- Sorafenib in advanced hepatocellular carcinoma
Josep M Llovet
Barcelona Clinic Liver Cancer Group, Institut d Investigacions Biomediques August Pi i Sunyer, Centro de Investigaciones en Red de Enfermedades Hepáticas y Digestivas Hospital Clínic Barcelona, Barcelona
N Engl J Med 359:378-90. 2008
..A preliminary study suggested that sorafenib, an oral multikinase inhibitor of the vascular endothelial growth factor receptor, the platelet-derived growth factor receptor, and Raf may be effective in hepatocellular carcinoma...
- Efficacy and safety of sorafenib in patients in the Asia-Pacific region with advanced hepatocellular carcinoma: a phase III randomised, double-blind, placebo-controlled trial
Ann Lii Cheng
National Taiwan University Hospital, Taipei, Taiwan
Lancet Oncol 10:25-34. 2009
- BAY 43-9006 exhibits broad spectrum oral antitumor activity and targets the RAF/MEK/ERK pathway and receptor tyrosine kinases involved in tumor progression and angiogenesis
Scott M Wilhelm
Bayer Pharmaceuticals Corporation, West Haven, Connecticut 06516, USA
Cancer Res 64:7099-109. 2004
..These data demonstrate that BAY 43-9006 is a novel dual action RAF kinase and VEGFR inhibitor that targets tumor cell proliferation and tumor angiogenesis...
- Comparative effectiveness of axitinib versus sorafenib in advanced renal cell carcinoma (AXIS): a randomised phase 3 trial
Brian I Rini
Cleveland Clinic Taussig Cancer Institute, Main Campus, Euclid Avenue, Cleveland, OH 44195, USA
Lancet 378:1931-9. 2011
- Sorafenib for treatment of renal cell carcinoma: Final efficacy and safety results of the phase III treatment approaches in renal cancer global evaluation trial
Institut Gustave Roussy, Villejuif, France
J Clin Oncol 27:3312-8. 2009
- Preclinical overview of sorafenib, a multikinase inhibitor that targets both Raf and VEGF and PDGF receptor tyrosine kinase signaling
Scott M Wilhelm
Bayer HealthCare Pharmaceuticals, 340 Changebridge Road, P O Box 1000, Montville, NJ 07045 1000, USA
Mol Cancer Ther 7:3129-40. 2008
..In particular, preclinical evidence that supports the different mechanisms of action of sorafenib is discussed...
- Sorafenib blocks the RAF/MEK/ERK pathway, inhibits tumor angiogenesis, and induces tumor cell apoptosis in hepatocellular carcinoma model PLC/PRF/5
Department of Cancer Biology, Bayer HealthCare Pharmaceuticals, West Haven, Connecticut 06516, USA
Cancer Res 66:11851-8. 2006
- Sorafenib in advanced clear-cell renal-cell carcinoma
Department of Medicine, Institut Gustave Roussy, Villejuif, France
N Engl J Med 356:125-34. 2007
..We conducted a phase 3, randomized, double-blind, placebo-controlled trial of sorafenib, a multikinase inhibitor of tumor-cell proliferation and angiogenesis, in patients with advanced clear-cell renal-cell carcinoma...
- Regorafenib (BAY 73-4506): a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity
Scott M Wilhelm
Bayer HealthCare Pharmaceuticals, Montville, NJ, USA
Int J Cancer 129:245-55. 2011
..These data demonstrate that regorafenib is a well-tolerated, orally active multikinase inhibitor with a distinct target profile that may have therapeutic benefit in human malignancies...
- Prognostic factors for overall survival in patients with metastatic renal cell carcinoma treated with vascular endothelial growth factor-targeted agents: results from a large, multicenter study
Daniel Y C Heng
FRCPC, Department of Medical Oncology, Tom Baker Cancer Center, University of Calgary, Calgary, Alberta, Canada
J Clin Oncol 27:5794-9. 2009
..There are no robust data on prognostic factors for overall survival (OS) in patients with metastatic renal cell carcinoma (RCC) treated with vascular endothelial growth factor (VEGF) -targeted therapy...
