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

General Information of Drug (ID: DM52HUD)

Drug Name

Dexloxiglumide Drug Info

Synonyms

Dexloxiglumide; 119817-90-2; (R)-4-(3,4-Dichlorobenzamido)-5-((3-methoxypropyl)(pentyl)amino)-5-oxopentanoic acid; UNII-69DY40RH9B; CR-2017; 69DY40RH9B; Dexloxiglumidum; Dexloxiglumida; Dexloxiglumide [INN]; Dexloxiglumidum [INN-Latin]; Dexloxiglumida [INN-Spanish]; PubChem16049; AC1Q3MXI; GTPL889; SCHEMBL366142; CHEMBL550781; AC1L24A8; DTXSID50152604; MolPort-006-170-001; CHEBI:135747; ZINC3801027; KS-000007QQ; AKOS000279054; PB12713; DB04856; CC-26372; AJ-45649; AK129760; AS-35102; KB-210163; AX8123879; CS-0054881; FT-0603098; Q-4119

Indication

Disease Entry	ICD 11	Status	REF
Pancreatic malfunction	DC30-DC3Z	Phase 2	[1]

Cross-matching ID

PubChem CID: 65937
ChEBI ID: CHEBI:135747
CAS Number: CAS 119817-90-2
TTD Drug ID: DM52HUD
INTEDE Drug ID: DR0470

Molecule-Related Drug Atlas

Molecule Type:

DTT

DME

Drug Status:

Approved Drug(s)

Clinical Trial Drug(s)

Discontinued Drug(s)

Download the Complete Related Drug List

Drug(s) Targeting Gastrin/cholecystokinin type B receptor (CCKBR)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Pentagastrin	DMRCLZB	Diagnostic imaging	N.A.	Approved	[6]
Ceruletide	DM2WE5K	Caerulein stimulated gastric and pancreatic secretion	5A4Y	Approved	[7]
GASTRAZOLE	DMO3ITF	Duodenal ulcer	DA63	Phase 3	[8]
Spiroglumide	DM7NJWY	Stomach disease	DA43-DA4Y	Phase 2	[9]
TT-223	DMCDMFP	Type-1 diabetes	5A10	Phase 2	[10]
Z 360	DM2M80G	Discovery agent	N.A.	Phase 2	[11]
S-0509	DM4KWEF	Ulcerative colitis	DD71	Phase 2	[12]
YF-476	DM54MAJ	Stomach ulcer	DA60.Z	Phase 2	[13]
Itriglumide	DM5UFRO	Anxiety disorder	6B00-6B0Z	Phase 2	[14]
Demogastrin	DMTULGS	Thyroid cancer	2D10	Phase 1	[15]
------------------------------------------------------------------------------------


⏷ Show the Full List of 10 Drug(s)

Drug(s) Targeting Cholecystokinin receptor type A (CCKAR)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
proglumide	DM4MF9V	Influenza virus infection	1E30-1E32	Phase 2	[16]
Lintitript	DMS5X94	Obesity	5B81	Discontinued in Phase 2	[17]
Tarazepide	DMX6ZYE	Gastrointestinal disease	DE2Z	Discontinued in Phase 2	[18]
GI 181771	DMIUFS4	Obesity	5B81	Discontinued in Phase 2	[19]
Pranazepide	DMP43IR	Pancreatic malfunction	DC30-DC3Z	Discontinued in Phase 2	[20]
CE-326597	DMXO49B	Obesity	5B81	Discontinued in Phase 2	[21]
UCL-2000; butabindide	DML51D0	Obesity	5B81	Discontinued in Phase 1	[22]
SSR-125180	DMSOBW2	Obesity	5B81	Discontinued in Phase 1	[23]
T-0632	DML4M5K	Pancreatic malfunction	DC30-DC3Z	Discontinued in Phase 1	[24]
SR-146131	DML7KCO	Obesity	5B81	Discontinued in Phase 1	[25]
------------------------------------------------------------------------------------


⏷ Show the Full List of 10 Drug(s)

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

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Doxorubicin	DMVP5YE	Acute myelogenous leukaemia	2A41	Approved	[26]
Progesterone	DMUY35B	Amenorrhea	GA20.0	Approved	[27]
Tamoxifen	DMLB0EZ	Breast cancer	2C60-2C65	Approved	[28]
Estradiol	DMUNTE3	Acne vulgaris	ED80	Approved	[29]
Acetaminophen	DMUIE76	Allergic rhinitis	CA08.0	Approved	[30]
Imatinib	DM7RJXL	Acute lymphoblastic leukaemia	2A85	Approved	[31]
Etoposide	DMNH3PG	Acute myelogenous leukaemia	2A41	Approved	[32]
Zidovudine	DM4KI7O	Human immunodeficiency virus infection	1C62	Approved	[33]
Prasterone	DM67VKL	Chronic obstructive pulmonary disease	CA22	Approved	[27]
Verapamil	DMA7PEW	Angina pectoris	BA40	Approved	[34]
------------------------------------------------------------------------------------


