Bilessglu (chiglitazar) / Chipscreen - LARVOL DELTA

Clinical observation of pioglitazone or sitaglipta sodium combined with metformin in the treatment of newly diagnosed type 2 diabetes with fatty liver (ChiCTR) - P4 | N=80 | Not yet recruiting | Sponsor: The First Affiliated Hospital of Chengdu Medical College; Chengdu Medical University First Affiliated Hospital"

New P4 trial • Diabetes • Hepatology • Metabolic Disorders • Metabolic Dysfunction-Associated Steatotic Liver Disease • Type 2 Diabetes Mellitus

Integrated Metabolomics and Lipidomics Analysis Reveals the Mechanism Behind the Action of Chiglitazar on the Protection Against Sepsis-Induced Acute Lung Injury. (PubMed, Metabolites) - "Co-treatment with EX-527 in LPS-stimulated BEAS-2B cells and CLP rats inhibited the effects of chiglitazar on the aforementioned signaling pathways and worsened the protective effects of chiglitazar on lung injury, respectively. Chiglitazar alleviates SALI by restoring NAD+ and TG synthesis, highlighting the balancing of metabolism as a promising therapeutic strategy in the management of SALI."

Journal • Acute Lung Injury • Infectious Disease • Metabolic Disorders • Respiratory Diseases • Septic Shock • PPARA

Administration of chiglitazar reverses chronic stress-induced depressive-like symptoms in mice via activation of hippocampal PPARα and BDNF. (PubMed, Front Pharmacol) - "Peroxisome proliferator-activated receptor α (PPARα) has been demonstrated to play a role in the pathophysiology of depression, and several PPARα agonists including WY14643, fenofibrate, and gemfibrozil, have all been reported to possess antidepressant-like efficacy in rodents. Genetic knockdown of hippocampal PPARα and BDNF also abolished the antidepressant-like actions of chiglitazar in mice. In summary, administration of chiglitazar reverses chronic stress-induced depressive-like symptoms in mice via activation of hippocampal PPARα and BDNF."

Journal • Preclinical • CNS Disorders • Depression • Gene Therapies • Psychiatry • BDNF • PPARA

Clinical study of insulin resistance and hormonal improvement by chiglitazar in polycystic ovary syndrome (ChiCTR) - P4 | N=112 | Not yet recruiting | Sponsor: The Second Affiliated Hospital of Chongqing Medical University; The Second Affiliated Hospital of Chongqing Medical University

New P4 trial • Polycystic Ovary Syndrome

A multicenter, prospective, single-arm clinical study on the treatment of refractory/relapsed acute myeloid leukemia R/RAML with Chiglitazar Sodium combined with Venetoclax and Azacitidine(CVA) (ChiCTR) - P2 | N=30 | Not yet recruiting | Sponsor: The First Affiliated Hospital of Xiamen University; The First Affiliated Hospital of Xiamen University

New P2 trial • Acute Myelogenous Leukemia • Hematological Malignancies • Leukemia • Myelodysplastic Syndrome • Oncology

A multicenter, randomized controlled study of silymarin and chiglitazar sodium in patients with T2DM and MASLD (ChiCTR) - P4 | N=250 | Not yet recruiting | Sponsor: Zhongda Hospital of Southeast University; Zhongda Hospital of Southeast University

New P4 trial • Diabetes • Hepatology • Metabolic Disorders • Metabolic Dysfunction-Associated Steatotic Liver Disease • Type 2 Diabetes Mellitus

Pan-PPAR Agonist Chiglitazar for the Treatment of High-Risk Metabolic Dysfunction-Associated Steatohepatitis Coexisting with Type 2 Diabetes: A Randomized, Double-Blind, Phase 2 Trial (APASL 2025) - P4 | "Chiglitazar demonstrated a favorable efficacy and safety profile in the treatment of T2DM patients at high risk of MASH. These findings support its further evaluation in a phase 3 trial. Table and Figure:Figure 1.Primary endpoints of the study Figure 2.Changes in clinical characteristics from baseline to week 24"

Clinical • P2 data • Diabetes • Fibrosis • Hepatitis C • Hepatology • Immunology • Metabolic Disorders • Metabolic Dysfunction-Associated Steatohepatitis • Type 2 Diabetes Mellitus

Comparing Efficacy of Chiglitazar, Pioglitazone, and Semaglutide in Type 2 Diabetes: A Retrospective Study. (PubMed, Diabetes Ther) - "Chiglitazar is particularly effective for participants with pronounced dawn phenomenon, semaglutide excels in lipid metabolism improvement and kidney protection, while pioglitazone remains effective for insulin resistance and glycemic control. These findings provide evidence-based guidance for individualized T2D management."

