General Information of Drug (ID: DM67P0F)

Drug Name
CS-038 Drug Info
Synonyms Chiglitazar; CS-00098; PPAR alpha/gamma agonist (diabetes), Chipscreen Biosciences
Indication
Disease Entry ICD 11 Status REF
Type-2 diabetes 5A11 Phase 3 [1]
Cross-matching ID
PubChem CID
71402018
CAS Number
CAS 743438-45-1
TTD Drug ID
DM67P0F

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DOT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Patented Agent(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [4]
Pioglitazone DMKJ485 Amyotrophic lateral sclerosis 8B60.0 Approved [5]
Lobeglitazone DMHY3IP Type-2 diabetes 5A11 Approved [6]
Rosiglitazone XR DMT45MU Type-2 diabetes 5A11 Approved [7]
Thiazolidinedione DMC1NBW Alzheimer disease 8A20 Approved [5]
Glitazone DMDN4A1 N. A. N. A. Phase 4 [8]
MURAGLITAZAR DMG3NFZ N. A. N. A. Phase 3 [9]
Rivoglitazone DMBY31K Ocular inflammation 9C61.24 Phase 3 [10]
Balaglitazone DMXBHR6 Type-1 diabetes 5A10 Phase 3 [11]
Ragaglitazar DMFSHEM Type-1 diabetes 5A10 Phase 3 [12]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Lobeglitazone DMHY3IP Type-2 diabetes 5A11 Approved [6]
Fenofibrate DMFKXDY Coronary atherosclerosis Approved [8]
Bezafibrate DMZDCS0 Hypercholesterolaemia 5C80.0 Approved [13]
Ciprofibrate DMGC5DB Hyperlipoproteinemia 5C80 Approved [8]
Pemafibrate DMD1VZL Hyperlipidemia 5C80.Z Approved [14]
MURAGLITAZAR DMG3NFZ N. A. N. A. Phase 3 [9]
Ragaglitazar DMFSHEM Type-1 diabetes 5A10 Phase 3 [12]
TESAGLITAZAR DMGRBN5 Type-1 diabetes 5A10 Phase 3 [15]
GFT-505 DM7ZOAE Non-alcoholic steatohepatitis DB92.1 Phase 3 [16]
ZYH-1 DMMBJYC Lipid metabolism disorder 5C52.Z Phase 3 [17]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Quercetin DM3NC4M Obesity 5B81 Approved [18]
obeticholic acid DM3Q1SM Primary biliary cholangitis DB96.1 Approved [19]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [20]
Isotretinoin DM4QTBN Acne vulgaris ED80 Approved [21]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [22]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [23]
Rosiglitazone DMILWZR Chronic kidney disease GB61 Approved [3]
Cupric Sulfate DMP0NFQ Fungal infection 1F29-1F2F Approved [24]
Arsenic DMTL2Y1 N. A. N. A. Approved [25]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [26]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [27]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [28]
Quercetin DM3NC4M Obesity 5B81 Approved [29]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [30]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [31]
Glucosamine DM4ZLFD Osteoarthritis FA00-FA05 Approved [32]
Isoniazid DM5JVS3 Latent tuberculosis infection Approved [33]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [34]
Aspirin DM672AH Acute coronary syndrome BA41 Approved [35]
Stavudine DM6DEK9 Human immunodeficiency virus infection 1C62 Approved [36]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Epinephrine DM3KJBC Acute asthma CA23 Approved [37]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [38]
Adenosine triphosphate DM79F6G Malnutrition 5B50-5B71 Approved [37]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [23]
Rosiglitazone DMILWZR Chronic kidney disease GB61 Approved [3]
Dexamethasone DMMWZET Acute adrenal insufficiency Approved [39]
Vitamin B3 DMQVRZH Chronic renal failure GB61.Z Approved [40]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [41]
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [42]
PMID28460551-Compound-2 DM4DOUB N. A. N. A. Patented [43]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
