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20 Diseases |  |
0 Trials |
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0 Trials |  |
45 News |  |
- | PF-02545920 / Pfizer
Journal: Phosphodiesterase 10A inhibitor PF-2545920 as a prospective agent for the clinical promotion of sperm motility. (Pubmed Central) - Jul 29, 2024
PF-2545920 also increased mitochondrial membrane potential (P < 0.001) and altered intracellular calcium (P < 0.05) in a dose-dependent manner, including increasing sperm hyaluronic acid penetrating ability (P < 0.05). Therefore, PF-2545920 might be an excellent choice for stimulating the sperm motility.
- | PF-02545920 / Pfizer, MCI-030 / ChemomAb
Journal: Phosphodiesterase 10A (PDE10A) as a novel target to suppress β-catenin and RAS signaling in epithelial ovarian cancer. (Pubmed Central) - Nov 4, 2022
Using small molecule inhibitors, Pf-2545920 and a novel NSAID-derived PDE10A inhibitor, MCI-030, we show that PDE10A inhibition leads to decreased ovarian cancer cell growth and induces cell cycle arrest and apoptosis...We also demonstrate that PDE10A inhibition leads to decreased Wnt-induced β-catenin nuclear translocation, as well as decreased EGF-mediated activation of RAS/MAPK and AKT pathways in ovarian cancer cells. These findings implicate PDE10A as novel target for ovarian cancer chemoprevention and treatment.
- | PF-02545920 / Pfizer
Preclinical, Journal: The Potent PDE10A Inhibitor MP-10 (PF-2545920) Suppresses Microglial Activation in LPS-Induced Neuroinflammation and MPTP-Induced Parkinson's Disease Mouse Models. (Pubmed Central) - Dec 16, 2021
These data collectively suggest that MP-10 may have therapeutic potential in PD and other neuroinflammatory disorders. Graphical Abstract.
- | PF-02545920 / Pfizer
Journal: Suppression of Proliferation of Human Glioblastoma Cells by Combined Phosphodiesterase and Multidrug Resistance-Associated Protein 1 Inhibition. (Pubmed Central) - Oct 31, 2021
In particular, a combination comprising the MRP1 inhibitor reversan, PF-2545920 and MY-5445, all at low micromolar concentrations, afforded nearly complete inhibition of glioblastoma cell growth. Thus, the potent suppression of glioblastoma cell viability may be achieved by combining MRP1 inhibitors with PDE inhibitors at a lower toxicity than that of the standard chemotherapeutic agents, thereby providing a new combination therapy for this challenging malignancy.
- fluorouracil topical / Generic mfg.
[VIRTUAL] Metabolic Drug Survey Highlights Cancer Cell Dependencies and Vulnerabilities (Poster Hall (Virtual Meeting)) - Nov 5, 2020 - Abstract #ASH2020ASH_4172;
CLIMET allows for identification of metabolic susceptibilities, grouping of cancer cells based on metabolic dependencies, as well as understanding of context-dependent mechanism of action of drugs. Functional drug testing may provide a rapid and robust approach to identify metabolic vulnerabilities, responding patients, and prioritize compounds for clinical evaluation as illustrated with our study.
- | PF-02545920 / Pfizer, PF-05180999 / Pfizer, PF-04447943 / Pfizer
Biomarker, Preclinical, Journal: Effect of phosphodiesterase (1B, 2A, 9A and 10A) inhibitors on central nervous system cyclic nucleotide levels of rats and mice. (Pubmed Central) - Jun 5, 2020
Male Sprague Dawley (Crl:CD [SD]) rats were dosed subcutaneously (sc) with a PDE1B inhibitor (DNS-0056), a PDE2A inhibitor (PF-05180999), a PDE9A inhibitor (PF-4447943), and a PDE10A inhibitor (MP10), each at a single dose of 10 or 30 mg/kg, or concomitantly with all 4 inhibitors at 10 mg/kg each...The drug exposures after concomitant treatment were also higher than in the individual inhibitor-treated animals. cGMP enhancement could be due to synergistic effects, though an additive effect of the combined inhibitor concentrations may also contribute.
- | risperidone / Generic mfg., Egis
Journal, Monotherapy: Phosphodiesterase 10A Inhibitor Monotherapy Is Not an Effective Treatment of Acute Schizophrenia. (Pubmed Central) - Apr 22, 2020
Neither dose of PF-02545920 was superior to placebo for the primary and most secondary end points. This indicates that PDE10A inhibition does not produce an antipsychotic effect in patients with acute exacerbation of schizophrenia.
