Investigational therapies up to Phase II which target PDGF receptors: potential anti-cancer therapeutics

Bibliography

• Fredriksson L, Li H, Eriksson U. The PDGF family: four gene products form five dimeric isoforms. Cytokine Growth Factor Rev 2004;15(4):197–204
   PubMed Web of Science ®Google Scholar
• Uutela M, Laurén J, Bergsten E, et al. Chromosomal location, exon structure, and vascular expression patterns of the human PDGFC and PDGFD genes. Circulation 2001;103(18):2242–7
   PubMed Web of Science ®Google Scholar
• Andrae J, Gallini R, Betsholtz C. Role of platelet-derived growth factors in physiology and medicine. Genes Dev 2008;22(10):1276–312
   PubMed Web of Science ®Google Scholar
• Roberts WG, Whalen PM, Soderstrom E, et al. Antiangiogenic and antitumor activity of a selective PDGFR tyrosine kinase inhibitor, CP-673,451. Cancer Res 2005;65(3):957–66
   PubMed Web of Science ®Google Scholar
• Oikawa T, Onozawa C, Sakaguchi M, et al. Three isoforms of platelet-derived growth factors all have the capability to induce angiogenesis in vivo. Biol Pharm Bull 1994;17(12):1686–8
   PubMed Web of Science ®Google Scholar
• Betsholtz C. Insight into the physiological functions of PDGF through genetic studies in mice. Cytokine Growth Factor Rev 2004;15(4):215–28
   PubMed Web of Science ®Google Scholar
• Jechlinger M, Sommer A, Moriggl R, et al. Autocrine PDGFR signaling promotes mammary cancer metastasis. J Clin Invest 2006;116(6):1561–70
   PubMed Web of Science ®Google Scholar
• Heinrich MC, Corless CL, Duensing A, et al. PDGFRA activating mutations in gastrointestinal stromal tumors. Science 2003;299(5607):708–10
   PubMed Web of Science ®Google Scholar
• Puputti M, Tynninen O, Sihto H, et al. Amplification of KIT, PDGFRA, VEGFR2, and EGFR in gliomas. Mol Cancer Res 2006;4(12):927–34
   PubMed Web of Science ®Google Scholar
• Shimizu A, O’Brien KP, Sjöblom T, et al. The dermatofibrosarcoma protuberans-associated collagen type Ialpha1/platelet-derived growth factor (PDGF) B-chain fusion gene generates a transforming protein that is processed to functional PDGF-BB. Cancer Res 1999;59(15):3719–23
   PubMed Web of Science ®Google Scholar
• Jones AV, Cross NCP. Oncogenic derivatives of platelet-derived growth factor receptors. Cell Mol Life Sci 2004;61(23):2912–23
   PubMed Web of Science ®Google Scholar
• Ustach CV, Taube ME, Hurst NJ, et al. A potential oncogenic activity of platelet-derived growth factor d in prostate cancer progression. Cancer Res 2004;64(5):1722–9
   PubMed Web of Science ®Google Scholar
• Fischer ANM, Fuchs E, Mikula M, et al. PDGF essentially links TGF-beta signaling to nuclear beta-catenin accumulation in hepatocellular carcinoma progression. Oncogene 2007;26(23):3395–405
   PubMed Web of Science ®Google Scholar
• Kawai T, Hiroi S, Torikata C. Expression in lung carcinomas of platelet-derived growth factor and its receptors. Lab Invest 1997;77(5):431–6
   PubMed Web of Science ®Google Scholar
• Bhardwaj B, Klassen J, Cossette N, et al. Localization of platelet-derived growth factor beta receptor expression in the periepithelial stroma of human breast carcinoma. Clin Cancer Res 1996;2(4):773–82
   PubMed Web of Science ®Google Scholar
• Henriksen R, Funa K, Wilander E, et al. Expression and prognostic significance of platelet-derived growth factor and its receptors in epithelial ovarian neoplasms. Cancer Res 1993;53(19):4550–4
