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- | ketamine / Generic mfg., dizocilpine (MK801) / Merck (MSD), MK-8189 / Merck (MSD)
Preclinical, Journal: Preclinical evaluation of MK-8189: A novel phosphodiesterase 10A inhibitor for the treatment of schizophrenia. (Pubmed Central) - Feb 2, 2025
MK-8189 significantly reversed an MK-801-induced deficit in prepulse inhibition at PDE10A EO of ?47% and higher...MK-8189 significantly attenuated a ketamine-induced deficit in object retrieval performance at exposure that yielded ?29% PDE10A EO...The PDE10A occupancy achieved by MK-8189 in behavioral studies was used to support dose selection in clinical trials. This work provides evidence to support exploration of higher levels of PDE10A occupancy in clinical trials to determine if this translates to improved efficacy in patients.
- || MK-8189 / Merck (MSD)
New P1 trial: A Study of MK-8189 Human Absorption, Metabolism, and Excretion in Healthy Male Participants (MK-8189-010) (clinicaltrials.gov) - Oct 3, 2024
P1, N=6, Completed, Sponsor: Merck Sharp & Dohme LLC
- || MK-8189 / Merck (MSD)
Trial completion: A Study of MK-8189 in Participants With Bipolar I Disorder (MK-8189-020) (clinicaltrials.gov) - Sep 19, 2024
P1, N=34, Completed, Sponsor: Merck Sharp & Dohme LLC
This work provides evidence to support exploration of higher levels of PDE10A occupancy in clinical trials to determine if this translates to improved efficacy in patients. Active, not recruiting --> Completed
- | MK-8189 / Merck (MSD)
Phase classification: An Active-Controlled Early Phase Study of MK-8189 in Adults With Schizophrenia (MK-8189-005) (clinicaltrials.gov) - Aug 28, 2024
P2, N=224, Completed, Sponsor: Merck Sharp & Dohme LLC
Active, not recruiting --> Completed Phase classification: P2a --> P2
- || MK-8189 / Merck (MSD)
Enrollment closed: A Study of MK-8189 in Participants With Bipolar I Disorder (MK-8189-020) (clinicaltrials.gov) - Aug 19, 2024
P1, N=32, Active, not recruiting, Sponsor: Merck Sharp & Dohme LLC
Phase classification: P2a --> P2 Recruiting --> Active, not recruiting
- |||| MK-8189 / Merck (MSD)
Trial completion: Efficacy and Safety of MK-8189 in Participants With an Acute Episode of Schizophrenia (MK-8189-008) (clinicaltrials.gov) - Jul 9, 2024
P2, N=500, Completed, Sponsor: Merck Sharp & Dohme LLC
Recruiting --> Active, not recruiting Active, not recruiting --> Completed
- || MK-8189 / Merck (MSD)
Enrollment open: A Study of MK-8189 in Participants With Bipolar I Disorder (MK-8189-020) (clinicaltrials.gov) - Apr 23, 2024
P1, N=32, Recruiting, Sponsor: Merck Sharp & Dohme LLC
Active, not recruiting --> Completed Not yet recruiting --> Recruiting
- || MK-5720 / Merck (MSD)
Trial completion, Enrollment change, Trial completion date, Trial primary completion date: A Study of MK-5720 in Participants With Schizophrenia (MK-5720-001) (clinicaltrials.gov) - Mar 26, 2024
P1, N=17, Completed, Sponsor: Merck Sharp & Dohme LLC