- | PF-02545920 / Pfizer
Journal: A Proof-of-Concept Study Evaluating the Phosphodiesterase 10A Inhibitor PF-02545920 in the Adjunctive Treatment of Suboptimally Controlled Symptoms of Schizophrenia. (Pubmed Central) - Feb 22, 2020
This indicates that PDE10A inhibition does not produce an antipsychotic effect in patients with acute exacerbation of schizophrenia. Current data and results of a prior monotherapy study in which PF-02545920 failed to differentiate from placebo refute the hypothesis that PDE10A inhibitors have use as antipsychotic agents for schizophrenia.
- | PF-02545920 / Pfizer
Trial termination: Open Label Extension Study To Investigate Long Term Safety, Tolerability And Efficacy Of Pf-02545920 In Subjects With Huntington's Disease Who Completed Study A8241021 (clinicaltrials.gov) - Mar 13, 2017
P2, N=188, Terminated, Sponsor: Pfizer
Recruiting --> Terminated; Study terminated on 15DEC2016 due to study A8241021 showing no significant difference on primary endpoint between PF-02545920 & placebo. No safety concerns.
- || PF-02545920 / Pfizer
Trial primary completion date: Open Label Extension Study To Investigate Long Term Safety, Tolerability And Efficacy Of Pf-02545920 In Subjects With Huntington's Disease Who Completed Study A8241021 (clinicaltrials.gov) - Feb 2, 2017
P2, N=230, Recruiting, Sponsor: Pfizer
No safety concerns. Trial primary completion date: Sep 2017 --> Feb 2017
- |||| PF-02545920 / Pfizer
Trial completion: Randomized, Placebo Controlled Study Of The Efficacy And Safety Of PF-02545920 In Subjects With Huntington's Disease (clinicaltrials.gov) - Oct 14, 2016
P2, N=272, Completed, Sponsor: Pfizer
Trial primary completion date: Sep 2017 --> Feb 2017 Recruiting --> Completed
- || PF-02545920 / Pfizer
Trial primary completion date: Open Label Extension Study To Investigate Long Term Safety, Tolerability And Efficacy Of Pf-02545920 In Subjects With Huntington's Disease Who Completed Study A8241021 (clinicaltrials.gov) - Feb 9, 2016
P2, N=260, Recruiting, Sponsor: Pfizer
Recruiting --> Completed Trial primary completion date: Jun 2017 --> Sep 2017
- || PF-02545920 / Pfizer
Trial primary completion date: Randomized, Placebo Controlled Study Of The Efficacy And Safety Of PF-02545920 In Subjects With Huntington's Disease (clinicaltrials.gov) - Sep 30, 2015
P2, N=260, Recruiting, Sponsor: Pfizer
Trial primary completion date: Jun 2017 --> Sep 2017 Trial primary completion date: Jun 2016 --> Oct 2016
- |||| PF-02545920 / Pfizer
Enrollment open: Open Label Extension Study To Investigate Long Term Safety, Tolerability And Efficacy Of Pf-02545920 In Subjects With Huntington's Disease Who Completed Study A8241021 (clinicaltrials.gov) - Mar 18, 2015
P2, N=260, Recruiting, Sponsor: Pfizer
Trial primary completion date: Jun 2016 --> Oct 2016 Not yet recruiting --> Recruiting
- | PF-02545920 / Pfizer
Trial completion, Enrollment change, Trial primary completion date: Study Evaluating The Safety, Tolerability And Brain Function Of 2 Doses Of PF-0254920 In Subjects With Early Huntington's Disease (clinicaltrials.gov) - Feb 19, 2015
P2, N=37, Completed, Sponsor: Pfizer
Not yet recruiting --> Recruiting Recruiting --> Completed | N=56 --> 37 | Trial primary completion date: Nov 2015 --> Jan 2015
- ||||| PF-02545920 / Pfizer
New P2 trial: Open Label Extension Study To Investigate Long Term Safety, Tolerability And Efficacy Of Pf-02545920 In Subjects With Huntington's Disease Who Completed Study A8241021 (clinicaltrials.gov) - Jan 22, 2015
P2, N=260, Not yet recruiting, Sponsor: Pfizer
- PF-02545920 / Pfizer
Trial completion, Enrollment change: A Study To Evaluate The PDE10 Enzyme Occupancy Following A Single Dose Of PF-02545920 In Healthy Male Volunteers (clinicaltrials.gov) - Nov 10, 2014
P1, N=9, Completed, Sponsor: Pfizer
Recruiting --> Completed | N=56 --> 37 | Trial primary completion date: Nov 2015 --> Jan 2015 Recruiting --> Completed | N=15 --> 9
- | PF-02545920 / Pfizer
Trial termination, Trial primary completion date: An Outpatient Study Of The Efficacy, Safety, And Tolerability Of PF-02545920 In The Adjunctive Treatment Of Sub-Optimally Controlled Symptoms of Schizophrenia (clinicaltrials.gov) - Oct 10, 2014
P2, N=239, Terminated, Sponsor: Pfizer
Recruiting --> Terminated | Trial primary completion date: Nov 2014 --> Aug 2014; A pre-planned interim analysis indicated the trial was unlikely to meet the pre-specified efficacy criteria. The decision was not based on any safety concerns.