- Signal transducer and activator of transcription 3 is a major kinase-independent target of sorafenib in hepatocellular carcinoma
Wei Tien Tai
National Center of Excellence for Clinical Trial and Research, National Taiwan University Hospital, Taipei, Taiwan
J Hepatol 55:1041-8. 2011
..Here, we report that sorafenib inhibits HCC via a kinase-independent mechanism: SHP-1 dependent STAT3 inactivation...
- Discovery and development of sorafenib: a multikinase inhibitor for treating cancer
Department of Cancer Research, Bayer Pharmaceuticals Corp, West Haven, Connecticut 06516, USA
Nat Rev Drug Discov 5:835-44. 2006
- Phase II trial of sorafenib in advanced thyroid cancer
Developmental TherapeuticsProgram of the Abramson CancerCenter, University of Pennsylvania, Philadelphia, PA 19104, USA
J Clin Oncol 26:4714-9. 2008
- Sorafenib in advanced melanoma: a Phase II randomised discontinuation trial analysis
Royal Marsden Hospital, Downs Road, Surrey SMT 5PT, UK
Br J Cancer 95:581-6. 2006
..i.d.). Ongoing trials in advanced melanoma are evaluating sorafenib combination therapies...
- Phase II study of sorafenib in patients with metastatic or recurrent sarcomas
Robert G Maki
Melanoma Sarcoma Program, Department of Medicine, Memorial Sloan Kettering Cancer Center, 1275 York Ave, Howard 909, New York, NY 10065, USA
J Clin Oncol 27:3133-40. 2009
..Further evaluation of sorafenib in these and possibly other sarcoma subtypes appears warranted, presumably in combination with cytotoxic or kinase-specific agents...
- Phase II study of axitinib in sorafenib-refractory metastatic renal cell carcinoma
Brian I Rini
Department of Solid Tumor Oncology and Urology, Cleveland Clinic Taussig Cancer Institute, 9500 Euclid Ave, Desk R35, Cleveland, OH 44195, USA
J Clin Oncol 27:4462-8. 2009
- Validation of ITD mutations in FLT3 as a therapeutic target in human acute myeloid leukaemia
Catherine C Smith
Division of Hematology Oncology, University of California, San Francisco, California 94143, USA
Nature 485:260-3. 2012
..Our findings demonstrate that FLT3-ITD can represent a driver lesion and valid therapeutic target in human AML. AC220-resistant FLT3 kinase domain mutants represent high-value targets for future FLT3 inhibitor development efforts...
- Sorafenib (BAY 43-9006) inhibits tumor growth and vascularization and induces tumor apoptosis and hypoxia in RCC xenograft models
Yong S Chang
Department of Protein Therapeutics, Bayer Research Center, Bayer HealthCare, Pharmaceuticals, 400 Morgan Lane, West Haven, CT 06516, USA
Cancer Chemother Pharmacol 59:561-74. 2007
..The effect of sorafenib on tumor growth and tumor histology was assessed in both ectopic and orthotopic mouse models of RCC...
- Epidermal growth factor receptor and HER-3 restrict cell response to sorafenib in hepatocellular carcinoma cells
Marie José Blivet-Van Eggelpoël
UPMC Univ Paris 06, UMR_S 938, F 75012 Paris, France
J Hepatol 57:108-15. 2012
..However, primary and acquired resistance is observed in patients. We examined whether gefitinib, which inhibits both epidermal growth factor receptor (EGFR) and HER-3 phosphorylation, could improve HCC cell response to sorafenib...
- Sorafenib induces cell death in chronic lymphocytic leukemia by translational downregulation of Mcl-1
Third Department of Medicine, Technical University, Munich, Germany
Leukemia 25:838-47. 2011
..Conclusively, sorafenib is highly active in CLL and may compose a new therapeutic option for patients who relapse after immunochemotherapy...
- A phase II trial of sorafenib in metastatic melanoma with tissue correlates
Patrick A Ott
Department of Medical Oncology, New York University School of Medicine, New York, New York, United States of America
PLoS ONE 5:e15588. 2010
..Sorafenib monotherapy in patients with metastatic melanoma was explored in this multi-institutional phase II study. In correlative studies the impact of sorafenib on cyclin D1 and Ki67 was assessed...
