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Cancer Treatment Reviews
Volume 36, Issue 6
, Pages 492-500
, October 2010
Dasatinib: A potent SRC inhibitor in clinical development for the treatment of solid tumors
References
- . The development of imatinib as a therapeutic agent for chronic myeloid leukemia. Blood. 2005;105:2640–2653
- . Tyrosine kinase inhibitors in cancer therapy. Clin Biochem. 2004;37:618–635
- . Identification and treatment of chemoresistant inoperable or metastatic GIST: experience with the selective tyrosine kinase inhibitor imatinib mesylate (STI571). Eur J Cancer. 2002;38:S52–S59
- . Epidermal growth factor-related peptides and their receptors in human malignancies. Crit Rev Oncol Hematol. 1995;19:183–232
- Second-line treatment of advanced non-small cell lung cancer. J Thorac Oncol. 2008;3:430–440
- FDA drug approval summary: lapatinib in combination with capecitabine for previously treated metastatic breast cancer that overexpresses HER-2. Oncologist. 2008;13:1114–1119
- Approval summary: sunitinib for the treatment of imatinib refractory or intolerant gastrointestinal stromal tumors and advanced renal cell carcinoma. Clin Cancer Res. 2007;13:1367–1373
- Sorafenib for the treatment of advanced renal cell carcinoma. Clin Cancer Res. 2006;12:7271–7278
- . Src family kinases and HER2 interactions in human breast cancer cell growth and survival. Oncogene. 2001;20:1465–1475
- . Src kinase becomes preferentially associated with the VEGFR, KDR/Flk-1, following VEGF stimulation of vascular endothelial cells. BMC Biochem. 2002;3:32
- . Multiple roles for Src in a PDGF-stimulated cell. Exp Cell Res. 1999;253:271–279
- . Src inhibitor dasatinib inhibits growth of breast cancer cells by modulating EGFR signaling. Cancer Lett. 2009;283:143–151
- . Targeting Src signaling in metastatic bone disease. Int J Cancer. 2008;124:1–6
- . Requirement of pp60c-src expression for osteoclasts to form ruffled borders and resorb bone in mice. J Clin Invest. 1992;90:1622–1627
- C-SRC tyrosine kinase activity is associated with tumor colonization in bone and lung in an animal model of human breast cancer metastasis. Cancer Res. 2003;63:5028–5033
- . Targeted disruption of the c-src proto-oncogene leads to osteopetrosis in mice. Cell. 1991;64:693–702
- Latent bone metastasis in breast cancer tied to Src-dependent survival signals. Cancer Cell. 2009;16:67–78
- . Dasatinib is a potent inhibitor of tumour-associated macrophages, osteoclasts and the FMS receptor. Leukemia. 2009;23:590–594
- . Effects of dasatinib on EphA2 receptor tyrosine kinase activity and downstream signalling in pancreatic cancer. Br J Cancer. 2008;99:1074–1082
- Discovery of N-(2-chloro-6-methyl-phenyl)-2-(6-(4-(2-hydroxyethyl)-piperazin-1-yl)-2-methylpyrimidin-4-ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. J Med Chem. 2004;47:6658–6661
- Sprycel for chronic myeloid leukemia and Philadelphia chromosome-positive acute lymphoblastic leukemia resistant to or intolerant of imatinib mesylate. Clin Cancer Res. 2008;14:352–359
- . The role of Src in prostate cancer. Ann Oncol. 2007;18:1765–1773
- FYN is overexpressed in human prostate cancer. BJU Int. 2009;103:171–177
- Interleukin-8 confers androgen-independent growth and migration of LNCaP: differential effects of tyrosine kinases Src and FAK. Oncogene. 2004;23:2197–2205
- Genomic strategy for targeting therapy in castration-resistant prostate cancer. J Clin Oncol. 2009;27:2022–2029
- . SRC family kinase activity is up-regulated in hormone-refractory prostate cancer. Clin Cancer Res. 2009;15:3540–3549
- Action of the Src family kinase inhibitor, dasatinib (BMS-354825), on human prostate cancer cells. Cancer Res. 2005;65:9185–9189
- Targeting SRC family kinases inhibits growth and lymph node metastases of prostate cancer in an orthotopic nude mouse model. Cancer Res. 2008;68:3323–3333
- . Elevated activity and expression of Src-family kinases in human breast carcinoma tissue versus matched non-tumor tissue. J Cancer Res Clin Oncol. 2001;127:226–230
- Dasatinib, an orally active small molecule inhibitor of both the src and abl kinases, selectively inhibits growth of basal-type/“triple-negative” breast cancer cell lines growing in vitro. Breast Cancer Res Treat. 2007;105:319–326
- Identification of candidate molecular markers predicting sensitivity in solid tumors to dasatinib: rationale for patient selection. Cancer Res. 2007;67:2226–2238
- . Dasatinib may also inhibit c-Kit in triple negative breast cancer cell lines. Breast Cancer Res Treat. 2008;107:303
- . An update of the mechanisms of resistance to EGFR-tyrosine kinase inhibitors in breast cancer: Gefitinib (Iressa) -induced changes in the expression and nucleo-cytoplasmic trafficking of HER-ligands (Review). Int J Mol Med. 2007;20:3–10
- Invasive ductal carcinoma of the breast with the “triple-negative” phenotype: prognostic implications of EGFR immunoreactivity. Breast Cancer Res Treat. 2009;116:317–328