⏷ Show the Full List of 10 Drug(s)

Drug(s) Metabolized By Cytochrome P450 3A5 (CYP3A5)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Doxorubicin	DMVP5YE	Acute myelogenous leukaemia	2A41	Approved	[35]
Progesterone	DMUY35B	Amenorrhea	GA20.0	Approved	[36]
Tamoxifen	DMLB0EZ	Breast cancer	2C60-2C65	Approved	[37]
Estradiol	DMUNTE3	Acne vulgaris	ED80	Approved	[38]
Acetaminophen	DMUIE76	Allergic rhinitis	CA08.0	Approved	[39]
Sulfasalazine	DMICA9H	Irritable bowel syndrome	DD91.0	Approved	[40]
Imatinib	DM7RJXL	Acute lymphoblastic leukaemia	2A85	Approved	[41]
Etoposide	DMNH3PG	Acute myelogenous leukaemia	2A41	Approved	[42]
Verapamil	DMA7PEW	Angina pectoris	BA40	Approved	[43]
Sorafenib	DMS8IFC	Adenocarcinoma	2D40	Approved	[38]
------------------------------------------------------------------------------------


⏷ Show the Full List of 10 Drug(s)

Drug(s) Metabolized By Cytochrome P450 2C9 (CYP2C9)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Progesterone	DMUY35B	Amenorrhea	GA20.0	Approved	[44]
Tamoxifen	DMLB0EZ	Breast cancer	2C60-2C65	Approved	[45]
Estradiol	DMUNTE3	Acne vulgaris	ED80	Approved	[46]
Acetaminophen	DMUIE76	Allergic rhinitis	CA08.0	Approved	[47]
Imatinib	DM7RJXL	Acute lymphoblastic leukaemia	2A85	Approved	[48]
Zidovudine	DM4KI7O	Human immunodeficiency virus infection	1C62	Approved	[47]
Verapamil	DMA7PEW	Angina pectoris	BA40	Approved	[49]
Diclofenac	DMPIHLS	Chronic renal failure	GB61.Z	Approved	[50]
Estrone	DM5T6US	Acne vulgaris	ED80	Approved	[51]
Valproate	DMCFE9I	Epilepsy	8A60-8A68	Approved	[52]
------------------------------------------------------------------------------------


⏷ Show the Full List of 10 Drug(s)

Drug(s) Metabolized By Cytochrome P450 2B6 (CYP2B6)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Tamoxifen	DMLB0EZ	Breast cancer	2C60-2C65	Approved	[53]
Verapamil	DMA7PEW	Angina pectoris	BA40	Approved	[47]
Diclofenac	DMPIHLS	Chronic renal failure	GB61.Z	Approved	[54]
Estrone	DM5T6US	Acne vulgaris	ED80	Approved	[46]
Valproate	DMCFE9I	Epilepsy	8A60-8A68	Approved	[55]
Irinotecan	DMP6SC2	Adenocarcinoma	2D40	Approved	[56]
Propofol	DMB4OLE	Anaesthesia	9A78.6	Approved	[57]
Nicotine	DMWX5CO	Lung cancer	2C25.0	Approved	[58]
Phenytoin	DMNOKBV	Epilepsy	8A60-8A68	Approved	[59]
Amitriptyline	DMK7F9S	Depression	6A70-6A7Z	Approved	[60]
------------------------------------------------------------------------------------


⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Download the Complete Interaction Atlas for Visualization in Cytoscape

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Cholecystokinin receptor type A (CCKAR)	TTCG0AL	CCKAR_HUMAN	Inhibitor	[2]
Gastrin/cholecystokinin type B receptor (CCKBR)	TTVFO0U	GASR_HUMAN	Inhibitor	[3]

------------------------------------------------------------------------------------

Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	MOA	REF
Cytochrome P450 3A4 (CYP3A4)	DE4LYSA	CP3A4_HUMAN	Substrate	[4]
Cytochrome P450 2C9 (CYP2C9)	DE5IED8	CP2C9_HUMAN	Substrate	[4]
Cytochrome P450 3A5 (CYP3A5)	DEIBDNY	CP3A5_HUMAN	Substrate	[4]
Cytochrome P450 2B6 (CYP2B6)	DEPKLMQ	CP2B6_HUMAN	Substrate	[5]

------------------------------------------------------------------------------------