Not yet recruiting --> Recruiting Recruiting --> Completed | N=64 --> 17 | Trial completion date: Sep 2024 --> Feb 2024 | Trial primary completion date: Sep 2024 --> Feb 2024
- ||| MK-8189 / Merck (MSD)
Enrollment closed: Efficacy and Safety of MK-8189 in Participants With an Acute Episode of Schizophrenia (MK-8189-008) (clinicaltrials.gov) - Mar 18, 2024
P2, N=500, Active, not recruiting, Sponsor: Merck Sharp & Dohme LLC
Recruiting --> Completed | N=64 --> 17 | Trial completion date: Sep 2024 --> Feb 2024 | Trial primary completion date: Sep 2024 --> Feb 2024 Recruiting --> Active, not recruiting
- ||| MK-8189 / Merck (MSD)
Trial completion: TQT: A Study To Evaluate The Effect Of A Supratherapeutic Dose Of MK-8189 On The QTc Interval In Participants With Schizophrenia (MK-8189-019) (clinicaltrials.gov) - Mar 11, 2024
P1, N=107, Completed, Sponsor: Merck Sharp & Dohme LLC
Recruiting --> Active, not recruiting Active, not recruiting --> Completed
- || MK-8189 / Merck (MSD)
New P1 trial: A Study of MK-8189 in Participants With Bipolar I Disorder (MK-8189-020) (clinicaltrials.gov) - Feb 23, 2024
P1, N=32, Not yet recruiting, Sponsor: Merck Sharp & Dohme LLC
- || MK-8189 / Merck (MSD)
Enrollment closed: TQT: A Study To Evaluate The Effect Of A Supratherapeutic Dose Of MK-8189 On The QTc Interval In Participants With Schizophrenia (MK-8189-019) (clinicaltrials.gov) - Feb 5, 2024
P1, N=84, Active, not recruiting, Sponsor: Merck Sharp & Dohme LLC
Active, not recruiting --> Completed Recruiting --> Active, not recruiting
- || MK-8189 / Merck (MSD)
Review, Journal: Fragment-to-Lead Medicinal Chemistry Publications in 2022. (Pubmed Central) - Jan 30, 2024
In addition, trends and new developments in the field are summarized. In 2022, 18 publications described successful fragment-to-lead studies, including the development of three clinical compounds (MTRX1719, MK-8189, and BI-823911).
- | MK-8189 / Merck (MSD)
Phase classification: Efficacy and Safety of MK-8189 in Participants With an Acute Episode of Schizophrenia (MK-8189-008) (clinicaltrials.gov) - Nov 27, 2023
P2, N=500, Recruiting, Sponsor: Merck Sharp & Dohme LLC
In 2022, 18 publications described successful fragment-to-lead studies, including the development of three clinical compounds (MTRX1719, MK-8189, and BI-823911). Phase classification: P2b --> P2
- ||| MK-5720 / Merck (MSD)
Enrollment open: A Study of MK-5720 in Participants With Schizophrenia (MK-5720-001) (clinicaltrials.gov) - Sep 22, 2023
P1, N=64, Recruiting, Sponsor: Merck Sharp & Dohme LLC
Phase classification: P2b --> P2 Not yet recruiting --> Recruiting
- | MK-8189 / Merck (MSD)
Preclinical, Journal, MRI: Magnetic resonance imaging detects white adipose tissue beiging in mice following PDE10A inhibitor treatment. (Pubmed Central) - Aug 28, 2023
Not yet recruiting --> Recruiting This work provides a detailed understanding of the mechanism of action of PDE10A inhibitor treatment on adipose tissue and body weight, and will be valuable to guide both the use of MK-8189 in schizophrenia and the potential application of the target for weight loss indication.
