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28 News |  |
- | PF-04447943 / Pfizer
Preclinical, Journal: PDE9A Inhibition Improves Coronary Microvascular Rarefaction and Left Ventricular Diastolic Dysfunction in the ZSF1 Rat Model of HFpEF. (Pubmed Central) - Nov 13, 2024
Thus, in the ZSF1 rat model of human HFpEF, PDE9A inhibition improves coronary vascular rarefaction and LV diastolic dysfunction, demonstrating the usefulness of PDE9A inhibitors in ameliorating CMD and LV diastolic dysfunction through augmenting PRDX-dependent antioxidant mechanisms.
- | PF-04447943 / Pfizer
Preclinical, Journal: Phosphodiesterase 9A inhibition improves aging-related increase in pulmonary vascular resistance in mice. (Pubmed Central) - Aug 20, 2024
Aged mice were treated with the selective PDE9A inhibitor PF04447943 (1 mg/kg/day) through intraperitoneal injections for 10 days...Additionally, changes in PVR were measured in response to perfusion of the endothelium-dependent agonist bradykinin or to nitric oxide (NO) donor sodium nitroprusside (SNP)...These data demonstrate a development of LV diastolic dysfunction and increase in PVR in aged mice. We propose that inhibitors of PDE9A could represent a novel therapeutic approach to specifically prevent aging-related pulmonary dysfunction.
- || Review, Journal: A systematic review on drugs for synaptic plasticity in the treatment of dementia. (Pubmed Central) - Oct 19, 2022
This could suggest that research on these drugs is still preliminary. Of all, three studies reported promising results on Levetiracetam, Bryostatin 1 and Masitinib.
- | PF-04447943 / Pfizer, osoresnontrine (BI 409306) / Boehringer Ingelheim
Journal: Combined ligand-based and structure-based design of PDE 9A inhibitors against Alzheimer's disease. (Pubmed Central) - Oct 7, 2022
The hits were subjected to molecular dynamics (MD) studies, wherein they formed stable complexes with PDE9 protein and had ligand RMSDs within acceptable limits. The processes involved in the combined ligand and structure-based strategies.
- | sildenafil / Generic mfg., vardenafil / Generic mfg.
Journal: Research progress of phosphodiesterase inhibitors in inflammatory bowel disease treatment. (Pubmed Central) - Jan 12, 2022
In clinical trials, PDE4 inhibitor apremilast showed more therapeutic advantage than tetomilast. This article reviews the recent research progress of PDE inhibitors in treatment of inflammatory bowel disease.
- | PF-04447943 / Pfizer
Journal: PDE9 Inhibitor PF-04447943 Attenuates DSS-Induced Colitis by Suppressing Oxidative Stress, Inflammation, and Regulating T-Cell Polarization. (Pubmed Central) - May 11, 2021
Importantly, PF reversed imbalance in Treg/T helper 17 cells (Th17) cells ratio, possibly by regulating dendritic cells and Treg developmental process. In summary, this study shows the protective effect of a PDE9A inhibitor in ulcerative colitis by suppressing oxidative stress and inflammation as well as reversing the Treg/Th17 cells imbalance.
- | sildenafil / Generic mfg., PF-04447943 / Pfizer
Preclinical, Journal: Cyclic nucleotide signalling compartmentation by phosphodiesterases in cultured vascular smooth muscle cells. (Pubmed Central) - Sep 2, 2020
In summary, this study shows the protective effect of a PDE9A inhibitor in ulcerative colitis by suppressing oxidative stress and inflammation as well as reversing the Treg/Th17 cells imbalance. Our work underscores the distinct role of PDE1, PDE5 and PDE9 in locally regulating the [cAMP] and [cGMP] , in vascular smooth muscle cells, strengthening the concept of PDEs as key actors of cyclic nucleotide subcellular compartmentation.
- || Clinical, Review, Journal: Phosphodiesterase Inhibitors for Alzheimer's Disease: A Systematic Review of Clinical Trials and Epidemiology with a Mechanistic Rationale. (Pubmed Central) - Jul 28, 2020
PF-04447943 and BI 409,306 are ineffective...Deprenyl/selegiline trials show only short-term benefits...Now, propentofylline is used to treat canine cognitive dysfunction, which, like AD, involves age-associated wild-type Aβ deposition. Phosphodiesterase inhibitors may prevent and treat AD.
- || PF-04447943 / Pfizer
Biomarker, Clinical, P1 data, Journal: PF-04447943, a Phosphodiesterase 9A Inhibitor, in Stable Sickle Cell Disease Patients: A Phase Ib Randomized, Placebo-Controlled Study. (Pubmed Central) - Jul 5, 2020
PF-04447943 demonstrated PK/PD effects suggestive of inhibiting pathways that may contribute to vaso-occlusion. This study also provides guidance regarding biomarkers for future SCD studies.
