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

General Information of Drug (ID: DMAPRGQ)

• Drug Name: R-1578 Drug Info
• Synonyms: MGluR2 antagonist (depression), Roche; MGluR2 antagonist (Alzheimer's disease/depression), Roche

Indication

Disease Entry	ICD 11	Status	REF
Mood disorder	6A60-6E23	Discontinued in Phase 2	[1]

• Cross-matching ID: TTD Drug ID: DMAPRGQ

Molecule-Related Drug Atlas

Drug(s) Targeting Metabotropic glutamate receptor 3 (mGluR3)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
LY404039	DMWZIRJ	Schizophrenia	6A20	Phase 3	[3]
RO-4995819	DMNTC7O	Major depressive disorder	6A70.3	Phase 2	[4]
Oleoyl-estrone	DM0RA8F	Alzheimer disease	8A20	Phase 2	[5]
MP-101	DMYCITZ	Alzheimer disease	8A20	Phase 2	[6]
BCI-838	DMRXDN3	Major depressive disorder	6A70.3	Phase 1	[7]
Pomaglumetad	DMTOLI5	Schizophrenia	6A20	Phase 1	[8]
BCI-632	DMZYCWT	Alzheimer disease	8A20	Phase 1	[9]
PMID25435285-Compound-16	DMKFX2G	N. A.	N. A.	Patented	[10]
PMID25435285-Compound-15	DMHBWNS	N. A.	N. A.	Patented	[10]
PMID25435285-Compound-20	DMG9FYH	N. A.	N. A.	Patented	[10]

Drug(s) Targeting Metabotropic glutamate receptor 2 (mGluR2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
RO-4995819	DMNTC7O	Major depressive disorder	6A70.3	Phase 2	[4]
Oleoyl-estrone	DM0RA8F	Alzheimer disease	8A20	Phase 2	[5]
MP-101	DMYCITZ	Alzheimer disease	8A20	Phase 2	[6]
JNJ-64281802	DMNMSVX	Dengue	1D20-1D2Z	Phase 2	[11]
BCI-838	DMRXDN3	Major depressive disorder	6A70.3	Phase 1	[7]
Pomaglumetad	DMTOLI5	Schizophrenia	6A20	Phase 1	[8]
BCI-632	DMZYCWT	Alzheimer disease	8A20	Phase 1	[9]
LY-2979165	DM16IX2	Bipolar disorder	6A60	Phase 1	[12]
JNJ-42491293	DMOL9JR	Psychiatric disorder	6E8Z	Phase 1	[13]
ADX71149	DMBUOX4	Epilepsy	8A60-8A68	Phase 1	[14]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Metabotropic glutamate receptor 2 (mGluR2)	TTXJ47W	GRM2_HUMAN	Antagonist	[2]
Metabotropic glutamate receptor 3 (mGluR3)	TT8A9EF	GRM3_HUMAN	Antagonist	[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 800034342)
• [2] Clinical pipeline report, company report or official report of Roche.
• [3] Positive allosteric modulators of the metabotropic glutamate receptor 2 for the treatment of schizophrenia. Expert Opin Ther Pat. 2009 Sep;19(9):1259-75.
• [4] Novel glutamatergic drugs for the treatment of mood disorders. Neuropsychiatr Dis Treat. 2013; 9: 1101-1112.
• [5] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [6] ClinicalTrials.gov (NCT03044249) A Study of MP-101 in Dementia-Related Psychosis and/or Agitation and Aggression. U.S. National Institutes of Health.
• [7] Metabotropic glutamate receptor subtype 2 (GRM2; MGLUR2); GRM3 (MGLUR3). SciBX 3(13); doi:10.1038/scibx.2010.413. April 1 2010
• [8] LY-2140023, a prodrug of the group II metabotropic glutamate receptor agonist LY-404039 for the potential treatment of schizophrenia. Curr Opin Investig Drugs. 2010 Jul;11(7):833-45.
• [9] Synthesis, in vitro pharmacology, structure-activity relationships, and pharmacokinetics of 3-alkoxy-2-amino-6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent and selective group II metabotropic glutamate receptor antagonists. J Med Chem. 2004 Aug 26;47(18):4570-87.
• [10] Novel metabotropic glutamate receptor 2/3 antagonists and their therapeutic applications: a patent review (2005 - present).Expert Opin Ther Pat. 2015 Jan;25(1):69-90.
• [11] Pharmacokinetic and pharmacodynamic characterisation of JNJ-40411813, a positive allosteric modulator of mGluR2, in two randomised, double-blind phase-I studies. J Psychopharmacol. 2015 Apr;29(4):414-25.
• [12] Annual Reports in Medicinal Chemistry. Volume 47, 2012, Page(78).
• [13] Opportunities and challenges in the discovery of allosteric modulators of GPCRs for treating CNS disorders. Nat Rev Drug Discov. 2014 Sep;13(9):692-708.
• [14] MGlu2 receptor-mediated modulation of conditioned avoidance behavior in rats. European journal of pharmacology. 01/2014; 727(1).