- ||| MK-5720 / Merck (MSD)
New P1 trial: A Study of MK-5720 in Participants With Schizophrenia (MK-5720-001) (clinicaltrials.gov) - Jul 20, 2023
P1, N=64, Not yet recruiting, Sponsor: Merck Sharp & Dohme LLC
- ||| MK-8189 / Merck (MSD)
Enrollment open: TQT: A Study To Evaluate The Effect Of A Supratherapeutic Dose Of MK-8189 On The QTc Interval In Participants With Schizophrenia (MK-8189-019) (clinicaltrials.gov) - Jul 13, 2023
P1, N=84, Recruiting, Sponsor: Merck Sharp & Dohme LLC
This work provides a detailed understanding of the mechanism of action of PDE10A inhibitor treatment on adipose tissue and body weight, and will be valuable to guide both the use of MK-8189 in schizophrenia and the potential application of the target for weight loss indication. Not yet recruiting --> Recruiting
- ||| MK-8189 / Merck (MSD)
New P1 trial: TQT: A Study To Evaluate The Effect Of A Supratherapeutic Dose Of MK-8189 On The QTc Interval In Participants With Schizophrenia (MK-8189-019) (clinicaltrials.gov) - Jun 8, 2023
P1, N=84, Not yet recruiting, Sponsor: Merck Sharp & Dohme LLC
- MK-8189 / Merck (MSD)
Pharmacological Profile and Relationship between PDE10A Enzyme Occupancy and Preclinical Efficacy for MK-8189, a Novel PDE10A Inhibitor (Salon 4) - Apr 15, 2023 - Abstract #ASCP2023ASCP_267;
Not yet recruiting --> Recruiting MK-8189 (0.25
- MK-8189 / Merck (MSD)
Weight Loss following PDE10A Inhibitor Schizophrenia Treatment Explained by Adipose Tissue Physiology Changes in Obese Mice (Salon 4) - Apr 15, 2023 - Abstract #ASCP2023ASCP_258;
Interestingly, MK-8189 was also observed to reduce body weight, particularly in those who were overweight and obese, while a significant weight gain was observed for the standard-of-care risperidone. Mice receiving THPP-6 showed greater weight loss than vehicle-treated animals (-7.1
- MK-8189 / Merck (MSD)
The Pharmacological Profile and the Relationship betweenPDE10A Enzyme Occupancy and Preclinical Efficacy for MK-8189, aNovel PDE10A Inhibitor () - Mar 10, 2023 - Abstract #SIRS2023SIR_295;
Mice receiving THPP-6 showed greater weight loss than vehicle-treated animals (-7.1 MK-8189(0.25
- ||| MK-8189 / Merck (MSD)
Trial completion: A Study of MK-8189 in Participants With Schizophrenia (MK-8189-014) (clinicaltrials.gov) - Mar 3, 2023
P1, N=53, Completed, Sponsor: Merck Sharp & Dohme LLC
MK-8189(0.25 Active, not recruiting --> Completed
- || MK-8189 / Merck (MSD)
Enrollment closed: A Study of MK-8189 in Participants With Schizophrenia (MK-8189-014) (clinicaltrials.gov) - Jan 25, 2023
P1, N=54, Active, not recruiting, Sponsor: Merck Sharp & Dohme LLC
Active, not recruiting --> Completed Recruiting --> Active, not recruiting
- || MK-8189 / Merck (MSD)
Trial completion: MK-8189 Safety and Tolerability in Participants With Alzheimer's Disease With or Without Symptoms of Agitation-Aggression and/or Psychosis (MK-8189-017) (clinicaltrials.gov) - Jan 20, 2023
P1, N=29, Completed, Sponsor: Merck Sharp & Dohme LLC
Recruiting --> Active, not recruiting Active, not recruiting --> Completed
- | MK-8189 / Merck (MSD)
Journal: Discovery of MK-8189, a Highly Potent and Selective PDE10A Inhibitor for the Treatment of Schizophrenia. (Pubmed Central) - Jan 11, 2023
With the goal of developing PDE10A inhibitors, early optimization of a fragment hit through rational design led to a series of potent pyrimidine PDE10A inhibitors that required further improvements in physicochemical properties, off-target activities, and pharmacokinetics. Herein we describe the discovery of an isomeric pyrimidine series that addresses the liabilities seen with earlier compounds and resulted in the invention of compound 18 (MK-8189), which is currently in Phase 2b clinical development for the treatment of schizophrenia.
