General Information of Drug (ID: DMFLJHQ)

Drug Name
LCQ908 Drug Info
Synonyms
Pradigastat; LCQ-908; 956136-95-1; UNII-2U23G6VNUZ; LCQ908; 2U23G6VNUZ; LCQ 908; Pradigastat [USAN:INN]; LCQ 908NXA; 2-[4-[4-[5-[[6-(trifluoromethyl)pyridin-3-yl]amino]pyridin-2-yl]phenyl]cyclohexyl]acetic acid; 2-{4-[4-(5-{[6-(trifluoromethyl)pyridin-3-yl]amino}pyridin-2-yl)phenyl]cyclohexyl}acetic acid; Pradigastat (USAN); LCQ908-NXA; SCHEMBL180536; GTPL7830; SCHEMBL1289309; CHEMBL2364624; SCHEMBL18286769; SCHEMBL16104874; GXALXAKNHIROPE-UHFFFAOYSA-N; BCP21089; ZINC253387875; AKOS027338695; DB12866; SB16971; CS-1222
Indication
Disease Entry ICD 11 Status REF
Familial chylomicronemia syndrome 5C80 Phase 3 [1]
Hepatitis C virus infection 1E51.1 Phase 3 [1]
Hypertriglyceridemia 5C80.1 Phase 3 [2]
Cross-matching ID
PubChem CID
53387035
CAS Number
CAS 956136-95-1
TTD Drug ID
DMFLJHQ
INTEDE Drug ID
DR1877

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DME
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Patented Agent(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Hesperetin DMKER83 High blood cholesterol level 5C80.00 Approved [5]
AZD7687 DMS9I6A Diabetic complication 5A2Y Phase 1 [6]
P-7435 DMNZQU5 Diabetic complication 5A2Y Phase 1 [7]
PMID25470667-Compound-Figure4-1A DMMVQW8 N. A. N. A. Patented [8]
Azole derivative 7 DMVUJGI N. A. N. A. Patented [8]
Carbamide derivative 3 DM4ISCQ N. A. N. A. Patented [8]
T863 DMX41ZF Discovery agent N.A. Patented [8]
Benzamide derivative 19 DM5YNTM N. A. N. A. Patented [8]
Lactam derivative 5 DMX5FYZ N. A. N. A. Patented [8]
Pyridine-carboximide derivative 2 DMHXWZB N. A. N. A. Patented [8]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [9]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [10]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [11]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [12]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [13]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [14]
Mycophenolate mofetil DMPQAGE Hepatosplenic T-cell lymphoma Approved [15]
Metronidazole DMTIVEN Abscess Approved [16]
Propofol DMB4OLE Anaesthesia 9A78.6 Approved [17]
Ethanol DMDRQZU Chronic pain MG30 Approved [18]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [19]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [20]
Diclofenac DMPIHLS Chronic renal failure GB61.Z Approved [21]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [22]
Mycophenolate mofetil DMPQAGE Hepatosplenic T-cell lymphoma Approved [23]
Ibuprofen DM8VCBE Dysmenorrhea GA34.3 Approved [21]
PITAVASTATIN CALCIUM DM1UJO0 Dyslipidemia 5C80-5C81 Approved [24]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [25]
Ezetimibe DM7A8TW Atherosclerosis BD40 Approved [26]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [27]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Diclofenac DMPIHLS Chronic renal failure GB61.Z Approved [28]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [14]
Ibuprofen DM8VCBE Dysmenorrhea GA34.3 Approved [21]
Atorvastatin DMF28YC Acute coronary syndrome BA41 Approved [29]
Cerivastatin DMXCM7H Hyperlipidaemia 5C80 Approved [30]
PITAVASTATIN CALCIUM DM1UJO0 Dyslipidemia 5C80-5C81 Approved [24]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [25]
Ezetimibe DM7A8TW Atherosclerosis BD40 Approved [31]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [27]
Losartan DM72JXH Diabetic kidney disease GB61.Z Approved [21]
⏷ 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
Diacylglycerol acyltransferase 1 (DGAT1) TTF8P9I DGAT1_HUMAN Modulator [3]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
UDP-glucuronosyltransferase 1A1 (UGT1A1) DEYGVN4 UD11_HUMAN Substrate [4]
UDP-glucuronosyltransferase 2B7 (UGT2B7) DEB3CV1 UD2B7_HUMAN Substrate [4]
UDP-glucuronosyltransferase 1A3 (UGT1A3) DEF2WXN UD13_HUMAN Substrate [4]