- Activation of phosphatidylinositol 3-kinase/Akt signaling pathway mediates acquired resistance to sorafenib in hepatocellular carcinoma cells
Kuen Feng Chen
Department of Medical Research, National Taiwan University Hospital, No 7, Chung Shan S Rd, Taipei, Taiwan
J Pharmacol Exp Ther 337:155-61. 2011
..In conclusion, activation of PI3K/Akt signaling pathway mediates acquired resistance to sorafenib in HCC, and the combination of sorafenib and MK-2206, an Akt inhibitor, overcomes the resistance at clinical achievable concentrations...
- PI-103 and sorafenib inhibit hepatocellular carcinoma cell proliferation by blocking Ras/Raf/MAPK and PI3K/AKT/mTOR pathways
Department of Surgery, University of Kentucky, College of Medicine, Lexington, KY 40536, USA
Anticancer Res 30:4951-8. 2010
..This study reports how sorafenib (a multi-kinase inhibitor) and PI-103 (a dual PI3K/mTOR inhibitor) alone and in combination inhibit the proliferation of the HCC cell line, Huh7...
- Phase III study of carboplatin and paclitaxel alone or with sorafenib in advanced non-small-cell lung cancer
Department of Clinical and Biological Sciences, University of Turin, San Luigi Hospital, Regione Gonzole 10, Orbassano, Torino, Italy 10043
J Clin Oncol 28:1835-42. 2010
..4%), hand-foot skin reaction (7.8%), and diarrhea (3.5%). CONCLUSION No clinical benefit was observed from adding sorafenib to CP chemotherapy as first-line treatment for NSCLC...
- Plasma biomarkers as predictors of outcome in patients with advanced hepatocellular carcinoma
Josep M Llovet
Barcelona Clinic Liver Cancer Group, Liver Unit, CIBERehd, Institut d Investigacions Biomédiques, August Pi i Sunyer, Hospital Clinic Barcelona, Barcelona, Spain
Clin Cancer Res 18:2290-300. 2012
..One of the objectives of the phase III, randomized, controlled Sorafenib HCC Assessment Randomized Protocol (SHARP) trial was to explore the ability of plasma biomarkers to predict prognosis and therapeutic efficacy...
- EGFR activation is a potential determinant of primary resistance of hepatocellular carcinoma cells to sorafenib
Inserm U1088, Faculte de Medecine, Universite de Picardie Jules Verne, Amiens, France
Int J Cancer 131:2961-9. 2012
..Our findings bear possible implications for the improvement of the efficacy of sorafenib in HCC, and might be useful for the identification of predictive biomarkers in this context...
- Dovitinib induces apoptosis and overcomes sorafenib resistance in hepatocellular carcinoma through SHP-1-mediated inhibition of STAT3
Wei Tien Tai
Department of Medical Research, National Taiwan University Hospital, Chung Shan S Rd, Taipei 100, Taiwan
Mol Cancer Ther 11:452-63. 2012
..In conclusion, dovitinib induces significant apoptosis in HCC cells and sorafenib-resistant cells via SHP-1-mediated inhibition of STAT3...
- Sorafenib induces apoptosis and autophagy in prostate cancer cells in vitro
Department of Oncology Pathology, Cancer Centrum Karolinska, Karolinska Institutet, 17176 Stockholm, Sweden
Int J Oncol 37:15-20. 2010
- Targeting autophagy enhances sorafenib lethality for hepatocellular carcinoma via ER stress-related apoptosis
Ying Hong Shi
Department of Liver Surgery, Liver Cancer Institute, Zhongshan Hospital, Fudan University, Shanghai, China
Autophagy 7:1159-72. 2011
..The combination of autophagy modulation and molecular targeted therapy is a promising therapeutic strategy in treatment of HCC...
- Sorafenib for the treatment of advanced renal cell carcinoma
Robert C Kane
Division of Drug Oncology Products, Center for Drug Evaluation and Research, U S Food and Drug Administration, Silver Spring, Maryland 20993 0004, USA
Clin Cancer Res 12:7271-8. 2006
..S. Food and Drug Administration (FDA) review and approval of sorafenib (Nexavar, BAY43-9006), a new small-molecule, oral, multi-kinase inhibitor for the treatment of patients with advanced renal cell carcinoma (RCC)...