- || MK-8189 / Merck (MSD)
Enrollment closed: MK-8189 Safety and Tolerability in Participants With Alzheimer's Disease With or Without Symptoms of Agitation-Aggression and/or Psychosis (MK-8189-017) (clinicaltrials.gov) - Nov 25, 2022
P1, N=28, Active, not recruiting, Sponsor: Merck Sharp & Dohme LLC
Herein we describe the discovery of an isomeric pyrimidine series that addresses the liabilities seen with earlier compounds and resulted in the invention of compound 18 (MK-8189), which is currently in Phase 2b clinical development for the treatment of schizophrenia. Recruiting --> Active, not recruiting
- | MK-8189 / Merck (MSD)
Trial completion date, Trial primary completion date: MK-8189 Safety and Tolerability in Participants With Alzheimer's Disease With or Without Symptoms of Agitation-Aggression and/or Psychosis (MK-8189-017) (clinicaltrials.gov) - Nov 14, 2022
P1, N=28, Recruiting, Sponsor: Merck Sharp & Dohme LLC
Recruiting --> Active, not recruiting Trial completion date: Nov 2023 --> Jan 2023 | Trial primary completion date: Nov 2023 --> Jan 2023
- MK-8189 / Merck (MSD)
Efficacy and Weight Effects of MK-8189, a Novel PDE10A Inhibitor for the Treatment of Schizophrenia (Grand Saguaro) - Oct 31, 2022 - Abstract #ACNP2022ACNP_1205;
P2a, P2b
This could be an important advantage over current antipsychotics which are associated with weight gain. Based on the signal detected in the phase 2a study, a phase 2b study (NCT04624243) is underway to evaluate a broader dose range of MK-8189.
- MK-8189 / Merck (MSD)
Initial clinical profile of the PDE10A inhibitor MK-8189 in people with an acute episode of schizophrenia (Poster area [IN-PERSON]) - Oct 13, 2022 - Abstract #ECNP2022ECNP_1136;
P2a, P2b
Participants were men and women between 18-50 years of age who currently met diagnostic criteria for schizophrenia according to DSM-5™, had a past diagnosis of schizophrenia with the onset of the first episode being ≥1 year prior to study entry, an illness duration of ≤ 20 years, and had responded positively to an antipsychotic medication other than clozapine in a prior psychotic episode. Based on the signal detected in this study, a phase 2b study (clinicaltrials.gov NCT04624243) is underway to evaluate a broader dose range of MK-8189.
- || MK-8189 / Merck (MSD)
Trial completion date, Trial primary completion date: Efficacy and Safety of MK-8189 in Participants With an Acute Episode of Schizophrenia (MK-8189-008) (clinicaltrials.gov) - Sep 21, 2022
P2b, N=576, Recruiting, Sponsor: Merck Sharp & Dohme LLC
Based on the signal detected in this study, a phase 2b study (clinicaltrials.gov NCT04624243) is underway to evaluate a broader dose range of MK-8189. Trial completion date: Apr 2023 --> Jun 2024 | Trial primary completion date: Apr 2023 --> Jun 2024
- ||| MK-8189 / Merck (MSD)
Enrollment open: A Study of MK-8189 in Participants With Schizophrenia (MK-8189-014) (clinicaltrials.gov) - Jul 20, 2022
P1, N=54, Recruiting, Sponsor: Merck Sharp & Dohme LLC
Trial completion date: Apr 2023 --> Jun 2024 | Trial primary completion date: Apr 2023 --> Jun 2024 Not yet recruiting --> Recruiting
- || MK-8189 / Merck (MSD)
Enrollment open: MK-8189 Safety and Tolerability in Participants With Alzheimer's Disease With or Without Symptoms of Agitation-Aggression and/or Psychosis (MK-8189-017) (clinicaltrials.gov) - Jul 8, 2022
P1, N=28, Recruiting, Sponsor: Merck Sharp & Dohme LLC
Not yet recruiting --> Recruiting Not yet recruiting --> Recruiting
- ||| MK-8189 / Merck (MSD)
New P1 trial: A Study of MK-8189 in Participants With Schizophrenia (MK-8189-014) (clinicaltrials.gov) - Jun 5, 2022
P1, N=54, Not yet recruiting, Sponsor: Merck Sharp & Dohme LLC
- MK-8189 / Merck (MSD)
Preclinical Characterization and Phase 1 Evaluation of the Tolerability, Pharmacokinetics, and Enzyme Occupancy of MK-8189, a Novel PDE10A Inhibitor () - May 6, 2022 - Abstract #SOBP2022SOBP_1081;
Not yet recruiting --> Recruiting These findings demonstrate that MK-8189 is generally well tolerated at exposures that achieve PDE10A occupancy targets identified in preclinical efficacy studies.