obeticholic acid DM3Q1SM Primary biliary cholangitis DB96.1 Approved [19]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [20]
Testosterone DM7HUNW Hot flushes GA30 Approved [44]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [22]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [23]
Ivermectin DMDBX5F Intestinal strongyloidiasis due to nematode parasite 1F6B Approved [45]
Fenofibrate DMFKXDY Coronary atherosclerosis Approved [46]
Ciprofibrate DMGC5DB Hyperlipoproteinemia 5C80 Approved [47]
Capsaicin DMGMF6V Back pain ME84.Z Approved [48]
Sodium Acetate Anhydrous DMH21E0 Hyponatraemia 5C72 Approved [49]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Peroxisome proliferator-activated receptor alpha (PPARA) TTJ584C PPARA_HUMAN Modulator [2]
Peroxisome proliferator-activated receptor gamma (PPAR-gamma) TTZMAO3 PPARG_HUMAN Modulator [2]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Hepatic triacylglycerol lipase (LIPC) OTZY5SC9 LIPC_HUMAN Gene/Protein Processing [3]
Hormone-sensitive lipase (LIPE) OTMMVJ8A LIPS_HUMAN Gene/Protein Processing [3]
Peroxisomal acyl-coenzyme A oxidase 1 (ACOX1) OTM0A0DY ACOX1_HUMAN Gene/Protein Processing [3]
Peroxisome proliferator-activated receptor gamma (PPARG) OTHMARHO PPARG_HUMAN Gene/Protein Processing [3]

References

1 ClinicalTrials.gov (NCT02173457) Study of Chiglitazar Compare With Sitagliptin in Type 2 Diabetes Patients. U.S. National Institutes of Health.
2 Determination of chiglitazar, a dual alpha/gamma peroxisome proliferator-activated receptor (PPAR) agonist, in human plasma by liquid chromatograph... Pharmazie. 2007 Nov;62(11):825-9.
3 In Vitro and In Vivo Characterizations of Chiglitazar, a Newly Identified PPAR Pan-Agonist. PPAR Res. 2012;2012:546548. doi: 10.1155/2012/546548. Epub 2012 Oct 22.
4 Expression of peroxisome proliferator-activated receptors (PPARs) in human urinary bladder carcinoma and growth inhibition by its agonists. Int J Cancer. 2003 May 1;104(5):597-602.
5 Functional PPAR-gamma receptor is a novel therapeutic target for ACTH-secreting pituitary adenomas. Nat Med. 2002 Nov;8(11):1281-7.
6 Tolerability and pharmacokinetics of lobeglitazone, a novel peroxisome proliferator-activated receptor-gamma agonist, after a single oral administration in healthy female subjects. Clin Drug Investig. 2014 Jul;34(7):467-74.
7 Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
8 Peroxisome proliferator-activated receptor alpha activators improve insulin sensitivity and reduce adiposity. J Biol Chem. 2000 Jun 2;275(22):16638-42.
9 Muraglitazar, a dual (alpha/gamma) PPAR activator: a randomized, double-blind, placebo-controlled, 24-week monotherapy trial in adult patients with... Clin Ther. 2005 Aug;27(8):1181-95.
10 A randomized-controlled trial to investigate the effects of rivoglitazone, a novel PPAR gamma agonist on glucose-lipid control in type 2 diabetes. Diabetes Obes Metab. 2011 Sep;13(9):806-13.
11 Balaglitazone: a second generation peroxisome proliferator-activated receptor (PPAR) gamma () agonist.Mini Rev Med Chem.2012 Feb;12(2):87-97.
12 Ragaglitazar: the pharmacokinetics, pharmacodynamics, and tolerability of a novel dual PPAR alpha and gamma agonist in healthy subjects and patients with type 2 diabetes. J Clin Pharmacol. 2003 Nov;43(11):1244-56.
13 Bezafibrate at clinically relevant doses decreases serum/liver triglycerides via down-regulation of sterol regulatory element-binding protein-1c in... Mol Pharmacol. 2009 Apr;75(4):782-92.
