albenatide (CJC-1134-PC) / ConjuChem, Changshan Kaijiejian Biopharma - LARVOL DELTA

Changshan Pharmaceutical (300255.SZ): Its holding subsidiary received the summary report of the phase III clinical study of ebenatide [Google translation] (jrj.com) - P3 | N=NA | "Changshan Pharmaceutical...announced that its holding subsidiary Changshan Kaijiejian recently received the summary report of the phase III clinical study of albenatide. The main efficacy analysis showed that after 24 weeks of double-blind treatment in the experimental group and the placebo group, statistical data showed that the superiority of the experimental group over the placebo group was established. CJC-1134-PC injection has a good safety profile in subjects with type 2 diabetes who have poor blood glucose control after receiving metformin alone or metformin combined with insulin secretagogues....In summary, type 2 diabetic subjects with poor blood sugar control after receiving metformin alone or metformin combined with insulin secretagogues can effectively control blood sugar levels after receiving CJC-1134-PC injection once a week, with overall poor The incident was expected to be controllable and no new security issues were discovered."

P3 data • Diabetes • Metabolic Disorders • Type 2 Diabetes Mellitus

Safety, tolerability, pharmacodynamics and pharmacokinetics of CJC-1134-PC in healthy Chinese subjects and type-2 diabetic subjects. (PubMed, Expert Opin Investig Drugs) - "The safety and PK/PD profiles of weekly CJC-1134-PC doses support Phase II studies with guidance on optimal dose selection. The clinical trial registration number for this work is ChiCTR-IPC-15007190."

Clinical • Journal • PK/PD data • Diabetes • Gastrointestinal Disorder • Metabolic Disorders • Type 2 Diabetes Mellitus

Role of glucagon-like peptide- 1 in vascular endothelial dysfunction -

Exendin-4 (1microg kg-1) & atorvastatin (30mg kg-1) treatments significantly attenuated increase in serum glucose & homocysteine but their concentrations remained markedly higher than sham control value

Exendin-4, a GLP-1 receptor agonist, directly induces adiponectin expression through protein kinase A pathway and prevents inflammatory adipokine expression (FluTrackers) - Ex-4 directly promotes adiponectin secretion via the protein kinase A pathway in 3T3-L1 adipocytes and may ameliorate insulin resistance

MOA • Diabetes

Increased & beta; cell apoptosis with multiorgan glucolipotoxicity by a combination of dietary sugar and fatty acid and protective effects of DPP-4 inhibitor des-fluoro-sitagliptin against them (ADA 2010) - GLP-1R agonist protected beta cells from hIAPP-induced beta cell death in vitro; Effect was potentially mediated through restoration of AKT and improved mitochondrial function

Diabetes

ConjuChem initiates phase 2 study of diabetes drug (Businesswire) - P2, N=225; ConjuChem, has initiated patient enrollment for its P2 clinical trial of its proprietary GLP-1 receptor agonist drug, CJC-1134-PC, in patients with T2D who are receiving metformin monotherapy; The PK & PD relationship of CJC-1134-PC & glycosylated hemoglobin (HbA1c) and/or fasting plasma glucose (FPG) will be evaluated; Results of P2 study will be used to establish optimal dose for future planned P3 studies

P2 initiation • Diabetes

Exendin-4 protects pancreatic beta cells from the cytotoxic effect of rapamycin by inhibiting JNK and p38 phosphorylation (Horm Metab Res) - Rapamycin was found to increase phosphorylation of c-Jun amino-terminal kinase & p38 in 30 minutes in MIN6 cells & Wistar rat islets while exendin-4 decreased their phosphorylation

Diabetes

Effects of exendin-4 on NOD and streptozotocindiabetic C57BL/6 mice (IDF 2009) - -

Diabetes