- MK-8189 / Merck (MSD)
Initial Assessment of the Clinical Profile of the PDE10A Inhibitor MK-8189 in Patients With an Acute Episode of Schizophrenia (Churchill) - May 6, 2022 - Abstract #SOBP2022SOBP_209;
P2a, P2b
These findings demonstrate that MK-8189 is generally well tolerated at exposures that achieve PDE10A occupancy targets identified in preclinical efficacy studies. Based on the signal detected in this study, a phase 2b study (NCT04624243) is underway to evaluate a broader dose range of MK-8189.
- MK-8189 / Merck (MSD)
MK-8189, a Novel PDE10A Inhibitor for the Treatment of Schizophrenia (Palomino Ballroom 4-10) - May 6, 2022 - Abstract #ASCP2022ASCP_112;
P2a, P2b
These findings suggest that PDE10A inhibition via MK-8189 could represent a new treatment approach for schizophrenia. Based on the signal detected in the phase 2a study, a phase 2b study (NCT04624243) is underway to evaluate a broader dose range of MK-8189.
- MK-8189 / Merck (MSD)
MK-8189, a Novel PDE10A Inhibitor for the Treatment of Schizophrenia (Salon A-E) - May 6, 2022 - Abstract #ASCP2022ASCP_28;
P2a, P2b
These findings suggest that PDE10A inhibition via MK-8189 could represent a new treatment approach for schizophrenia. Based on the signal detected in the phase 2a study, a phase 2b study (NCT04624243) is underway to evaluate a broader dose range of MK-8189.
- ||| MK-8189 / Merck (MSD)
Trial completion, Enrollment change: Safety, Tolerability, and Pharmacokinetics Study of Elpipodect (MK-8189) in Participants With Schizophrenia and Healthy Participants (MK-8189-011) (clinicaltrials.gov) - Apr 8, 2022
P1, N=63, Completed, Sponsor: Merck Sharp & Dohme Corp.
Based on the signal detected in the phase 2a study, a phase 2b study (NCT04624243) is underway to evaluate a broader dose range of MK-8189. Active, not recruiting --> Completed | N=100 --> 63
- MK-8189 / Merck (MSD)
Phase classification: MK-8189 Safety and Tolerability in Participants With Alzheimer's Disease With or Without Symptoms of Agitation-Aggression and/or Psychosis (MK-8189-017) (clinicaltrials.gov) - Mar 28, 2022
P1, N=28, Not yet recruiting, Sponsor: Merck Sharp & Dohme Corp.
Active, not recruiting --> Completed | N=100 --> 63 Phase classification: P1/2 --> P1
- || MK-8189 / Merck (MSD)
Enrollment closed: Safety, Tolerability, and Pharmacokinetics Study of Elpipodect (MK-8189) in Participants With Schizophrenia and Healthy Participants (MK-8189-011) (clinicaltrials.gov) - Mar 10, 2022
P1, N=100, Active, not recruiting, Sponsor: Merck Sharp & Dohme Corp.
Phase classification: P1/2 --> P1 Recruiting --> Active, not recruiting
- || MK-8189 / Merck (MSD)
Trial completion: A Study to Investigate the Influence of Hepatic Impairment on MK-8189 Treatment (MK-8189-012) (clinicaltrials.gov) - Mar 8, 2022
P1, N=14, Completed, Sponsor: Merck Sharp & Dohme Corp.
