Target Information
| Target General Infomation | |||||
|---|---|---|---|---|---|
| Target ID |
T86704
|
||||
| Target Name |
Phosphodiesterase (PDE) 3
|
||||
| Target Type |
Successful
|
||||
| Disease | Asthma [ICD10: J45] | ||||
| Allergic rhinitis [ICD9: 472.0, 477, 995.3; ICD10: J00, J30, J31.0, T78.4] | |||||
| Allergy [ICD9: 995.3; ICD10: T78.4] | |||||
| Arteriosclerosis [ICD9: 440; ICD10: I70] | |||||
| Chronic obstructive pulmonary disease [ICD9: 490-492, 494-496; ICD10: J40-J44, J47] | |||||
| Cardiovascular disorder [ICD10: I00-I99] | |||||
| Cough [ICD9: 786.2; ICD10: R05] | |||||
| Congestive heart failure [ICD9: 428; ICD10: I50] | |||||
| Cardiotonic [ICD10: I50] | |||||
| Heart failure [ICD9: 428; ICD10: I50] | |||||
| Intermittent claudication [ICD9: 440.21; ICD10: I73.9] | |||||
| Septic shock [ICD9: 785.52; ICD10: A41.9] | |||||
| BioChemical Class |
Hydrolases (EC:3)
|
||||
| EC Number |
EC 3.1.4.17
|
||||
| Drugs and Mode of Action | |||||
| Drug(s) | Cilostazol | Drug Info | Approved | Intermittent claudication | [1], [2] |
| Enoximone | Drug Info | Approved | Congestive heart failure | [3] | |
| Inamrinone Lactate | Drug Info | Approved | Cardiotonic | [4] | |
| Milrinone | Drug Info | Approved | Congestive heart failure | [5], [3] | |
| Oxtriphylline | Drug Info | Approved | Cough | [6] | |
| K-134 | Drug Info | Phase 2 | Arteriosclerosis | [7] | |
| Org-30029 | Drug Info | Phase 2 | Heart failure | [8] | |
| RPL-554 | Drug Info | Phase 2 | Allergic rhinitis | [9] | |
| Tipelukast | Drug Info | Phase 2 | Asthma | [10] | |
| 349U85.HCL | Drug Info | Phase 1 | Cardiovascular disorder | [11], [12] | |
| SDZ-MKS-492 | Drug Info | Phase 1 | Asthma | [13], [14] | |
| NSP-805 | Drug Info | Discontinued in Phase 2 | Heart failure | [15] | |
| OPC-8490 | Drug Info | Discontinued in Phase 2 | Cardiovascular disorder | [16] | |
| Org-9731 | Drug Info | Discontinued in Phase 2 | Heart failure | [17] | |
| Pumafentrine | Drug Info | Discontinued in Phase 2 | Asthma | [18] | |
| Tolafentrine | Drug Info | Discontinued in Phase 2 | Chronic obstructive pulmonary disease | [19] | |
| NIP-520 | Drug Info | Discontinued in Phase 1 | Asthma | [20] | |
| R 80122 | Drug Info | Discontinued in Phase 1 | Cardiovascular disorder | [21] | |
| Benafentrine dimaleate | Drug Info | Terminated | Septic shock | [22] | |
| Org-9935 | Drug Info | Terminated | Asthma | [23] | |
| SDZ-ISQ-844 | Drug Info | Terminated | Asthma | [24] | |
| Siguazodan | Drug Info | Terminated | Allergy | [25] | |
| UD-CG-212 | Drug Info | Terminated | Heart failure | [26] | |
| ZARDAVERINE | Drug Info | Terminated | Chronic obstructive pulmonary disease | [27] | |
| Modulator | 349U85.HCL | Drug Info | [12] | ||
| Benafentrine dimaleate | Drug Info | [28] | |||
| Cilostazol | Drug Info | [29] | |||
| Enoximone | Drug Info | ||||
| Inamrinone Lactate | Drug Info | ||||
| K-134 | Drug Info | [30], [31] | |||
| Milrinone | Drug Info | [29] | |||
| NIP-520 | Drug Info | [32] | |||
| NSP-805 | Drug Info | ||||
| OPC-8490 | Drug Info | ||||
| Org-30029 | Drug Info | [8] | |||
| Org-9731 | Drug Info | [33] | |||
| Org-9935 | Drug Info | ||||
| Oxtriphylline | Drug Info | [29] | |||
| Pumafentrine | Drug Info | ||||
| R 80122 | Drug Info | [34] | |||
| RPL-554 | Drug Info | ||||
| SDZ-ISQ-844 | Drug Info | [35] | |||
| SDZ-MKS-492 | Drug Info | [13], [14] | |||
| Siguazodan | Drug Info | ||||
| Tipelukast | Drug Info | ||||
| Tolafentrine | Drug Info | ||||
| UD-CG-212 | Drug Info | ||||
| ZARDAVERINE | Drug Info | ||||
| References | |||||
| REF 1 | Emerging drugs in peripheral arterial disease. Expert Opin Emerg Drugs. 2006 Mar;11(1):75-90. | ||||
| REF 2 | (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. (Ligand id: 7148). | ||||
| REF 3 | Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. Epub 2007 Feb 20. | ||||