- PF-02545920 / Pfizer
Enrollment change: A Study To Evaluate The PDE10 Enzyme Occupancy Following A Single Dose Of PF-02545920 In Healthy Male Volunteers (clinicaltrials.gov) - Oct 10, 2014
P1, N=15, Recruiting, Sponsor: Pfizer
The decision was not based on any safety concerns. N=12 --> 15
- |||| PF-02545920 / Pfizer
Enrollment open, Trial primary completion date: Randomized, Placebo Controlled Study Of The Efficacy And Safety Of PF-02545920 In Subjects With Huntington's Disease (clinicaltrials.gov) - Oct 4, 2014
P2, N=260, Recruiting, Sponsor: Pfizer
N=12 --> 15 Not yet recruiting --> Recruiting | Trial primary completion date: Feb 2016 --> Jun 2016
- ||||| PF-02545920 / Pfizer
New P2 trial: Randomized, Placebo Controlled Study Of The Efficacy And Safety Of PF-02545920 In Subjects With Huntington's Disease (clinicaltrials.gov) - Jul 23, 2014
P2, N=260, Not yet recruiting, Sponsor: Pfizer
- PF-02545920 / Pfizer
Trial primary completion date: A Study To Evaluate The PDE10 Enzyme Occupancy Following A Single Dose Of PF-02545920 In Healthy Male Volunteers (clinicaltrials.gov) - Jul 6, 2014
P1, N=12, Recruiting, Sponsor: Pfizer
Not yet recruiting --> Recruiting | Trial primary completion date: Feb 2016 --> Jun 2016 Trial primary completion date: Jul 2014 --> Aug 2014
- || PF-02545920 / Pfizer
Trial primary completion date: An Outpatient Study Of The Efficacy, Safety, And Tolerability Of PF-02545920 In The Adjunctive Treatment Of Sub-Optimally Controlled Symptoms of Schizophrenia (clinicaltrials.gov) - Jun 19, 2014
P2, N=249, Recruiting, Sponsor: Pfizer
Trial primary completion date: Jul 2014 --> Aug 2014 Trial primary completion date: Aug 2014 --> Nov 2014
- PF-02545920 / Pfizer
Trial completion date: A Study To Evaluate The PDE10 Enzyme Occupancy Following A Single Dose Of PF-02545920 In Healthy Male Volunteers (clinicaltrials.gov) - May 12, 2014
P1, N=12, Recruiting, Sponsor: Pfizer
Trial primary completion date: Aug 2014 --> Nov 2014 Trial completion date: Jul 2014 --> Aug 2014
- PF-02545920 / Pfizer
Trial initiation date: A Study To Evaluate The PDE10 Enzyme Occupancy Following A Single Dose Of PF-02545920 In Healthy Male Volunteers (clinicaltrials.gov) - Apr 14, 2014
P1, N=12, Recruiting, Sponsor: Pfizer
Trial completion date: Jul 2014 --> Aug 2014 Initiation date: Feb 2014 --> Mar 2014
- PF-02545920 / Pfizer
Enrollment open: A Study To Evaluate The PDE10 Enzyme Occupancy Following A Single Dose Of PF-02545920 In Healthy Male Volunteers (clinicaltrials.gov) - Apr 14, 2014
P1, N=12, Recruiting, Sponsor: Pfizer
Initiation date: Feb 2014 --> Mar 2014 Not yet recruiting --> Recruiting
- PF-02545920 / Pfizer
Trial termination: Effects Of PF-02545920 On Ketamine-Induced Abnormal Prefrontal Brain Response To Associative Learning In Healthy Subjects (clinicaltrials.gov) - Mar 18, 2014
P1, N=4, Terminated, Sponsor: Pfizer
Not yet recruiting --> Recruiting Completed --> Terminated; See termination reason in detailed description.