Recruiting --> Active, not recruiting Active, not recruiting --> Completed
- ||| Rexulti (brexpiprazole) / Lundbeck, Otsuka
Clinical, Review, Journal, Adverse events: New and emerging treatments for schizophrenia: a narrative review of their pharmacology, efficacy and side effect profile relative to established antipsychotics. (Pubmed Central) - Mar 3, 2022
These medications largely have favourable cardiometabolic side-effect profiles. Overall, the novel pharmacology, clinical trial and tolerability data indicate these compounds are promising new additions to the therapeutic arsenal.
- || MK-8189 / Merck (MSD)
Trial completion date, Trial primary completion date: Efficacy and Safety of MK-8189 in Participants With an Acute Episode of Schizophrenia (MK-8189-008) (clinicaltrials.gov) - Feb 21, 2022
P2b, N=576, Recruiting, Sponsor: Merck Sharp & Dohme Corp.
Overall, the novel pharmacology, clinical trial and tolerability data indicate these compounds are promising new additions to the therapeutic arsenal. Trial completion date: Oct 2022 --> Apr 2023 | Trial primary completion date: Oct 2022 --> Apr 2023
- || MK-8189 / Merck (MSD)
New P1 trial, New P1/2 trial: MK-8189 Safety and Tolerability in Participants With Alzheimer's Disease With or Without Symptoms of Agitation-Aggression and/or Psychosis (MK-8189-017) (clinicaltrials.gov) - Feb 7, 2022
P1/2, N=28, Not yet recruiting, Sponsor: Merck Sharp & Dohme Corp.
- || MK-8189 / Merck (MSD)
Enrollment closed: A Study to Investigate the Influence of Hepatic Impairment on MK-8189 Treatment (MK-8189-012) (clinicaltrials.gov) - Feb 2, 2022
P1, N=16, Active, not recruiting, Sponsor: Merck Sharp & Dohme Corp.
Trial completion date: Oct 2022 --> Apr 2023 | Trial primary completion date: Oct 2022 --> Apr 2023 Recruiting --> Active, not recruiting
- || MK-8189 / Merck (MSD)
Trial completion date, Trial primary completion date: Efficacy and Safety of MK-8189 in Participants With an Acute Episode of Schizophrenia (MK-8189-008) (clinicaltrials.gov) - Aug 18, 2021
P2b, N=576, Recruiting, Sponsor: Merck Sharp & Dohme Corp.
Recruiting --> Active, not recruiting Trial completion date: Jul 2022 --> Oct 2022 | Trial primary completion date: Jul 2022 --> Oct 2022
- || MK-8189 / Merck (MSD)
Trial completion date, Trial primary completion date: Safety, Tolerability, and Pharmacokinetics Study of Elpipodect (MK-8189) in Participants With Schizophrenia and Healthy Participants (MK-8189-011) (clinicaltrials.gov) - Jun 29, 2021
P1, N=100, Recruiting, Sponsor: Merck Sharp & Dohme Corp.
Trial completion date: Jul 2022 --> Oct 2022 | Trial primary completion date: Jul 2022 --> Oct 2022 Trial completion date: Sep 2021 --> Jan 2022 | Trial primary completion date: Sep 2021 --> Jan 2022
- || MK-8189 / Merck (MSD)
Enrollment change: Safety, Tolerability, and Pharmacokinetics Study of Elpipodect (MK-8189) in Participants With Schizophrenia and Healthy Participants (MK-8189-011) (clinicaltrials.gov) - Jun 1, 2021
P1, N=100, Recruiting, Sponsor: Merck Sharp & Dohme Corp.
Trial completion date: Sep 2021 --> Jan 2022 | Trial primary completion date: Sep 2021 --> Jan 2022 N=72 --> 100
- || MK-8189 / Merck (MSD)
Enrollment open: A Study to Investigate the Influence of Hepatic Impairment on MK-8189 Treatment (MK-8189-012) (clinicaltrials.gov) - Mar 9, 2021
P1, N=16, Recruiting, Sponsor: Merck Sharp & Dohme Corp.
N=72 --> 100 Not yet recruiting --> Recruiting