General Information of Drug (ID: DMWD39E)

Drug Name
TR-14035 Drug Info
Synonyms
232271-19-1; TR-14035; (S)-2-(2,6-Dichlorobenzamido)-3-(2',6'-dimethoxy-[1,1'-biphenyl]-4-yl)propanoic acid; CHEMBL91485; N-(2,6-DICHLOROBENZOYL)-4-(2,6-DIMETHOXYPHENYL)-L-PHENYLALANINE; C24H21Cl2NO5; DRSJLVGDSNWQBI-SFHVURJKSA-N; TR 14035; SCHEMBL1222491; BDBM16801; CTK8C1530; MolPort-023-334-229; ZINC1490484; ANW-66841; N-Acyl-4-arylphenylalanine analogue.; AKOS016008162; CS-1812; CS-W000631; MP-2027; NCGC00390619-01; SB683698; HY-15770; AK-95353; AJ-26339; KB-210922; TC-155586; AB0077984; AX8237663; ST24020804; Z4458
Indication
Disease Entry ICD 11 Status REF
Multiple sclerosis 8A40 Discontinued in Phase 1 [1]
Cross-matching ID
PubChem CID
9912743
CAS Number
CAS 232271-19-1
TTD Drug ID
DMWD39E
VARIDT Drug ID
DR01351

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DTP
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Discontinued Drug(s)
Investigative Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
MLN0002 DMP2LZ8 Crohn disease DD70 Approved [5]
TRK-170 DM13G5R Inflammatory bowel disease DD72 Phase 2 [6]
PN-943 DMUZLKW Ulcerative colitis DD71 Phase 2 [7]
MORF-057 DMS274E Crohn disease DD70 Phase 2 [8]
GS-1427 DMDDBG1 Inflammation 1A00-CA43.1 Phase 1 [9]
R1295 DMT8V9G Rheumatoid arthritis FA20 Discontinued in Phase 1 [10]
⏷ Show the Full List of 6 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
AJM-300 DM5K6J4 Crohn disease DD70 Phase 3 [11]
TRK-170 DM13G5R Inflammatory bowel disease DD72 Phase 2 [6]
R411 DMP7J0S Asthma CA23 Phase 2 [12]
CDP323 DMXYLTI Multiple sclerosis 8A40 Phase 2 [13]
Firategrast DMW2QYT Multiple sclerosis 8A40 Phase 2 [14]
HMR-1031 DM695QT Arthritis FA20 Phase 1 [15]
BIIB107 DMIA57S Multiple sclerosis 8A40 Phase 1 [16]
CY-9652 DMPBCLA Inflammation 1A00-CA43.1 Terminated [17]
TCS2314 DMBVYQR Discovery agent N.A. Investigative [18]
⏷ Show the Full List of 9 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Methotrexate DM2TEOL Anterior urethra cancer Approved [19]
Dinoprostone DMTYOPD Medical abortion JA00.1Z Approved [20]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [21]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [22]
Sorafenib DMS8IFC Adenocarcinoma 2D40 Approved [21]
Pravastatin DM6A0X7 Adult acute monocytic leukemia Approved [23]
Mycophenolate mofetil DMPQAGE Hepatosplenic T-cell lymphoma Approved [24]
Atorvastatin DMF28YC Acute coronary syndrome BA41 Approved [25]
Cerivastatin DMXCM7H Hyperlipidaemia 5C80 Approved [26]
PITAVASTATIN CALCIUM DM1UJO0 Dyslipidemia 5C80-5C81 Approved [23]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Methotrexate DM2TEOL Anterior urethra cancer Approved [27]
Dinoprostone DMTYOPD Medical abortion JA00.1Z Approved [28]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [29]
Atorvastatin DMF28YC Acute coronary syndrome BA41 Approved [30]
PITAVASTATIN CALCIUM DM1UJO0 Dyslipidemia 5C80-5C81 Approved [31]
Rosuvastatin DMMIQ7G Arteriosclerosis BD40 Approved [32]
Saquinavir DMG814N Human immunodeficiency virus infection 1C62 Approved [33]
Enalapril DMNFUZR Congestive heart failure BD10 Approved [34]
Cholic Acid DM7OKQV Cholelithiasis DC11 Approved [35]
Liothyronine DM6IR3P Congenital hypothyroidism Approved [36]
⏷ 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
Integrin alpha-4/beta-1 (ITGA4/B1) TT6S84X ITA4_HUMAN-ITB1_HUMAN Modulator [2]
Integrin alpha-4/beta-7 (ITGA4/B7) TT7ZMI1 ITA4_HUMAN-ITB7_HUMAN Modulator [2]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
Organic anion transporting polypeptide 1A2 (SLCO1A2) DTE2B1D SO1A2_HUMAN Substrate [3]
Organic anion transporting polypeptide 1B1 (SLCO1B1) DT3D8F0 SO1B1_HUMAN Substrate [4]

