Target Information

Target General Infomation
Target ID
T52624
Former ID
TTDS00261
Target Name
Platelet-derived growth factor receptor
Synonyms
PDGF-R; PDGFR kinase; Platelet-derived growth factor receptor tyrosine kinase
Target Type
Successful
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
Target Validation
T52624
EC Number
EC 2.7.1.112
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 522688ClinicalTrials.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 523930ClinicalTrials.gov (NCT01610869) Low Dose Cyclophosphamide +/-- Nintedanib in Advanced Ovarian Cancer. U.S. National Institutes of Health.
Ref 524516ClinicalTrials.gov (NCT01979952) Nintedanib Twice Daily vs Placebo in Patients Diagnosed With Idiopathic Pulmonary Fibrosis (IPF). U.S. National Institutes of Health.
Ref 524899ClinicalTrials.gov (NCT02231164) LUME-Columbus: Nintedanib Plus Docetaxel in Advanced Non-small Cell Lung Cancer With Translational Research. U.S. National Institutes of Health.
Ref 527156A phase I surrogate endpoint study of SU6668 in patients with solid tumors. Invest New Drugs. 2004 Nov;22(4):459-66.
Ref 530677Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
Ref 536294Emerging treatments for pulmonary arterial hypertension. Expert Opin Emerg Drugs. 2006 Nov;11(4):609-19.
Ref 536297Emerging drugs for diabetic foot ulcers. Expert Opin Emerg Drugs. 2006 Nov;11(4):709-24.
Ref 536674A 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 546905Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800011016)
Ref 548058Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021605)
Ref 551750Clinical pipeline report, company report or official report of Tyrogenex.
Ref 556264Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
Ref 530677Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
Ref 5331232014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
Ref 536137Dose-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 536297Emerging drugs for diabetic foot ulcers. Expert Opin Emerg Drugs. 2006 Nov;11(4):709-24.
Ref 536474A 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 536783Osteitis 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 537551Phase 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 550250Clinical pipeline report, company report or official report of Amgen (2009).
Ref 550468National Cancer Institute Drug Dictionary (drug id 695817).
Ref 551087Axitinib for renal cell carcinoma. Expert Opin Investig Drugs. 2008 May;17(5):741-8.
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 1587926URL: https://www.ebi.ac.uk/chembl/ The ChEMBL database in 2017

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