Publications
Discover some of the most recent publications from the latest advances in neuroscience at Cerevel.
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Disclaimer: Our scientific content is evidence-based, scientifically balanced, and non-promotional. It undergoes rigorous internal medical review and is updated regularly to reflect new information.
Publications
August, 2023
Treatment Patterns and Healthcare Resource Use in Medicare Beneficiaries with Parkinson’s Disease
Objective: To assess treatment patterns, healthcare resource utilization (HRU), and costs associated with PD symptoms and treatment-related adverse events (AEs) among Medicare beneficiaries in the United States.
July, 2023
Medication Experiences of People with Parkinson’s Disease
Objective: To better understand experiences with medications from the perspective of people with PD.
July, 2023
Dopamine agonists in Parkinson’s disease: Impact of D1-like or D2-like dopamine receptor subtype selectivity and avenues for future treatment
Background: Dopamine agonists (DAs) have demonstrated efficacy for the treatment of Parkinson’s disease (PD) but are limited by adverse effects (AEs). DAs can vary considerably in their receptor subtype selectivity and affinity, chemical composition, receptor occupancy, and intrinsic activity on the receptor.
June, 2023
Evaluation of Darigabat QTc Prolongation in Healthy Volunteers: a Concentration-QTcF Analysis
Evaluation of Darigabat QTc Prolongation in Healthy Volunteers: a Concentration-QTcF Analysis
May, 2023
Quantifying the tolerability of antipsychotic treatment-related side effects in schizophrenia: a survey study of patients and caregiver proxies
Objective: To quantify tolerance for side effects associated with antipsychotics, as reported directly by patients and by caregiver proxy respondents.
May, 2023
Dopamine D1 Agonists: First Potential Treatment for Late-Stage Parkinson’s Disease
Background: Current pharmacotherapy has limited efficacy and/or intolerable side effects in late-stage Parkinson’s disease (LsPD) patients whose daily life depends primarily on caregivers and palliative care. Clinical metrics inadequately gauge efficacy in LsPD patients.
April, 2023
Darigabat Reduces Acute Panic and Fear Symptoms Induced by CO2 Inhalation in Healthy Participants
Objective: The objective of the current trial was to characterize the anxiolytic effect of darigabat in a CO2 inhalation translational model of panic and fear in healthy participants.
April, 2023
Impact of the Highly Selective D1-Like Partial Dopamine Agonist Tavapadon on Daytime Sleepiness: Evidence From a Phase 2 Clinical Trial
Objective: To report daytime sleepiness data from the phase 2 clinical trial of tavapadon in participants with early early-stage Parkinson’s disease (PD) utilizing the Epworth Sleepiness Scale (ESS).
April, 2023
Perspectives on Parkinson’s Disease Medications: A Qualitative Study of People With Parkinson’s Disease
Objective: To explore the thoughts, beliefs, and expectations of people with Parkinson’s disease ( PwPD ) regarding their PD medications.
April, 2023
Work Loss and Direct and Indirect Costs Associated with Parkinson’s Disease
Purpose: To examine work loss and indirect costs during the three-year periods prior to and following initial diagnosis of Parkinson’s disease (PD) in patients and in spouses of PD patients, as well as direct costs of healthcare.
March, 2023
Rationale and Development of Tavapadon, a D1/D5-Selective Partial Dopamine Agonist for the Treatment of Parkinson’s Disease
Objective: This review summarizes currently available evidence of tavapadon’s therapeutic potential for the treatment of early through advanced PD.
December, 2022
CVL-354, a novel, brain penetrant and selective kappa opioid receptor antagonist
Objective: To characterize in vitro and in vivo binding, selectivity, and functional activity of CVL 354 a novel KOR antagonist.
December, 2022
A novel, short-acting kappa opioid receptor antagonist blocks the analgesic effects of U50,488 and attenuates symptoms of spontaneous oxycodone withdrawal in rats
Objective: Determine if CVL-354 is a short-acting (<24 hours) kappa opioid receptor antagonist.
December, 2022
Evaluation of Kappa and Mu Opioid Receptor Occupancy by CVL-354 Using PET in Nonhuman Primates
Objective: The objective of this study was to measure the RO of varying doses of CVL-354 at kappa and mu receptors in nonhuman primates using radiotracers [11C]LY27950502,3 and [11C]carfentanil ([11C]CFN), respectively
December, 2022
Evaluation of Selective Muscarinic M4 Agonists on Cortical Oscillations: a Sleep-EEG Study in Rats
Background: A primary role for the M4 muscarinic acetylcholine receptor (M4 mAChR) is to function as an inhibitory autoreceptor
December, 2022
Dopamine agonist monotherapy utilization in patients with Parkinson’s disease
Objective: To characterize patients with Parkinson’s disease (PD) who initiated dopamine agonist (DA) monotherapy, describe medication utilization and provider types, and estimate medication adherence and discontinuation rates.
