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

General Information of Drug (ID: DMHEW40)

Drug Name

E-2078 Drug Info

Synonyms

66A-078

Indication

Disease Entry	ICD 11	Status	REF
Pain	MG30-MG3Z	Discontinued in Phase 2	[1]

Cross-matching ID

PubChem CID: 122220
CAS Number: CAS 103613-84-9
TTD Drug ID: DMHEW40

Molecule-Related Drug Atlas

Molecule Type:

DTT

Drug Status:

Approved Drug(s)

Clinical Trial Drug(s)

Download the Complete Related Drug List

Drug(s) Targeting Opioid receptor kappa (OPRK1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Nalbuphine	DMOSQGU	Pain	MG30-MG3Z	Approved	[3]
Nalfurafine hcl	DMA9DHW	Uremic pruritus	EC90.10	Approved	[4]
CHLOROXINE	DMFZBMQ	Erythema	ME64.0	Approved	[5]
Difelikefalin	DMHZBEO	Pruritus	EC90	Approved	[6]
Dezocine	DMJDB0Y	Pain	MG30-MG3Z	Approved	[7]
Asimadoline	DMND3AB	Diarrhea-predominant irritable bowel syndrome	DD91.01	Phase 3	[8]
JNJ 67953964	DMJ8Y5N	Major depressive disorder	6A70.3	Phase 3	[9]
PHN-131	DM1SV8I	Pain	MG30-MG3Z	Phase 2/3	[10]
CR-845	DMJYTUQ	Pain	MG30-MG3Z	Phase 2/3	[11]
Carfentanil	DM7ADGX	N. A.	N. A.	Phase 2	[12]
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Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

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Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Opioid receptor kappa (OPRK1)	TTQW87Y	OPRK_HUMAN	Modulator	[2]

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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: 1648).
2	Systemic effects of E-2078, a stabilized dynorphin A(1-8) analog, in rhesus monkeys. Psychopharmacology (Berl). 1999 Apr;143(2):190-6.
3	Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
4	Drug design and synthesis of a novel kappa opioid receptor agonist with an oxabicyclo[2.2.2]octane skeleton and its pharmacology. Bioorg Med Chem Lett. 2010 Jan 1;20(1):121-4.
5	In silico identification and biochemical evaluation of novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2). Bioorg Med Chem Lett. 2010 Dec 15;20(24):7331-6.
6	Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
7	Pharmacological profiles of opioid ligands at kappa opioid receptors. BMC Pharmacol. 2006 Jan 25;6:3.
8	Emerging drugs for irritable bowel syndrome. Expert Opin Emerg Drugs. 2006 May;11(2):293-313.
9	Kappa Opioid Receptor Antagonists as Potential Therapeutics for Mood and Substance Use Disorders. Handb Exp Pharmacol. 2022;271:473-491.
10	Nalbuphine: an autoradiographic opioid receptor binding profile in the central nervous system of an agonist/antagonist analgesic. J Pharmacol Exp Ther. 1988 Jan;244(1):391-402.
11	Peptide Kappa Opioid Receptor Ligands: Potential for Drug Development. AAPS J. 2009 June; 11(2): 312-322.
12	Wax PM, Becker CE, Curry SC: Unexpected gas casualties in Moscow: a medical toxicology perspective. Ann Emerg Med. 2003 May;41(5):700-5.