Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DMMZQ7V)

• Drug Name: Granotapide Drug Info
• Synonyms: JTT-130

Indication

Disease Entry	ICD 11	Status	REF
Hyperlipidaemia	5C80	Phase 2	[1]

• Cross-matching ID:
  PubChem CID: 11607299
  CAS Number: CAS 594842-13-4
  TTD Drug ID: DMMZQ7V

Molecule-Related Drug Atlas

Drug(s) Targeting Microsomal triglyceride transfer protein (MTTP)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
BMS-201038	DMQTAGO	Familial hypercholesterolemia	5C80.00	Approved	[4]
SLx-4090	DMM3AI8	Diabetic complication	5A2Y	Phase 2	[5]
Implitapide	DMTN16K	Hyperlipidaemia	5C80	Phase 2	[6]
JNJ-16269110	DMPFG7H	Type-2 diabetes	5A11	Phase 2	[7]
KD020	DMZ416B	Kidney disease	GC2Z	Phase 1/2	[8]
GR-328713	DMUANK9	Arteriosclerosis	BD40	Discontinued in Phase 1	[9]
DIRLOTAPIDE	DM2MV9O	Discovery agent	N.A.	Investigative	[10]

Drug(s) Affected By Apolipoprotein B-100 (APOB)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Indinavir	DM0T3YH	Human immunodeficiency virus infection	1C62	Approved	[11]
Hydrogen peroxide	DM1NG5W	Infectious disease	1A00-CA43.1	Approved	[12]
Sulindac	DM2QHZU	Acute myelogenous leukaemia	2A41	Approved	[11]
Simvastatin	DM30SGU	Arteriosclerosis	BD40	Approved	[13]
Quercetin	DM3NC4M	Obesity	5B81	Approved	[14]
obeticholic acid	DM3Q1SM	Primary biliary cholangitis	DB96.1	Approved	[15]
Troglitazone	DM3VFPD	Diabetic complication	5A2Y	Approved	[11]
Glucosamine	DM4ZLFD	Osteoarthritis	FA00-FA05	Approved	[16]
Rifampicin	DM5DSFZ	Non-insulin dependent diabetes	5A11	Approved	[11]
Aluminium	DM6ECN9	Hyperhidrosis	EE00	Approved	[17]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Microsomal triglyceride transfer protein (MTTP)	TTUS1RD	MTP_HUMAN	Inhibitor	[2]

Drug Off-Target (DOT)

DOT Name	DOT ID	UniProt ID	Interaction	REF
Apolipoprotein B-100 (APOB)	OTH0UOCZ	APOB_HUMAN	Protein Interaction/Cellular Processes	[3]

References

• [1] ClinicalTrials.gov (NCT00929539) Safety and Efficacy Study of JTT-130 in Obese Type 2 Diabetic Patients. U.S. National Institutes of Health.
• [2] JTT-130, a novel intestine-specific inhibitor of microsomal triglyceride transfer protein, suppresses food intake and gastric emptying with the elevation of plasma peptide YY and glucagon-like peptide-1 in a dietary fat-dependent manner. J Pharmacol Exp Ther. 2011 Mar;336(3):850-6.
• [3] Pharmacological characterization of diethyl-2-({3-dimethylcarbamoyl-4-[(4'-trifluoromethylbiphenyl-2-carbonyl)amino]phenyl}acetyloxymethyl)-2-phenylmalonate (JTT-130), an intestine-specific inhibitor of microsomal triglyceride transfer protein. J Pharmacol Exp Ther. 2011 Feb;336(2):321-7. doi: 10.1124/jpet.110.173807. Epub 2010 Oct 25.
• [4] Dyslipidemia and cardiovascular diseases. Curr Opin Lipidol. 2009 Apr;20(2):157-8.
• [5] A small-molecule inhibitor of enterocytic microsomal triglyceride transfer protein, SLx-4090: biochemical, pharmacodynamic, pharmacokinetic, and safety profile. J Pharmacol Exp Ther. 2011 Jun;337(3):775-85.
• [6] Novel nonstatin strategies to lower low-density lipoprotein cholesterol. Curr Atheroscler Rep. 2009 Jan;11(1):67-70.
• [7] ClinicalTrials.gov (NCT00672386) A Study of the Safety and Effectiveness of a R256918 in Patients With Type 2 Diabetes. U.S. National Institutes of Health.
• [8] Clinical pipeline report, company report or official report of Kadmon Pharmaceuticals.
• [9] Patent CN101237870 B.
• [10] In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlota... Bioorg Med Chem Lett. 2007 Apr 1;17(7):1996-9.
• [11] Drug-induced hepatic steatosis in absence of severe mitochondrial dysfunction in HepaRG cells: proof of multiple mechanism-based toxicity. Cell Biol Toxicol. 2021 Apr;37(2):151-175. doi: 10.1007/s10565-020-09537-1. Epub 2020 Jun 14.
• [12] Global gene expression analysis reveals differences in cellular responses to hydroxyl- and superoxide anion radical-induced oxidative stress in caco-2 cells. Toxicol Sci. 2010 Apr;114(2):193-203. doi: 10.1093/toxsci/kfp309. Epub 2009 Dec 31.
• [13] Effect of simvastatin treatment on the electronegative low-density lipoprotein present in patients with heterozygous familial hypercholesterolemia. Am J Cardiol. 1999 Sep 15;84(6):655-9. doi: 10.1016/s0002-9149(99)00411-7.
• [14] 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.
• [15] Pharmacotoxicology of clinically-relevant concentrations of obeticholic acid in an organotypic human hepatocyte system. Toxicol In Vitro. 2017 Mar;39:93-103.
• [16] Glucosamine-induced endoplasmic reticulum stress promotes ApoB100 degradation: evidence for Grp78-mediated targeting to proteasomal degradation. Arterioscler Thromb Vasc Biol. 2005 Mar;25(3):571-7. doi: 10.1161/01.ATV.0000154142.61859.94. Epub 2004 Dec 23.
• [17] Aluminum-induced mitochondrial dysfunction leads to lipid accumulation in human hepatocytes: a link to obesity. Cell Physiol Biochem. 2007;20(5):627-38. doi: 10.1159/000107546.