14 Pemafibrate: First Global Approval. Drugs. 2017 Oct;77(16):1805-1810.
15 Tesaglitazar, a dual PPAR-/ agonist, hamster carcinogenicity, investigative animal and clinical studies.Toxicol Pathol.2012;40(1):18-32.
16 Dual peroxisome proliferator-activated receptor / agonist GFT505 improves hepatic and peripheral insulin sensitivity in abdominally obese subjects.Diabetes Care.2013 Oct;36(10):2923-30.
17 Pharmacokinetics, safety, and tolerability of saroglitazar (ZYH1), a predominantly PPARalpha agonist with moderate PPARgamma agonist activity in healthy human subjects. Clin Drug Investig. 2013 Nov;33(11):809-16.
18 Comparison of phenotypic and transcriptomic effects of false-positive genotoxins, true genotoxins and non-genotoxins using HepG2 cells. Mutagenesis. 2011 Sep;26(5):593-604.
19 Pharmacotoxicology of clinically-relevant concentrations of obeticholic acid in an organotypic human hepatocyte system. Toxicol In Vitro. 2017 Mar;39:93-103.
20 Transcriptional and Metabolic Dissection of ATRA-Induced Granulocytic Differentiation in NB4 Acute Promyelocytic Leukemia Cells. Cells. 2020 Nov 5;9(11):2423. doi: 10.3390/cells9112423.
21 Temporal changes in gene expression in the skin of patients treated with isotretinoin provide insight into its mechanism of action. Dermatoendocrinol. 2009 May;1(3):177-87.
22 Comparison of HepG2 and HepaRG by whole-genome gene expression analysis for the purpose of chemical hazard identification. Toxicol Sci. 2010 May;115(1):66-79.
23 Integrated 'omics analysis reveals new drug-induced mitochondrial perturbations in human hepatocytes. Toxicol Lett. 2018 Jun 1;289:1-13.
24 Physiological and toxicological transcriptome changes in HepG2 cells exposed to copper. Physiol Genomics. 2009 Aug 7;38(3):386-401.
25 Prenatal arsenic exposure and the epigenome: identifying sites of 5-methylcytosine alterations that predict functional changes in gene expression in newborn cord blood and subsequent birth outcomes. Toxicol Sci. 2015 Jan;143(1):97-106. doi: 10.1093/toxsci/kfu210. Epub 2014 Oct 10.
26 Multiple microRNAs function as self-protective modules in acetaminophen-induced hepatotoxicity in humans. Arch Toxicol. 2018 Feb;92(2):845-858.
27 COX-2 and PPAR-gama confer cannabidiol-induced apoptosis of human lung cancer cells. Mol Cancer Ther. 2013 Jan;12(1):69-82.
28 Protective effects of myricitrin against osteoporosis via reducing reactive oxygen species and bone-resorbing cytokines. Toxicol Appl Pharmacol. 2014 Nov 1;280(3):550-60.
29 The effect of quercetin and kaempferol aglycones and glucuronides on peroxisome proliferator-activated receptor-gamma (PPAR-). Food Funct. 2015 Apr;6(4):1098-107. doi: 10.1039/c5fo00076a.
30 Induction of solid tumor differentiation by the peroxisome proliferator-activated receptor-gamma ligand troglitazone in patients with liposarcoma. Proc Natl Acad Sci U S A. 1999 Mar 30;96(7):3951-6. doi: 10.1073/pnas.96.7.3951.
31 Development of a neural teratogenicity test based on human embryonic stem cells: response to retinoic acid exposure. Toxicol Sci. 2011 Dec;124(2):370-7.
32 Glucosamine sulfate reduces prostaglandin E(2) production in osteoarthritic chondrocytes through inhibition of microsomal PGE synthase-1. J Rheumatol. 2012 Mar;39(3):635-44. doi: 10.3899/jrheum.110621. Epub 2011 Nov 15.
33 Isoniazid suppresses antioxidant response element activities and impairs adipogenesis in mouse and human preadipocytes. Toxicol Appl Pharmacol. 2013 Dec 15;273(3):435-41. doi: 10.1016/j.taap.2013.10.005. Epub 2013 Oct 12.
