General Information of Drug (ID: DM5E6MK)

Drug Name
J-104132 Drug Info
Synonyms L-753037; (5S,6R,7R)-2-Butyl-7-[2-[2(S)-carboxypropyl]-4-methoxyphenyl]-5-(3,4-methylenedioxyphenyl)-6,7-dihydro-5H-cyclopenta[b]pyridine-6-carboxylic acid
Indication
Disease Entry ICD 11 Status REF
Pulmonary arterial hypertension BB01.0 Discontinued in Phase 2 [1]
Cross-matching ID
PubChem CID
186002
CAS Number
CAS 198279-45-7
TTD Drug ID
DM5E6MK

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Discontinued Drug(s)
Preclinical Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Bosentan DMIOGBU Pulmonary arterial hypertension BB01.0 Approved [3]
Ambrisentan DMD1QXW Pulmonary arterial hypertension BB01.0 Approved [4]
Macitentan DMP79A1 Cardiovascular disease BA00-BE2Z Approved [5]
Sparsentan DMMP51W IgA nephropathy MF8Y Approved [6]
LU302146 DMMJVXZ Pulmonary hypertension BB01 Approved [7]
Atrasentan DMM74PK Diabetic nephropathy GB61.Z Phase 3 [8]
Clazosentan DMQSBX4 Cerebral vasospasm BA85.Z Phase 3 [9]
PF-1228305 DMS1EQ7 Pulmonary hypertension BB01 Phase 3 [10]
Darusentan DMN8DQH Hypotension BA20-BA21 Phase 3 [11]
BQ-123 DM0MO8I Pulmonary arterial hypertension BB01.0 Phase 2 [12]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Bosentan DMIOGBU Pulmonary arterial hypertension BB01.0 Approved [3]
Macitentan DMP79A1 Cardiovascular disease BA00-BE2Z Approved [5]
BQ788 DM6KRLW Acute kidney injury GB60 Phase 3 [13]
PD-145065 DMWVBTQ Hypertension BA00-BA04 Phase 2 [14]
SPI-1620 DMNPRMC Solid tumour/cancer 2A00-2F9Z Phase 2 [15]
ENB003 DMK2B3S Melanoma 2C30 Phase 1/2 [16]
ENRASENTAN DM05F1Z Pulmonary arterial hypertension BB01.0 Discontinued in Phase 2 [17]
SB-209670 DMJYW80 Arrhythmia BC9Z Discontinued in Phase 2 [18]
ET-1 DMA85ND N. A. N. A. Phase 0 [19]
PD142893 DMFA27N N. A. N. A. Terminated [20]
⏷ 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
Endothelin A receptor (EDNRA) TTKRD0G EDNRA_HUMAN Modulator [2]
Endothelin B receptor (EDNRB) TT3ZTGU EDNRB_HUMAN Modulator [2]

References

1 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010566)
2 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.
3 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
4 Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
5 Radium 223 dichloride for prostate cancer treatment. Drug Des Devel Ther. 2017 Sep 6;11:2643-2651.
6 Designed multiple ligands. An emerging drug discovery paradigm. J Med Chem. 2005 Oct 20;48(21):6523-43.
7 Influence of endothelin receptor antagonists on myocardial protein kinase C isoforms in uraemic cardiomyopathy. Clin Sci (Lond). 2002 Aug;103 Suppl 48:276S-279S.
8 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.
9 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.
10 Pfizer. Product Development Pipeline. March 31 2009.
11 Endothelin ETA receptor blockade with darusentan increases sodium and potassium excretion in aging rats. J Cardiovasc Pharmacol. 2006 Mar;47(3):456-62.
12 Endothelin in heart failure: a promising therapeutic target Heart. 1997 Feb;77(2):93-4.
13 BQ788, an endothelin ET(B) receptor antagonist, attenuates stab wound injury-induced reactive astrocytes in rat brain. Glia. 1999 May;26(3):268-71.
14 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.
15 Clinical pipeline report, company report or official report of Spectrum Phamaceuticals (2009).
16 ClinicalTrials.gov (NCT04205227) A Phase 1/2A Trial of ENB 003 in Combination With Pembrolizumab in Subjects With Advanced Solid Tumors. U.S.National Institutes of Health.
17 Enrasentan, an antagonist of endothelin receptors. Cardiovasc Drug Rev. 2003 Spring;21(1):1-16.
18 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.
19 IRL 2500: A potent ETB selective endothelin antagonist, Bioorg. Med. Chem. Lett. 6(19):2323-2328 (1996).
20 Human optic nerve head astrocytes as a target for endothelin-1. Invest Ophthalmol Vis Sci. 2002 Aug;43(8):2704-13.