General Information of DTT (ID: TTKRD0G)

DTT Name Endothelin A receptor (EDNRA) DTT Info
Gene Name EDNRA

Molecule-Related Drug & Molecule List

Molecule-Related Drug List
Molecule Type:
DTT
DTP
DME
Drug Status:
Discontinued Drug(s)
Approved Drug(s)
Clinical Trial Drug(s)
Preclinical Drug(s)
Investigative Drug(s)
5 Approved Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Ambrisentan DMD1QXW Pulmonary arterial hypertension BB01.0 Approved [1]
Bosentan DMIOGBU Pulmonary arterial hypertension BB01.0 Approved [2]
LU302146 DMMJVXZ Pulmonary hypertension BB01 Approved [3]
Macitentan DMP79A1 Cardiovascular disease BA00-BE2Z Approved [4]
Sparsentan DMMP51W IgA nephropathy MF8Y Approved [5]
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10 Clinical Trial Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Atrasentan DMM74PK Diabetic nephropathy GB61.Z Phase 3 [6]
Clazosentan DMQSBX4 Cerebral vasospasm BA85.Z Phase 3 [7]
Darusentan DMN8DQH Hypotension BA20-BA21 Phase 3 [8]
PF-1228305 DMS1EQ7 Pulmonary hypertension BB01 Phase 3 [9]
BQ-123 DM0MO8I Pulmonary arterial hypertension BB01.0 Phase 2 [10]
FR139317 DMEL5SV Hypertension BA00-BA04 Phase 2 [11]
PD-145065 DMWVBTQ Hypertension BA00-BA04 Phase 2 [12]
TBC-3711 DMZCA0K Hypotension BA20-BA21 Phase 2 [13]
YM-598 DMUPJWH Prostate cancer 2C82.0 Phase 2 [14]
PMZ-2123 DMQ82SH Cerebral oedema in diabetic ketoacidosis 8D60.1 Phase 1 [15]
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⏷ Show the Full List of 10 Clinical Trial Drug(s)
21 Discontinued Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Sitaxsentan DMKM5HB Pulmonary arterial hypertension BB01.0 Withdrawn from market [16]
TBC 11251 (TBC) DMFR79T Pulmonary arterial hypertension BB01.0 Withdrawn from market [17]
Zibotentan DMIK6C9 Prostate cancer 2C82.0 Discontinued in Phase 3 [18]
97-139 DMG0I6L Cerebrovascular disease 8B2Z Discontinued in Phase 2 [19]
Avosentan DM2I8NT Diabetic nephropathy GB61.Z Discontinued in Phase 2 [20]
BMS-193884 DMODK2J Pulmonary arterial hypertension BB01.0 Discontinued in Phase 2 [21]
EDONENTAN HYDRATE DMRPUEC Pulmonary arterial hypertension BB01.0 Discontinued in Phase 2 [22]
ENRASENTAN DM05F1Z Pulmonary arterial hypertension BB01.0 Discontinued in Phase 2 [23]
J-104132 DM5E6MK Pulmonary arterial hypertension BB01.0 Discontinued in Phase 2 [24]
SB-209670 DMJYW80 Arrhythmia BC9Z Discontinued in Phase 2 [25]
A-216546 DMHT84I Solid tumour/cancer 2A00-2F9Z Discontinued in Phase 1 [26]
SB-234551 DMX7PNY Nerve injury ND56.4 Discontinued in Phase 1 [27]
ZD-1611 DMUDLFM Hypotension BA20-BA21 Discontinued in Phase 1 [28]
50-235 DMM3UK5 Hypertension BA00-BA04 Terminated [30]
BMS-182874 DM5PG6C Hypertension BA00-BA04 Terminated [31]
BQ-518 DM3O4BG Hypertension BA00-BA04 Terminated [32]
BQ610 DMPRNQL N. A. N. A. Terminated [33]
MX-6120 DMXW67H Heart disease BA41-BA42 Terminated [34]
PD-155080 DMQCNWD Hypertension BA00-BA04 Terminated [35]
PD142893 DMFA27N N. A. N. A. Terminated [33]
PD156707 DMAVZEJ N. A. N. A. Terminated [36]
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⏷ Show the Full List of 21 Discontinued Drug(s)
1 Preclinical Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
ET-1 DMA85ND N. A. N. A. Phase 0 [29]
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19 Investigative Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
2-HYDROXY-3,5-DIIODOBENZOIC ACID DMDOHRF Discovery agent N.A. Investigative [37]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one DMM9X0G Discovery agent N.A. Investigative [38]
Ac-bhg-F-N-Y-Y-W DM1KDJV Discovery agent N.A. Investigative [39]
Ac-w-F-F-N-Y-Y-W DMP89K4 Discovery agent N.A. Investigative [39]
Asterric acid DMJAPFH Discovery agent N.A. Investigative [40]
Bhg-F-N-Y-Y-W DMVH4LK Discovery agent N.A. Investigative [39]
BMS-187308 DMJ218E Discovery agent N.A. Investigative [41]
Endothelin-2 DMOEIYQ Discovery agent N.A. Investigative [29]
HJP-272 DMWIOCY Premature labour JB00 Investigative [42]
LU302872 DM7F3SE Discovery agent N.A. Investigative [3]
PD-163140 DMBZ09U Discovery agent N.A. Investigative [43]
PD164333 DM5421R Discovery agent N.A. Investigative [44]
sarafotoxin S6b DMR6PJ5 Discovery agent N.A. Investigative [45]
Trp-Ile-Ile-Asp-Leu-Hisc(Cys-Ser-Val-Tyr-Phe-Cys) DM48QTG Discovery agent N.A. Investigative [46]
Trp-Ile-Ile-Asp-Leu-Hisc(Cys-Val-Tyr-Phe-Cys) DMOZX8M Discovery agent N.A. Investigative [46]
W-F-F-N--Y-Y-W DMAXOIS Discovery agent N.A. Investigative [39]
[125I]PD151242 DM4HLO5 Discovery agent N.A. Investigative [47]
[3H]BQ123 DMG8T3W Discovery agent N.A. Investigative [48]
[3H]S0139 DM32IAB Discovery agent N.A. Investigative [42]
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⏷ Show the Full List of 19 Investigative Drug(s)
Molecule Interaction Atlas