   PubMed Web of Science ®Google Scholar
• Sundberg C, Ljungström M, Lindmark G, et al. Microvascular pericytes express platelet-derived growth factor-beta receptors in human healing wounds and colorectal adenocarcinoma. Am J Pathol 1993;143(5):1377–88
   PubMed Web of Science ®Google Scholar
• Hanahan D, Coussens LM. Accessories to the crime: functions of cells recruited to the tumor microenvironment. Cancer Cell 2012;21(3):309–22
   PubMed Web of Science ®Google Scholar
• Shao ZM, Nguyen M, Barsky SH. Human breast carcinoma desmoplasia is PDGF initiated. Oncogene 2000;19(38):4337–45
   PubMed Web of Science ®Google Scholar
• Tejada ML, Yu L, Dong J, et al. Tumor-driven paracrine platelet-derived growth factor receptor alpha signaling is a key determinant of stromal cell recruitment in a model of human lung carcinoma. Clin Cancer Res 2006;12(9):2676–88
   PubMed Web of Science ®Google Scholar
• Campbell JS, Hughes SD, Gilbertson DG, et al. Platelet-derived growth factor C induces liver fibrosis, steatosis, and hepatocellular carcinoma. Proc Natl Acad Sci USA 2005;102(9):3389–94
   PubMed Web of Science ®Google Scholar
• Anderberg C, Li H, Fredriksson L, et al. Paracrine signaling by platelet-derived growth factor-CC promotes tumor growth by recruitment of cancer-associated fibroblasts. Cancer Res 2009;69(1):369–78
   PubMed Web of Science ®Google Scholar
• Bandapalli OR, Macher-Goeppinger S, Schirmacher P, Brand K. Paracrine signalling in colorectal liver metastases involving tumor cell-derived PDGF-C and hepatic stellate cell-derived PAK-2. Clin Exp Metastasis 2012;29(5):409–17
   PubMed Web of Science ®Google Scholar
• Strawn LM, Mann E, Elliger SS, et al. Inhibition of glioma cell growth by a truncated platelet-derived growth factor-beta receptor. J Biol Chem 1994;269(33):21215–22
   PubMed Web of Science ®Google Scholar
• Uehara H, Kim SJ, Karashima T, et al. Effects of blocking platelet-derived growth factor-receptor signaling in a mouse model of experimental prostate cancer bone metastases. J Natl Cancer Inst 2003;95(6):458–70
   PubMed Web of Science ®Google Scholar
• Garofalo A, Naumova E, Manenti L, et al. The combination of the tyrosine kinase receptor inhibitor SU6668 with paclitaxel affects ascites formation and tumor spread in ovarian carcinoma xenografts growing orthotopically. Clin Cancer Res 2003;9(9):3476–85
   PubMed Web of Science ®Google Scholar
• Machida S, Saga Y, Takei Y, et al. Inhibition of peritoneal dissemination of ovarian cancer by tyrosine kinase receptor inhibitor SU6668 (TSU-68). Int J Cancer 2005;114(2):224–9
   PubMed Web of Science ®Google Scholar
• Sjöblom T, Shimizu A, O’Brien KP, et al. Growth inhibition of dermatofibrosarcoma protuberans tumors by the platelet-derived growth factor receptor antagonist STI571 through induction of apoptosis. Cancer Res 2001;61(15):5778–83
   PubMed Web of Science ®Google Scholar
• Xi Y, Chen M, Liu X, et al. CP-673451, a platelet-derived growth-factor receptor inhibitor, suppresses lung cancer cell proliferation and migration. Onco Targets Ther 2014;7:1215–21
   PubMed Web of Science ®Google Scholar
• Corless CL, Schroeder A, Griffith D, et al. PDGFRA mutations in gastrointestinal stromal tumors: frequency, spectrum and in vitro sensitivity to imatinib. J Clin Oncol 2005;23(23):5357–64
   PubMed Web of Science ®Google Scholar