References

1 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7830).
2 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
3 DGAT1 inhibitors as anti-obesity and anti-diabetic agents. Curr Opin Drug Discov Devel. 2010 Jul;13(4):489-96.
4 Pradigastat disposition in humans: in vivo and in vitro investigations. Xenobiotica. 2017 Dec;47(12):1077-1089.
5 In vitro inhibition of diacylglycerol acyltransferase by prenylflavonoids from Sophora flavescens. Planta Med. 2004 Mar;70(3):258-60.
6 Clinical pipeline report, company report or official report of AstraZeneca (2011).
7 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800033014)
8 Acyltransferase inhibitors: a patent review (2010-present).Expert Opin Ther Pat. 2015 Feb;25(2):145-58.
9 Functional significance of UDP-glucuronosyltransferase variants in the metabolism of active tamoxifen metabolites. Cancer Res. 2009 Mar 1;69(5):1892-900.
10 Functional characterization of human and cynomolgus monkey UDP-glucuronosyltransferase 1A1 enzymes. Life Sci. 2010 Aug 14;87(7-8):261-8.
11 Effect of UDP-glucuronosyltransferase (UGT) 1A polymorphism (rs8330 and rs10929303) on glucuronidation status of acetaminophen. Dose Response. 2017 Sep 11;15(3):1559325817723731.
12 UDP-glucuronosyltransferase 1A1 is the principal enzyme responsible for etoposide glucuronidation in human liver and intestinal microsomes: structural characterization of phenolic and alcoholic glucuronides of etoposide and estimation of enzyme kinetics. Drug Metab Dispos. 2007 Mar;35(3):371-80.
13 Interindividual variability in pharmacokinetics of generic nucleoside reverse transcriptase inhibitors in TB/HIV-coinfected Ghanaian patients: UGT2B7*1c is associated with faster zidovudine clearance and glucuronidation. J Clin Pharmacol. 2009 Sep;49(9):1079-90.
14 Effect of aging on glucuronidation of valproic acid in human liver microsomes and the role of UDP-glucuronosyltransferase UGT1A4, UGT1A8, and UGT1A10. Drug Metab Dispos. 2009 Jan;37(1):229-36.
15 Characterization of rat intestinal microsomal UDP-glucuronosyltransferase activity toward mycophenolic acid. Drug Metab Dispos. 2006 Sep;34(9):1632-9.
16 Drug-drug interactions for UDP-glucuronosyltransferase substrates: a pharmacokinetic explanation for typically observed low exposure (AUCi/AUC) ratios. Drug Metab Dispos. 2004 Nov;32(11):1201-8.
17 Substrate-dependent modulation of UDP-glucuronosyltransferase 1A1 (UGT1A1) by propofol in recombinant human UGT1A1 and human liver microsomes. Basic Clin Pharmacol Toxicol. 2007 Sep;101(3):211-4.
18 Identification and preliminary characterization of UDP-glucuronosyltransferases catalyzing formation of ethyl glucuronide. Anal Bioanal Chem. 2014 Apr;406(9-10):2325-32.
19 Metabolism and transport of tamoxifen in relation to its effectiveness: new perspectives on an ongoing controversy. Future Oncol. 2014 Jan;10(1):107-22.
20 Determination of UDP-glucuronosyltransferase UGT2B7 activity in human liver microsomes by ultra-performance liquid chromatography with MS detection. J Chromatogr B Analyt Technol Biomed Life Sci. 2008 Jul 1;870(1):84-90.
21 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.
22 Pharmacokinetic and pharmacodynamic interaction of lorazepam and valproic acid in relation to UGT2B7 genetic polymorphism in healthy subjects. Clin Pharmacol Ther. 2008 Apr;83(4):595-600.
23 PharmGKB summary: mycophenolic acid pathway. Pharmacogenet Genomics. 2014 Jan;24(1):73-9.
24 Pitavastatin: a review in hypercholesterolemia. Am J Cardiovasc Drugs. 2017 Apr;17(2):157-168.
25 Troglitazone glucuronidation in human liver and intestine microsomes: high catalytic activity of UGT1A8 and UGT1A10. Drug Metab Dispos. 2002 Dec;30(12):1462-9.
26 Ezetimibe: a review of its metabolism, pharmacokinetics and drug interactions. Clin Pharmacokinet. 2005;44(5):467-94.
27 Pharmacogenomics of statins: understanding susceptibility to adverse effects. Pharmgenomics Pers Med. 2016 Oct 3;9:97-106.
28 Glucuronidation of nonsteroidal anti-inflammatory drugs: identifying the enzymes responsible in human liver microsomes. Drug Metab Dispos. 2005 Jul;33(7):1027-35.
29 UGT1A1*28 is associated with decreased systemic exposure of atorvastatin lactone. Mol Diagn Ther. 2013 Aug;17(4):233-7.
30 Cerivastatin, genetic variants, and the risk of rhabdomyolysis. Pharmacogenet Genomics. 2011 May;21(5):280-8.
31 Drug interactions between the immunosuppressant tacrolimus and the cholesterol absorption inhibitor ezetimibe in healthy volunteers. Clin Pharmacol Ther. 2011 Apr;89(4):524-8.