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- | tavapadon (CVL-751) / AbbVie
Journal: Orally Bioavailable Dopamine D1/D5 Receptor-Biased Agonists to Study the Role of ?-Arrestin in Treatment-Related Dyskinesia in Parkinson's Disease. (Pubmed Central) - Jul 10, 2025
At particular doses, compound 24 produced efficacy comparable to L-DOPA, but with fewer concomitant dyskinesias. This first in vivo study suggests that ?-arrestin may have a positive influence on reducing dyskinesias following acute administration.
- | tavapadon (CVL-751) / AbbVie
Journal: Estimation of Dopamine D1 Receptor Agonist Binding Kinetics Using Time-Resolved Functional Assays: Relation to Agonist-Induced Receptor Internalization by Investigational Antiparkinsonian Therapeutics. (Pubmed Central) - Jul 2, 2025
Tavapadon and apomorphine were partial agonists in both assays, whereas A77636 and dihydrexidine showed efficacies similar to dopamine. While our results do not provide evidence for a direct correlation between agonist dissociation and liability to tolerance induction, the possibility remains that certain combinations of agonist characteristics, such as high efficacy paired with slow dissociation, are associated with tolerance induction by D1R agonists.
- icalcaprant (CVL-354) / AbbVie
Development of a Kappa Opioid Receptor Antagonist (CVL-354) to Mitigate the Physical Symptoms of Opioid Withdrawal to Facilitate Abrupt Opioid Discontinuation in Adults (Maurepas, Third Floor) - Jun 8, 2025 - Abstract #CPDD2025CPDD_1243;
- icalcaprant (CVL-354) / AbbVie, INDV-2000 / Indivior
NIDA (Maurepas, Third Floor) - Jun 8, 2025 - Abstract #CPDD2025CPDD_953;
Frank Gray (Indivior) will present on the development of the selective orexin-1 receptor antagonist, INDV-2000, for OUD...Georgette Suidan (AbbVie) will present on the development of kappa opioid antagonist, CVL-354, for opioid withdrawal...Nicholas Cosford (Sanford Burnham Prebys Medical Discovery Institute) will present progress on the development of metabotropic glutamate 2/3 receptor (mGluR2/3) positive allosteric modulators (PAMs) for OUD and other SUD indications. Beyond highlighting these respective targets and projects, this symposium will bring attention to those targets from the original ten most wanted paper that have yet to be advanced and foster discussion focused on new potential therapeutic targets.
- | tavapadon (CVL-751) / AbbVie
Journal: Characterization of G?s and G?olf activation by catechol and non-catechol dopamine D1 receptor agonists. (Pubmed Central) - May 19, 2025
In contrast, the non-catechol agonist tavapadon acted as a full agonist at G?olf and a partial agonist at G?s. The effects of these ligands on the thalamocortical and striatonigral electrophysiological events, as well as on the locomotor activity and cognitive function of mice agreed with their selectivity profiles in
- | PF-06412562 / Pfizer, AbbVie
Journal: A Translational Neuroscience & Computational Evaluation of a D1R Partial Agonist for Schizophrenia (TRANSCENDS): Rationale and Study Design of a Brain-Based Clinical Trial. (Pubmed Central) - May 5, 2025
Specifically, this study will assess whether the D1R/D5R partial agonist CVL-562 induces a dose-dependent engagement of spatial working memory circuits in schizophrenia using fMRI...This ensures high-standards for regulatory compliance, data quality, and data sharing across sites, improving aspects of current clinical trial data management. We share the study design and approach with the goal of advancing future pro-cognitive drug development and strategies for developing mechanistically-driven biomarkers in psychiatry.
- || emraclidine (CVL-231) / AbbVie
Trial completion: CVL-231-1006: A Multiple Dose Trial of Emraclidine in Elderly Participants and in Participants With Dementia Due to Alzheimer's Disease (clinicaltrials.gov) - May 2, 2025
P1, N=17, Completed, Sponsor: AbbVie
We share the study design and approach with the goal of advancing future pro-cognitive drug development and strategies for developing mechanistically-driven biomarkers in psychiatry. Active, not recruiting --> Completed
- || tavapadon (CVL-751) / AbbVie
Review, Journal: Managing impulse control and related behavioral disorders in Parkinson's disease: where we are in 2025? (Pubmed Central) - May 2, 2025
Insights into ICDs pathophysiology and DA-specific pharmacodynamics indicate safer profiles for certain preparations (e.g. rotigotine patches) and possibly for D1/D5 agonists like tavapadon. Invasive treatments, including deep brain stimulation and infusion therapies, should be prioritized in advanced-stage PD complicated by ICBDs.