• Mathew P, Thall PF, Wen S, et al. Dynamic change in phosphorylated platelet-derived growth factor receptor in peripheral blood leukocytes following docetaxel therapy predicts progression-free and overall survival in prostate cancer. Br J Cancer 2008;99(9):1426–32
   PubMed Web of Science ®Google Scholar
• Matei D, Emerson RE, Schilder J, et al. Imatinib mesylate in combination with docetaxel for the treatment of patients with advanced, platinum-resistant ovarian cancer and primary peritoneal carcinomatosis : a Hoosier Oncology Group trial. Cancer 2008;113(4):723–32
   PubMed Web of Science ®Google Scholar
• Hu-Lowe DD, Zou HY, Grazzini ML, et al. Nonclinical antiangiogenesis and antitumor activities of axitinib (AG-013736), an oral, potent, and selective inhibitor of vascular endothelial growth factor receptor tyrosine kinases 1, 2, 3. Clin Cancer Res 2008;14(22):7272–83
   PubMed Web of Science ®Google Scholar
• Heinrich MC, Griffith D, McKinley A, et al. Crenolanib inhibits the drug-resistant PDGFRA D842V mutation associated with imatinib-resistant gastrointestinal stromal tumors. Clin Cancer Res 2012;18(16):4375–84
   PubMed Web of Science ®Google Scholar
• Chen Z, Lee FY, Bhalla KN, Wu J. Potent inhibition of platelet-derived growth factor-induced responses in vascular smooth muscle cells by BMS-354825 (dasatinib). Mol Pharmacol 2006;69(5):1527–33
   PubMed Web of Science ®Google Scholar
• Trudel S, Li ZH, Wei E, et al. CHIR-258, a novel, multitargeted tyrosine kinase inhibitor for the potential treatment of t(4;14) multiple myeloma. Blood 2005;105(7):2941–8
   PubMed Web of Science ®Google Scholar
• Heinrich MC, Corless CL, Demetri GD, et al. Kinase mutations and imatinib response in patients with metastatic gastrointestinal stromal tumor. J Clin Oncol 2003;21(23):4342–9
   PubMed Web of Science ®Google Scholar
• Matsui J, Yamamoto Y, Funahashi Y, et al. E7080, a novel inhibitor that targets multiple kinases, has potent antitumor activities against stem cell factor producing human small cell lung cancer H146, based on angiogenesis inhibition. Int J Cancer 2008;122(3):664–71
   PubMed Web of Science ®Google Scholar
• Albert DH, Tapang P, Magoc TJ, et al. Preclinical activity of ABT-869, a multitargeted receptor tyrosine kinase inhibitor. Mol Cancer Ther 2006;5(4):995–1006
   PubMed Web of Science ®Google Scholar
• Dubreuil P, Letard S, Ciufolini M, et al. Masitinib (AB1010), a potent and selective tyrosine kinase inhibitor targeting KIT. PLoS One 2009;4(9):e7258
   PubMed Web of Science ®Google Scholar
• Polverino A, Coxon A, Starnes C, et al. AMG 706, an oral, multikinase inhibitor that selectively targets vascular endothelial growth factor, platelet-derived growth factor, and kit receptors, potently inhibits angiogenesis and induces regression in tumor xenografts. Cancer Res 2006;66(17):8715–21
   PubMed Web of Science ®Google Scholar
• Weisberg E, Manley PW, Breitenstein W, et al. Characterization of AMN107, a selective inhibitor of native and mutant Bcr-Abl. Cancer Cell 2005;7(2):129–41
   PubMed Web of Science ®Google Scholar
• Hilberg F, Roth GJ, Krssak M, et al. BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. Cancer Res 2008;68(12):4774–82
   PubMed Web of Science ®Google Scholar
• Laird AD, Vajkoczy P, Shawver LK, et al. SU6668 is a potent antiangiogenic and antitumor agent that induces regression of established tumors. Cancer Res 2000;60(15):4152–60
   PubMed Web of Science ®Google Scholar
