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

General Information of Drug (ID: DM94R8B)

Drug Name

RS-100975 Drug Info

Synonyms

RS-97078; Ro-70-0004

Indication

Disease Entry	ICD 11	Status	REF
Prostate disease	GA91	Discontinued in Phase 1	[1]

Cross-matching ID

Molecule-Related Drug Atlas

Molecule Type:

DTT

Drug Status:

Approved Drug(s)

Clinical Trial Drug(s)

Patented Agent(s)

Discontinued Drug(s)

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Drug(s) Targeting Adrenergic receptor alpha-1A (ADRA1A)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
SILODOSIN	DMJSBT6	Benign prostatic hyperplasia	GA90	Approved	[3]
NAFTOPIDIL	DMQ8R4E	Hypertension	BA00-BA04	Approved	[3]
Tamsulosin	DM5QF9V	Benign prostatic hyperplasia	GA90	Approved	[4]
Xatral	DMLHOA0	Benign prostatic hyperplasia	GA90	Approved	[5]
Dutasteride + tamsulosin	DM6P8HU	Benign prostatic hyperplasia	GA90	Phase 3	[6]
Besipirdine	DMLVNTA	Cognitive impairment	6D71	Phase 3	[7]
MEDETOMIDINE	DMX9Y7V	Pain	MG30-MG3Z	Phase 2	[8]
PMID30124346-Compound-LDT8	DM5MUNG	Benign prostatic hyperplasia	GA90	Patented	[9]
PMID30124346-Compound-LDT66	DMJMTNL	Benign prostatic hyperplasia	GA90	Patented	[9]
TIOSPIRONE	DME5QDP	N. A.	N. A.	Discontinued in Phase 3	[10]
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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
Adrenergic receptor alpha-1A (ADRA1A)	TTNGILX	ADA1A_HUMAN	Antagonist	[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: 497).
2	In vitro alpha1-adrenoceptor pharmacology of Ro 70-0004 and RS-100329, novel alpha1A-adrenoceptor selective antagonists. Br J Pharmacol. 1999 May;127(1):252-8.
3	Pharmacophore identification of alpha(1A)-adrenoceptor antagonists. Bioorg Med Chem Lett. 2005 Feb 1;15(3):657-64.
4	Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
5	Pharma & Vaccines. Product Development Pipeline. April 29 2009.
6	Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
7	Alpha-Adrenergic activity and cardiovascular effects of besipirdine HCl (HP 749) and metabolite P7480 in vitro and in the conscious rat and dog. J Pharmacol Exp Ther. 1997 Apr;281(1):337-46.
8	A structure-activity relationship study of benzylic modifications of 4-[1-(1-naphthyl)ethyl]-1H-imidazoles on alpha 1- and alpha 2-adrenergic recep... J Med Chem. 1994 Jul 22;37(15):2328-33.
9	5-HT1A receptor ligands and their therapeutic applications: review of new patents.Expert Opin Ther Pat. 2018 Sep;28(9):679-689.
10	3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents. J Med Chem. 1996 Jan 5;39(1):143-8.