- | PF-02545920 / Pfizer
Trial completion: A Study To Examine The Safety, Tolerability And Pharmacokinetics Of PF-02545920 In Psychiatrically Stable Subjects With Schizophrenia (clinicaltrials.gov) - Nov 11, 2013
P1, N=37, Completed, Sponsor: Pfizer
Completed --> Terminated; See termination reason in detailed description. Active, not recruiting --> Completed
- |||| PF-02545920 / Pfizer
Enrollment open: An Outpatient Study Of The Efficacy, Safety, And Tolerability Of PF-02545920 In The Adjunctive Treatment Of Sub-Optimally Controlled Symptoms of Schizophrenia (clinicaltrials.gov) - Oct 29, 2013
P2, N=249, Recruiting, Sponsor: Pfizer
Active, not recruiting --> Completed Not yet recruiting --> Recruiting
- |||| PF-02545920 / Pfizer
Enrollment open: Study Evaluating The Safety, Tolerability And Brain Function Of 2 Doses Of PF-0254920 In Subjects With Early Huntington's Disease (clinicaltrials.gov) - Oct 10, 2013
P2, N=56, Recruiting, Sponsor: Pfizer
Not yet recruiting --> Recruiting Not yet recruiting --> Recruiting
- ||||| PF-02545920 / Pfizer
New P2 trial: An Outpatient Study Of The Efficacy, Safety, And Tolerability Of PF-02545920 In The Adjunctive Treatment Of Sub-Optimally Controlled Symptoms of Schizophrenia (clinicaltrials.gov) - Sep 9, 2013
P2, N=249, Recruiting, Sponsor: Pfizer
- | PF-02545920 / Pfizer
New P1 trial: A Study To Evaluate The PDE10 Enzyme Occupancy Following A Single Dose Of PF-02545920 In Healthy Male Volunteers (clinicaltrials.gov) - Aug 5, 2013
P1, N=12, Recruiting, Sponsor: Pfizer
- ||| PF-02545920 / Pfizer
Trial initiation date: Study Evaluating The Safety, Tolerability And Brain Function Of 2 Doses Of PF-0254920 In Subjects With Early Huntington's Disease (clinicaltrials.gov) - Jul 6, 2013
P2, N=56, Recruiting, Sponsor: Pfizer
Not yet recruiting --> Recruiting Initiation date: Jun 2013 --> Sep 2013
- | PF-02545920 / Pfizer
New P1 trial: A Study To Examine The Safety, Tolerability And Pharmacokinetics Of PF-02545920 In Psychiatrically Stable Subjects With Schizophrenia (clinicaltrials.gov) - Apr 9, 2013
P1, N=37, Completed, Sponsor: Pfizer
- ||||| PF-02545920 / Pfizer
New P2 trial: Study Evaluating The Safety, Tolerability And Brain Function Of 2 Doses Of PF-0254920 In Subjects With Early Huntington's Disease (clinicaltrials.gov) - Mar 5, 2013
P2, N=56, Recruiting, Sponsor: Pfizer
- PF-02545920 / Pfizer
Enrollment change: Effects Of PF-02545920 On Ketamine-Induced Abnormal Prefrontal Brain Response To Associative Learning In Healthy Subjects (clinicaltrials.gov) - Nov 26, 2012
P1, N=4, Terminated, Sponsor: Pfizer
Initiation date: Jun 2013 --> Sep 2013 N=20 --> 4
- PF-02545920 / Pfizer
Trial initiation date: Effects Of PF-02545920 On Ketamine-Induced Abnormal Prefrontal Brain Response To Associative Learning In Healthy Subjects (clinicaltrials.gov) - Apr 15, 2012
P1, N=4, Terminated, Sponsor: Pfizer
N=20 --> 4 Initiation date: Dec 2010 --> Apr 2011
- |||| PF-02545920 / Pfizer
Trial completion: An Inpatient Study Of The Efficacy, Safety, And Tolerability Of PF-02545920 In The Treatment Of Acute Exacerbation Of Schizophrenia (clinicaltrials.gov) - Apr 8, 2012
P2, N=259, Completed, Sponsor: Pfizer
Initiation date: Dec 2010 --> Apr 2011 Recruiting --> Completed
- | PF-02545920 / Pfizer
Trial completion, FDG PET: Evaluation Of Striatal Glucose Metabolism With Positron Emission Tomography Following PF-02545920 In Healthy Subjects (clinicaltrials.gov) - Nov 14, 2011
P1, N=34, Completed, Sponsor: Pfizer
Recruiting --> Completed Recruiting --> Completed