December, 2022
Emraclidine, a novel positive allosteric modulator of cholinergic M4 receptors, for the treatment of schizophrenia: a two-part, randomised, double-blind, placebo-controlled, phase 1b trial
Background: Emraclidine is a novel, brain-penetrant, highly selective M4 receptor positive allosteric modulator in development for the treatment of schizophrenia.
November, 2022
Binding and Signal Profiling of Full and Partial M4 Agonists
Objective: The aim of this study was to understand the agonism and the binding profile of M4 ligands with differentdegrees of intrinsic activities by using multiple probes, evaluating different signaling events/pathways, and by performing experiments at steady state, as well as at multiple time points.
November, 2022
Pronounced antiseizure activity of the subtype-selective GABAA positive allosteric modulator darigabat in a mouse model of drug-resistant focal epilepsy
Aim: Darigabat is an α2/3/5 subunit-selective positive allosteric modulator of GABAAreceptors that has demonstrated broad-spectrum activity in several preclinical models of epilepsy as well as in a clinical photoepilepsy trial.
November, 2022
Efficacy of Subtype-Selective, Full vs Partial M4 Muscarinic Receptor Agonists in Modulating Amphetamine-Induced Brain Activity Assessed by Functional MRI (fMRI) in Rats
Objective: To investigate the effects of systemic subcutaneous (SC) administration of 2 different test compounds (TC) – a full (CV-0000042) compared with a partial (CV-0000071) M4 receptor agonist – at 2 doses each on amphetamine-induced brain activity in anesthetized Sprague-Dawley rats (Crl:CD(SD)) using relative cerebral blood volume (rCBV) functional MRI (fMRI) readout
November, 2022
Efficacy of CV-0000042, a Novel M4 Receptor Full Agonist,and CV-0000071, a Novel M4 Receptor Partial Agonist, in Preclinical In Vivo Models
Objective: To evaluate preclinical antipsychotic properties of M4 agonism while minimizing offtarget side effects using the novel M4 full agonist CV-0000042 and novel M4 partial agonist CV-0000071.
October, 2022
Assessment of Extrapyramidal Symptoms in a Medicaid Population with Schizophrenia Newly Prescribed Second Generation Antipsychotic Medications
Objective: To describe the 1 year incidence of EPS in patients with schizophrenia newly initiated on an SGA medication within a Medicaid population
October, 2022
Considerations for determining the efficacy of new antiseizure medications in children age 1 month to younger than 2 years
Objective: Drug treatment for children with epilepsy should, ideally, be governed by evidence from adequate and well-controlled clinical studies.
June, 2022
PET mapping of receptor occupancy using joint direct parametric reconstruction: in-vivo studies
Background: Receptor occupancy (RO) studies using PET play a critical role in the development of drugs targeting the central nervous system to quantify target engagement, assess drug performance [1]
May, 2022
Darigabat Reduces Acute Panic and Fear Symptoms Induced by CO2 Inhalation in Healthy Participants
The objective of the current study was to characterize the anxiolytic effect of darigabat in a CO2 inhalation model of panic and fear in healthy volunteers
May, 2022
Setting the TEMPO: A Phase 3 Program to Investigate Tavapadon, a Selective D1/D5 Partial Agonist, for Parkinson’s Disease
Objective: To describe the design of the phase 3 TEMPO program that will evaluate the efficacy, safety, and tolerability of once-daily (QD) tavapadon in early-stage and advanced Parkinson’s disease (PD).
April, 2022
Ensuring the Continuity of Data Collection in a Focal Epilepsy Clinical Trial During the COVID-19 Pandemic
Learn MoreApril, 2022
CVL-231 as a Novel Positive Allosteric Modulator Targeting M4 Muscarinic Receptors: Results From a Phase 1b Trial in Patients With Schizophrenia
Objective: To describe the safety, tolerability, and pharmacodynamics (PD) of emraclidine 30 mg once daily (QD) and emraclidine 20 mg twice daily (BID) in patients with acute schizophrenia.