- . Characterization of human epidermal growth factor receptor and c-Src interactions in human breast tumor cells. Mol Carcinog. 1998;21:261–272
- . Development and malignant progression of astrocytomas in GFAP-v-src transgenic mice. Oncogene. 1997;14:2005–2013
- . Improving the prognosis for patients with glioblastoma: the rationale for targeting Src. J Neurooncol. 2009;95:151–163
- Bead-based profiling of tyrosine kinase phosphorylation identifies SRC as a potential target for glioblastoma therapy. Nat Biotechnol. 2009;27:77–83
- Pp60c-src activation in lung adenocarcinoma. Eur J Cancer. 2003;39:1447–1455
- . Expression of pp60c-src in human small cell and non-small cell lung carcinomas. Eur J Cancer. 1992;28:372–377
- . Increase in activity and level of pp60c-src in progressive stages of human colorectal cancer. J Clin Invest. 1993;91:53–60
- . Molecular prognostic markers in pancreatic cancer. Cancer Control. 2000;7:421–427
- Epithelial to mesenchymal transition in head and neck squamous carcinoma: association of Src activation with E-cadherin down-regulation, vimentin expression, and aggressive tumor features. Cancer. 2008;112:2088–2100
- Development of transgenic mice that inducibly express an active form of c-Src in the epidermis. Mol Carcinog. 2004;40:189–200
- . Dasatinib (BMS-3548285) tyrosine kinase inhibitor suppresses invasion and induces cell cycle arrest and apoptosis of head and neck squamous cell carinoma and non-small cell lung cancer cell. Clin Cancer Res. 2005;11:6924–6932
- . Dasatinib (BMS-354825) selectively induces apoptosis in lung cancer cells dependent on epidermal growth factor receptor signaling for survival. Cancer Res. 2006;66:5542–5548
- Identification of potential biomarkers for measuring inhibition of Src kinase activity in colon cancer cells following treatment with dasatinib. Mol Cancer Ther. 2006;5:3014–3022
- Inhibition of Src expression and activity inhibits tumor progression and metastasis of human pancreatic adenocarcinoma cells in an orthotopic nude mouse model. Am J Pathol. 2006;168:962–972
- . Inhibition of Src family kinases with dasatinib blocks migration and invasion of human melanoma cells. Mol Cancer Res. 2008;6:1766–1774
- . Preclinical evaluation of dasatinib, a potent Src kinase inhibitor, in melanoma cell lines. J Transl Med. 2008;6:53
- Dasatinib inhibits migration and invasion in diverse human sarcoma cell lines and induces apoptosis in bone sarcoma cells dependent on SRC kinase for survival. Cancer Res. 2007;67:2800–2808
- . In vitro antiproliferative and antimigratory activity of dasatinib in neuroblastoma and Ewing sarcoma cell lines. Oncol Rep. 2008;19:353–359
- . Mechanisms of bone metastasis. N Engl J Med. 2004;350:1655–1664
- Dasatinib in patients with hormone-refractory progressive prostate cancer: a phase II study. J Clin Oncol. 2008;26:288s;(abstract 5156)
- Luo FR, Camuso A, McGlinchey K, et al. Evaluation of anti-osteoclastic activity of the novel, oral multi-targeted kinase inhibitor dasatinib (BMS-354825). In: Proceedings of the molecular targets and cancer therapeutics meeting; 2005. p. 173 (abstract B178).
- Therapeutic concentrations of dasatinib inhibit in vitro osteoclastogenesis. Leukemia. 2009;23:994–997
- . Dasatinib inhibits the growth of prostate cancer in bone and provides additional protection from osteolysis. Br J Cancer. 2009;101:263–268
- . Src continues aging: current and future clinical directions. Clin Cancer Res. 2007;13:7232–7236
- Epidermal growth factor receptor cooperates with Src family kinases in acquired resistance to cetuximab. Cancer Biol Ther. 2009;8:696–703
- Dasatinib synergizes with doxorubicin to block growth, migration, and invasion of breast cancer cells. Br J Cancer. 2009;101:38–47
- Synergistic cell growth inhibition by the combination of amrubicin and Akt-suppressing tyrosine kinase inhibitors in small cell lung cancer cells: implication of c-Src and its inhibitor. Int J Oncol. 2009;34:689–696
- Src activation in melanoma and Src inhibitors as therapeutic agents in melanoma. Melanoma Res. 2009;19:167–175
- Synergistic activity of the SRC family kinase inhibitor dasatinib and oxaliplatin in colon carcinoma cells is mediated by oxidative stress. Cancer Res. 2009;69:3842–3849
- . Abrogation of signal transducer and activator of transcription 3 reactivation after Src kinase inhibition results in synergistic antitumor effects. Clin Cancer Res. 2007;13:4233–4244
- . Dasatinib-induced autophagy is enhanced in combination with temozolomide in glioma. Mol Cancer Ther. 2009;8:394–406
- Inhibition of Hsp90 activates osteoclast c-Src signaling and promotes growth of prostate carcinoma cells in bone. Proc Natl Acad Sci USA. 2008;105:15541–15546
- Bristol-Myers Squibb. Synopsis: final clinical study report for CA180021. Available at <http://ctr.bms.com/pdf//CA180021.pdf> (accessed March 2009).
