succinobucol (AGI-1067) / Merck (MSD) - LARVOL DELTA

PLGA Nanoparticles Containing VCAM-1 Inhibitor Succinobucol and Chemotherapeutic Doxorubicin as Therapy against Primary Tumors and Their Lung Metastases. (PubMed, Pharmaceutics) - "Additionally, the in vivo experiments showed that Co-NPs could efficiently suppress not only primary melanoma but also its lung metastases. In conclusion, PLGA nanoparticles containing VCAM-1 inhibitor Suc and chemotherapeutic Dox as therapy against primary tumors and their lung metastases provides a promising drug delivery strategy for the treatment of metastatic malignant tumors."

Journal • Melanoma • Oncology • Solid Tumor • VCAM1

Examining anti-inflammatory therapies in the prevention of cardiovascular events: protocol for a systematic review and network meta-analysis of randomised controlled trials. (PubMed, BMJ Open) - "These include (but are not limited to): non-steroidal anti-inflammatory drugs (NSAIDs), colchicine, prednisone, methotrexate, canakinumab, pexelizumab, anakinra, succinobucol, losmapimod, inclacumab, atreleuton, LP-PLA (darapladib) and sPLA (varespladib). The findings will be disseminated through a peer-reviewed journal. CRD42022303289."

Journal • Retrospective data • Review • Atherosclerosis • Cardiovascular • Congestive Heart Failure • Dyslipidemia • Heart Failure • Immunology • Inflammation • Myocardial Infarction

[VIRTUAL] LIPID-INDUCED ENDOTHELIAL VASCULAR CELL ADHESION MOLECULE 1 PROMOTES NASH PATHOGENESIS (AASLD 2020) - "VCAM-1 neutralizing antibody M/K-2.7 (VCAM-1Ab) or the VCAM-1 pharmacological inhibitor AGI-1067 was administered intraperitoneally... Lipotoxic stress enhances the expression of LSEC VCAM-1 mainly via an MLK3-dependent mechanism. Inhibition of VCAM-1 is salutary in murine NASH, and might serve as a potential therapeutic strategy for human NASH."

Addiction (Opioid and Alcohol) • Fibrosis • Hepatology • Immunology • Inflammation • Liver Cirrhosis • Liver Failure • Non-alcoholic Steatohepatitis • CD68 • COL1A1 • IL1B • TNFA • VCAM1

Preferential Targeting Cerebral Ischemic Lesions with Cancer Cell-Inspired Nanovehicle for Ischemic Stroke Treatment. (PubMed, Nano Lett) - "Inspired by the intriguing blood-brain barrier (BBB)-penetrating ability of 4T1 cancer cells upon their brain metastasis, we herein designed a promising biomimetic nanoplatform by camouflaging a succinobucol-loaded pH-sensitive polymeric nanovehicle with a 4T1 cell membrane (MPP/SCB), aiming to promote the preferential targeting of cerebral ischemic lesions to attenuate the ischemia/reperfusion injury...Moreover, MPP/SCB produced notable enhancement of microvascular reperfusion in the ischemic hemisphere, resulting in a 69.9% reduction of infarct volume and showing remarkable neuroprotective effects of tMCAO rats, which was superior to the counterpart uncamouflaged nanovehicles (PP/SCB). Therefore, this design provides a promising nanoplatform to target the cerebral ischemic lesions for ischemic stroke therapy."

Journal • Cardiovascular • Ischemic stroke • Oncology • Reperfusion Injury • Solid Tumor

A HYDROPHILIC DERIVATIVE OF PROBUCOL (PROBGL2) IMPROVES GLUCOSE TOLERANCE AND INSULIN SENSITIVITY. (ISHyp 2016) - " Our data show that probucol and its hydrophilic derivative, ProBGL2 ameliorate glucose tolerance, insulin resistance and cardiac hypertrophy in HFD-fed mice and those are independent of the canonical potency of probucol such as lipid-lowering or antioxidant activities. ProBGL2 should be a novel potent anti-diabetic agent."

Biosimilar • Diabetes

LIPID-INDUCED ENDOTHELIAL VASCULAR CELL ADHESION MOLECULE 1 PLAYS A PIVOTAL ROLE IN NASH PATHOGENESIS (DDW 2020) - "AGI-1067 (AGI), a known VCAM-1 inhibitor, or VCAM-1 neutralizing antibody M/K-2.7 (Vcam1Ab) was given by intraperitoneal injection... Lipotoxic stress enhances the expression of LSEC VCAM-1 mainly through a MAPK/NF-κB pathway. Inhibition of VCAM-1 might be a potential anti-inflammatory therapeutic strategy for NASH."

Fibrosis • Gastroenterology • Hepatology • Immunology • Liver Cirrhosis • Metabolic Disorders • Non-alcoholic Fatty Liver Disease • Non-alcoholic Steatohepatitis • MAPK8