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 | [536297] |
Imatinib | Drug Info | Approved | Chronic myelogenous leukaemia | [536294], [541030] | |
Nintedanib | Drug Info | Approved | Idiopathic pulmonary fibrosis | [556264] | |
Pazopanib HCl | Drug Info | Approved | Renal cancer | [530677] | |
Trapidil | Drug Info | Phase 4 | Discovery agent | [522688] | |
Imatinib | Drug Info | Phase 3 | Intestinal cancer; Myeloid leukemia | [536294], [541030] | |
Nintedanib | Drug Info | Phase 3 | Non-small cell lung cancer | [524516], [524899], [541221] | |
BAY-57-9352 | Drug Info | Phase 2 | Solid tumours | [548058] | |
Imatinib | Drug Info | Phase 2 | Glioma; Lung cancer; Prostate cancer; Solid tumours | [536294], [541030] | |
Nintedanib | Drug Info | Phase 2 | Ovarian cancer | [523930], [541221] | |
TKI258 | Drug Info | Phase 1/2 | Advanced or metastatic renal cell cancer | [536674], [541242] | |
SU-6668 | Drug Info | Phase 1 | Advanced solid tumor | [527156], [542760] | |
X-82 | Drug Info | Phase 1 | Advanced solid tumor; Macular degeneration | [551750] | |
Motesanib | Drug Info | Discontinued in Phase 3 | Non-small cell lung cancer | [541005], [546905] | |
Binder | Alkaloid staurosporin | Drug Info | [551871] | ||
Inhibitor | BAY-57-9352 | Drug Info | [536474] | ||
Imatinib | Drug Info | [536474] | |||
Motesanib | Drug Info | [537551], [550250], [551087] | |||
Pazopanib HCl | Drug Info | [530677] | |||
SU-6668 | Drug Info | [536137], [536474] | |||
TKI258 | Drug Info | [536474] | |||
Trapidil | Drug Info | [536783] | |||
Activator | CT-102 | Drug Info | [536297] | ||
PDGF gene therapy | Drug Info | [536297] | |||
Modulator | Nintedanib | Drug Info | [533123] | ||
X-82 | Drug Info | [550468] | |||
References | |||||
Ref 522688 | 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 523930 | ClinicalTrials.gov (NCT01610869) Low Dose Cyclophosphamide +/-- Nintedanib in Advanced Ovarian Cancer. U.S. National Institutes of Health. | ||||
Ref 524516 | ClinicalTrials.gov (NCT01979952) Nintedanib Twice Daily vs Placebo in Patients Diagnosed With Idiopathic Pulmonary Fibrosis (IPF). U.S. National Institutes of Health. | ||||
Ref 524899 | 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 527156 | A phase I surrogate endpoint study of SU6668 in patients with solid tumors. Invest New Drugs. 2004 Nov;22(4):459-66. | ||||
Ref 536294 | Emerging treatments for pulmonary arterial hypertension. Expert Opin Emerg Drugs. 2006 Nov;11(4):609-19. | ||||
Ref 536674 | 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 541005 | (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 541030 | (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 541221 | (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 541242 | (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 542760 | (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 546905 | 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 536137 | 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 536474 | 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 536783 | 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 537551 | 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. |
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