Journal • Retrospective data • Cardiovascular • Diabetes • Dyslipidemia • Inflammation • Metabolic Disorders • Renal Disease • Type 2 Diabetes Mellitus

Evaluation of the Regulatory Effect of the Pan-PPAR Agonist Chiglitazar on the Dawn Phenomenon. (PubMed, Diabetes Ther) - "Chiglitazar effectively reduces DP intensity and improves glycemic control, independent of its effects on lipid metabolism. These findings suggest a potential link between chiglitazar's mechanism and circadian rhythm regulation, possibly through the modulation of REV-ERB nuclear receptors. Further research is needed to confirm this hypothesis and evaluate the long-term clinical benefits of chiglitazar in diabetes management."

Journal • Diabetes • Metabolic Disorders

The Efficacy and Safety of Chiglitazar in Patients with MAFLD-related Cirrhosis (clinicaltrials.gov) - P=N/A | N=195 | Not yet recruiting | Sponsor: Beijing Friendship Hospital

New trial • Fibrosis • Gastroenterology • Hepatology • Immunology • Liver Cirrhosis • Metabolic Disorders • Metabolic Dysfunction-Associated Steatotic Liver Disease

Therapeutic effects of chiglitazar combined with Rosa roxburghii Tratt. in inpatients with antipsychotic-induced metabolic syndrome. (PubMed, Pak J Pharm Sci) - "Importantly, the Chiglitazar + RRT group exhibited a significantly lower PANSS score at 12 weeks compared to baseline, indicating improved psychiatric symptoms. Chiglitazar combined with RRT effectively improves metabolic parameters, reduces inflammation and ameliorates psychiatric symptoms in inpatients with antipsychotic-induced MetS."

Biomarker • Clinical • Journal • CNS Disorders • Inflammation • Mental Retardation • Metabolic Disorders • Psychiatry • IL6 • TNFA

Chiglitazar/Metformin in Non-obese Women With PCOS (clinicaltrials.gov) - P2/3 | N=55 | Completed | Sponsor: Shengjing Hospital | Enrolling by invitation ➔ Completed | N=40 ➔ 55 | Trial completion date: May 2026 ➔ Nov 2024 | Trial primary completion date: Apr 2026 ➔ Oct 2024

Enrollment change • Trial completion • Trial completion date • Trial primary completion date • Obesity • Polycystic Ovary Syndrome

Chiglitazar Sodium Combined With Venetoclax and Azacitidine (CVA) for the Treatment of R/R AML (clinicaltrials.gov) - P1 | N=30 | Recruiting | Sponsor: The First Affiliated Hospital of Xiamen University

New P1 trial • Acute Myelogenous Leukemia • Hematological Malignancies • Leukemia • Oncology

Chiglitazar diminishes the warburg effect through PPARγ/mTOR/PKM2 and increases the sensitivity of imatinib in chronic myeloid leukemia. (PubMed, Exp Hematol Oncol) - "Our results demonstrated the potential of Chi to overcome IM resistance in vitro and in vivo. By inhibiting the Warburg effect through the PPARγ/mTOR/PKM2 pathway, Chi resensitizes CML cells towards imatinib treatment. Combining IM with Chi is an alternative therapeutic option for CML management, especially for IM-resistant CML patients."

Journal • Chronic Myeloid Leukemia • Hematological Malignancies • Leukemia • Oncology • Transplantation • PKM • PPARG

Resensitizing the Imatinib-Resistant Chronic Myeloid Leukemia through Reshaping the Glucose Mtabolism By Insulin Sensitizer (ASH 2024) - "Chiglitazar (Chi), a novel Insulin Sensitizer, reduced the glucose metabolism in stem-like cell of Acute Myeloid Leumia (AML) according to our previous study. Finally, in vivo data confirmed the anti-leukemic effect of Chi and IM combination regimen in CDX (cell derived xnograft) models. Thus, we concluded that combining Chi and IM serves as a potential thrapeutic regimen in CML clinical management."

Acute Myelogenous Leukemia • Chronic Myeloid Leukemia • Hematological Malignancies • Leukemia • Oncology • PKM • PPARG

Chiglitazar ameliorates dehydroepiandrosterone-induced polycystic ovary syndrome in rats. (PubMed, J Ovarian Res) - "Chiglitazar significantly improved ovulation in rats with PCOS and may be a potential novel therapeutic strategy for PCOS."

