1 study of 30 patients, sunobinop was well tolerated by patients, with no study discontinuation due to AEs. Doses were identified that had a beneficial effect on sleep measures without eliciting next-day residual effects (<3 mg). These data suggest that sunobinop has the potential to be developed as a therapeutic option for the treatment of sleep disturbances, including DSM-5 insomnia; however, larger confirmatory studies are warranted."

Clinical • Journal • CNS Disorders • Insomnia • Mental Retardation • Psychiatry • Sleep Disorder

Study of Sunobinop on Alcohol Consumption in Alcohol Use Disorder (clinicaltrials.gov) - P2 | N=200 | Recruiting | Sponsor: Imbrium Therapeutics | Trial completion date: Jul 2025 ➔ Mar 2026 | Trial primary completion date: Jul 2025 ➔ Mar 2026

Trial completion date • Trial primary completion date • Addiction (Opioid and Alcohol)

Study of Sunobinop on Craving in Alcohol Use Disorder (clinicaltrials.gov) - P2 | N=40 | Completed | Sponsor: Imbrium Therapeutics | Recruiting ➔ Completed

Trial completion • Addiction (Opioid and Alcohol)

In vitro pharmacological evaluation of the novel NOP receptor partial agonist sunobinop. (PubMed, Biochem Pharmacol) - "Notably, it demonstrated competitive antagonism in the NOP - β-Arrestin 2 recruitment and ex vivo electrically stimulated mouse Vas Deferens, assays characterized by low amplification. The findings reported here confirm and extend the characterization of sunobinop as a tool for studying NOP receptor pharmacology providing new insights into its mode of action, relevant to its clinical evaluation."

Journal • Preclinical • CNS Disorders • Insomnia • Sleep Disorder • ARRB1

Imbrium Therapeutics Achieves Last Patient Last Visit in Clinical Trial of Potential Treatment for Interstitial Cystitis/Bladder Pain Syndrome (Businesswire) - "Imbrium Therapeutics...has achieved last patient last visit in its Phase 1b study of the investigational drug sunobinop as a potential treatment for interstitial cystitis/bladder pain syndrome (IC/BPS). IC/BPS is a chronic painful and debilitating urologic disorder that negatively affects patients’ quality of life and can lead to radical lifestyle and behavioral modifications....Forty-seven female patients with IC/BPS were enrolled in this multicenter, randomized, double-blind, placebo-controlled, crossover study. The study was designed to assess impact of once-a-day sunobinop taken at bedtime for 6 weeks on key disease symptoms, such as bladder pain and discomfort as well as urinary urgency and frequency, in subjects with IC/BPS compared to placebo."

Enrollment closed • Interstitial Cystitis • Pain

Study of Sunobinop on Craving in Alcohol Use Disorder (clinicaltrials.gov) - P2 | N=40 | Recruiting | Sponsor: Imbrium Therapeutics | Not yet recruiting ➔ Recruiting

Enrollment open • Addiction (Opioid and Alcohol)

Study of V117957 in Interstitial Cystitis/Bladder Pain Syndrome (clinicaltrials.gov) - P1 | N=47 | Completed | Sponsor: Imbrium Therapeutics | Active, not recruiting ➔ Completed | Trial completion date: Jun 2026 ➔ Jan 2025 | Trial primary completion date: Jun 2026 ➔ Jan 2025

Trial completion • Trial completion date • Trial primary completion date • Interstitial Cystitis • Musculoskeletal Pain • Pain

Study of Sunobinop on Craving in Alcohol Use Disorder (clinicaltrials.gov) - P2 | N=40 | Not yet recruiting | Sponsor: Imbrium Therapeutics | Initiation date: Sep 2024 ➔ Feb 2025

Trial initiation date • Addiction (Opioid and Alcohol)

Study of V117957 in Interstitial Cystitis/Bladder Pain Syndrome (clinicaltrials.gov) - P1 | N=44 | Active, not recruiting | Sponsor: Imbrium Therapeutics | Recruiting ➔ Active, not recruiting

Enrollment closed • Interstitial Cystitis • Musculoskeletal Pain • Pain

Study of Sunobinop on Alcohol Consumption in Alcohol Use Disorder (clinicaltrials.gov) - P2 | N=200 | Recruiting | Sponsor: Imbrium Therapeutics | Not yet recruiting ➔ Recruiting

Enrollment open • Addiction (Opioid and Alcohol)

Evaluation of sunobinop for next-day residual effects in healthy participants. (PubMed, Front Pharmacol) - "No deaths occurred during the study or discontinuations due to an AE. Overall, a nighttime oral dose of sunobinop up to 2 mg was safe and generally well tolerated in healthy participants with limited next-day residual effects that were consistent with other sedative/hypnotic drugs."

Clinical • Journal • CNS Disorders • Insomnia • Sleep Disorder

Study of Sunobinop on Craving in Alcohol Use Disorder (clinicaltrials.gov) - P2 | N=40 | Not yet recruiting | Sponsor: Imbrium Therapeutics

New P2 trial • Addiction (Opioid and Alcohol)

Study of Sunobinop on Alcohol Consumption in Alcohol Use Disorder (clinicaltrials.gov) - P2 | N=200 | Not yet recruiting | Sponsor: Imbrium Therapeutics

New P2 trial • Addiction (Opioid and Alcohol)

Study of V117957 in Overactive Bladder Syndrome (clinicaltrials.gov) - P1 | N=51 | Completed | Sponsor: Imbrium Therapeutics | Active, not recruiting ➔ Completed | Trial completion date: Dec 2024 ➔ May 2024 | Trial primary completion date: Dec 2024 ➔ May 2024

Trial completion • Trial completion date • Trial primary completion date • Overactive Bladder

Study of V117957 in Overactive Bladder Syndrome (clinicaltrials.gov) - P1 | N=44 | Active, not recruiting | Sponsor: Imbrium Therapeutics | Recruiting ➔ Active, not recruiting

Enrollment closed • Overactive Bladder

Safety, Tolerability, and Pharmacokinetics of Single- and Multiple-Ascending Doses of Sunobinop in Healthy Participants. (PubMed, Clin Pharmacol Drug Dev) - "Most treatment-emergent adverse events (TEAEs) were mild in severity; 1 severe TEAE occurred and all TEAEs resolved by the end of the studies. Sunobinop was generally well-tolerated and safe across the range of doses evaluated and presents a clinical profile suitable for continued development."

Clinical • Journal • PK/PD data

Study of V117957 in Interstitial Cystitis/Bladder Pain Syndrome (clinicaltrials.gov) - P1 | N=44 | Recruiting | Sponsor: Imbrium Therapeutics

New P1 trial • Interstitial Cystitis • Musculoskeletal Pain • Pain

The nociceptin/orphanin-FQ receptor partial agonist sunobinop promotes non-REM sleep in rodents and patients with insomnia. (PubMed, J Clin Invest) - No abstract available

Journal • Preclinical • CNS Disorders • Insomnia • Sleep Disorder

Study of V117957 in Overactive Bladder Syndrome (clinicaltrials.gov) - P1 | N=44 | Recruiting | Sponsor: Imbrium Therapeutics

New P1 trial • Overactive Bladder

Sunobinop: A novel selective partial agonist at nociception/orphanin-FQ peptide (NOP) with sleep promoting and wake suppressing actions (WSS 2023) - No abstract available