| REF 4 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | ||||
| REF 5 | (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. (Ligand id: 5225). | ||||
| REF 6 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 086742. | ||||
| REF 7 | ClinicalTrials.gov (NCT00783081) Safety and Efficacy of K-134 for the Treatment of Intermittent Claudication. U.S. National Institutes of Health. | ||||
| REF 8 | Effects of the positive inotropic agent Org 30029 on developed force and aequorin light transients in intact canine ventricular myocardium. Circ Res. 1993 Mar;72(3):597-606. | ||||
| REF 9 | ClinicalTrials.gov (NCT02427165) Comparison of RPL554 With Placebo and Salbutamol in Asthmatic Patients. U.S. National Institutes of Health. | ||||
| REF 10 | ClinicalTrials.gov (NCT02503657) Safety and Tolerability Study in Subjects With Idiopathic Pulmonary Fibrosis (IPF). | ||||
| REF 11 | Cardiovascular pharmacology of the vasodilator-cardiotonic agent, 349U85. J Cardiovasc Pharmacol. 1992 Oct;20(4):579-89. | ||||
| REF 12 | Pharmacokinetics and pharmacodynamics of a new cardiotonic vasodilator agent, 349U85, in normal subjects. Clin Pharmacol Ther. 1994 Jan;55(1):55-63. | ||||
| REF 13 | Effects of MKS-492 on antigen-induced bronchoconstriction and allergic reaction in guinea pigs and rats. Jpn J Pharmacol. 1993 Dec;63(4):405-13. | ||||
| REF 14 | Effects of a cyclic nucleotide phosphodiesterase isoenzyme type III inhibitor, SDZ MKS 492 on airway responsiveness in beagles. Arerugi. 1993 Aug;42(8):920-5. | ||||
| REF 15 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002110) | ||||
| REF 16 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000283) | ||||
| REF 17 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005468) | ||||
| REF 18 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013080) | ||||
| REF 19 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003767) | ||||
| REF 20 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800012535) | ||||
| REF 21 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001304) | ||||
| REF 22 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000110) | ||||
| REF 23 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010891) | ||||
| REF 24 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005292) | ||||
| REF 25 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000375) | ||||
| REF 26 | Electrophysiological actions of the pimobendan metabolite, UD-CG 212 Cl, in guinea pig myocardium. J Pharmacol Exp Ther. 1992 Jan;260(1):58-63. | ||||
| REF 27 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000057) | ||||
| REF 28 | Studies on anti-allergic action of AH 21-132, a novel isozyme-selective phosphodiesterase inhibitor in airways. Jpn J Pharmacol. 1995 Feb;67(2):149-56. | ||||
| REF 29 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. | ||||
| REF 30 | A phase II dose-ranging study of the phosphodiesterase inhibitor K-134 in patients with peripheral artery disease and claudication. J Vasc Surg. 2012 Feb;55(2):381-389.e1. | ||||
| REF 31 | K-134, a Phosphodiesterase 3 Inhibitor, Prevents Brain Damage by Inhibiting Thrombus Formation in a Rat Cerebral Infarction Model. PLoS One. 2012; 7(10): e46432. | ||||
| REF 32 | Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41. | ||||
| REF 33 | The effects of various drugs on the myocardial inotropic response. Gen Pharmacol. 1995 Jan;26(1):1-31. | ||||
| REF 34 | Inhibition of human cardiac cyclic AMP-phosphodiesterases by R 80122, a new selective cyclic AMP-phosphodiesterase III inhibitor: a comparison with other cardiotonic compounds. J Pharmacol Exp Ther. 1992 Oct;263(1):6-14. | ||||
| REF 35 | Effects of inhaled SDZ ISQ 844, a cyclic nucleotide phosphodiesterase isoenzyme type III/IV inhibitor, on airway responsiveness in beagles. Arerugi. 1994 Apr;43(4):551-6. | ||||
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