The purpose of this study is to explore the efficacy of Aggrenox in patients with SARS-CoV-2 infection with symptoms consistent with COVID-19. An anticipated total of 132 participants will be randomly divided almost equally into 2 groups: one group will receive Dipyridamole ER 200mg/ Aspirin 25mg orally/enterally along with the standard of care and the other group with receive the standard of care only but no Dipyridamole ER 200mg/ Aspirin 25mg. Participants will be screened, enrolled, receive treatment, and followed for 28 days. The clinical and laboratory outcomes of all the participants enrolled in the study will be evaluated at the end of the study to explore if there is any difference in the outcomes between 2 groups.

Start Date21 Oct 2020

Sponsor / Collaborator

Rutgers State University of New Jersey

[+1]

NCT04360720

/ RecruitingPhase 3IIT

PercutaNEOus Coronary Intervention Followed by Monotherapy INstead of Dual Antiplatelet Therapy in the SETting of Acute Coronary Syndromes: The NEO-MINDSET Trial A Drug Reduction Study for Patients With Acute Coronary Syndrome in the Unified Health System in Brazil

Phase-3, randomized, multicenter, parallel-group study with blind evaluation of endpoints and intention-to-treat analysis.
The general purpose of the study is evaluate the non-inferiority hypothesis for ischemic events and the superiority hypothesis for bleeding events resulting from platelet P2Y12 receptor inhibitors given as monotherapy in comparison with conventional dual antiplatelet therapy in acute coronary syndrome patients treated with percutaneous coronary intervention in the context of the Unified Health System in Brazil.

Start Date15 Oct 2020

Sponsor / Collaborator

Hospital Israelita Albert Einstein

100 Clinical Results associated with PDE5A x COX

100 Translational Medicine associated with PDE5A x COX

0 Patents (Medical) associated with PDE5A x COX

Literatures (Medical) associated with PDE5A x COX

01 Jan 2025·Anti-Cancer Agents in Medicinal Chemistry

Novel Celecoxib Derivative, RF26, Blocks Colon Cancer Cell Growth by Inhibiting PDE5, Activating cGMP/PKG Signaling, and Suppressing β-catenin-dependent Transcription

Article

Author: Da Silva, Luciana Madeira ; Abadi, Ashraf H. ; Abdel-Halim, Mohammad ; Keeton, Adam B. ; Zhou, Gang ; Piazza, Gary A. ; Sigler, Sara ; Maxuitenko, Yulia Y. ; Berry, Kristy L. ; Engel, Matthias ; Fathalla, Reem K.

Background:Previous studies have reported that the cGMP-specific PDE5 isozyme is overexpressed in colon adenomas and adenocarcinomas and essential for colon cancer cell proliferation, while PDE5 selective inhibitors (e.g., sildenafil) have been reported to have cancer chemopreventive activity.Aim:This study aimed to determine the anticancer activity of a novel PDE5 inhibitor, RF26, using colorectal cancer (CRC) cells and the role of PDE5 in CRC tumor growth in vivo.Objective:The objective of this study was to characterize the anticancer activity of a novel celecoxib derivative, RF26, in CRC cells previously reported to lack COX-2 inhibition but have potent PDE5 inhibitory activity.Methods:Anticancer activity of RF26 was studied using human CRC cell lines. Its effects on intracellular cGMP levels, cGMP-dependent protein kinase (PKG) activity, β-catenin levels, TCF/LEF transcriptional activity, cell cycle distribution, and apoptosis were measured. CRISPR/cas9 PDE5 knockout techniques were used to determine if PDE5 mediates the anticancer activity of RF26 and validate PDE5 as a cancer target.Results:RF26 was appreciably more potent than celecoxib and sildenafil to suppress CRC cell growth and was effective at concentrations that increased intracellular cGMP levels and activated PKG signaling. RF26 suppressed β-catenin levels and TCF/LEF transcriptional activity and induced G1 cell cycle arrest and apoptosis within the same concentration range. CRISPR/cas9 PDE5 knockout CRC cells displayed reduced sensitivity to RF26, proliferated slower than parental cells, and failed to establish tumors in mice.Conclusion:Further evaluation of RF26 for the prevention or treatment of cancer and studying the role of PDE5 in tumorigenesis are warranted.