References

1 Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
2 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
3 Influence of endothelin receptor antagonists on myocardial protein kinase C isoforms in uraemic cardiomyopathy. Clin Sci (Lond). 2002 Aug;103 Suppl 48:276S-279S.
4 Radium 223 dichloride for prostate cancer treatment. Drug Des Devel Ther. 2017 Sep 6;11:2643-2651.
5 Designed multiple ligands. An emerging drug discovery paradigm. J Med Chem. 2005 Oct 20;48(21):6523-43.
6 Effects of a selective ET(A)-receptor antagonist, atrasentan (ABT-627), in murine models of allergic asthma: demonstration of mouse strain specificity. Clin Sci (Lond). 2002 Aug;103 Suppl 48:367S-370S.
7 Effects of the selective endothelin A (ET(A)) receptor antagonist Clazosentan on cerebral perfusion and cerebral oxygenation following severe subar... Acta Neurochir (Wien). 2007;149(9):911-8; discussion 918.
8 Endothelin ETA receptor blockade with darusentan increases sodium and potassium excretion in aging rats. J Cardiovasc Pharmacol. 2006 Mar;47(3):456-62.
9 Pfizer. Product Development Pipeline. March 31 2009.
10 Endothelin in heart failure: a promising therapeutic target Heart. 1997 Feb;77(2):93-4.
11 Reduction of bFGF-induced smooth muscle cell proliferation and endothelin receptor mRNA expression by mevastatin and atorvastatin. Biochem Pharmacol. 2002 Aug 1;64(3):497-505.
12 Reversal of established responses to endothelin-1 in vivo and in vitro by the endothelin receptor antagonists, BQ-123 and PD 145065. Br J Pharmacol. 1994 May;112(1):207-13.
13 TBC3711, an ET(A) receptor antagonist, reduces neonatal hypoxia-induced pulmonary hypertension in piglets. Pediatr Res. 2001 Sep;50(3):374-83.
14 Role of the endothelin axis and its antagonists in the treatment of cancer. Br J Pharmacol. 2011 May; 163(2): 220-233.
15 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
16 Emerging treatments for pulmonary arterial hypertension. Expert Opin Emerg Drugs. 2006 Nov;11(4):609-19.
17 Systemic administration of the endothelin-A receptor antagonist TBC 11251 attenuates cerebral vasospasm after experimental subarachnoid hemorrhage:... Neurosurgery. 1998 Dec;43(6):1409-17; discussion 1417-8.
18 Clinical pipeline report, company report or official report of AstraZeneca (2009).
19 S-0139 (Shionogi). Curr Opin Investig Drugs. 2002 Jul;3(7):1051-6.
20 Agents in development for the treatment of diabetic nephropathy. Expert Opin Emerg Drugs. 2008 Sep;13(3):447-63.
21 Vasodilator effects of the endothelin ETA receptor selective antagonist BMS-193884 in healthy men
22 US patent application no. 9,062,094, Dipeptide-based prodrug linkers for aliphatic amine-containing drugs.
23 Enrasentan, an antagonist of endothelin receptors. Cardiovasc Drug Rev. 2003 Spring;21(1):1-16.
24 Pharmacological properties of J-104132 (L-753,037), a potent, orally active, mixed ETA/ETB endothelin receptor antagonist. J Pharmacol Exp Ther. 1999 Jun;289(3):1262-70.
25 Effects of the endothelin receptor antagonist, SB 209670, on circulatory failure and organ injury in endotoxic shock in the anaesthetized rat. Br J Pharmacol. 1996 May;118(1):198-204.
