Chiglitazar (Carfloglitazar, Trade name: Bilessglu®), a new-generation insulin sensitizing candidate drug for the treatment of type 2 diabetes mellitus (T2DM), is a Class 1 innovative drug developed independently by Chipscreen Biosciences. With a chemical structure completely different from that of thiazolidinediones (TZD), Chiglitazar is a configuration-restricted pan-PPAR agonist that can activate all three PPAR subtypes (α, γ and δ) in moderation as well as effectively prevent the phosphorylation of PPARγ through adipokines and inflammatory cytokines-mediated CDK5 activation, thereby selectively altering the expression of a series of genes associated with insulin sensitization.
Chiglitazar can control blood glucose level and ameliorate the lipid and energy metabolic disorders that accompany T2DM, helping to prevent and control cardiovascular complications. This makes Chiglitazar a potentially more comprehensive treatment option for T2DM.
Figure. Potential mechanisms of action of Chiglitazar
- In September 2019, a new drug application (NDA) of Chiglitazar for T2MD was successfully lodged, and has now progressed to the on-site inspection stage.
- In October 2020, a Phase III clinical trial of Chiglitazar in combination with Metformin in the treatment of T2DM was started, and is currently proceeding well.
- In March 2021, an investigational new drug (IND) application to conduct a Phase II clinical trial of Chiglitazar for nonalcoholic steatohepatitis (NASH) was submitted following pre-communication with the Center for Drug Evaluation (CDE) of NMPA.
- In Oct. 2021, Chiglitazar was approved for marketing by the National Medical Products Administration (NMPA) to treat Type 2 Diabetes, becoming the world's first PPAR full agonist approved for treating Type 2 Diabetes.
At present, Chipscreen Biosciences is conducting registered clinical trials of Chiglitazar as monotherapy or combination therapy, including a phase III clinical trial of Chiglitazar in combination with metformin in patients with Type 2 Diabetes poorly controlled with metformin monotherapy and a phase II clinical trial of Chiglitazar in patients with Nonalcoholic Steatohepatitis (NASH) as associated with elevated triglycerides and insulin resistance.