• Kumar R, Crouthamel M-C, Rominger DH, et al. Myelosuppression and kinase selectivity of multikinase angiogenesis inhibitors. Br J Cancer 2009;101(10):1717–23
   PubMed Web of Science ®Google Scholar
• O’Hare T, Shakespeare WC, Zhu X, et al. AP24534, a pan-BCR-ABL inhibitor for chronic myeloid leukemia, potently inhibits the T315I mutant and overcomes mutation-based resistance. Cancer Cell 2009;16(5):401–12
   PubMed Web of Science ®Google Scholar
• Wilhelm SM, Dumas J, Adnane L, et al. Regorafenib (BAY 73-4506): a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity. Int J Cancer 2011;129(1):245–55
   PubMed Web of Science ®Google Scholar
• Steeghs N, Gelderblom H, Roodt JO, et al. Hypertension and rarefaction during treatment with telatinib, a small molecule angiogenesis inhibitor. Clin Cancer Res 2008;14(11):3470–6
   PubMed Web of Science ®Google Scholar
• Nakamura K, Taguchi E, Miura T, et al. KRN951, a highly potent inhibitor of vascular endothelial growth factor receptor tyrosine kinases, has antitumor activities and affects functional vascular properties. Cancer Res 2006;66(18):9134–42
   PubMed Web of Science ®Google Scholar
• Wood JM, Bold G, Buchdunger E, et al. PTK787/ZK 222584, a novel and potent inhibitor of vascular endothelial growth factor receptor tyrosine kinases, impairs vascular endothelial growth factor-induced responses and tumor growth after oral administration. Cancer Res 2000;60(8):2178–89
   PubMed Web of Science ®Google Scholar
• Mayer EL, Baurain J-F, Sparano J, et al. A phase 2 trial of dasatinib in patients with advanced HER2-positive and/or hormone receptor-positive breast cancer. Clin Cancer Res 2011;17(21):6897–904
   PubMed Web of Science ®Google Scholar
• Finn RS, Bengala C, Ibrahim N, et al. Dasatinib as a single agent in triple-negative breast cancer: results of an open-label phase 2 study. Clin Cancer Res 2011;17(21):6905–13
   PubMed Web of Science ®Google Scholar
• Schilder RJ, Brady WE, Lankes HA, et al. Phase II evaluation of dasatinib in the treatment of recurrent or persistent epithelial ovarian or primary peritoneal carcinoma: a Gynecologic Oncology Group study. Gynecol Oncol 2012;127(1):70–4
   PubMed Web of Science ®Google Scholar
• Twardowski PW, Beumer JH, Chen CS, et al. A phase II trial of dasatinib in patients with metastatic castration-resistant prostate cancer treated previously with chemotherapy. Anticancer Drugs 2013;24(7):743–53
   PubMed Web of Science ®Google Scholar
• Araujo JC, Trudel GC, Paliwal P. Long-term use of dasatinib in patients with metastatic castration-resistant prostate cancer after receiving the combination of dasatinib and docetaxel. Cancer Manag Res 2013;6:25–30
   PubMedGoogle Scholar
• Brunner AM, Costa DB, Heist RS, et al. Treatment-related toxicities in a phase II trial of dasatinib in patients with squamous cell carcinoma of the lung. J Thorac Oncol 2013;8(11):1434–7
   PubMed Web of Science ®Google Scholar
• Chee CE, Krishnamurthi S, Nock CJ, et al. Phase II study of dasatinib (BMS-354825) in patients with metastatic adenocarcinoma of the pancreas. Oncologist 2013;18(10):1091–2
   PubMed Web of Science ®Google Scholar
• Araujo JC, Trudel GC, Saad F, et al. Docetaxel and dasatinib or placebo in men with metastatic castration-resistant prostate cancer (READY): a randomised, double-blind phase 3 trial. Lancet Oncol 2013;14(13):1307–16
   PubMed Web of Science ®Google Scholar