01 Jan 2025·International Immunopharmacology

Unveiling the substantial role of rutin in the management of drug-induced nephropathy using network pharmacology and molecular docking

Article

Author: Kamboj, Sonia ; Mittal, Nitish ; Jain, Akash ; Chaudhary, Jasmine ; Thakur, Prashant

INTRODUCTIONFlavonoids including quercetin, kaempferol, myricetin, rutin etc. have always been a part of traditional Chinese medicine for the treatment of several ailments. Rutin (RT), also known as rutoside, sophorin is one of the flavanol glycoside having structure resemblance with quercetin. It is found to exhibit several biological activities viz. anti-inflammatory, anticancer, antioxidant, cardioprotective, antidepressant, neuroprotective etc. but the mechanisms by which it exhibits these effects is still under research.AIMThe protective effects of rutin against drug induced nephropathy have already been discovered. Therefore, in this study, the main focus is to explore the mechanism by which rutin provides protection against drug-induced nephropathy using modern method like network pharmacology and molecular docking.MATERIALS AND METHODSGenes linked to drug-induced nephropathy and targets connected with rutin were obtained by searching through a number of extensive databases, including David software, Venn plot database, Swiss target prediction database, String database, Gene card & OMIM database, and Pubchem. In order to locate mapping targets, the acquired targets were examined and intersected. A protein-protein interaction (PPI) network was then built to find potential targets.RESULTSFrom the KEGG pathway, the target pathway responsible for drug-induced nephropathy were found to be XDH, HSD17B2, MET, PRKCB, CD38, ALDH2, CDK1, PTK2, CYP19A1, TNF, F2, PTGS2, ESR1, GSK3B, GLO1, ALOX12, MMP3, PRKCZ, CXCR1, CA4, EGFR, PDE5A, F10, AKR1B1, DRD4, TERT, CA3, PLG, TP53, PRKCH, PIK3R1, PRKACA, CYP1B1, ALOX5, PLK1, CHEK1, KCNH2, PRKCD, MAPT, MPO, NOX4, AVPR2, ACHE, MCL1, KDR, ABCG2, CCR1, PIK3CG, FLT3, ADORA1, IL2, SYK, IGF1R, CA2, SERPINE1, INSR, PRKCA, APP, MMP9. From these identified targets, the 14 selected pathways which have major role in providing protection in drug-induced nephropathy have been discussed.CONCLUSIONAs RT can inhibit various metabolic and proinflammatory pathways involved, it can help in prevention and treatment of drug-induced nephropathy.FUTURE ASPECTSThe revelation of mode of action of bioactive constituent rutin against drug-induced nephropathy provides a theoretical basis for designing more promising compounds in future for treatment of nephropathy.

01 May 2021·Seminars in Nuclear MedicineQ2 · MEDICINE

PET Agents in Dementia: An Overview

Q2 · MEDICINE

Review

Author: de Deyn, Peter Paul ; Marcolini, Sofia ; Dierckx, Rudi A J O ; van Waarde, Aren

This article presents an overview of imaging agents for PET that have been applied for research and diagnostic purposes in patients affected by dementia. Classified by the target which the agents visualize, seven groups of tracers can be distinguished, namely radiopharmaceuticals for: (1) Misfolded proteins (ß-amyloid, tau, α-synuclein), (2) Neuroinflammation (overexpression of translocator protein), (3) Elements of the cholinergic system, (4) Elements of monoamine neurotransmitter systems, (5) Synaptic density, (6) Cerebral energy metabolism (glucose transport/ hexokinase), and (7) Various other proteins. This last category contains proteins involved in mechanisms underlying neuroinflammation or cognitive impairment, which may also be potential therapeutic targets. Many receptors belong to this category: AMPA, cannabinoid, colony stimulating factor 1, metabotropic glutamate receptor 1 and 5 (mGluR1, mGluR5), opioid (kappa, mu), purinergic (P2X7, P2Y12), sigma-1, sigma-2, receptor for advanced glycation endproducts, and triggering receptor expressed on myeloid cells-1, besides several enzymes: cyclooxygenase-1 and 2 (COX-1, COX-2), phosphodiesterase-5 and 10 (PDE5, PDE10), and tropomyosin receptor kinase. Significant advances in neuroimaging have been made in the last 15 years. The use of 2-[¹⁸F]-fluoro-2-deoxy-D-glucose (FDG) for quantification of regional cerebral glucose metabolism is well-established. Three tracers for ß-amyloid plaques have been approved by the Food and Drug Administration and European Medicines Agency. Several tracers for tau neurofibrillary tangles are already applied in clinical research. Since many novel agents are in the preclinical or experimental stage of development, further advances in nuclear medicine imaging can be expected in the near future. PET studies with established tracers and tracers for novel targets may result in early diagnosis and better classification of neurodegenerative disorders and in accurate monitoring of therapy trials which involve these targets. PET data have prognostic value and may be used to assess the response of the human brain to interventions, or to select the appropriate treatment strategy for an individual patient.

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