- The Bcl-xL inhibitor, ABT-737, efficiently induces apoptosis and suppresses growth of hepatoma cells in combination with sorafenib
Department of Gastroenterology and Hepatology, Osaka University Graduate School of Medicine, Suita, Osaka, Japan
Hepatology 52:1310-21. 2010
..Sorafenib, not alone but in combination with ABT-737, efficiently induced apoptosis in hepatoma cells. This combination also led to stronger suppression of xenograft tumors than sorafenib alone...
- Doxorubicin plus sorafenib vs doxorubicin alone in patients with advanced hepatocellular carcinoma: a randomized trial
Ghassan K Abou-Alfa
Department of Medicine, Memorial Sloan Kettering Cancer Center, 1275 York Ave, New York, NY 10065, USA
JAMA 304:2154-60. 2010
..The combination of sorafenib and doxorubicin in patients with advanced HCC has not been evaluated in a phase 2 or 3 trial...
- AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML)
Patrick P Zarrinkar
Ambit Biosciences, San Diego, CA 92121, USA
Blood 114:2984-92. 2009
- A phase II study of sorafenib in patients with chemo-naive castration-resistant prostate cancer
K N Chi
Department of Medical Oncology, Vancouver Centre, BC Cancer Agency, Vancouver, British Columbia
Ann Oncol 19:746-51. 2008
..The purpose of this trial was to evaluate the antitumor activity of sorafenib, a multikinase inhibitor of cell proliferation and angiogenesis, in patients with castration-resistant prostate cancer...
- SWOG 0514: a phase II study of sorafenib in patients with unresectable or metastatic gallbladder carcinoma and cholangiocarcinoma
Anthony B El-Khoueiry
University of Southern California Norris Comprehensive Cancer Center, 1441 Eastlake Ave, Suite 3459, Los Angeles, CA 90033, USA
Invest New Drugs 30:1646-51. 2012
..Based on the role of the Ras-Raf-Mek-Erk pathway and the VEGF axis in biliary carcinomas, we conducted a phase II study of sorafenib in patients with advanced biliary cancers...
- Sorafenib inhibits transforming growth factor β1-mediated epithelial-mesenchymal transition and apoptosis in mouse hepatocytes
Yue Lei Chen
Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, Shanghai, China
Hepatology 53:1708-18. 2011
- A phase I study of E7080, a multitargeted tyrosine kinase inhibitor, in patients with advanced solid tumours
D S Boss
Division of Medical Oncology, Department of Clinical Pharmacology, The Netherlands Cancer Institute, Plesmanlaan 121, Amsterdam, The Netherlands
Br J Cancer 106:1598-604. 2012
- Phase 2 trial of linifanib (ABT-869) in patients with advanced renal cell cancer after sunitinib failure
Nizar M Tannir
University of Texas, MD Anderson Cancer Center, Houston, 77030, USA
Eur J Cancer 47:2706-14. 2011
..This study assessed the efficacy and safety of linifanib in patients with advanced renal cell carcinoma (RCC) who were previously treated with sunitinib...
- Phase I dose-escalation study and biomarker analysis of E7080 in patients with advanced solid tumors
Department of Internal Medicine, National Cancer Center Hospital, Tokyo, Japan
Clin Cancer Res 17:2528-37. 2011
..This Phase I study investigated maximum tolerated dose (MTD), dose-limiting toxicity (DLT), pharmacokinetics (PK), pharmacodynamics (PD), and efficacy in patients with advanced solid tumors...
- Molecular mechanisms of sorafenib action in liver cancer cells
Institute of Biomedicine and Molecular Immunology Alberto Monroy, National Research Council CNR, Palermo, Italy
Cell Cycle 11:2843-55. 2012
..Further functional analyses may determine whether these genes can serve as potential molecular targets for more effective anti-HCC strategies...
- Comparison of tumor response by Response Evaluation Criteria in Solid Tumors (RECIST) and modified RECIST in patients treated with sorafenib for hepatocellular carcinoma
Department of Medical Oncology, Eugene Marquis Center, Rennes, France
Cancer 118:147-56. 2012
..In the current study, mRECIST were evaluated and were compared with RECIST in patients who received Sor for advanced HCC...
- The efficacy of TACE combined sorafenib in advanced stages hepatocellullar carcinoma
Xu Dong Qu
Department of Radiology, Zhong Shan Hospital, Fudan University, Fenglin Road, Shanghai 200032, People s Republic of China
BMC Cancer 12:263. 2012
..The present study sought to understand the efficacy of the combination of TACE and sorafenib in the treatment of advanced HCC...