• Weigel MT, Rath K, Alkatout I, et al. Nilotinib in combination with carboplatin and paclitaxel is a candidate for ovarian cancer treatment. Oncology 2014;87(4):232–45
   PubMed Web of Science ®Google Scholar
• Kanda T, Ishikawa T, Takahashi T, Nishida T. Nilotinib for treatment of gastrointestinal stromal tumors: out of the equation? Expert Opin Pharmacother 2013;14(13):1859–67
   PubMed Web of Science ®Google Scholar
• Lewis NL, Lewis LD, Eder JP, et al. Phase I study of the safety, tolerability, and pharmacokinetics of oral CP-868,596, a highly specific platelet-derived growth factor receptor tyrosine kinase inhibitor in patients with advanced cancers. J Clin Oncol 2009;27(31):5262–9
   PubMed Web of Science ®Google Scholar
• Zimmerman EI, Turner DC, Buaboonnam J, et al. Crenolanib is active against models of drug-resistant FLT3-ITD-positive acute myeloid leukemia. Blood 2013;122(22):3607–15
   PubMed Web of Science ®Google Scholar
• Angevin E, Lopez-Martin JA, Lin C-C, et al. Phase I study of dovitinib (TKI258), an oral FGFR, VEGFR, and PDGFR inhibitor, in advanced or metastatic renal cell carcinoma. Clin Cancer Res 2013;19(5):1257–68
   PubMed Web of Science ®Google Scholar
• Kang Y-K, Yoo C, Ryoo B-Y, et al. Phase II study of dovitinib in patients with metastatic and/or unresectable gastrointestinal stromal tumours after failure of imatinib and sunitinib. Br J Cancer 2013;109(9):2309–15
   PubMed Web of Science ®Google Scholar
• Motzer RJ, Porta C, Vogelzang NJ, et al. Dovitinib versus sorafenib for third-line targeted treatment of patients with metastatic renal cell carcinoma: an open-label, randomised phase 3 trial. Lancet Oncol 2014;15(3):286–96
   PubMed Web of Science ®Google Scholar
• Glen H, Mason S, Patel H, et al. E7080, a multi-targeted tyrosine kinase inhibitor suppresses tumor cell migration and invasion. BMC Cancer 2011;11:309
   PubMed Web of Science ®Google Scholar
• Lenvatinib slows progression of thyroid cancer. Cancer Discov 2014;4(8):OF7
   Google Scholar
• Ikeda AK, Judelson DR, Federman N, et al. ABT-869 inhibits the proliferation of Ewing Sarcoma cells and suppresses platelet-derived growth factor receptor beta and c-KIT signaling pathways. Mol Cancer Ther 2010;9(3):653–60
   PubMed Web of Science ®Google Scholar
• O’Neil BH, Cainap C, Van Cutsem E, et al. Randomized phase II open-label study of mFOLFOX6 in combination with linifanib or bevacizumab for metastatic colorectal cancer. Clin Colorectal Cancer 2014;13(3):156–163.e2
   PubMed Web of Science ®Google Scholar
• Toh HC, Chen P-J, Carr BI, et al. Phase 2 trial of linifanib (ABT-869) in patients with unresectable or metastatic hepatocellular carcinoma. Cancer 2013;119(2):380–7
   PubMed Web of Science ®Google Scholar
• Tan E-H, Goss GD, Salgia R, et al. Phase 2 trial of Linifanib (ABT-869) in patients with advanced non-small cell lung cancer. J Thorac Oncol 2011;6(8):1418–25
   PubMed Web of Science ®Google Scholar
• Mitry E, Hammel P, Deplanque G, et al. Safety and activity of masitinib in combination with gemcitabine in patients with advanced pancreatic cancer. Cancer Chemother Pharmacol 2010;66(2):395–403
   PubMed Web of Science ®Google Scholar
• Adenis A, Blay J-Y, Bui-Nguyen B, et al. Masitinib in advanced gastrointestinal stromal tumor (GIST) after failure of imatinib: a randomized controlled open-label trial. Ann Oncol 2014;25(9):1762–9
   PubMed Web of Science ®Google Scholar