References

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2 Pharmacokinetics and metabolism of TR-14035, a novel antagonist of a4ss1/a4ss7 integrin mediated cell adhesion, in rat and dog. Xenobiotica. 2005 Apr;35(4):373-89.
3 Characterization of hepatobiliary transport systems of a novel alpha4beta1/alpha4beta7 dual antagonist, TR-14035. Pharm Res. 2006 Nov;23(11):2646-56.
4 Cellular entry of thyroid hormones by organic anion transporting polypeptides. Best Pract Res Clin Endocrinol Metab. 2007 Jun;21(2):209-21.
5 2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
6 Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
7 Single- and Multiple-Dose Pharmacokinetics and Pharmacodynamics of PN-943, a Gastrointestinal-Restricted Oral Peptide Antagonist of alpha4beta7, in Healthy Volunteers. Clin Pharmacol Drug Dev. 2021 Nov;10(11):1263-1278.
8 ClinicalTrials.gov (NCT05291689) A Phase 2a, Open-label, Single-arm Study to Evaluate the Efficacy, Safety, and Tolerability of MORF-057 in Adults With Moderately to Severely Active Ulcerative Colitis (EMERALD-1). U.S.National Institutes of Health.
9 Clinical pipeline report, company report or official report of Gilead
10 Vedolizumab: an 47 integrin inhibitor for inflammatory bowel diseases.Ann Pharmacother.2014 Dec;48(12):1629-35.
11 Oral treatment with a novel small molecule alpha 4 integrin antagonist, AJM300, prevents the development of experimental colitis in mice. J Crohns Colitis. 2013 Dec;7(11):e533-42.
12 Integrins as therapeutic targets: lessons and opportunities. Nat Rev Drug Discov. 2010 Oct;9(10):804-20.
13 Pharmacodynamic consequences of administration of VLA-4 antagonist CDP323 to multiple sclerosis subjects: a randomized, double-blind phase 1/2 study.PLoS One.2013;8(3):e58438.
14 Firategrast for relapsing remitting multiple sclerosis: a phase 2, randomised, double-blind, placebo-controlled trial.Lancet Neurol.2012 Feb;11(2):131-9.
15 Pharmacoscintigraphic comparison of HMR 1031, a VLA-4 antagonist, in healthy volunteers following delivery via a nebulizer and a dry powder inhaler. Am J Ther. 2004 Mar-Apr;11(2):103-13.
16 ClinicalTrials.gov (NCT04593121) A Phase 1, Randomized, Blinded, Placebo-Controlled, Single- and Multiple-Ascending-Dose Study of the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of BIIB107 in Healthy Adult Participants. U.S.National Institutes of Health.
17 US patent application no. 2010,0278,784, Methods and compositions for treating skin conditions.
18 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. (Target id: 2580).
19 Preclinical Mouse Models To Study Human OATP1B1- and OATP1B3-Mediated Drug-Drug Interactions in Vivo. Mol Pharm. 2015 Dec 7;12(12):4259-69.
20 Organic anion transporting polypeptide 1B1: a genetically polymorphic transporter of major importance for hepatic drug uptake. Pharmacol Rev. 2011 Mar;63(1):157-81.
21 Contribution of OATP1B1 and OATP1B3 to the disposition of sorafenib and sorafenib-glucuronide. Clin Cancer Res. 2013 Mar 15;19(6):1458-66.
22 Identification of drugs and drug metabolites as substrates of multidrug resistance protein 2 (MRP2) using triple-transfected MDCK-OATP1B1-UGT1A1-MRP2 cells. Br J Pharmacol. 2012 Mar;165(6):1836-1847.
23 The effect of SLCO1B1*15 on the disposition of pravastatin and pitavastatin is substrate dependent: the contribution of transporting activity changes by SLCO1B1*15. Pharmacogenet Genomics. 2008 May;18(5):424-33.
24 Influence of SLCO1B1, 1B3, 2B1 and ABCC2 genetic polymorphisms on mycophenolic acid pharmacokinetics in Japanese renal transplant recipients. Eur J Clin Pharmacol. 2007 Dec;63(12):1161-9.
25 Rifampicin alters atorvastatin plasma concentration on the basis of SLCO1B1 521T>C polymorphism. Clin Chim Acta. 2009 Jul;405(1-2):49-52.
26 FDA Drug Development and Drug Interactions
27 Interaction of methotrexate with organic-anion transporting polypeptide 1A2 and its genetic variants. J Pharmacol Exp Ther. 2006 Aug;318(2):521-9.
28 Localization of organic anion transporting polypeptide 4 (Oatp4) in rat liver and comparison of its substrate specificity with Oatp1, Oatp2 and Oatp3. Pflugers Arch. 2001 Nov;443(2):188-95.
29 Environmental and genetic factors affecting transport of imatinib by OATP1A2. Clin Pharmacol Ther. 2011 Jun;89(6):816-20.
30 Influence of the flavonoids apigenin, kaempferol, and quercetin on the function of organic anion transporting polypeptides 1A2 and 2B1. Biochem Pharmacol. 2010 Dec 1;80(11):1746-53.
31 Transporter-mediated influx and efflux mechanisms of pitavastatin, a new inhibitor of HMG-CoA reductase. J Pharm Pharmacol. 2005 Oct;57(10):1305-11.
32 Drug and bile acid transporters in rosuvastatin hepatic uptake: function, expression, and pharmacogenetics. Gastroenterology. 2006 May;130(6):1793-806.
33 Human organic anion-transporting polypeptide OATP-A (SLC21A3) acts in concert with P-glycoprotein and multidrug resistance protein 2 in the vectorial transport of Saquinavir in Hep G2 cells. Mol Pharm. 2004 Jan 12;1(1):49-56.
34 Uptake of enalapril and expression of organic anion transporting polypeptide 1 in zonal, isolated rat hepatocytes. Drug Metab Dispos. 2000 Jul;28(7):801-6.
35 Molecular and functional characterization of an organic anion transporting polypeptide cloned from human liver. Gastroenterology. 1995 Oct;109(4):1274-82.
36 Identification of thyroid hormone transporters in humans: different molecules are involved in a tissue-specific manner. Endocrinology. 2001 May;142(5):2005-12.