- Sorafenib: a clinical and pharmacologic review
Roswell Park Cancer Institute, Elm and Carlton Streets, Buffalo, NY 14263, USA
Expert Opin Pharmacother 11:1943-55. 2010
..Sorafenib is approved for the treatment of advanced inoperable hepatocellular cancer and advanced renal cell cancer...
- Sorafenib inhibits activation of human peripheral blood T cells by targeting LCK phosphorylation
State Key Laboratory of Pharmaceutical Biotechnology, School of Life Sciences, Nanjing University, Nanjing, China
Leukemia 22:1226-33. 2008
..These findings suggest that sorafenib may cause the loss of T-cell immune response by inducing apoptosis and targeting LCK. This could potentially lead to immunosuppression in patients with cancer...
- Validation of an HPLC-UV method for sorafenib determination in human plasma and application to cancer patients in routine clinical practice
Laboratoire de Pharmacologie Toxicologie, Service de Pharmacie, France
J Pharm Biomed Anal 49:1109-14. 2009
..Finally, large interindividual variability and higher exposure in patients experiencing severe toxicity support the need for therapeutic drug monitoring to ensure an optimal exposure to sorafenib...
- Sorafenib, a multikinase inhibitor, enhances the response of melanoma to regional chemotherapy
Christina K Augustine
Department of Surgery, Duke University Medical Center, Durham, North Carolina, USA
Mol Cancer Ther 9:2090-101. 2010
..These results show that sorafenib in combination with chemotherapy provides a novel approach to enhance chemotherapeutic efficacy in the regional treatment of in-transit melanoma...
- Practical efficacy of sorafenib monotherapy for advanced hepatocellular carcinoma patients in a Hepatitis B virus-endemic area
Ju Hyun Shim
Center for Liver Cancer, National Cancer Center, 809 Madu 1 dong, Ilsan gu, Goyang, Goyang, Gyeonggi, 411 769, Republic of Korea
J Cancer Res Clin Oncol 135:617-25. 2009
..This study was conducted to assess the efficacy and safety of sorafenib monotherapy in clinical practice settings for Korean patients with hepatocellular carcinoma (HCC) related primarily to HBV infection...
- Beneficial effects of sorafenib on splanchnic, intrahepatic, and portocollateral circulations in portal hypertensive and cirrhotic rats
Hepatic Hemodynamic Laboratory, Liver Unit, Hospital Clinic, CIBERehd, Barcelona, Spain
Hepatology 49:1245-56. 2009
..Notably, beneficial effects of sorafenib against tissue damage and inflammation were also observed in splanchnic organs...
- Apoptosis induced by the kinase inhibitor BAY 43-9006 in human leukemia cells involves down-regulation of Mcl-1 through inhibition of translation
Departments of Medicine, Biochemistry, and Pharmacology, Virginia Commonwealth University, School of Medicine, Richmond, Virginia 23298
J Biol Chem 280:35217-27. 2005
..Together, these findings demonstrate that BAY 43-9006 mediates cell death in human leukemia cells, at least in part, through down-regulation of Mcl-1 via inhibition of translation...
- Sorafenib inhibits STAT3 activation to enhance TRAIL-mediated apoptosis in human pancreatic cancer cells
Divisions of Oncology and Gastroenterology Hepatology, Mayo Cancer Center, Mayo Clinic, Rochester, Minnesota 55905, USA
Mol Cancer Ther 9:742-50. 2010
..These data indicate that targeting STAT3 may enhance treatment efficacy against pancreatic cancer...
- Safety and efficacy results of the advanced renal cell carcinoma sorafenib expanded access program in North America
Walter M Stadler
Department of Medicine, University of Chicago Medical Center, Chicago, Illinois
Cancer 116:1272-80. 2010
..The Advanced Renal Cell Carcinoma Sorafenib (ARCCS) program made sorafenib available to patients with advanced renal cell carcinoma (RCC) before regulatory approval...