• Rosen LS, Kurzrock R, Mulay M, et al. Safety, pharmacokinetics, and efficacy of AMG 706, an oral multikinase inhibitor, in patients with advanced solid tumors. J Clin Oncol 2007;25(17):2369–76
   PubMed Web of Science ®Google Scholar
• Schilder RJ, Sill MW, Lankes HA, et al. A phase II evaluation of motesanib (AMG 706) in the treatment of persistent or recurrent ovarian, fallopian tube and primary peritoneal carcinomas: a Gynecologic Oncology Group study. Gynecol Oncol 2013;129(1):86–91
   PubMed Web of Science ®Google Scholar
• Novello S, Scagliotti GV, Sydorenko O, et al. Motesanib plus carboplatin/paclitaxel in patients with advanced squamous non-small-cell lung cancer: results from the randomized controlled MONET1 study. J Thorac Oncol 2014;9(8):1154–61
   PubMed Web of Science ®Google Scholar
• Scagliotti GV, Vynnychenko I, Park K, et al. International, randomized, placebo-controlled, double-blind phase III study of motesanib plus carboplatin/paclitaxel in patients with advanced nonsquamous non-small-cell lung cancer: MONET1. J Clin Oncol 2012;30(23):2829–36
   PubMed Web of Science ®Google Scholar
• Benjamin RS, Schöffski P, Hartmann JT, et al. Efficacy and safety of motesanib, an oral inhibitor of VEGF, PDGF, and Kit receptors, in patients with imatinib-resistant gastrointestinal stromal tumors. Cancer Chemother Pharmacol 2011;68(1):69–77
   PubMed Web of Science ®Google Scholar
• Schlumberger MJ, Elisei R, Bastholt L, et al. 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;27(23):3794–801
   PubMed Web of Science ®Google Scholar
• Casanovas O, Hicklin DJ, Bergers G, Hanahan D. Drug resistance by evasion of antiangiogenic targeting of VEGF signaling in late-stage pancreatic islet tumors. Cancer Cell 2005;8(4):299–309
   PubMed Web of Science ®Google Scholar
• Reck M, Kaiser R, Mellemgaard A, et al. Docetaxel plus nintedanib versus docetaxel plus placebo in patients with previously treated non-small-cell lung cancer (LUME-Lung 1): a phase 3, double-blind, randomised controlled trial. Lancet Oncol 2014;15(2):143–55
   PubMed Web of Science ®Google Scholar
• Hanna NH, Kaiser R, Sullivan RN, et al. Lume-lung 2: a multicenter, randomized, double-blind, phase III study of nintedanib plus pemetrexed versus placebo plus pemetrexed in patients with advanced nonsquamous non-small cell lung cancer (NSCLC) after failure of first-line chemotherapy. J Clin Oncol 2013;31(Suppl):abstract 8034
   Google Scholar
• Kuenen BC, Giaccone G, Ruijter R, et al. Dose-finding study of the multitargeted tyrosine kinase inhibitor SU6668 in patients with advanced malignancies. Clin Cancer Res 2005;11(17):6240–6
   PubMed Web of Science ®Google Scholar
• Strumberg D, Schultheis B, Adamietz IA, et al. Phase I dose escalation study of telatinib (BAY 57-9352) in patients with advanced solid tumours. Br J Cancer 2008;99(10):1579–85
   PubMed Web of Science ®Google Scholar
• Eskens FALM, Steeghs N, Verweij J, et al. Phase I dose escalation study of telatinib, a tyrosine kinase inhibitor of vascular endothelial growth factor receptor 2 and 3, platelet-derived growth factor receptor beta, and c-Kit, in patients with advanced or metastatic solid tumors. J Clin Oncol 2009;27(25):4169–76
   PubMed Web of Science ®Google Scholar
• Langenberg MHG, Witteveen PO, Roodhart J, et al. Phase I evaluation of telatinib, a VEGF receptor tyrosine kinase inhibitor, in combination with bevacizumab in subjects with advanced solid tumors. Ann Oncol 2011;22(11):2508–15