- Phase I dose-escalation and pharmacokinetic study of dasatinib (BMS-354825), a Src and multi-kinase inhibitor, in patients with advanced solid tumors. Clin Cancer Res. 2009;15:6232–6240
- Phase I open-labeled trial of gemcitabine and dasatinib in advanced solid tumors. J Clin Oncol. 2008;26:637s;(abstract 14626)
- A phase I study of gemcitabine plus dasatinib (GD) or gemcitabine plus dasatinib plus cetuximab (GDC) in refractory solid tumors. J Clin Oncol. 2009;27:(abstract e15506)
- . Phase I and pharmacokinetic (PK) study of dasatinib (D) and cetuximab (C) in patients (pts) with advanced solid malignancies. J Clin Oncol. 2009;27:156s;(abstract 3540)
- A phase II study of once-daily dasatinib for patients with castration-resistant prostate cancer (CA180085). J Clin Oncol. 2009;27:270s;(abstract 5147)
- Araujo J, Gallick G, Trudel G, et al. Dasatinib and docetaxel combination treatment for patients with castration-resistant progressive prostate cancer: a phase 1/2 study (CA180-086). In: Proc ASCO-GU; 2009 (abstract 177).
- Dasatinib and docetaxel combination treatment for patients with castration-resistant progressive prostate cancer: A phase I/II study (CA180086). J Clin Oncol. 2009;27:249s;(abstract 5061)
- Dasatinib plus capecitabine (Cap) for progressive advanced breast cancer (ABC): phase I study CA180004. J Clin Oncol. 2009;27:43s;(abstract 1012)
- Phase II trial of dasatinib in triple-negative breast cancer: results of study CA180059. Proc SABCS. 2008;(abstract 3118)
- Dasatinib in advanced HER2/neu amplified and ER/PR-positive breast cancer: phase II study CA180088. J Clin Oncol. 2009;27:43s;(abstract 1011)
- Phase I trial evaluating the epidermal growth factor receptor inhibitor erlotinib in combination with the SRC kinase inhibitor dasatinib for patients with recurrent non-small cell lung cancer (NSCLC). J Clin Oncol. 2008;26:635s;(abstract 14605)
- Phase II study of dasatinib in non-small cell lung cancer (NSCLC). J Clin Oncol. 2009;27:(abstract e19015)
- A Phase I trial of dasatinib (SPRYCEL) and erlotinib (TARCEVA) for patients with recurrent malignant glioma. Neuro-Oncology. 2008;10:(abstract MA-85)
- Phase 2 trial of dasatinib in patients with recurrent glioblastoma (RTOG 0627). Neuro-Oncology. 2008;10:(abstract MA-30)
- Phase IB study of Src inhibition with dasatinib in combination with 5-fluorouracil, leucovorin, oxaliplatin (FOLFOX) and cetuximab in metastatic colorectal cancer. Proc AACR. 2008;(abstract LB-69)
- Phase II study of dasatinib in the treatment of head and neck squamous cell carcinoma (HNSCC). J Clin Oncol. 2009;27:306s;(abstract 6022)
- A phase II trial of dasatinib in advanced melanoma. J Clin Oncol. 2009;27:463s;(abstract 9010)
- . Inhibition of SRC tyrosine kinase impairs inherent and acquired gemcitabine resistance in human pancreatic adenocarcinoma cells. Clin Cancer Res. 2004;10:2307–2318
- Phase II study of dasatinib in patients with metastatic castration-resistant prostate cancer. Clin Cancer Res. 2009;15:7421–7428
- . Effect of dasatinib on bone metabolism in multiple myeloma. J Clin Oncol. 2008;26:471s;(abstract 8568)
- Activity of dasatinib against L576P KIT mutant melanoma: molecular, cellular, and clinical correlates. Mol Cancer Ther. 2009;8:2079–2085
PII: S0305-7372(10)00035-6
doi: 10.1016/j.ctrv.2010.02.015
« Previous
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Cancer Treatment Reviews
Volume 36, Issue 6
, Pages 492-500
, October 2010