- Metastatic renal carcinoma: evaluation of antiangiogenic therapy with dynamic contrast-enhanced CT
Laure S Fournier
Department of Radiology, Assistance Publique Hopitaux de Paris, Hopital Europeen Georges Pompidou, 20 rue Leblanc, Paris 75015, France FR
Radiology 256:511-8. 2010
- FLT3-mutant allelic burden and clinical status are predictive of response to FLT3 inhibitors in AML
Keith W Pratz
Sidney Kimmel Comprehensive Cancer Center, Johns Hopkins University, Baltimore, MD 21231, USA
Blood 115:1425-32. 2010
..These results have important implications for the potential therapeutic use of FLT3 inhibitors in that patients with newly diagnosed FLT3-mutant AML might be less likely to respond clinically to highly selective FLT3 inhibition...
- Potentiation of alpha7 nicotinic acetylcholine receptors via an allosteric transmembrane site
Gareth T Young
Department of Neuroscience, Physiology and Pharmacology, University College London, Gower Street, London WC1E 6BT, United Kingdom
Proc Natl Acad Sci U S A 105:14686-91. 2008
..Our findings suggest that this is a conserved modulatory allosteric site within neurotransmitter-gated ion channels...
- Phase III trial of carboplatin and paclitaxel with or without sorafenib in metastatic melanoma
Keith T Flaherty
Massachusetts General Hospital, 55 Fruit St, Yawkey 9E, Boston, MA 02114, USA
J Clin Oncol 31:373-9. 2013
..The primary objective of this study was to determine whether carboplatin, paclitaxel, and sorafenib (CPS) improve overall survival (OS) compared with carboplatin and paclitaxel (CP) in chemotherapy-naive patients with metastatic melanoma...
- Perfusion MRI for monitoring the effect of sorafenib on experimental prostate carcinoma: a validation study
Clemens C Cyran
Department of Clinical Radiology, Center for Experimental Radiology, University Hospitals Munich, Campus Grosshadern, Ludwig Maximilians University Munich, Marchioninistrasse 15, 81377 Munich, Germany
AJR Am J Roentgenol 198:384-91. 2012
- New insights into the antifibrotic effects of sorafenib on hepatic stellate cells and liver fibrosis
Department of Gastroenterology, The Second Hospital of Hebei Medical University, Hebei Key Laboratory of Gastroenterology, Hebei Institute of Gastroenterology, Shijiazhuang, Hebei, China
J Hepatol 53:132-44. 2010
- Effect of sorafenib on murine liver regeneration
Department of Clinical Research, University of Bern, Switzerland
Hepatology 53:577-86. 2011
..An increase of VEGF-A levels was observed in mice receiving sorafenib. Wound-healing complications were observed in animals receiving sorafenib after surgery and confirmed on histological sections...
- Ras pathway activation in hepatocellular carcinoma and anti-tumoral effect of combined sorafenib and rapamycin in vivo
Mount Sinai Liver Cancer Program, Mount Sinai School of Medicine, 1425 Madison Avenue, New York, NY 10029, USA
J Hepatol 51:725-33. 2009
..We investigated the molecular alterations of the Ras pathway in HCC and the antineoplastic effects of sorafenib in combination with rapamycin, an inhibitor of mTOR pathway, in experimental models...
- Tyrosine kinase inhibitors are potent acute pulmonary vasodilators in rats
Department of Pharmacology, University of South Alabama, Mobile, Alabama, USA
Am J Respir Cell Mol Biol 45:804-8. 2011
..Vascular smooth muscle relaxation mediated via activation of myosin light chain phosphatase (Ca(2+) desensitization) appears to play a role in the imatinib-induced pulmonary vasodilation...
- Erg K+ channels modulate contractile activity in the bovine epididymal duct
Institute of Vegetative Physiology and Pathophysiology, University Medical Center, Hamburg Eppendorf, Hamburg, Germany
Am J Physiol Regul Integr Comp Physiol 294:R895-904. 2008
..In summary, these data provide strong evidence for a physiological role of erg1 channels in regulating epididymal motility patterns...
- The combination of sorafenib with transarterial chemoembolisation for hepatocellular carcinoma
Division of Gastroenterology, Hepatology and Nutrition, Section of Hepatobiliary Diseases, Department of Medicine, University of Florida, Gainesville, FL 32610 0214, USA
Aliment Pharmacol Ther 34:205-13. 2011
..Standard of practice involves using transarterial therapy for multifocal hepatocellular carcinoma (HCC) alone and sorafenib only for more advanced HCC, but the sorafenib and transarterial therapy combination may provide greater efficacy...