   PubMed Web of Science ®Google Scholar
• Langenberg MHG, Witteveen PO, Roodhart JM, et al. Phase I evaluation of telatinib, a vascular endothelial growth factor receptor tyrosine kinase inhibitor, in combination with irinotecan and capecitabine in patients with advanced solid tumors. Clin Cancer Res 2010;16(7):2187–97
   PubMed Web of Science ®Google Scholar
• Eskens FALM, de Jonge MJA, Bhargava P, et al. Biologic and clinical activity of tivozanib (AV-951, KRN-951), a selective inhibitor of VEGF receptor-1, -2, and -3 tyrosine kinases, in a 4-week-on, 2-week-off schedule in patients with advanced solid tumors. Clin Cancer Res 2011;17(22):7156–63
   PubMed Web of Science ®Google Scholar
• Mayer EL, Scheulen ME, Beckman J, et al. A Phase I dose-escalation study of the VEGFR inhibitor tivozanib hydrochloride with weekly paclitaxel in metastatic breast cancer. Breast Cancer Res Treat 2013;140(2):331–9
   PubMed Web of Science ®Google Scholar
• Wolpin BM, Ng K, Zhu AX, et al. Multicenter phase II study of tivozanib (AV-951) and everolimus (RAD001) for patients with refractory, metastatic colorectal cancer. Oncologist 2013;18(4):377–8
   PubMed Web of Science ®Google Scholar
• Motzer RJ, Nosov D, Eisen T, et al. Tivozanib versus sorafenib as initial targeted therapy for patients with metastatic renal cell carcinoma: results from a phase III trial. J Clin Oncol 2013;31(30):3791–9
   PubMed Web of Science ®Google Scholar
• Gerber DE, Gupta P, Dellinger MT, et al. Stromal platelet-derived growth factor receptor α (PDGFRα) provides a therapeutic target independent of tumor cell PDGFRα expression in lung cancer xenografts. Mol Cancer Ther 2012;11(11):2473–82
   PubMed Web of Science ®Google Scholar
• Laing N, McDermott B, Wen S, et al. Inhibition of platelet-derived growth factor receptor α by MEDI-575 reduces tumor growth and stromal fibroblast content in a model of non-small cell lung cancer. Mol Pharmacol 2013;83(6):1247–56
   PubMed Web of Science ®Google Scholar
• Chiorean EG, Sweeney C, Youssoufian H, et al. A phase I study of olaratumab, an anti-platelet-derived growth factor receptor alpha (PDGFRα) monoclonal antibody, in patients with advanced solid tumors. Cancer Chemother Pharmacol 2014;73(3):595–604
   PubMed Web of Science ®Google Scholar
• Matsuo K, Nishimura M, Komurov K, et al. Platelet-derived growth factor receptor alpha (PDGFRα) targeting and relevant biomarkers in ovarian carcinoma. Gynecol Oncol 2014;132(1):166–75
   PubMed Web of Science ®Google Scholar
• Becerra CR, Conkling P, Vogelzang N, et al. A phase I dose-escalation study of MEDI-575, a PDGFRα monoclonal antibody, in adults with advanced solid tumors. Cancer Chemother Pharmacol 2014;74(5):917–25
   PubMed Web of Science ®Google Scholar
• Druker BJ. Translation of the Philadelphia chromosome into therapy for CML. Blood 2008;112(13):4808–17
   PubMed Web of Science ®Google Scholar
• Joensuu H, Roberts PJ, Sarlomo-Rikala M, et al. Effect of the tyrosine kinase inhibitor STI571 in a patient with a metastatic gastrointestinal stromal tumor. N Engl J Med 2001;344(14):1052–6
   PubMed Web of Science ®Google Scholar
• Rosell R, Moran T, Queralt C, et al. Screening for epidermal growth factor receptor mutations in lung cancer. N Engl J Med 2009;361(10):958–67
   PubMed Web of Science ®Google Scholar
