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

General Information of Drug (ID: DMXMSYB)

• Drug Name: Ro 46-8443 Drug Info
• Synonyms: Ro468443

Indication

Disease Entry	ICD 11	Status	REF
Discovery agent	N.A.	Investigative	[1]

• Cross-matching ID:
  PubChem CID: 5312146
  TTD Drug ID: DMXMSYB

Molecule-Related Drug Atlas

Drug(s) Targeting Endothelin B receptor (EDNRB)

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	[4]
BQ788	DM6KRLW	Acute kidney injury	GB60	Phase 3	[5]
PD-145065	DMWVBTQ	Hypertension	BA00-BA04	Phase 2	[6]
SPI-1620	DMNPRMC	Solid tumour/cancer	2A00-2F9Z	Phase 2	[7]
ENB003	DMK2B3S	Melanoma	2C30	Phase 1/2	[8]
J-104132	DM5E6MK	Pulmonary arterial hypertension	BB01.0	Discontinued in Phase 2	[9]
ENRASENTAN	DM05F1Z	Pulmonary arterial hypertension	BB01.0	Discontinued in Phase 2	[10]
SB-209670	DMJYW80	Arrhythmia	BC9Z	Discontinued in Phase 2	[11]
ET-1	DMA85ND	N. A.	N. A.	Phase 0	[12]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Endothelin B receptor (EDNRB)	TT3ZTGU	EDNRB_HUMAN	Antagonist	[2]

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: 1011).
• [2] 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: 220).
• [3] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [4] Radium 223 dichloride for prostate cancer treatment. Drug Des Devel Ther. 2017 Sep 6;11:2643-2651.
• [5] BQ788, an endothelin ET(B) receptor antagonist, attenuates stab wound injury-induced reactive astrocytes in rat brain. Glia. 1999 May;26(3):268-71.
• [6] 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.
• [7] Clinical pipeline report, company report or official report of Spectrum Phamaceuticals (2009).
• [8] 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.
• [9] 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.
• [10] Enrasentan, an antagonist of endothelin receptors. Cardiovasc Drug Rev. 2003 Spring;21(1):1-16.
• [11] 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.
• [12] IRL 2500: A potent ETB selective endothelin antagonist, Bioorg. Med. Chem. Lett. 6(19):2323-2328 (1996).