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

General Information of Drug (ID: DMQTAGO)

• Drug Name: BMS-201038 Drug Info
• Synonyms: AEGR 733; AEGR733; BMS 201038; BMS 201238; BMS201038; AEGR-733; BMS 201038-01

Indication

Disease Entry	ICD 11	Status	REF
Familial hypercholesterolemia	5C80.00	Approved	[1]

• Cross-matching ID:
  PubChem CID: 9853053
  ChEBI ID: CHEBI:72297
  CAS Number: CAS 182431-12-5
  TTD Drug ID: DMQTAGO

Molecule-Related Drug Atlas

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

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
SLx-4090	DMM3AI8	Diabetic complication	5A2Y	Phase 2	[5]
Granotapide	DMMZQ7V	Hyperlipidaemia	5C80	Phase 2	[6]
Implitapide	DMTN16K	Hyperlipidaemia	5C80	Phase 2	[7]
JNJ-16269110	DMPFG7H	Type-2 diabetes	5A11	Phase 2	[8]
KD020	DMZ416B	Kidney disease	GC2Z	Phase 1/2	[9]
GR-328713	DMUANK9	Arteriosclerosis	BD40	Discontinued in Phase 1	[10]
DIRLOTAPIDE	DM2MV9O	Discovery agent	N.A.	Investigative	[11]

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	[3]
Hydrogen peroxide	DM1NG5W	Infectious disease	1A00-CA43.1	Approved	[12]
Sulindac	DM2QHZU	Acute myelogenous leukaemia	2A41	Approved	[3]
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	[3]
Glucosamine	DM4ZLFD	Osteoarthritis	FA00-FA05	Approved	[16]
Rifampicin	DM5DSFZ	Non-insulin dependent diabetes	5A11	Approved	[3]
Aluminium	DM6ECN9	Hyperhidrosis	EE00	Approved	[17]

Drug(s) Affected By Cytochrome P450 3A4 (CYP3A4)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Eplerenone	DMF0NQR	Heart failure	BD10-BD13	Approved	[18]
Cannabidiol	DM0659E	Dravet syndrome	8A61.11	Approved	[19]
Isotretinoin	DM4QTBN	Acne vulgaris	ED80	Approved	[20]
Voriconazole	DMAOL2S	Aspergillosis	1F20	Approved	[21]
Proguanil	DMBL79I	Malaria	1F40-1F45	Approved	[22]
Ivermectin	DMDBX5F	Intestinal strongyloidiasis due to nematode parasite	1F6B	Approved	[22]
Loratadine	DMF3AN7	Allergy	4A80-4A85	Approved	[23]
Nelfinavir mesylate	DMFX6G8	N. A.	N. A.	Approved	[24]
Capsaicin	DMGMF6V	Back pain	ME84.Z	Approved	[25]
Axitinib	DMGVH6N	Renal cell carcinoma	2C90	Approved	[26]

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]
Cytochrome P450 3A4 (CYP3A4)	OTQGYY83	CP3A4_HUMAN	Drug Response	[4]

References

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• [2] Dyslipidemia and cardiovascular diseases. Curr Opin Lipidol. 2009 Apr;20(2):157-8.
• [3] 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.
• [4] ADReCS-Target: target profiles for aiding drug safety research and application. Nucleic Acids Res. 2018 Jan 4;46(D1):D911-D917. doi: 10.1093/nar/gkx899.
• [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] 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.
• [7] Novel nonstatin strategies to lower low-density lipoprotein cholesterol. Curr Atheroscler Rep. 2009 Jan;11(1):67-70.
• [8] 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.
• [9] Clinical pipeline report, company report or official report of Kadmon Pharmaceuticals.
• [10] Patent CN101237870 B.
• [11] 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.
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• [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.
• [18] The relative role of CYP3A4 and CYP3A5 in eplerenone metabolism. Toxicol Lett. 2019 Oct 15;315:9-13.
• [19] Characterization of the structural determinants required for potent mechanism-based inhibition of human cytochrome P450 1A1 by cannabidiol. Chem Biol Interact. 2014 May 25;215:62-8.
• [20] Retinoids activate the RXR/SXR-mediated pathway and induce the endogenous CYP3A4 activity in Huh7 human hepatoma cells. Toxicol Sci. 2006 Jul;92(1):51-60.
• [21] The novel azole R126638 is a selective inhibitor of ergosterol synthesis in Candida albicans, Trichophyton spp., and Microsporum canis. Antimicrob Agents Chemother. 2004 Sep;48(9):3272-8.
• [22] Application of higher throughput screening (HTS) inhibition assays to evaluate the interaction of antiparasitic drugs with cytochrome P450s. Drug Metab Dispos. 2001 Jan;29(1):30-5.
• [23] Cetirizine and loratadine-based antihistamines with 5-lipoxygenase inhibitory activity. Bioorg Med Chem Lett. 2004 Nov 15;14(22):5591-4.
• [24] Mechanism-based inactivation of CYP3A by HIV protease inhibitors. J Pharmacol Exp Ther. 2005 Feb;312(2):583-91.
• [25] Studies of the toxicological potential of capsinoids, XIII: inhibitory effects of capsaicin and capsinoids on cytochrome P450 3A4 in human liver microsomes. Int J Toxicol. 2010 Mar;29(2 Suppl):22S-6S.
• [26] Investigation of the effects of axitinib on the pharmacokinetics of loperamide and its main metabolite N-demethylated loperamide in rats by UPLC-MS/MS. Chem Biol Interact. 2019 Sep 1;310:108744. doi: 10.1016/j.cbi.2019.108744. Epub 2019 Jul 9.