General Information of DTT (ID: TTJ0IQB)

DTT Name Phosphodiesterase 5A (PDE5A) DTT Info
Gene Name PDE5A

Molecule-Related Drug & Molecule List

Molecule-Related Drug List
Molecule Type:
DTT
DTP
DME
Drug Status:
Discontinued Drug(s)
Approved Drug(s)
Clinical Trial Drug(s)
Investigative Drug(s)
7 Approved Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Avanafil DM75CXN Erectile dysfunction HA01.1 Approved [1]
Dipyridamole DMXY30O Atrial fibrillation BC81.3 Approved [2]
Papaverine DMCA9QP Brain ischaemia 8B1Z Approved [3]
Rhucin DM3ADGP Erectile dysfunction HA01.1 Approved [4]
Tadalafil DMJZHT1 Benign prostatic hyperplasia GA90 Approved [5]
Udenafil DM1IQRP Erectile dysfunction HA01.1 Approved [6]
Vardenafil DMTBGW8 Cystic fibrosis CA25 Approved [7]
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⏷ Show the Full List of 7 Approved Drug(s)
4 Clinical Trial Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
EXISULIND DMBY56U Colorectal cancer 2B91.Z Phase 3 [8]
ICARIIN DMOJQGT N. A. N. A. Phase 3 [9]
PF-489791 DM3C8GQ Chronic obstructive pulmonary disease CA22 Phase 2 [10]
UK-371800 DMI8795 Erectile dysfunction HA01.1 Phase 1 [11]
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12 Discontinued Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
BRL-61063 DMV3Y8R Allergy 4A80-4A85 Discontinued in Phase 2 [12]
DASANTAFIL DMOWIGC Erectile dysfunction HA01.1 Discontinued in Phase 2 [1]
E-4021 DMWIA56 Cardiovascular disease BA00-BE2Z Discontinued in Phase 2 [13]
EMR-62203 DMIQRJW Erectile dysfunction HA01.1 Discontinued in Phase 2 [14]
SINITRODIL DMMZ2JT Angina pectoris BA40 Discontinued in Phase 2 [1]
SLX-2101 DM1J0YB Erectile dysfunction HA01.1 Discontinued in Phase 2 [15]
UK-369003 DMHXRZF Erectile dysfunction HA01.1 Discontinued in Phase 1/2 [16]
FR-229934 DMT6R8I Erectile dysfunction HA01.1 Terminated [17]
IMAZODAN DMWTFO3 N. A. N. A. Terminated [18]
SKF-96231 DMS2M58 Asthma CA23 Terminated [19]
Trequinsin DMQRSMD N. A. N. A. Terminated [20]
ZAPRINAST DMGH3T5 N. A. N. A. Terminated [21]
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⏷ Show the Full List of 12 Discontinued Drug(s)
23 Investigative Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
3,7-Bis(2-hydroxyethyl)icaritin DMQADXL Discovery agent N.A. Investigative [9]
7-(2-Hydroxyethyl)-3-O-rhamnosylicariin DMBIY98 Discovery agent N.A. Investigative [9]
8-prenylapigenin DM2VC0E Discovery agent N.A. Investigative [9]
8-prenylquercetin DMZC1SV Discovery agent N.A. Investigative [9]
Aom-0890 DMT4I2W Erectile dysfunction HA01.1 Investigative [22]
Benzo[1,3]dioxol-5-ylmethyl-quinazolin-4-yl-amine DM067NL Discovery agent N.A. Investigative [23]
Cartazolate DMSKT8G Discovery agent N.A. Investigative [24]
CKD-533 DMH204Y Erectile dysfunction HA01.1 Investigative [22]
Gamma-Glutamyl[S-(2-Iodobenzyl)Cysteinyl]Glycine DMHNJDE Discovery agent N.A. Investigative [25]
Guanosine-5'-Monophosphate DM3SLZK Discovery agent N.A. Investigative [25]
Icariside II DM3DB8X Discovery agent N.A. Investigative [9]
isobutylmethylxanthine DM46F5X Discovery agent N.A. Investigative [26]
KURAIDIN DMLDUJ1 Discovery agent N.A. Investigative [27]
KURARINOL DMRV5YE Discovery agent N.A. Investigative [27]
LORNEIC ACID A DM0ECUK Discovery agent N.A. Investigative [28]
ROLIPRAM DMJ03UM Discovery agent N.A. Investigative [23]
RWJ-387273 DM28IKN Discovery agent N.A. Investigative [29]
SCH-57726 DMDK8TR Discovery agent N.A. Investigative [30]
SCH51866 DMCWSJP Discovery agent N.A. Investigative [31]
SOPHOFLAVESCENOL DM8Y1S7 Discovery agent N.A. Investigative [27]
SOPHORAFLAVANONE B DMUVKX5 Discovery agent N.A. Investigative [9]
T0156 DMZE9TW Discovery agent N.A. Investigative [32]
TPN-729 DMW9G7H Erectile dysfunction HA01.1 Investigative [22]
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⏷ Show the Full List of 23 Investigative Drug(s)
Molecule Interaction Atlas