Journal • Preclinical • Atherosclerosis • Cardiovascular • Dyslipidemia • Metabolic Disorders • Polycystic Ovary Syndrome • SLC2A4

PPARA variant rs1800234 had a dose dependent pharmacogenetics impact on the therapeutic response to chiglitazar. (PubMed, Pharmacogenomics) - "It could help explain the absence of a dose effect of chiglitazar and serve as a potential biomarker for the chosen dose of chiglitazar in the future. In addition, our study provided important reference for the design and clinical application of multi-target drugs."

Biomarker • Clinical • Journal • Type 2 Diabetes Mellitus • PPARA

A RANDOMIZED, DOUBLE-BLIND, PLACEBO-CONTROLLED PHASE 2 TRIAL TO EVALUATE THE EFFICACY AND SAFETY OF CHIGLITAZAR IN NASH PATIENTS (AASLD 2024) - "Chiglitazar at both doses effectively reduces LFC, liver inflammation and damage, demonstrating a dose-dependent relationship. It also shows a trend in improving fibrosis, with a dose-dependent effect, and is well-tolerated."

Clinical • P2 data • Addiction (Opioid and Alcohol) • Fibrosis • Hepatology • Immunology • Inflammation • Liver Failure • Metabolic Dysfunction-Associated Steatohepatitis • Metabolic Dysfunction-Associated Steatotic Liver Disease

Combinations of HDAC inhibitor and PPAR agonist induce ferroptosis of leukemic stem cell-like cells in acute myeloid leukemia. (PubMed, Clin Cancer Res) - "Our findings suggest that treatment with CS055 combined with chiglitazar, will target LSCs by inducing ferroptosis and may confer an effective approach for the treatment of AML."

Journal • Acute Myelogenous Leukemia • Hematological Malignancies • Leukemia • Oncology • ATF3 • ATF4 • CD34 • HDAC3 • SLC7A11

Combinations of HDAC inhibitor and PPAR agonist induce ferroptosis of leukemic stem cell-like cells in acute myeloid leukemia (Clin Cancer Res) - "We report that the histone deacetylase inhibitor CS055, in combination with peroxisome proliferator-activated receptor (PPAR) pan-agonist (chiglitazar), synergistically targets leukemia stem-like cells from leukemia cell lines and patient samples, while sparing normal hematopoietic progenitor cells. Mechanistically, chiglitazar enhances the inhibitory effect of CS055 on HDAC3 and induces ferroptosis in LSCs-like cells by down-regulating the expression of ferroptosis suppressor SLC7A11."

Preclinical • Acute Myelogenous Leukemia

Chiglitazar attenuates high-fat diet-induced nonalcoholic fatty liver disease by modulating multiple pathways in mice. (PubMed, Mol Cell Endocrinol) - "This study demonstrated the potential therapeutic effect of chiglitazar on NAFLD. Chiglitazar ameliorated NAFLD by modulating multiple pathways."

Journal • Preclinical • Dyslipidemia • Hepatology • Inflammation • Metabolic Disorders • Metabolic Dysfunction-Associated Steatotic Liver Disease

RECAM: Chiglitazar Added to Metformin for Type 2 Diabetes (clinicaltrials.gov) - P3 | N=533 | Completed | Sponsor: Chipscreen Biosciences, Ltd. | Recruiting ➔ Completed

Trial completion • Diabetes • Metabolic Disorders • Type 2 Diabetes Mellitus

Pharmacokinetics of Chiglitazar in Subjects With Hepatic Impairment and Normal Hepatic Function (clinicaltrials.gov) - P1 | N=24 | Completed | Sponsor: Chipscreen Biosciences, Ltd. | Recruiting ➔ Completed | N=44 ➔ 24

Enrollment change • Trial completion • Hepatology

Pharmacokinetics of Chiglitazar in Subjects With Renal Impairment and Normal Renal Function (clinicaltrials.gov) - P1 | N=24 | Completed | Sponsor: Chipscreen Biosciences, Ltd. | Recruiting ➔ Completed | Trial completion date: Dec 2023 ➔ Jul 2023 | Trial primary completion date: Dec 2023 ➔ Jul 2023

Trial completion • Trial completion date • Trial primary completion date • Renal Disease

A Phase II Clinical Trial of Chiglitazar for NASH (clinicaltrials.gov) - P2 | N=104 | Completed | Sponsor: Chipscreen Biosciences, Ltd. | Recruiting ➔ Completed

Trial completion • Hepatitis C • Hepatology • Hypertriglyceridemia • Metabolic Dysfunction-Associated Steatohepatitis