- ||| tavapadon (CVL-751) / AbbVie
Enrollment open: A Study to Assess the Relative Bioavailability of Oral Tavapadon in Healthy Adult Participants (clinicaltrials.gov) - Apr 8, 2025
P1, N=84, Recruiting, Sponsor: AbbVie
Invasive treatments, including deep brain stimulation and infusion therapies, should be prioritized in advanced-stage PD complicated by ICBDs. Not yet recruiting --> Recruiting
- ||| darigabat (CVL-865) / AbbVie
Trial completion, Enrollment change: A Study to Evaluate Efficacy, Safety, and Tolerability of Darigabat in Participants With Panic Disorder (clinicaltrials.gov) - Apr 4, 2025
P2, N=80, Completed, Sponsor: AbbVie
Not yet recruiting --> Recruiting Recruiting --> Completed | N=246 --> 80
- | clozapine / Generic mfg.
Journal: The mechanism of action of clozapine. (Pubmed Central) - Apr 2, 2025
Here we describe how the unique pharmacology of clozapine in the peripheral nervous system held clues for solving the puzzle of clozapine in the central nervous system. Clozapine appears to have been the prototype for a new class of antipsychotics, now entering clinical psychiatry, which activates muscarinic acetylcholine receptors.
- || emraclidine (CVL-231) / AbbVie
Enrollment closed, Enrollment change: CVL-231-1006: A Multiple Dose Trial of Emraclidine in Elderly Participants and in Participants With Dementia Due to Alzheimer's Disease (clinicaltrials.gov) - Mar 26, 2025
P1, N=17, Active, not recruiting, Sponsor: AbbVie
Clozapine appears to have been the prototype for a new class of antipsychotics, now entering clinical psychiatry, which activates muscarinic acetylcholine receptors. Recruiting --> Active, not recruiting | N=78 --> 17
- ||| tavapadon (CVL-751) / AbbVie
New P1 trial: A Study to Assess the Relative Bioavailability of Oral Tavapadon in Healthy Adult Participants (clinicaltrials.gov) - Mar 26, 2025
P1, N=84, Not yet recruiting, Sponsor: AbbVie
- || Review, Journal: Novel pharmaceutical treatment approaches for schizophrenia: a systematic literature review. (Pubmed Central) - Mar 19, 2025
Novel treatments for schizophrenia show promise in managing both positive and negative symptoms, with generally favorable safety profiles. Future studies should focus on large-scale, long-term trials to refine their efficacy, safety, and clinical applicability.
- HOW THE THERAPEUTIC APPROACH TO EARLY PARKINSON (Hall E) - Mar 10, 2025 - Abstract #ADPD2025ADPD_729;
BIAL BIA 28-6156 activator of the GCase enzyme is under investigation in patients with GBA mutation. The combination of symptomatic and disease modifying therapy, the use of accurate biomarkers and more precise treatment will be the future in the treatment of PD.
- tavapadon (CVL-751) / AbbVie
Efficacy and Safety of Fixed-Dose Tavapadon, an Oral, Once-Daily, Selective D1/D5 Partial Dopamine Agonist for the Treatment of Early Parkinson's Disease (San Diego Convention Center | 6A; In-Person; Virtual) - Mar 8, 2025 - Abstract #AAN2025AAN_2030;
P3
Conclusions In individuals with early PD, tavapadon as monotherapy was effective with an acceptable safety profile. Other trials evaluating tavapadon as flexible-dose monotherapy (TEMPO-2) or adjunctive therapy (TEMPO-3) are completed, and an open-label extension trial evaluating long-term use of tavapadon (TEMPO-4) is ongoing.