- | PF-04447943 / Pfizer
Preclinical, Journal: Phosphodiesterase 9A Inhibition Facilitates Corticostriatal Transmission in Wild-Type and Transgenic Rats That Model Huntington's Disease. (Pubmed Central) - Jun 27, 2020
PDE9A inhibition also increased the proportion of MSNs responding to cortical stimulation and reversed deficits in spike probability observed in TG5 rats. As PDE9A is a cGMP specific enzyme, drugs such as PF-04447943 which act to facilitate striatal cGMP signaling and glutamatergic corticostriatal transmission could be useful therapeutic agents for restoring striatal function and alleviating motor and cognitive symptoms associated with HD.
- | 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.
- | PF-04447943 / Pfizer
Trial completion: A Study To Evaluate The Effect Of PF-04447943 On Qtc Interval In Healthy Adult Subjects (clinicaltrials.gov) - Nov 23, 2016
P1, N=44, Completed, Sponsor: Pfizer
cGMP enhancement could be due to synergistic effects, though an additive effect of the combined inhibitor concentrations may also contribute. Active, not recruiting --> Completed
- | PF-04447943 / Pfizer
Trial completion, Enrollment change: Safety, Tolerability, Pharmacokinetics, And Pharmacodynamics Study Of PF-04447943, Co-Administered With And Without Hydroxyurea, In Subjects With Stable Sickle Cell Disease (clinicaltrials.gov) - Oct 31, 2016
P1b, N=30, Completed, Sponsor: Pfizer
Active, not recruiting --> Completed Recruiting --> Completed | N=64 --> 30
- PF-04447943 / Pfizer
Enrollment closed: A Study To Evaluate The Effect Of PF-04447943 On Qtc Interval In Healthy Adult Subjects (clinicaltrials.gov) - Sep 16, 2016
P1, N=44, Active, not recruiting, Sponsor: Pfizer
Recruiting --> Completed | N=64 --> 30 Recruiting --> Active, not recruiting
- PF-04447943 / Pfizer
Enrollment open: A Study To Evaluate The Effect Of PF-04447943 On Qtc Interval In Healthy Adult Subjects (clinicaltrials.gov) - Jul 20, 2016
P1, N=44, Recruiting, Sponsor: Pfizer
Recruiting --> Active, not recruiting Not yet recruiting --> Recruiting
- | PF-04447943 / Pfizer
Phase classification: Safety, Tolerability, Pharmacokinetics, And Pharmacodynamics Study Of PF-04447943, Co-Administered With And Without Hydroxyurea, In Subjects With Stable Sickle Cell Disease (clinicaltrials.gov) - Jun 15, 2016
P1b, N=64, Recruiting, Sponsor: Pfizer
Not yet recruiting --> Recruiting Phase classification: P1 --> P1b
- | PF-04447943 / Pfizer
New P1 trial: A Study To Evaluate The Effect Of PF-04447943 On Qtc Interval In Healthy Adult Subjects (clinicaltrials.gov) - May 31, 2016
P1, N=44, Not yet recruiting, Sponsor: Pfizer
- || PF-04447943 / Pfizer
Trial primary completion date: Safety, Tolerability, Pharmacokinetics, And Pharmacodynamics Study Of PF-04447943, Co-Administered With And Without Hydroxyurea, In Subjects With Stable Sickle Cell Disease (clinicaltrials.gov) - Oct 7, 2015
P1, N=64, Recruiting, Sponsor: Pfizer
Phase classification: P1 --> P1b Trial primary completion date: Feb 2016 --> Jul 2016
- || PF-04447943 / Pfizer
Trial primary completion date: Safety, Tolerability, Pharmacokinetics, And Pharmacodynamics Study Of PF-04447943, Co-Administered With And Without Hydroxyurea, In Subjects With Stable Sickle Cell Disease (clinicaltrials.gov) - Feb 5, 2015
P1, N=64, Recruiting, Sponsor: Pfizer
Trial primary completion date: Feb 2016 --> Jul 2016 Trial primary completion date: May 2015 --> Feb 2016
- ||| PF-04447943 / Pfizer
Enrollment open: Safety, Tolerability, Pharmacokinetics, And Pharmacodynamics Study Of PF-04447943, Co-Administered With And Without Hydroxyurea, In Subjects With Stable Sickle Cell Disease (clinicaltrials.gov) - Jan 12, 2015
P1, N=64, Recruiting, Sponsor: Pfizer
Trial primary completion date: May 2015 --> Feb 2016 Not yet recruiting --> Recruiting
- ||| PF-04447943 / Pfizer
New P1 trial: Safety, Tolerability, Pharmacokinetics, And Pharmacodynamics Study Of PF-04447943, Co-Administered With And Without Hydroxyurea, In Subjects With Stable Sickle Cell Disease (clinicaltrials.gov) - Apr 13, 2014
P1, N=64, Not yet recruiting, Sponsor: Pfizer