References

1	Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
2	Full agonists of CCK8 containing a nonhydrolyzable sulfated tyrosine residue. J Med Chem. 1989 Feb;32(2):445-9.
3	Synthesis and stereochemical structure-activity relationships of 1,3-dioxoperhydropyrido[1,2-c]pyrimidine derivatives: potent and selective cholecy... J Med Chem. 1997 Oct 10;40(21):3402-7.
4	Pharmacokinetic profile of dexloxiglumide. Clin Pharmacokinet. 2006;45(12):1177-88.
5	Effect of azole antifungals ketoconazole and fluconazole on the pharmacokinetics of dexloxiglumide. Br J Clin Pharmacol. 2005 Nov;60(5):498-507.
6	Functional interactions between endocannabinoid and CCK neurotransmitter systems may be critical for extinction learning. Neuropsychopharmacology. 2009 Jan;34(2):509-21.
7	Comparison of postprandial and ceruletide serum bile acid stimulation in dogs. J Vet Intern Med. 2008 Jul-Aug;22(4):873-8.
8	Gastrazole (JB95008), a novel CCK2/gastrin receptor antagonist, in the treatment of advanced pancreatic cancer: results from two randomised controlled trials. Br J Cancer. 2006 April 24; 94(8): 1107-1115.
9	Effect of dexloxiglumide and spiroglumide, two new CCK-receptor antagonists, on gastric emptying and secretion in the rat: evaluation of their receptor selectivity in vivo. Aliment Pharmacol Ther. 1996 Jun;10(3):411-9.
10	The effect of glucagon-like peptide-1 on energy expenditure and substrate metabolism in humans. Int J Obes Relat Metab Disord. 2000 Mar;24(3):288-98.
11	Z-360, a novel cholecystokinin-2/gastrin receptor antagonist, inhibits gemcitabine-induced expression of the vascular endothelial growth factor gen... Biol Pharm Bull. 2010;33(2):216-22.
12	Selective action of a CCK-B/gastrin receptor antagonist, S-0509, on pentagastrin-, peptone meal- and beer-stimulated gastric acid secretion in dogs. Aliment Pharmacol Ther. 2000 Apr;14(4):479-88.
13	CCK-B receptor antagonist YF476 inhibits pancreatic enzyme secretion at a duodenal level in pigs. Scand J Gastroenterol. 2004 Sep;39(9):886-90.
14	Role of CCK/gastrin receptors in gastrointestinal/metabolic diseases and results of human studies using gastrin/CCK receptor agonists/antagonists in these diseases. Curr Top Med Chem. 2007; 7(12): 1211-1231.
15	Demonstration of new sites of expression of the CCK-B/gastrin receptor in pancreatic acinar AR42J cells using immunoelectron microscopy. Regul Pept. 1999 Oct 22;84(1-3):81-9.
16	Pharmacological properties of lorglumide as a member of a new class of cholecystokinin antagonists. Arzneimittelforschung. 1987 Nov;37(11):1265-8.
17	A cholecystokinin-1 receptor agonist (CCK-8) mediates increased permeability of brain barriers to leptin. Br J Pharmacol. 2008 Jul;154(5):1009-15.
18	Melatonin as modulator of pancreatic enzyme secretion and pancreatoprotector. J Physiol Pharmacol. 2007 Dec;58 Suppl 6:65-80.
19	Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2003 Jul-Aug;25(6):483-506.
20	Dual CCK-A and -B receptor antagonists (I) C9-methyl-1,4-benzodiazepines, Bioorg. Med. Chem. Lett. 7(2):169-174 (1997).
21	Obesity Pharmacotherapy: Current Perspectives and Future Directions. Curr Cardiol Rev. 2013 February; 9(1): 33-54.
22	Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60.
23	US patent application no. 8,748,419, Antagonists.
24	Effect of T-0632, a cholecystokininA receptor antagonist, on experimental acute pancreatitis. Jpn J Pharmacol. 1997 Feb;73(2):105-12.
25	SR146131: a new potent, orally active, and selective nonpeptide cholecystokinin subtype 1 receptor agonist. I. In vitro studies. J Pharmacol Exp Ther. 1999 May;289(2):742-51.
26	Expression levels and activation of a PXR variant are directly related to drug resistance in osteosarcoma cell lines. Cancer. 2007 Mar 1;109(5):957-65.
27	Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
28	Comprehensive evaluation of tamoxifen sequential biotransformation by the human cytochrome P450 system in vitro: prominent roles for CYP3A and CYP2D6. J Pharmacol Exp Ther. 2004 Sep;310(3):1062-75.
29	Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