- tavapadon (CVL-751) / AbbVie
Efficacy and Safety of Flexible-Dose Tavapadon, an Orally Administered, Once-Daily, Selective D1/D5 Partial Dopamine Agonist for the Treatment of Early Parkinson's Disease (San Diego Convention Center | 6A; In-Person; Virtual) - Mar 8, 2025 - Abstract #AAN2025AAN_2029;
P3
Conclusions TEMPO-2 results demonstrate the efficacy and acceptable safety profile of flexible-dose tavapadon as monotherapy in adults with early PD. Trials evaluating tavapadon as fixed-dose monotherapy (TEMPO-1) or adjunctive therapy (TEMPO-3) are completed; an open-label extension trial evaluating long-term use of tavapadon (TEMPO-4) is ongoing.
- || emraclidine (CVL-231) / AbbVie
Trial completion: A Study to Evaluate the Effect of Hepatic Impairment on the Pharmacokinetics of Emraclidine (clinicaltrials.gov) - Mar 5, 2025
P1, N=38, Completed, Sponsor: Cerevel Therapeutics, LLC
Trials evaluating tavapadon as fixed-dose monotherapy (TEMPO-1) or adjunctive therapy (TEMPO-3) are completed; an open-label extension trial evaluating long-term use of tavapadon (TEMPO-4) is ongoing. Recruiting --> Completed
- ||| emraclidine (CVL-231) / AbbVie
Trial completion, Trial completion date: A Study to Evaluate Pharmacokinetic and Safety Trial of Emraclidine in Participants With Renal Impairment Compared With Participants With Normal Renal Function (clinicaltrials.gov) - Mar 5, 2025
P1, N=58, Completed, Sponsor: Cerevel Therapeutics, LLC
Recruiting --> Completed Active, not recruiting --> Completed | Trial completion date: Jun 2025 --> Dec 2024
- ||| emraclidine (CVL-231) / AbbVie
Enrollment closed: A Study to Evaluate Safety and Tolerability of CVL-231 (Emraclidine) in Adult Participants With Schizophrenia (clinicaltrials.gov) - Feb 12, 2025
P2, N=850, Active, not recruiting, Sponsor: Cerevel Therapeutics, LLC
Active, not recruiting --> Completed | Trial completion date: Jun 2025 --> Dec 2024 Recruiting --> Active, not recruiting
- || icalcaprant (CVL-354) / AbbVie
Trial completion: 529 DDI ITZ: A Study to Assess Change in How Oral Icalcaprant With Itraconazole Moves Through the Body in Healthy Adult Participants (clinicaltrials.gov) - Jan 28, 2025
P1, N=12, Completed, Sponsor: AbbVie
Recruiting --> Active, not recruiting Active, not recruiting --> Completed
- ||| PF-06412562 / Pfizer, AbbVie
Trial completion, Trial completion date: A Translational and Neurocomputational Evaluation of a Dopamine Receptor 1 Partial Agonist for Schizophrenia (clinicaltrials.gov) - Jan 28, 2025
P1/2, N=112, Completed, Sponsor: Yale University
Active, not recruiting --> Completed Active, not recruiting --> Completed | Trial completion date: Dec 2024 --> Mar 2024
- || icalcaprant (CVL-354) / AbbVie
Trial completion, Adverse events: A Single Dose Study to Assess Adverse Events and How Oral Icalcaprant Moves Through the Body in Healthy Adult Japanese and Han Chinese Participants (clinicaltrials.gov) - Jan 28, 2025
P1, N=16, Completed, Sponsor: AbbVie
Active, not recruiting --> Completed | Trial completion date: Dec 2024 --> Mar 2024 Active, not recruiting --> Completed
- | basmisanil (RG1662) / Roche, darigabat (CVL-865) / AbbVie
Journal: New Insights Into Pharmacology of GABAA Receptor Alpha Subunits-Selective Modulators. (Pubmed Central) - Jan 10, 2025
Future drug discovery efforts are encouraged to focus on positive allosteric modulators that selectively target the ?2, ?3 subunits and negative/positive allosteric modulators that target the ?5 subunit of the GABAA receptor. The pursuit of ligands possessing only anxiolytic effects or those enhancing cognition continues to be an important focus for future research, with promising advancements depicted in recent studies.