April, 2022
Levodopa and Dopamine Agonist Medication Utilization among Patients with Parkinson’s Disease Enrolled in Commercial and Medicare Advantage Part D Health Plans
Objective: Perform an updated characterization of medication utilization among PD patients prescribed levodopa or dopamine agonist treatments. Estimate predictors of medication discontinuation among patients prescribed levodopa and dopamine agonist treatments.
April, 2022
Darigabat: pronounced antiepileptic activity in the mesial temporal lobe mouse model of drug- resistant focal epilepsy
Learn MoreApril, 2022
CVL‑231 as a novel positive allosteric modulator targeting M4 muscarinic receptors: results from a phase 1b trial in patients with schizophrenia. 2022 Congress of the Schizophrenia International Research Society
Learn MoreApril, 2022
Pharmacokinetics, Pharmacodynamics, and Safety of the Highly Selective Dopamine D1/D5 Agonist Tavapadon: Summary of Early Phase Clinical Studies
Objective: To describe the pharmacokinetic (PK), pharmacodynamic, and safety data from early phase clinical studies of tavapadon.
January, 2022
Levodopa treatment patterns in Parkinson’s disease: A retrospective chart review
Background: Medication regimens for Parkinson’s disease (PD) may change as the disease progresses, symptoms fluctuate, or medication-related adverse events occur. This study evaluated treatment trends by observation year for patients initially receiving monotherapy with levodopa and a peripheral dopa decarboxylase inhibitor (PDDI).
December, 2021
Neuroimaging of M4 Muscarinic Acetylcholine Receptors Using [11c]Mk-6884 In Rhesus Macaques
Objective: Characterize PET imaging and quantitative performance of [11C]MK-6884 using arterial input function-based and reference tissue-based kinetic modelling methods.
December, 2021
CVL-231 as a Novel Positive Allosteric Modulator of Cholinergic M4 Receptors for the Treatmentof Schizophrenia: Results From an Early Proof-of-Concept Study in Patients With Schizophrenia
Objective: To assess the safety, tolerability, pharmacokinetics (PK), and pharmacodynamics of CVL-231 30 mg once daily (QD) and 20 mg twice daily (BID) in patients with schizophrenia who are experiencing acute exacerbation of psychosis.
December, 2021
Natural history and patterns of treatment change in Parkinson’s disease: A retrospective chart review
Background: Parkinson’s disease (PD) management seeks to balance the benefits and harms of current medications and evolves as the disease progresses. The natural history of PD and associated patterns of treatment change were analyzed to identify unmet needs in treatment of PD symptoms.
December, 2021
Evaluation of M4 Muscarinic Receptor Occupancy by CVL-231 Using [11C]MK-6884 PET in Nonhuman Primates
Objective: Using [11C]MK-6884, an M4 positive allosteric modulator radioligand, this study evaluated M4 receptor occupancy (RO) of CVL-231 in the striatum of nonhuman primates as a function of CVL-231 dose and plasma concentration.
December, 2021
CVL‑231 as a novel positive allosteric modulator of cholinergic M4 receptors for the treatment of schizophrenia: results from an early proof‑of‑concept study in patients with schizophrenia. 60th Annual Meeting of American College of Neuropsychopharmacology
Learn MoreNovember, 2021
Establishing Signature Profile of Muscarinic M4 Selective Molecules by Evaluating Their Orthosteric/Allosteric Binding Properties and Biased Signaling
Learn MoreSeptember, 2021
Dopamine D1 Receptor Agonist PET Tracer Development: Assessment in Nonhuman Primates
Background: Non-catechol-based high-affinity selective dopamine D1 receptor (D1R) agonists were recently described, and candidate PET ligands were selected on the basis of favorable properties.
August, 2021
CVL‑865: The Journey to REALIZE. 2020 Epilepsy Foundation Pipeline Virtual Conference
Learn MoreJuly, 2021
Safety, Tolerability, and Pharmacokinetics of Multiple Repeated Oral Doses of the α2/3/5-Subtype Selective GABAA -Positive Allosteric Modulator PF-06372865 in Healthy Volunteers
Background: Multiple-dose pharmacokinetics (PK) and safety were investigated in this phase 1 study of PF-06372865, a positive allosteric modulator of α2/3/5 subunit-containing γ-aminobutyric acid A receptors (NCT03351751).
June, 2021
Parkinson disease among patients treated for benign prostatic hyperplasia with α1 adrenergic receptor antagonists
Background: Recently the α1 adrenergic receptor antagonist terazosin was shown to activate PGK1, a possible target for the mitochondrial deficits in Parkinson disease related to its function as the initial enzyme in ATP synthesis during glycolysis.