- Inhibiting oncogenic signaling by sorafenib activates PUMA via GSK3β and NF-κB to suppress tumor cell growth
Department of Pharmacology and Chemical Biology, Hillman Cancer Center, University of Pittsburgh, Pittsburgh, PA 15213, USA
Oncogene 31:4848-58. 2012
..They provide a rationale for manipulating the apoptotic machinery to improve sensitivity and overcome resistance to the therapies that target oncogenic kinase signaling...
- Sorafenib for the treatment of unresectable hepatocellular carcinoma
Robert C Kane
Office of Oncology Drug Products, Center for Drug Evaluation and Research, US Food and Drug Administration, Silver Spring, MD 20993 0004, USA
Oncologist 14:95-100. 2009
..Montville, NJ, and Onyx Pharmaceuticals Corp., Emeryville, CA), an oral kinase inhibitor, for the treatment of patients with unresectable hepatocellular carcinoma (HCC)...
- Neurotoxicity induced by okadaic acid in the human neuroblastoma SH-SY5Y line can be differentially prevented by α7 and β2* nicotinic stimulation
Laura del Barrio
Instituto Teofilo Hernando, Facultad de Medicina, Universidad Auto noma de Madrid, 28029 Madrid, Spain
Toxicol Sci 123:193-205. 2011
..Therefore, targeting nAChR could offer a strategy for reducing neurodegeneration secondary to hyperphosphorylation of protein τ...
- Gemcitabine plus sorafenib in patients with advanced pancreatic cancer: a phase II trial of the University of Chicago Phase II Consortium
Hedy Lee Kindler
Department of Medicine, Section of Hematology Oncology, University of Chicago, 5841 South Maryland Avenue, MC 2115, Chicago, IL 60637, USA
Invest New Drugs 30:382-6. 2012
..Sorafenib, an inhibitor of B-raf, VEGFR2, and PDGFR-β, has activity against pancreatic cancer in preclinical models. In a phase I trial of gemcitabine plus sorafenib, 57% of pancreatic cancer patients achieved stable disease...
- Dynamic contrast-enhanced computed tomography imaging biomarkers correlated with immunohistochemistry for monitoring the effects of sorafenib on experimental prostate carcinomas
Clemens C Cyran
Department of Clinical Radiology, Center for Experimental Radiology, University Hospitals Munich Campus Grosshadern, Ludwig Maximilians University Munich, Munich, Germany
Invest Radiol 47:49-57. 2012
- Complete remission with tyrosine kinase inhibitors in renal cell carcinoma
Medical Oncology Department, Institut Gustave Roussy, 114 rue Edouard Vaillant, 94805 Villejuif, France
J Clin Oncol 30:482-7. 2012
..It remains a matter of debate whether therapy should be continued after CR...
- Phase II study of sorafenib in patients with relapsed or refractory lymphoma
Medical Oncology, Fondazione IRCCS Istituto Nazionale Tumori, Milano, Italy
Br J Haematol 158:108-19. 2012
..Sorafenib was well tolerated and had a clinical activity that warrants development of combination regimens...
- A double-blind, randomised, placebo-controlled, phase 2b study evaluating sorafenib in combination with paclitaxel as a first-line therapy in patients with HER2-negative advanced breast cancer
William J Gradishar
Northwestern University Feinberg School of Medicine, Chicago, IL 60611, USA
Eur J Cancer 49:312-22. 2013
- Blockade of STAT3 activation by sorafenib derivatives through enhancing SHP-1 phosphatase activity
Kuen Feng Chen
Department of Medical Research, National Taiwan University Hospital, Taipei, Taiwan
Eur J Med Chem 55:220-7. 2012
..In light of the pivotal role of phospho-STAT3 in promoting tumorigenesis and drug resistance, this novel SHP-1-activating agent may have therapeutic relevance in cancer therapy...
- Safety and effectiveness of sorafenib in patients with hepatocellular carcinoma in clinical practice
Giovan Giuseppe Di Costanzo
Liver Unit, Cardarelli Hospital, Naples, Italy
Dig Liver Dis 44:788-92. 2012
..Sorafenib is currently the only approved systemic treatment for hepatocellular carcinoma...