- || emraclidine (CVL-231) / AbbVie
Enrollment closed: A Study to Evaluate Pharmacokinetic and Safety Trial of Emraclidine in Participants With Renal Impairment Compared With Participants With Normal Renal Function (clinicaltrials.gov) - Jan 8, 2025
P1, N=60, Active, not recruiting, Sponsor: Cerevel Therapeutics, LLC
The pursuit of ligands possessing only anxiolytic effects or those enhancing cognition continues to be an important focus for future research, with promising advancements depicted in recent studies. Recruiting --> Active, not recruiting
- ||| darigabat (CVL-865) / AbbVie
Trial completion, Trial completion date, Trial primary completion date: An Open-label Extension Trial of CVL-865 as Adjunctive Therapy in the Treatment of Focal Onset Seizures (clinicaltrials.gov) - Jan 8, 2025
P2, N=105, Completed, Sponsor: Cerevel Therapeutics, LLC
Recruiting --> Active, not recruiting Active, not recruiting --> Completed | Trial completion date: Jul 2025 --> Dec 2024 | Trial primary completion date: Jul 2025 --> Dec 2024
- || icalcaprant (CVL-354) / AbbVie
Enrollment closed, Adverse events: A Single Dose Study to Assess Adverse Events and How Oral Icalcaprant Moves Through the Body in Healthy Adult Japanese and Han Chinese Participants (clinicaltrials.gov) - Dec 27, 2024
P1, N=16, Active, not recruiting, Sponsor: AbbVie
Active, not recruiting --> Completed | Trial completion date: Jul 2025 --> Dec 2024 | Trial primary completion date: Jul 2025 --> Dec 2024 Recruiting --> Active, not recruiting
- || icalcaprant (CVL-354) / AbbVie
Enrollment closed: 529 DDI ITZ: A Study to Assess Change in How Oral Icalcaprant With Itraconazole Moves Through the Body in Healthy Adult Participants (clinicaltrials.gov) - Dec 27, 2024
P1, N=12, Active, not recruiting, Sponsor: AbbVie
Recruiting --> Active, not recruiting Recruiting --> Active, not recruiting
- |||| emraclidine (CVL-231) / AbbVie
Trial completion: A Trial of 15 and 30 mg Doses of CVL-231 (Emraclidine) in Participants With Schizophrenia (clinicaltrials.gov) - Dec 20, 2024
P2, N=391, Completed, Sponsor: Cerevel Therapeutics, LLC
Recruiting --> Active, not recruiting Active, not recruiting --> Completed
- || icalcaprant (CVL-354) / AbbVie
New P1 trial, Adverse events: A Single Dose Study to Assess Adverse Events and How Oral Icalcaprant Moves Through the Body in Healthy Adult Japanese and Han Chinese Participants (clinicaltrials.gov) - Dec 9, 2024
P1, N=16, Recruiting, Sponsor: AbbVie
- || icalcaprant (CVL-354) / AbbVie
New P1 trial: 529 DDI ITZ: A Study to Assess Change in How Oral Icalcaprant With Itraconazole Moves Through the Body in Healthy Adult Participants (clinicaltrials.gov) - Dec 9, 2024
P1, N=12, Recruiting, Sponsor: AbbVie
- ||||||| tavapadon (CVL-751) / AbbVie
Trial completion: TEMPO-2: Flexible-Dose Trial in Early Parkinson's Disease (PD) (clinicaltrials.gov) - Nov 1, 2024
P3, N=304, Completed, Sponsor: Cerevel Therapeutics, LLC
Active, not recruiting --> Completed Active, not recruiting --> Completed
- ||||| tavapadon (CVL-751) / AbbVie
Enrollment closed: TEMPO-4: Open-label Trial in Parkinson's Disease (PD) (clinicaltrials.gov) - Oct 31, 2024
P3, N=992, Active, not recruiting, Sponsor: Cerevel Therapeutics, LLC
Active, not recruiting --> Completed Enrolling by invitation --> Active, not recruiting
- || KRM-81 / RespireRx, BAER-101 / AstraZeneca, Fortress, darigabat (CVL-865) / AbbVie
Review, Journal: Nonsedating anxiolytics. (Pubmed Central) - Oct 27, 2024
This has rekindled the interest in the GABAA-receptor (GABAAR) positive allosteric modulator (PAM) compounds, which have a long history in treatment of anxiety beginning with diazepam, chlordiazepoxide, and alprazolam...Advances in molecular biology gave birth to a host of subtype selective GABAAR-PAMs which suffered from signs of sedation and motor impairment and only three compounds progressed to proof-of-concept studies (TPA-023, AZD7325 and PF-06372865)...In preclinical studies KRM-II-81 produced anxiolytic-like effects but with minimal sedation, respiratory depression, and abuse liability. Thus, KRM-II-81 is a newly discovered, non- BZD anxiolytic compound, which targets a selective population of GABAAR for improved therapeutic gain and reduced side effects.