April, 2021
A Novel Positive Allosteric Modulator of the Cholinergic M4 Receptor for the Treatment of Schizophrenia
Learn MoreNovember, 2020
Progress report on new antiepileptic drugs: a summary of the Fifteenth Eilat Conference on New Antiepileptic Drugs and Devices (EILAT XV). II. Drugs in more advanced clinical development. Epilepsia
The Fifteenth Eilat Conference on New Antiepileptic Drugs and Devices (EILAT XV) was held as a fully virtual conference from July 27 to July 30, 2020 for the sessions on drugs…
September, 2020
Claims Data Analysis of Parkinson’s Disease Medication Utilization
Objective: Characterize prominent medication utilization patterns among patients with Parkinson’s disease (PD).
September, 2020
An analysis of Parkinson’s disease medication treatment patterns among Medicaid patients.
Objective: To describe patient demographic and medication utilization patterns within a state Medicaid program for patients diagnosed with Parkinson’s disease(PD).
September, 2020
Claims data analysis of Parkinson’s disease medication utilization. MDS‑International Parkinson and Movement Disorder Society Virtual Congress 2020
Objective: Characterize prominent medication utilization patterns among patients with Parkinson’s disease (PD).
April, 2020
Dopaminergic D1 Receptor Stimulation Affects Effort and Risk Preferences
Background: Activation of D1 receptors has been related to successful goal-directed behavior, but it remains unclear whether D1 receptor activation causally tips the balance of weighing costs and benefits in humans.
March, 2020
PF-06649751 efficacy and safety in early Parkinson’s disease: a randomized, placebo-controlled trial
Background: PF-06649751 is a novel, oral, non-catechol-based, D1/D5 dopamine receptor partial agonist under investigation for the treatment of motor symptoms associated with Parkinson’s disease.
February, 2020
D1 Agonist Improved Movement of Parkinsonian Nonhuman Primates with Limited Dyskinesia Side Effects
Background: Parkinson’s disease is a progressive neurodegenerative disease characterized by striatal dopaminergic loss. L-DOPA treatment replaces lost dopamine and enables motor function; however, eventually, fluctuating efficacy and side effects associated with its use become challenging for many patients.
September, 2019
Efficacy, Safety and Tolerability of Tavapadon in Subjects With Early Stage Parkinson’s Disease
Objective: To evaluate the efficacy and safety of tavapadon (formerly known as PF-06649751) in subjects with early stage Parkinson’s disease.
September, 2019
Utility of the double‑blind crossover design protocol for proof‑of‑principle photosensitivity model assessment of PF‑06372865. 2019 International Society for CNS Clinical Trials and Methodology
Learn MoreSeptember, 2019
Analgesic potential of PF-06372865, an α2/α3/α5 subtype-selective GABAA partial agonist, in humans
Background: This study investigated the analgesic effects of two doses (15 and 65 mg) of PF-06372865, a novel α2/α3/α5 gamma-aminobutyric acid A (GABAA) subunit selective partial positive allosteric modulator (PAM), compared with placebo and pregabalin (300 mg) as a positive control.
April, 2019
Design and Identification of a Novel, Functionally Subtype Selective GABAA Positive Allosteric Modulator (PF-06372865)
Background: The design, optimization, and evaluation of a series of novel imidazopyridazine-based subtype-selective positive allosteric modulators (PAMs) for the GABAA ligand-gated ion channel are described.
April, 2019
Photosensitive epilepsy: Robust clinical efficacy of a selective GABA potentiator
Objective: The objective of this phase 2a study was to assess the activity of PF-06372865, a positive allosteric modulator (PAM) of α2/3/5 subunit-containing GABAAreceptors with minimal activity at α1-containing receptors, which are believed to mediate many of the adverse events associated with benzodiazepines, in the epilepsy photosensitivity model as a proof-of-principle of efficacy.
February, 2019
Pronounced antiepileptic activity of the subtype-selective GABAA -positive allosteric modulator PF-06372865 in the GAERS absence epilepsy model
Objective: Antiepileptic drugs that modulate GABA have the potential to aggravate or improve the symptoms of absence epilepsy.
July, 2018
Phase 1 Parkinson’s Disease Studies Show the Dopamine D1/D5 Agonist PF-06649751 is Safe and Well Tolerated
Background: There is a need for new therapies in Parkinson’s disease that may help to address known limitations of current options.