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

General Information of Drug (ID: DMBYQJH)

• Drug Name: GSK256066 Drug Info
• Synonyms: GSK-256066

Indication

Disease Entry	ICD 11	Status	REF
Asthma	CA23	Discontinued in Phase 2	[1]

• Cross-matching ID:
  PubChem CID: 9827968
  CAS Number: CAS 13122-87-7
  TTD Drug ID: DMBYQJH

Molecule-Related Drug Atlas

Drug(s) Targeting Phosphodiesterase 4A (PDE4A)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Dyphylline	DM8DZC1	Acute bronchial asthma	CA23	Approved	[3]
Enprofylline	DMFYZKN	Asthma	CA23	Approved	[4]
DENBUFYLLINE	DM2R15Q	Cognitive impairment	6D71	Phase 3	[5]
SOTB07	DMIG4OX	Asthma	CA23	Phase 3	[6]
Tofisopam	DMTGNWU	Hyperuricaemia	5C55.Y	Phase 2	[7]
AN-2898	DMDK7CL	Atopic dermatitis	EA80	Phase 2	[8]
GPD-1116	DMOQ7YI	Asthma	CA23	Phase 2	[9]
TA-7906	DMZTAJL	Atopic dermatitis	EA80	Phase 2	[10]
HT-0712	DM2WP8F	Cognitive impairment	6D71	Phase 2	[6]
TOFIMILAST	DMLCUAS	Chronic obstructive pulmonary disease	CA22	Phase 2	[11]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Phosphodiesterase 4A (PDE4A)	TTZ97H5	PDE4A_HUMAN	Inhibitor	[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 800024245)
• [2] Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
• [3] Ocular hypotension induced by topical dopaminergic drugs and phosphodiesterase inhibitors. Eur J Pharmacol. 1994 Jun 2;258(1-2):85-94.
• [4] Effects of enprofylline, a new xanthine derivate, on human pregnant myometrium. Am J Obstet Gynecol. 1987 Apr;156(4):958-62.
• [5] Pyrazolopyrimidine-2,4-dione sulfonamides: novel and selective calcitonin inducers. J Med Chem. 2002 May 23;45(11):2342-5.
• [6] 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: 1300).
• [7] The atypical anxiolytic drug, tofisopam, selectively blocks phosphodiesterase isoenzymes and is active in the mouse model of negative symptoms of psychosis. J Neural Transm (Vienna). 2010 Nov;117(11):1319-25.
• [8] An assessment of the genetic toxicology of novel boron-containing therapeutic agents. Environ Mol Mutagen. 2013 Jun;54(5):338-46.
• [9] Phosphodiesterase 4 inhibitor GPD-1116 markedly attenuates the development of cigarette smoke-induced emphysema in senescence-accelerated mice P1 s... Am J Physiol Lung Cell Mol Physiol. 2008 Feb;294(2):L196-204.
• [10] Potential role of phosphodiesterase 7 in human T cell function: comparative effects of two phosphodiesterase inhibitors. Clin Exp Immunol. 2002 Jun;128(3):460-6.
• [11] GSK256066, an exceptionally high-affinity and selective inhibitor of phosphodiesterase 4 suitable for administration by inhalation: in vitro, kinetic, and in vivo characterization. J Pharmacol Exp Ther. 2011 Apr;337(1):145-54.