References

1 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
2 Anti-platelet therapy: phosphodiesterase inhibitors.Br J Clin Pharmacol.2011 Oct;72(4):634-46.
3 Effects of icariin on cGMP-specific PDE5 and cAMP-specific PDE4 activities. Asian J Androl. 2003 Mar;5(1):15-8.
4 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.
5 Pulmonary arterial hypertension: the most devastating vascular complication of systemic sclerosis. Rheumatology (Oxford). 2009 Jun;48 Suppl 3:iii25-31.
6 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.
7 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.
8 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.
9 Potent inhibition of human phosphodiesterase-5 by icariin derivatives. J Nat Prod. 2008 Sep;71(9):1513-7.
10 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.
11 Highly potent and selective chiral inhibitors of PDE5: an illustration of Pfeiffer's rule. Bioorg Med Chem Lett. 2008 Dec 1;18(23):6033-6.
12 Inhibition of cyclic nucleotide phosphodiesterase by derivatives of 1,3-bis(cyclopropylmethyl)xanthine. J Med Chem. 1994 Feb 18;37(4):476-85.
13 Potency and mechanism of action of E4021, a type 5 phosphodiesterase isozyme-selective inhibitor, on the photoreceptor phosphodiesterase depend on the state of activation of the enzyme. Mol Pharmacol. 1999 Mar;55(3):508-14.
14 WO patent application no. 2006,0180,88, Use of a pde 5 inhibitor for treating and preventing hypopigmentary disorders.
15 Novel phosphodiesterase-5 (PDE5) inhibitors in the alleviation of erectile dysfunction due to diabetes and ageing-induced oxidative stress. Expert Opin Investig Drugs. 2008 Jun;17(6):855-64.
16 Pfizer. Product Development Pipeline. March 31 2009.
17 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014897)
18 Cardiotonic agents. 1. 4,5-Dihydro-6-[4-(1H-imidazol-1-yl)phenyl]-3 (2H)-pyridazinones: novel positive inotropic agents for the treatment of conges... J Med Chem. 1984 Sep;27(9):1099-101.
19 Analogue-based Drug Discovery II. Janos Fischer,C. Robin Ganellin. Page(150).
20 Inhibition of cyclic adenosine-3',5'-monophosphate phosphodiesterase from vascular smooth muscle by rolipram analogues. J Med Chem. 1989 Jul;32(7):1450-7.
21 4-(3-Chloro-4-methoxybenzyl)aminophthalazines: synthesis and inhibitory activity toward phosphodiesterase 5. J Med Chem. 2000 Jun 29;43(13):2523-9.
22 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: 1304).
23 Cyclic GMP phosphodiesterase inhibitors. 2. Requirement of 6-substitution of quinazoline derivatives for potent and selective inhibitory activity. J Med Chem. 1994 Jun 24;37(13):2106-11.
24 Substituted pyrazolopyridines as potent and selective PDE5 inhibitors: potential agents for treatment of erectile dysfunction. J Med Chem. 2001 Mar 29;44(7):1025-7.
25 How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
26 The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
27 A prenylated flavonol, sophoflavescenol: a potent and selective inhibitor of cGMP phosphodiesterase 5. Bioorg Med Chem Lett. 2002 Sep 2;12(17):2313-6.
28 Lorneic acids, trialkyl-substituted aromatic acids from a marine-derived actinomycete. J Nat Prod. 2009 Nov;72(11):2046-8.
29 DOI: 10.1021/op060099f
30 The Gif system as a tool in medicinal chemistry: The oxidation of Sch 57726 under GoAggIII conditions, Bioorg. Med. Chem. Lett. 7(11):1381-1386 (1997).
31 Antiplatelet and antiproliferative effects of SCH 51866, a novel type 1 and type 5 phosphodiesterase inhibitor. J Cardiovasc Pharmacol. 1996 Dec;28(6):862-9.
32 Enzymological and pharmacological profile of T-0156, a potent and selective phosphodiesterase type 5 inhibitor. Eur J Pharmacol. 2002 Dec 5;456(1-3):91-8.