26 Pharmacology of A-216546: a highly selective antagonist for endothelin ET(A) receptor. Eur J Pharmacol. 1999 Feb 5;366(2-3):189-201.
27 Effects of the novel selective endothelin ET(A) receptor antagonist, SB 234551, on the cardiovascular responses to endotoxaemia in conscious rats. Br J Pharmacol. 2001 Aug;133(8):1371-7.
28 Pharmacological profile of ZD1611, a novel, orally active endothelin ETA receptor antagonist. J Pharmacol Exp Ther. 1999 Sep;290(3):1085-91.
29 5-OHKF and NorKA, depsipeptides from a Hawaiian collection of Bryopsis pennata: binding properties for NorKA to the human neuropeptide Y Y1 receptor. J Nat Prod. 2009 Dec;72(12):2172-6.
30 Structure-activity relationships of an endothelin ETA receptor antagonist, 50-235, and its derivatives. Eur J Pharmacol. 1993 Oct 15;247(2):219-21.
31 Biphenylsulfonamide endothelin receptor antagonists. 2. Discovery of 4'-oxazolyl biphenylsulfonamides as a new class of potent, highly selective ET... J Med Chem. 2000 Aug 10;43(16):3111-7.
32 Structure-activity relationships of cyclic pentapeptide endothelin A receptor antagonists. J Med Chem. 1995 Oct 13;38(21):4309-24.
33 Human optic nerve head astrocytes as a target for endothelin-1. Invest Ophthalmol Vis Sci. 2002 Aug;43(8):2704-13.
34 Endothelin receptor antagonists in heart failure: current status and future directions. Drugs. 2004;64(10):1029-40.
35 Potency of PD155080, an orally active ETA receptor antagonist, determined for human endothelin receptors. J Cardiovasc Pharmacol. 1995;26 Suppl 3:S362-4.
36 Discovery and development of an endothelin A receptor-selective antagonist PD 156707. Pharm Biotechnol. 1998;11:81-112.
37 Allosteric inhibition of endothelin ETA receptors by 3, 5-dibromosalicylic acid. Mol Pharmacol. 2000 Dec;58(6):1461-9.
38 Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 rec... J Med Chem. 2010 Sep 9;53(17):6386-97.
39 Res-701-1, synthesis and a reevaluation of its effects on the endothelin receptors, Bioorg. Med. Chem. Lett. 5(6):621-626 (1995).
40 New chlorinated diphenyl ethers from an Aspergillus species. J Nat Prod. 2002 Jan;65(1):7-10.
41 Biphenylsulfonamide endothelin antagonists: structure-activity relationships of a series of mono- and disubstituted analogues and pharmacology of t... J Med Chem. 1998 Dec 17;41(26):5198-218.
42 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: 219).
43 gamma-Carbamate butenolide analogues as potent ETA selective endothelin receptor antagonists and prodrugs, Bioorg. Med. Chem. Lett. 7(3):297-302 (1997).
44 Characterization of [125I]-PD164333, an ETA selective non-peptide radiolabelled antagonist, in normal and diseased human tissues. Br J Pharmacol. 1998 Jan;123(2):223-30.
45 ETA receptor-mediated constrictor responses to endothelin peptides in human blood vessels in vitro. Br J Pharmacol. 1995 May;115(1):191-7.
46 Structure-activity relationships in a series of monocyclic endothelin analogues, Bioorg. Med. Chem. Lett. 4(4):567-572 (1994).
47 [125I]-PD151242: a selective radioligand for human ETA receptors. Br J Pharmacol. 1994 Jan;111(1):4-6.
48 [3H]BQ-123, a highly specific and reversible radioligand for the endothelin ETA receptor subtype. Eur J Pharmacol. 1995 Feb 14;274(1-3):1-6.