• Rosell R, Carcereny E, Gervais R, et al. Erlotinib versus standard chemotherapy as first-line treatment for European patients with advanced EGFR mutation-positive non-small-cell lung cancer (EURTAC): a multicentre, open-label, randomised phase 3 trial. Lancet Oncol 2012;13(3):239–46
   PubMed Web of Science ®Google Scholar
• Wu Y-L, Zhou C, Hu C-P, et al. Afatinib versus cisplatin plus gemcitabine for first-line treatment of Asian patients with advanced non-small-cell lung cancer harbouring EGFR mutations (LUX-Lung 6): an open-label, randomised phase 3 trial. Lancet Oncol 2014;15(2):213–22
   PubMed Web of Science ®Google Scholar
• Sordella R, Bell DW, Haber DA, Settleman J. Gefitinib-sensitizing EGFR mutations in lung cancer activate anti-apoptotic pathways. Science 2004;305(5687):1163–7
   PubMed Web of Science ®Google Scholar
• Negri T, Bozzi F, Conca E, et al. Oncogenic and ligand-dependent activation of KIT/PDGFRA in surgical samples of imatinib-treated gastrointestinal stromal tumours (GISTs). J Pathol 2009;217(1):103–12
   PubMed Web of Science ®Google Scholar
• Sawyers CL. Imatinib GIST keeps finding new indications: successful treatment of dermatofibrosarcoma protuberans by targeted inhibition of the platelet-derived growth factor receptor. J Clin Oncol 2002;20(17):3568–9
   PubMed Web of Science ®Google Scholar
• Golub TR, Barker GF, Lovett M, Gilliland DG. Fusion of PDGF receptor beta to a novel ets-like gene, tel, in chronic myelomonocytic leukemia with t(5;12) chromosomal translocation. Cell 1994;77(2):307–16
   PubMed Web of Science ®Google Scholar
• McLornan DP, List A, Mufti GJ. Applying synthetic lethality for the selective targeting of cancer. N Engl J Med 2014;371(18):1725–35
   PubMed Web of Science ®Google Scholar
• Arrondeau J, Mir O, Boudou-Rouquette P, et al. Sorafenib exposure decreases over time in patients with hepatocellular carcinoma. Invest New Drugs 2012;30(5):2046–9
   PubMed Web of Science ®Google Scholar
• Bellesoeur A, Carton E, Mir O, et al. Critical role of sorafenib exposure over time for its antitumor activity in thyroid cancer. Invest New Drugs 2014;32(3):569–72
   PubMed Web of Science ®Google Scholar
• Huillard O, Boissier E, Blanchet B, et al. Drug safety evaluation of sorafenib for treatment of solid tumors: consequences for the risk assessment and management of cancer patients. Expert Opin Drug Saf 2014;13(5):663–73
   PubMed Web of Science ®Google Scholar
• Hutson TE, Lesovoy V, Al-Shukri S, et al. Axitinib versus sorafenib as first-line therapy in patients with metastatic renal-cell carcinoma: a randomised open-label phase 3 trial. Lancet Oncol 2013;14(13):1287–94
   PubMed Web of Science ®Google Scholar
• McCarty MF, Somcio RJ, Stoeltzing O, et al. Overexpression of PDGF-BB decreases colorectal and pancreatic cancer growth by increasing tumor pericyte content. J Clin Invest 2007;117(8):2114–22
   PubMed Web of Science ®Google Scholar
• Griffin RJ, Williams BW, Wild R, et al. Simultaneous inhibition of the receptor kinase activity of vascular endothelial, fibroblast, and platelet-derived growth factors suppresses tumor growth and enhances tumor radiation response. Cancer Res 2002;62(6):1702–6
   PubMed Web of Science ®Google Scholar
• Crawford Y, Kasman I, Yu L, et al. PDGF-C mediates the angiogenic and tumorigenic properties of fibroblasts associated with tumors refractory to anti-VEGF treatment. Cancer Cell 2009;15(1):21–34
   PubMed Web of Science ®Google Scholar