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

General Information of Drug (ID: DMO628K)

• Drug Name: Arbaclofen placarbil Drug Info
• Synonyms: AP; R-baclofen - XenoPort; XP-19986

Indication

Disease Entry	ICD 11	Status	REF
Fragile X syndrome	LD55	Phase 3	[1]
Alcohol dependence	6C40.2	Phase 2	[2]

• Cross-matching ID:
  PubChem CID: 11281011
  CAS Number: CAS 847353-30-4
  TTD Drug ID: DMO628K

Molecule-Related Drug Atlas

Drug(s) Targeting GABA(A) receptor gamma-3 (GABRG3)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Zolpidem	DMWOSKJ	Insomnia	7A00-7A0Z	Approved	[4]
Allopregnanolone	DMNLHAC	Depression	6A70-6A7Z	approved	[2]
Clobazam - Lundbeck	DMW1OQ0	Anxiety disorder	6B00-6B0Z	Approved	[5]
Flumazenil	DMPCG2L	Benzodiazepine overdose	PC91	Approved	[4]
Stiripentol	DMMSDOY	Dravet syndrome	8A61.11	Approved	[6]
Thiamylal	DMHDF7B	Anaesthesia	9A78.6	Approved	[5]
Ganaxolone	DMXJMKF	Epileptic seizures	8A61-8A6Z	Approved	[2]
Mebutamate	DM0KYI4	Anxiety disorder	6B00-6B0Z	Approved	[5]
Metharbital	DM5A38V	Epilepsy	8A60-8A68	Approved	[5]
Etomidate	DMZI3WO	Anaesthesia	9A78.6	Approved	[5]

Drug(s) Targeting Gamma-aminobutyric acid B receptor (GABBR)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Gabapentin	DM6T924	Complex partial seizure	8A68.0	Approved	[7]
Gamma Hydroxybutyric Acid	DMGBKVD	Narcolepsy	7A20	Approved	[5]
Baclofen	DM0QV1J	Multiple sclerosis	8A40	Approved	[8]
Progabide	DM671NG	Depression	6A70-6A7Z	Approved	[9]
[3H](R)-(-)-baclofen	DMLRHM5	Multiple sclerosis	8A40	Phase 3	[10]
Arabaclofen	DMZB9RI	Fragile X syndrome	LD55	Phase 3	[11]
GSK683699	DMTW79H	Inflammatory bowel disease	DD72	Phase 2	[12]
SGS742	DM5XYFH	Schizophrenia	6A20	Phase 2	[13]
SSTarbaclofen	DMRGTZ2	Autism spectrum disorder	6A02	Phase 2	[14]
ASP8062	DMR1MIV	Fibromyalgia	MG30.01	Phase 2	[15]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
GABA(A) receptor gamma-3 (GABRG3)	TTEX6LM	GBRG3_HUMAN	Agonist	[2]
Gamma-aminobutyric acid B receptor (GABBR)	TTDCVZW	GABR1_HUMAN; GABR2_HUMAN	Modulator	[3]

References

• [1] ClinicalTrials.gov (NCT01325220) Efficacy and Safety Study of STX209 (Arbaclofen) for the Treatment of Social Withdrawal in Children With Fragile X Syndrome. U.S. National Institutes of Health.
• [2] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [3] Arbaclofen placarbil, a novel R-baclofen prodrug: improved absorption, distribution, metabolism, and elimination properties compared with R-baclofen.J Pharmacol Exp Ther.2009 Sep;330(3):911-21.
• [4] 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: 415).
• [5] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [6] Stiripentol, a putative antiepileptic drug, enhances the duration of opening of GABA-A receptor channels. Epilepsia. 2006 Apr;47(4):704-16.
• [7] Gabapentin increases a tonic inhibitory conductance in hippocampal pyramidal neurons. Anesthesiology. 2006 Aug;105(2):325-33.
• [8] Synthesis and pharmacology of the baclofen homologues 5-amino-4-(4-chlorophenyl)pentanoic acid and the R- and S-enantiomers of 5-amino-3-(4-chlorop... J Med Chem. 1999 Jun 3;42(11):2053-9.
• [9] Interactions between dopamine and GABA in the control of ambulatory activity and neophobia in the mouse. Pharmacol Biochem Behav. 1998 Jan;59(1):239-47.
• [10] 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: 242).
• [11] Impact of acamprosate on behavior and brain-derived neurotrophic factor: an open-label study in youth with fragile X syndrome. Psychopharmacology (Berl). 2013 Jul;228(1):75-84.
• [12] 3-Thienyl- and 3-furylaminobutyric acids. Synthesis and binding GABAB receptor studies. J Med Chem. 1991 Aug;34(8):2557-60.
• [13] SGS742: the first GABA(B) receptor antagonist in clinical trials. Biochem Pharmacol. 2004 Oct 15;68(8):1479-87.
• [14] Reversal of disease-related pathologies in the fragile X mouse model by selective activation of GABAB receptors with arbaclofen. Sci Transl Med. 2012 Sep 19;4(152):152ra128.
• [15] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)