30	Metabolic interactions between acetaminophen (paracetamol) and two flavonoids, luteolin and quercetin, through in-vitro inhibition studies. J Pharm Pharmacol. 2017 Dec;69(12):1762-1772.
31	Potent mechanism-based inhibition of CYP3A4 by imatinib explains its liability to interact with CYP3A4 substrates. Br J Pharmacol. 2012 Apr;165(8):2787-98.
32	Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
33	The metabolism of zidovudine by human liver microsomes in vitro: formation of 3'-amino-3'-deoxythymidine. Biochem Pharmacol. 1994 Jul 19;48(2):267-76.
34	Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675.
35	Drug related genetic polymorphisms affecting adverse reactions to methotrexate, vinblastine, doxorubicin and cisplatin in patients with urothelial cancer. J Urol. 2008 Dec;180(6):2389-95.
36	Human prostate CYP3A5: identification of a unique 5'-untranslated sequence and characterization of purified recombinant protein. Biochem Biophys Res Commun. 1999 Jul 14;260(3):676-81.
37	Polymorphisms in cytochrome P4503A5 (CYP3A5) may be associated with race and tumor characteristics, but not metabolism and side effects of tamoxifen in breast cancer patients. Cancer Lett. 2005 Jan 10;217(1):61-72.
38	Drug Interactions Flockhart Table
39	Induction of hepatic CYP2E1 by a subtoxic dose of acetaminophen in rats: increase in dichloromethane metabolism and carboxyhemoglobin elevation. Drug Metab Dispos. 2007 Oct;35(10):1754-8.
40	Urinary 6 beta-hydroxycortisol excretion in rheumatoid arthritis. Br J Rheumatol. 1997 Jan;36(1):54-8.
41	Clinical pharmacokinetics of imatinib. Clin Pharmacokinet. 2005;44(9):879-94.
42	Kinetics and regulation of cytochrome P450-mediated etoposide metabolism. Drug Metab Dispos. 2004 Sep;32(9):993-1000.
43	Differential mechanism-based inhibition of CYP3A4 and CYP3A5 by verapamil. Drug Metab Dispos. 2005 May;33(5):664-71.
44	Progesterone and testosterone hydroxylation by cytochromes P450 2C19, 2C9, and 3A4 in human liver microsomes. Arch Biochem Biophys. 1997 Oct 1;346(1):161-9.
45	Tamoxifen inhibits cytochrome P450 2C9 activity in breast cancer patients. J Chemother. 2006 Aug;18(4):421-4.
46	Characterization of the oxidative metabolites of 17beta-estradiol and estrone formed by 15 selectively expressed human cytochrome p450 isoforms. Endocrinology. 2003 Aug;144(8):3382-98.
47	Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448.
48	Drug-drug interactions with imatinib: an observational study. Medicine (Baltimore). 2016 Oct;95(40):e5076.
49	Drug interactions with calcium channel blockers: possible involvement of metabolite-intermediate complexation with CYP3A. Drug Metab Dispos. 2000 Feb;28(2):125-30.
50	New insights into the structural features and functional relevance of human cytochrome P450 2C9. Part I. Curr Drug Metab. 2009 Dec;10(10):1075-126.
51	A potential role for the estrogen-metabolizing cytochrome P450 enzymes in human breast carcinogenesis. Breast Cancer Res Treat. 2003 Dec;82(3):191-7.
52	A mechanistic approach to antiepileptic drug interactions. Ann Pharmacother. 1998 May;32(5):554-63.
53	Effect of tamoxifen on the enzymatic activity of human cytochrome CYP2B6. J Pharmacol Exp Ther. 2002 Jun;301(3):945-52.
54	Hepatic metabolism of diclofenac: role of human CYP in the minor oxidative pathways. Biochem Pharmacol. 1999 Sep 1;58(5):787-96.
55	Insights into CYP2B6-mediated drug-drug interactions. Acta Pharm Sin B. 2016 Sep;6(5):413-425.
56	Drugs that may have potential CYP2B6 interactions.
57	Involvement of human cytochrome P450 2B6 in the omega- and 4-hydroxylation of the anesthetic agent propofol. Xenobiotica. 2007 Jul;37(7):717-24.
58	Nicotine and 4-(methylnitrosamino)-1-(3-pyridyl)-butanone metabolism by cytochrome P450 2B6. Drug Metab Dispos. 2005 Dec;33(12):1760-4.
59	PharmGKB summary: phenytoin pathway. Pharmacogenet Genomics. 2012 Jun;22(6):466-70.
60	Application of the relative activity factor approach in scaling from heterologously expressed cytochromes p450 to human liver microsomes: studies on amitriptyline as a model substrate. J Pharmacol Exp Ther. 2001 Apr;297(1):326-37.