Cametor (cetilistat) / Norgine - LARVOL DELTA

Novel method to prevent severe postoperative pancreatic fistula caused by lipolysis. (PubMed, J Hepatobiliary Pancreat Sci) - "Intraperitoneal administration of water-solubilized cetilistat prevented severe inflammation and multiple failures associated with severe POPF. The incorporation of water-solubilized cetilistat into the PEG-HG is a promising delivery system for clinical application."

Journal • Inflammation

Pterostilbene alleviates cafeteria diet-induced obesity and underlying depression in adolescent male Swiss albino mice and affects insulin resistance, inflammation, HPA axis dysfunction and SIRT1 mediated leptin-ghrelin signaling. (PubMed, Horm Behav) - "Obesity induced depressed (OID) mice were treated with PTE (10, 20, 40 mg/kg), standard antiobesity drug cetilistat (10 mg/kg), antidepressant fluoxetine (10 mg/kg) for 28 days. It also restored normal cellular architecture of the brain and adipose tissue and increased the Silent mating type information regulation 2 homolog1 (SIRT1), leptin and ghrelin receptors gene expression in the brain. Thus, it can be concluded that PTE might have inhibited OID like behavior in mice via inhibition of IR, modulating neuroinflammation and hypothalamic-pituitary-adrenal axis dysfunction and upregulating SIRT1 mediated leptin-ghrelin signaling."

Journal • Preclinical • CNS Disorders • Depression • Genetic Disorders • Inflammation • Mood Disorders • Obesity • Psychiatry • IL6 • LEP • SIRT1 • TNFA

Pancreatic lipase and its related proteins: where are we now? (PubMed, Drug Discov Today) - "In this review, we summarize the structure and function of PTL, PLRP1, and PLRP2, and the metabolic fate of PTL inhibitors. We also discuss the current status of clinical trials on orlistat and its combinations for obesity treatment."

Journal • Review • Genetic Disorders • Obesity

Metabolic profiling, antioxidant, and enzyme inhibition potential of Iris pseudacorus L. from Egypt and Japan: A comparative study. (PubMed, Sci Rep) - "Moreover, IPR-J and IPR-E exhibited promising α-glucosidase inhibitory activity displaying IC values of 18.52 µg/mL, 57.89 µg/mL, respectively being more potent as compared to acarbose with IC value of 362.088 µg/mL. All extracts exerted significant lipase inhibitory activity exhibiting IC values of 2.35, 4.81, 2.22 and 0.42 µg/mL, respectively compared to cetilistat with IC value of 7.47 µg/mL...ADMET prediction (absorption, distribution, metabolism, excretion, and toxicity) showed that most of the phytoconstituents exhibited promising pharmacokinetic, pharmacodynamics and tolerable toxicity properties. According to our findings, I. pseudacorus might be considered as a valuable source for designing novel phytopharmaceuticals."

Journal • Tyrosinase

Repurposing FDA-approved drugs cetilistat, abiraterone, diiodohydroxyquinoline, bexarotene, and remdesivir as potential inhibitors against RNA dependent RNA polymerase of SARS-CoV-2: A comparative in silico perspective. (PubMed, Inform Med Unlocked) - "Furthermore, to validate the potency of these drugs, we compared them to the antiviral remdesivir, which inhibits RdRp. Our finding indicated that the selected drugs have a high potential to be developed as RdRp inhibitors and, with further validation studies, could serve as potential drugs for the treatment of COVID-19."

FDA event • Journal • Infectious Disease • Novel Coronavirus Disease • Respiratory Diseases

Inhibitory activity of FDA-approved drugs cetilistat, abiraterone, diiodohydroxyquinoline, bexarotene, remdesivir, and hydroxychloroquine on COVID-19 main protease and human ACE2 receptor: A comparative in silico approach. (PubMed, Inform Med Unlocked) - "The MD simulation results demonstrated that these drugs interact to stabilize the systems, allowing them to be used as effective inhibitors of these proteins. Meanwhile, bexarotene, abiraterone, cetilistat, and diiodohydroxyquinoline's systemic effects should be further investigated in suitable ex vivo human organ culture or organoids, animal models, or clinical trials."

FDA event • Journal • Infectious Disease • Novel Coronavirus Disease • Respiratory Diseases

Discovery of the FDA-approved drugs bexarotene, cetilistat, diiodohydroxyquinoline, and abiraterone as potential COVID-19 treatments with a robust two-tier screening system. (PubMed, Pharmacol Res) - "A few clinically approved drugs, such as remdesivir, chloroquine, hydroxychloroquine, nafamostat, camostat, and ivermectin, exhibited anti-SARS-CoV-2 activity in vitro and/or in a small number of patients. Bexarotene demonstrated the highest Cmax:EC ratio (1.69) which was higher than those of chloroquine, hydroxychloroquine, and ivermectin. These results demonstrated the efficacy of the two-tier screening system and identified potential COVID-19 treatments which can achieve effective levels if given by inhalation or systemically depending on their pharmacokinetics."

FDA event • Journal • Infectious Disease • Novel Coronavirus Disease • Oncology

New and emerging drug molecules against obesity (J Cardiovasc Pharmacol Ther) - PMID: 24064009; “Cetilistat, a lipase inhibitor is claimed to have superior safety profile to orlistat...have limited success in early clinical development include velneperit, tesofensine, and beloranib .Tesofensine is a triple monoamine re-uptake inhibitor, velneperit acts as a neuropeptide Y5 receptor antagonist and beloranib is a methionine amino peptidase 2 inhibitor.”

Review • Obesity

In vivo metabolic investigation of Cetilistatin normal vs pseudo germ free rats by UPLC-Q-TOF/MS/MS and in silico toxicological evaluation of its metabolites. (PubMed, Biomed Chromatogr) - "Cetilistat is a pancreatic lipase inhibitor approved for management of obesity, following the serious adverse effects exhibited by its analogueorlistat. Four metabolites of Cetilistat were observed in in vivomatrices. Conforming to anticipation,significant changes were observed both qualitatively as well as quantitatively implying that formation of metabolites was both CYP enzymes and gut microflora mediated."

Journal • Preclinical • Genetic Disorders • Metabolic Disorders • Obesity

"https://t.co/OBLeAntqnz" (@medpedshosp)