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

General Information of Drug (ID: DMV3Y8R)

• Drug Name: BRL-61063 Drug Info
• Synonyms: Cipamfylline; 132210-43-6; UNII-AFP56R140L; AFP56R140L; CHEMBL356323; Cipamfylline [USAN:INN]; Cipamfyllinum; AC1Q6LCD; 8-Amino-1,3-bis(cyclopropylmethyl)xanthine; Cipamfylline (USAN/INN); AC1L2G0B; SCHEMBL26990; MLS006010682; SCHEMBL8327157; Brl 61063; 8-amino-1,3-bis(cyclopropylmethyl)-7H-purine-2,6-dione; DTXSID50157437; Cipamfylline, > KSPYMJJKQMWWNB-UHFFFAOYSA-N; ZINC3781835; BDBM50040348; 1,3-dicyclopropylmethyl-8-amino xanthine; SMR004701664; 8-Amino-1,3-di(cyclopropylmethyl)xanthine; D03516

Indication

Disease Entry	ICD 11	Status	REF
Allergy	4A80-4A85	Discontinued in Phase 2	[1]

• Cross-matching ID:
  PubChem CID: 71356
  CAS Number: CAS 132210-43-6
  TTD Drug ID: DMV3Y8R

Molecule-Related Drug Atlas

Drug(s) Targeting Phosphodiesterase 5A (PDE5A)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Tadalafil	DMJZHT1	Benign prostatic hyperplasia	GA90	Approved	[3]
Udenafil	DM1IQRP	Erectile dysfunction	HA01.1	Approved	[4]
Vardenafil	DMTBGW8	Cystic fibrosis	CA25	Approved	[5]
Dipyridamole	DMXY30O	Atrial fibrillation	BC81.3	Approved	[6]
Papaverine	DMCA9QP	Brain ischaemia	8B1Z	Approved	[7]
Avanafil	DM75CXN	Erectile dysfunction	HA01.1	Approved	[8]
Rhucin	DM3ADGP	Erectile dysfunction	HA01.1	Approved	[9]
ICARIIN	DMOJQGT	N. A.	N. A.	Phase 3	[10]
EXISULIND	DMBY56U	Colorectal cancer	2B91.Z	Phase 3	[11]
PF-489791	DM3C8GQ	Chronic obstructive pulmonary disease	CA22	Phase 2	[12]

Drug(s) Targeting Adenosine A1 receptor (ADORA1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Caffeine	DMKBJWP	Allergic rhinitis	CA08.0	Approved	[13]
Rolofylline	DMSZPR3	Heart failure	BD10-BD13	Phase 3	[14]
Tonapofylline	DMBH316	Acute and chronic heart failure	BD1Z	Phase 2	[15]
AMP-579	DMJ4GPR	Hyperlipidaemia	5C80	Phase 2	[16]
SELODENOSON	DMQM3IX	Cardiac arrhythmias	BC9Z	Phase 2	[17]
Apaxifylline	DMQMV9F	Cognitive impairment	6D71	Phase 2	[18]
SLV320	DM867BJ	Heart failure	BD10-BD13	Phase 2	[19]
DTI-0009	DMV84OK	Atrial fibrillation	BC81.3	Phase 2	[17]
Capadenoson	DMYWO62	Atrial fibrillation	BC81.3	Phase 2	[20]
BAY 1067197	DM4JGNH	Heart failure	BD10-BD13	Phase 2	[21]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Adenosine A1 receptor (ADORA1)	TTK25J1	AA1R_HUMAN	Inhibitor	[2]
Phosphodiesterase 5A (PDE5A)	TTJ0IQB	PDE5A_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 800004678)
• [2] Inhibition of cyclic nucleotide phosphodiesterase by derivatives of 1,3-bis(cyclopropylmethyl)xanthine. J Med Chem. 1994 Feb 18;37(4):476-85.
• [3] Pulmonary arterial hypertension: the most devastating vascular complication of systemic sclerosis. Rheumatology (Oxford). 2009 Jun;48 Suppl 3:iii25-31.
• [4] Increased expression of the nitric oxide synthase gene and protein in corpus cavernosum by repeated dosing of udenafil in a rat model of chemical d... Asian J Androl. 2009 Jul;11(4):435-42.
• [5] The effect of vardenafil, a potent and highly selective phosphodiesterase-5 inhibitor for the treatment of erectile dysfunction, on the cardiovascular response to exercise in patients with coronary artery disease. J Am Coll Cardiol. 2002 Dec 4;40(11):2006-12.
• [6] Anti-platelet therapy: phosphodiesterase inhibitors.Br J Clin Pharmacol.2011 Oct;72(4):634-46.
• [7] Effects of icariin on cGMP-specific PDE5 and cAMP-specific PDE4 activities. Asian J Androl. 2003 Mar;5(1):15-8.
• [8] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
• [9] cGMP-hydrolytic activity and its inhibition by sildenafil in normal and failing human and mouse myocardium. J Pharmacol Exp Ther. 2009 Sep;330(3):884-91.
• [10] Potent inhibition of human phosphodiesterase-5 by icariin derivatives. J Nat Prod. 2008 Sep;71(9):1513-7.
• [11] Exisulind induction of apoptosis involves guanosine 3',5'-cyclic monophosphate phosphodiesterase inhibition, protein kinase G activation, and attenuated beta-catenin. Cancer Res. 2000 Jul 1;60(13):3338-42.
• [12] Highlights of the society for medicinesresearch symposium held december 10th 2009 at the national heart and lung institute, London, UK. Drugs of the Future 2010, 35(4): 349-358.
• [13] Caffeine as a psychomotor stimulant: mechanism of action. Cell Mol Life Sci. 2004 Apr;61(7-8):857-72.
• [14] Association between the PDE4D gene and ischaemic stroke in the Chinese Han population. Clin Sci (Lond). 2009 Aug 17;117(7):265-72.
• [15] 2-Amino-5-benzoyl-4-phenylthiazoles: Development of potent and selective adenosine A1 receptor antagonists. Bioorg Med Chem. 2010 Mar 15;18(6):2195-2203.
• [16] Adenosine A1/A2a receptor agonist AMP-579 induces acute and delayed preconditioning against in vivo myocardial stunning. Am J Physiol Heart Circ Physiol. 2004 Dec;287(6):H2746-53.
• [17] Recent developments in adenosine receptor ligands and their potential as novel drugs. Biochim Biophys Acta. 2011 May;1808(5):1290-308.
• [18] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004779)
• [19] Role of matrix metalloproteinases and their tissue inhibitors as potential biomarkers of left ventricular remodelling in the athlete's heart. Clin Sci (Lond). 2009 Jul 16;117(4):157-64.
• [20] A1 adenosine receptor agonists and their potential therapeutic applications. Expert Opin Investig Drugs. 2008 Dec;17(12):1901-10.
• [21] Separation of on-target efficacy from adverse effects through rational design of a bitopic adenosine receptor agonist. Current Issue vol. 111 no. 12 Celine Valant, 4614-4619.