Target Information
Target General Infomation | |||||
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Target ID |
T52624
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Former ID |
TTDS00261
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Target Name |
Platelet-derived growth factor receptor
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Synonyms |
PDGF-R; PDGFR kinase; Platelet-derived growth factor receptor tyrosine kinase
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Target Type |
Successful
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Disease | Advanced or metastatic renal cell cancer [ICD9: 189; ICD10: C64] | ||||
Advanced solid tumor [ICD9: 140-199; ICD10: C00-C75, C7A, C7B] | |||||
Advanced solid tumor; Macular degeneration [ICD9:140-199, 362.5; ICD10: C00-C75, C7A, C7B, H35.3] | |||||
Chronic myelogenous leukaemia [ICD9: 205.1; ICD10: C92.1] | |||||
Diabetic foot ulcer [ICD9: 707; ICD10: L88-L89] | |||||
Glioma; Lung cancer; Prostate cancer; Solid tumours [ICD9: 140-199, 191, 210-229; ICD10: C00-C75, C71, C7A, C7B, D10-D36, D3A] | |||||
Intestinal cancer; Myeloid leukemia [ICD9: 152, 153, 205; ICD10: C17, C18, C92] | |||||
Idiopathic pulmonary fibrosis; Non-small cell lung cancer [ICD9:516.3; ICD10: J84.1, C33-C34] | |||||
Non-small cell lung cancer [ICD10: C33-C34] | |||||
Ovarian cancer [ICD9: 183; ICD10: C56] | |||||
Renal cancer [ICD9: 140-229, 189; ICD10: C64] | |||||
Solid tumours [ICD9: 140-199, 210-229; ICD10: C00-D48] | |||||
BioChemical Class |
Kinase
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Target Validation |
T52624
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EC Number |
EC 2.7.1.112
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Drugs and Mode of Action | |||||
Drug(s) | CT-102 | Drug Info | Approved | Diabetic foot ulcer | [1] |
Imatinib | Drug Info | Approved | Chronic myelogenous leukaemia | [2], [3] | |
Nintedanib | Drug Info | Approved | Idiopathic pulmonary fibrosis | [4] | |
Pazopanib HCl | Drug Info | Approved | Renal cancer | [5] | |
Trapidil | Drug Info | Phase 4 | Discovery agent | [6] | |
Imatinib | Drug Info | Phase 3 | Intestinal cancer; Myeloid leukemia | [2], [3] | |
Nintedanib | Drug Info | Phase 3 | Non-small cell lung cancer | [7], [8], [9] | |
BAY-57-9352 | Drug Info | Phase 2 | Solid tumours | [10] | |
Imatinib | Drug Info | Phase 2 | Glioma; Lung cancer; Prostate cancer; Solid tumours | [2], [3] | |
Nintedanib | Drug Info | Phase 2 | Ovarian cancer | [11], [9] | |
TKI258 | Drug Info | Phase 1/2 | Advanced or metastatic renal cell cancer | [12], [13] | |
SU-6668 | Drug Info | Phase 1 | Advanced solid tumor | [14], [15] | |
X-82 | Drug Info | Phase 1 | Advanced solid tumor; Macular degeneration | [16] | |
Motesanib | Drug Info | Discontinued in Phase 3 | Non-small cell lung cancer | [17], [18] | |
Binder | Alkaloid staurosporin | Drug Info | [19] | ||
Inhibitor | BAY-57-9352 | Drug Info | [20] | ||
Imatinib | Drug Info | [20] | |||
Motesanib | Drug Info | [21], [22], [23] | |||
Pazopanib HCl | Drug Info | [5] | |||
SU-6668 | Drug Info | [24], [20] | |||
TKI258 | Drug Info | [20] | |||
Trapidil | Drug Info | [25] | |||
Activator | CT-102 | Drug Info | [1] | ||
PDGF gene therapy | Drug Info | [1] | |||
Modulator | Nintedanib | Drug Info | [26] | ||
X-82 | Drug Info | [27] | |||
References | |||||
REF 1 | Emerging drugs for diabetic foot ulcers. Expert Opin Emerg Drugs. 2006 Nov;11(4):709-24. | ||||
REF 2 | Emerging treatments for pulmonary arterial hypertension. Expert Opin Emerg Drugs. 2006 Nov;11(4):609-19. | ||||
REF 3 | (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: 5687). | ||||
REF 4 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. | ||||
REF 5 | Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92. | ||||
REF 6 | ClinicalTrials.gov (NCT00914420) Optical Coherence Tomography (OCT) Evaluation of Re-endothelization: A Comparison of the Intrepide Stent Versus Taxus . U.S. National Institutes of Health. | ||||
REF 7 | ClinicalTrials.gov (NCT01979952) Nintedanib Twice Daily vs Placebo in Patients Diagnosed With Idiopathic Pulmonary Fibrosis (IPF). U.S. National Institutes of Health. | ||||
REF 8 | ClinicalTrials.gov (NCT02231164) LUME-Columbus: Nintedanib Plus Docetaxel in Advanced Non-small Cell Lung Cancer With Translational Research. U.S. National Institutes of Health. | ||||
REF 9 | (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: 5936). | ||||
REF 10 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021605) | ||||
REF 11 | ClinicalTrials.gov (NCT01610869) Low Dose Cyclophosphamide +/-- Nintedanib in Advanced Ovarian Cancer. U.S. National Institutes of Health. | ||||
REF 12 | A phase I pharmacokinetic and pharmacodynamic study of TKI258, an oral, multitargeted receptor tyrosine kinase inhibitor in patients with advanced solid tumors. Clin Cancer Res. 2008 Apr 1;14(7):2075-81. | ||||
REF 13 | (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: 5962). | ||||
REF 14 | A phase I surrogate endpoint study of SU6668 in patients with solid tumors. Invest New Drugs. 2004 Nov;22(4):459-66. | ||||
REF 15 | (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: 7816). | ||||
REF 16 | Clinical pipeline report, company report or official report of Tyrogenex. | ||||
REF 17 | (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: 5660). | ||||
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 800011016) | ||||
REF 19 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | ||||
REF 20 | A comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development. Curr Top Med Chem. 2007;7(14):1408-22. | ||||
REF 21 | Phase II study of safety and efficacy of motesanib in patients with progressive or symptomatic, advanced or metastatic medullary thyroid cancer. J Clin Oncol. 2009 Aug 10;27(23):3794-801. Epub 2009 Jun 29. | ||||
REF 22 | Clinical pipeline report, company report or official report of Amgen (2009). | ||||
REF 23 | Axitinib for renal cell carcinoma. Expert Opin Investig Drugs. 2008 May;17(5):741-8. | ||||
REF 24 | Dose-finding study of the multitargeted tyrosine kinase inhibitor SU6668 in patients with advanced malignancies. Clin Cancer Res. 2005 Sep 1;11(17):6240-6. | ||||
REF 25 | Osteitis fibrosa is mediated by Platelet-Derived Growth Factor-A via a phosphoinositide 3-kinase-dependent signaling pathway in a rat model for chronic hyperparathyroidism. Endocrinology. 2008 Nov;149(11):5735-46. Epub 2008 Jul 17. | ||||
REF 26 | 2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81. | ||||
REF 27 | National Cancer Institute Drug Dictionary (drug id 695817). |
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