- tavapadon (CVL-751) / AbbVie
Efficacy and Safety of Tavapadon, an Orally Administered, Once-Daily, Selective D1/D5 Partial Dopamine Agonist, Adjunctive to Levodopa for Treatment of Parkinson's Disease With Motor Fluctuations () - Sep 27, 2024 - Abstract #MDSCongress2024MDS_Congress_2067;
P3
Overall, 507 adults aged 40-80 years were enrolled. Participants receiving tavapadon (5
- | tavapadon (CVL-751) / AbbVie, SCH-23390 / Boehringer Ingelheim
Journal: Discovery and structure (Pubmed Central) - Sep 14, 2024
Participants receiving tavapadon (5 Previously, PF-06649751 (tavapadon), PF-2562 and PW0464 have been discovered as potent and selective G protein-biased D1/D5 receptor agonists with optimal pharmacokinetic properties...We observed that 5j (10
- || icalcaprant (CVL-354) / AbbVie
Trial completion: Positron Emission Tomography (PET) Trial to Evaluate Target Occupancy of CVL-354 at Kappa and Mu Opioid Receptors in Brain Following Oral Dosing (clinicaltrials.gov) - Aug 26, 2024
P1, N=19, Completed, Sponsor: Cerevel Therapeutics, LLC
Previously, PF-06649751 (tavapadon), PF-2562 and PW0464 have been discovered as potent and selective G protein-biased D1/D5 receptor agonists with optimal pharmacokinetic properties...We observed that 5j (10 Recruiting --> Completed
- ||| emraclidine (CVL-231) / AbbVie
Enrollment closed: A Trial of 10 and 30 mg Doses of CVL-231 (Emraclidine) in Participants With Schizophrenia (clinicaltrials.gov) - Aug 22, 2024
P2, N=372, Active, not recruiting, Sponsor: Cerevel Therapeutics, LLC
Recruiting --> Completed Recruiting --> Active, not recruiting
- ||| emraclidine (CVL-231) / AbbVie
Enrollment closed: A Trial of 15 and 30 mg Doses of CVL-231 (Emraclidine) in Participants With Schizophrenia (clinicaltrials.gov) - Aug 1, 2024
P2, N=372, Active, not recruiting, Sponsor: Cerevel Therapeutics, LLC
Recruiting --> Active, not recruiting Recruiting --> Active, not recruiting
- || darigabat (CVL-865) / Cerevel Therap
Trial completion: CVL-865-HV-1004: A Trial to Assess the Absorption, Metabolism, Excretion, and Mass Balance of [14C]-Darigabat After a Single Oral Dose in Healthy Male Participants (clinicaltrials.gov) - Jul 30, 2024
P1, N=8, Completed, Sponsor: Cerevel Therapeutics, LLC
Recruiting --> Active, not recruiting Recruiting --> Completed
- ||||||| tavapadon (CVL-751) / AbbVie
Trial completion, Trial completion date: TEMPO-1: Fixed-Dose Trial in Early Parkinson's Disease (PD) (clinicaltrials.gov) - Jul 29, 2024
P3, N=522, Completed, Sponsor: Cerevel Therapeutics, LLC
Recruiting --> Completed Active, not recruiting --> Completed | Trial completion date: Oct 2024 --> Jun 2024
- || emraclidine (CVL-231) / Cerevel Therap
Trial completion: A Trial to Evaluate the Effect of Esomeprazole on the Pharmacokinetics of Emraclidine in Healthy Adult Participants (clinicaltrials.gov) - Jul 24, 2024
P1, N=20, Completed, Sponsor: Cerevel Therapeutics, LLC
Active, not recruiting --> Completed | Trial completion date: Oct 2024 --> Jun 2024 Not yet recruiting --> Completed
- ||| darigabat (CVL-865) / AbbVie
Trial completion: A Trial of the Efficacy and Safety of CVL-865 as Adjunctive Therapy in the Treatment of Focal Onset Seizures (clinicaltrials.gov) - Jul 9, 2024
P2, N=154, Completed, Sponsor: Cerevel Therapeutics, LLC