34 Regulatory role of KEAP1 and NRF2 in PPAR expression and chemoresistance in human non-small-cell lung carcinoma cells. Free Radic Biol Med. 2012 Aug 15;53(4):758-68. doi: 10.1016/j.freeradbiomed.2012.05.041. Epub 2012 Jun 7.
35 Aspirin inhibits MMP-9 mRNA expression and release via the PPARalpha/gamma and COX-2/mPGES-1-mediated pathways in macrophages derived from THP-1 cells. Biomed Pharmacother. 2010 Feb;64(2):118-23. doi: 10.1016/j.biopha.2009.04.033. Epub 2009 Oct 17.
36 Mitochondrial proliferation, DNA depletion and adipocyte differentiation in subcutaneous adipose tissue of HIV-positive HAART recipients. Antivir Ther. 2003 Aug;8(4):323-31.
37 Hormone-sensitive lipase in human adipose tissue, isolated adipocytes, and cultured adipocytes. Pediatr Res. 1982 Dec;16(12):982-8. doi: 10.1203/00006450-198212000-00002.
38 Adipocyte differentiation, mitochondrial gene expression and fat distribution: differences between zidovudine and tenofovir after 6 months. Antivir Ther. 2009;14(8):1089-100. doi: 10.3851/IMP1457.
39 Identification of mechanisms of action of bisphenol a-induced human preadipocyte differentiation by transcriptional profiling. Obesity (Silver Spring). 2014 Nov;22(11):2333-43.
40 Effects of extended-release niacin on lipid profile and adipocyte biology in patients with impaired glucose tolerance. Atherosclerosis. 2009 Jul;205(1):207-13. doi: 10.1016/j.atherosclerosis.2008.11.026. Epub 2008 Dec 3.
41 Activation of AIFM2 enhances apoptosis of human lung cancer cells undergoing toxicological stress. Toxicol Lett. 2016 Sep 6;258:227-236.
42 Bringing in vitro analysis closer to in vivo: studying doxorubicin toxicity and associated mechanisms in 3D human microtissues with PBPK-based dose modelling. Toxicol Lett. 2018 Sep 15;294:184-192.
43 Cell-based two-dimensional morphological assessment system to predict cancer drug-induced cardiotoxicity using human induced pluripotent stem cell-derived cardiomyocytes. Toxicol Appl Pharmacol. 2019 Nov 15;383:114761. doi: 10.1016/j.taap.2019.114761. Epub 2019 Sep 15.
44 The exosome-like vesicles derived from androgen exposed-prostate stromal cells promote epithelial cells proliferation and epithelial-mesenchymal transition. Toxicol Appl Pharmacol. 2021 Jan 15;411:115384. doi: 10.1016/j.taap.2020.115384. Epub 2020 Dec 25.
45 Quantitative proteomics reveals a broad-spectrum antiviral property of ivermectin, benefiting for COVID-19 treatment. J Cell Physiol. 2021 Apr;236(4):2959-2975. doi: 10.1002/jcp.30055. Epub 2020 Sep 22.
46 Linalool is a PPARalpha ligand that reduces plasma TG levels and rewires the hepatic transcriptome and plasma metabolome. J Lipid Res. 2014 Jun;55(6):1098-110.
47 Fish oil and fenofibrate prevented phosphorylation-dependent hepatic sortilin 1 degradation in Western diet-fed mice. J Biol Chem. 2014 Aug 8;289(32):22437-49. doi: 10.1074/jbc.M114.548933. Epub 2014 Jul 1.
48 Induction of the endoplasmic reticulum stress protein GADD153/CHOP by capsaicin in prostate PC-3 cells: a microarray study. Biochem Biophys Res Commun. 2008 Aug 8;372(4):785-91.
49 Transcriptional Regulation of Human Arylamine N-Acetyltransferase 2 Gene by Glucose and Insulin in Liver Cancer Cell Lines. Toxicol Sci. 2022 Nov 23;190(2):158-172. doi: 10.1093/toxsci/kfac103.