VCP979 / Monash University - LARVOL DELTA

Novel small-molecule compound VCP979 attenuates renal fibrosis in male rats with unilateral ureteral obstruction. (PubMed, Exp Biol Med (Maywood)) - "Mechanistically, VCP979 treatment inhibited the activation of p38 mitogen-activated protein kinase, nuclear factor-kappa B, and transforming growth factor-β1/Smads signaling pathways. These results indicated that VCP979 could be an effective therapeutic agent for alleviating renal fibrosis and inflammation in the rat model of UUO via its antifibrotic and anti-inflammatory effects."

Journal • Preclinical • Chronic Kidney Disease • Fibrosis • Immunology • Inflammation • Nephrology • Renal Disease • NF-κβ • TGFB1

The Effect of Antiseizure Medications and Cardioprotective Drugs on Cardiac Remodelling in a Post-status Epilepticus Rat Model of Temporal Lobe Epilepsy (AES 2022) - "This study aims to investigate functional and structural cardiac abnormalities in a rat model of chronic mesial temporal lobe epilepsy (TLE), and to investigate whether administration of the antiseizure medication levetiracetam (LEV), the cardioprotective drugs atenolol (B-blocker) or VCP979 (MAP kinase antagonist) could alleviate the changes in cardiac structure and function. Kainic acid (KA) was used to induce status epilepticus (SE) and subsequent chronic epilepsy in male Wistar rats (n=32). Our findings indicates that chronic epilepsy was associated with increased cardiac fibrosis. While the mechanisms underlying the cardiac fibrosis and potential cardiac dysfunction remains to be determined, we found that the novel anti-fibrotic and anti-inflammatory agent VCP979 may help prevent the development of myocardial fibrosis in chronic epilepsy, but a larger number of subjects and further investigation are required to confirm this hypothesis."

Preclinical • CNS Disorders • Epilepsy • Fibrosis • Immunology

Reducing White Adipose Tissue Browning Using p38α MAPK Inhibitors Ameliorates Cancer-Associated Cachexia as Assessed by Magnetic Resonance Imaging. (PubMed, Nutrients) - "Blockade of p38 MAPK reduced the WAT browning that contributes to CAC. Thus, p38 MARK inhibitors can potentially be used as a therapy for treating CAC. Non-invasive MRI can also be applied to assess the progression and treatment responses of CAC."

Journal • MRI • Cachexia • Gastrointestinal Cancer • Hepatology • Oncology • Pancreatic Cancer • Solid Tumor

A novel small molecule compound VCP979 improves ventricular remodeling in murine models of myocardial ischemia/reperfusion injury. (PubMed, Int J Mol Med) - "In addition, VCP979 attenuated the activation of p38‑mitogen‑activated protein kinase in both Ang II‑induced NCFs and hearts subjected to MI/R injury. These findings indicated that the novel small‑molecule compound VCP979 can improve ventricular remodeling in murine hearts against MI/R injury, suggesting its potential therapeutic function in patients subjected to MI/R injury."

Journal • Preclinical • Cardiovascular • Congestive Heart Failure • Fibrosis • Heart Failure • Immunology • Myocardial Ischemia • Reperfusion Injury

A Novel Anti-inflammation and Anti-fibrosis Agent, Vcp979, Treatment Attenuates Ventricular Remodeling and Improves Cardiac Function in Murine Model of Myocardial Ischemia/Reperfusion Injury (AHA 2019) - "=VLOOKUP(B6,'[1]AHA 2019_Abstracts'!$T$1:$U$131,2,0)"

Preclinical

A Novel Anti-inflammation and Anti-fibrosis Agent, Vcp979, Treatment Attenuates Ventricular Remodeling and Improves Cardiac Function in Murine Model of Myocardial Ischemia/Reperfusion Injury (AHA 2019) - "This study provides evidence that VCP979 treatment prevent cardiac remodeling and improve cardiac function indicating its ability to prevent the development of heart failure post MI/R. Therefore, VCP979 has the potential to be a novel therapy for patients subjected to MI/R."

Preclinical

Effects of VCP979 Novel p38 Mitogen Activated Protein Kinase Inhibitor on Progression of Pancreatic Cancer in Mouse Model with Diabetic Conditions. (PubMed, J Biomed Nanotechnol) - "In addition, type 2 diabetes mellitus promoted a more aggressive phenotype associated with up-regulated p38 MAPK activity, which was effectively inhibited by VCP979. Furthermore, the findings from this study suggest that VCP979 may exert its tumor-suppressing effects via regulation of p38 MAPK/Nuclear factor-κB (NF-κB) signal pathway, reduction of its downstream inflammation, as well as attenuations of epithelial-mesenchymal transition (EMT) in pancreatic cancer non-diabetic and diabetic conditions."

Journal • Preclinical

Diffusion Tensor Imaging Evaluation of Axonal/White Matter Remodeling in a Mouse Model of Diabetic Stroke Treated with Novel p38 MAPK Inhibitor, VCP979. (PubMed, J Biomed Nanotechnol) - "Thus, VCP979 improves axonal/WM remodeling and functional outcomes in a diabetic mouse stroke model. DTI may aid in visualizing axonal/WM remodeling and evaluating the therapeutic efficacy of VCP979."

Journal • Preclinical