Not yet recruiting --> Completed Active, not recruiting --> Completed
- || darigabat (CVL-865) / Cerevel Therap
Enrollment open: CVL-865-HV-1004: A Trial to Assess the Absorption, Metabolism, Excretion, and Mass Balance of [14C]-Darigabat After a Single Oral Dose in Healthy Male Participants (clinicaltrials.gov) - Jun 25, 2024
P1, N=8, Recruiting, Sponsor: Cerevel Therapeutics, LLC
Active, not recruiting --> Completed Not yet recruiting --> Recruiting
- | emraclidine (CVL-231) / Cerevel Therap
Journal: Design and Synthesis of Clinical Candidate PF-06852231 (CVL-231): A Brain Penetrant, Selective, Positive Allosteric Modulator of the M4 Muscarinic Acetylcholine Receptor. (Pubmed Central) - Jun 18, 2024
A major challenge in capitalizing on this allosteric site to date has been achieving a balance of suitable potency and brain penetration. Herein, we describe the design of a brain penetrant series of M4 selective positive allosteric modulators (PAMs), ultimately culminating in the identification of 21 (PF-06852231, now CVL-231/emraclidine), which is under active clinical development as a novel mechanism and approach for the treatment of schizophrenia.
- || darigabat (CVL-865) / AbbVie
Enrollment closed: An Open-label Extension Trial of CVL-865 as Adjunctive Therapy in the Treatment of Focal Onset Seizures (clinicaltrials.gov) - Jun 13, 2024
P2, N=105, Active, not recruiting, Sponsor: Cerevel Therapeutics, LLC
Herein, we describe the design of a brain penetrant series of M4 selective positive allosteric modulators (PAMs), ultimately culminating in the identification of 21 (PF-06852231, now CVL-231/emraclidine), which is under active clinical development as a novel mechanism and approach for the treatment of schizophrenia. Enrolling by invitation --> Active, not recruiting
- || darigabat (CVL-865) / Cerevel Therap
New P1 trial: CVL-865-HV-1004: A Trial to Assess the Absorption, Metabolism, Excretion, and Mass Balance of [14C]-Darigabat After a Single Oral Dose in Healthy Male Participants (clinicaltrials.gov) - May 29, 2024
P1, N=8, Not yet recruiting, Sponsor: Cerevel Therapeutics, LLC
- || darigabat (CVL-865) / AbbVie
Enrollment closed: A Trial of the Efficacy and Safety of CVL-865 as Adjunctive Therapy in the Treatment of Focal Onset Seizures (clinicaltrials.gov) - May 15, 2024
P2, N=154, Active, not recruiting, Sponsor: Cerevel Therapeutics, LLC
Enrolling by invitation --> Active, not recruiting Recruiting --> Active, not recruiting
- || PF-06412562 / Pfizer, AbbVie
Enrollment closed, Trial primary completion date: A Translational and Neurocomputational Evaluation of a Dopamine Receptor 1 Partial Agonist for Schizophrenia (clinicaltrials.gov) - May 7, 2024
P1/2, N=120, Active, not recruiting, Sponsor: Yale University
Recruiting --> Active, not recruiting Recruiting --> Active, not recruiting | Trial primary completion date: Sep 2024 --> Mar 2024
- || emraclidine (CVL-231) / Cerevel Therap
Trial completion: A Study to Assess Mass Balance, Pharmacokinetics, Metabolism, and Excretion of Emraclidine in Healthy Adult Male Participants (clinicaltrials.gov) - May 2, 2024
P1, N=8, Completed, Sponsor: Cerevel Therapeutics, LLC
Recruiting --> Active, not recruiting | Trial primary completion date: Sep 2024 --> Mar 2024 Recruiting --> Completed