- Regorafenib for patients with previously untreated metastatic or unresectable renal-cell carcinoma: a single-group phase 2 trial
Cambridge University Health Partners, Cambridge, UK
Lancet Oncol 13:1055-62. 2012
..This phase 2, open-label, non-randomised study assessed the safety and efficacy of the multikinase inhibitor regorafenib for treatment of renal-cell carcinoma...
- Sorafenib in treatment of patients with advanced hepatocellular carcinoma: a systematic review
Liver Cancer Institute, Zhongshan Hospital, Fudan University, and Shanghai Key Laboratory for Organ Transplantation, Shanghai 200032, China
Hepatobiliary Pancreat Dis Int 11:458-66. 2012
..This study aimed to assess the efficacy and safety of sorafenib in advanced HCC patients and explore its true value for specific subgroups...
- Forchlorfenuron, a phenylurea cytokinin, disturbs septin organization in Saccharomyces cerevisiae
Department of Biological Sciences, Graduate School of Science, The University of Tokyo, Hongo, Tokyo 113 0033, Japan
Genes Genet Syst 79:199-206. 2004
..Taken together, these findings indicate that FCF maybe a promising drug for investigating the structure and function of septin...
- Targeting the FMS-like tyrosine kinase 3 in acute myeloid leukemia
Sylvester Comprehensive Cancer Center, University of Miami Leonard M Miller School of Medicine, Miami, FL, USA
Leukemia 26:2176-85. 2012
..Novel combination regimens are also discussed...
- BCL-2 family inhibitors enhance histone deacetylase inhibitor and sorafenib lethality via autophagy and overcome blockade of the extrinsic pathway to facilitate killing
Aditi Pandya Martin
Department of Biochemistry and Molecular Biology, Massey Cancer Center, Virginia Commonwealth University, Richmond, VA 23298 0035, USA
Mol Pharmacol 76:327-41. 2009
- Sorafenib as adjuvant therapy for high-risk hepatocellular carcinoma in liver transplant recipients: feasibility and efficacy
Departments of Medicine, The University of California at Los Angeles, Los Angeles, CA, USA
Exp Clin Transplant 8:307-13. 2010
..Liver transplant can be a definitive treatment for hepatocellular carcinoma. However, recurrence limits long-term survival. Sorafenib is the first agent to improve survival for patients with advanced hepatocellular carcinoma...
- Radiation therapy and sorafenib: clinical data and rationale for the combination in metastatic renal cell carcinoma
Department of Radiation Oncology, Duke University Medical Center, Durham, NC 27710, USA
Clin Genitourin Cancer 5:291-4. 2007
..This combination is promising and requires further study...
- Induction of DNA damage-inducible gene GADD45beta contributes to sorafenib-induced apoptosis in hepatocellular carcinoma cells
Da Liang Ou
National Center of Excellence for Clinical Trial and Research, Department of Oncology, National Taiwan University Hospital, Graduate Institute of Toxicology, Department of Clinical Laboratory Sciences and Medical Biotechnology, College of Medicine, National Taiwan University, Taipei, Taiwan
Cancer Res 70:9309-18. 2010
..Together, our findings suggest that GADD45β induction contributes to sorafenib-induced apoptosis in HCC cells, prompting further studies to validate its potential value in predicting sorafenib efficacy...
- Regorafenib (BAY 73-4506) in advanced colorectal cancer: a phase I study
Department of Hematology and Medical Oncology, University of Bochum, Marienhospital Herne, Hölkeskampring 40, D 44625 Herne, Germany
Br J Cancer 106:1722-7. 2012
..In a phase I dose-escalation study, regorafenib demonstrated tolerability and antitumour activity in solid tumour patients. The study was expanded to focus on patients with metastatic colorectal cancer (CRC)...
- The multikinase inhibitor sorafenib induces caspase-dependent apoptosis in PC-3 prostate cancer cells
Department of Nuclear Medicine, National Key Discipline of Medical Imaging and Nuclear Medicine, West China Hospital, Sichuan University, Chengdu, China
Asian J Androl 12:527-34. 2010
..In conclusion, sorafenib induces apoptosis through a caspase-dependent mechanism with down-regulated anti-apoptotic proteins in androgen-independent prostate cancer cells in vitro...
- Antitumor activity and safety of tivozanib (AV-951) in a phase II randomized discontinuation trial in patients with renal cell carcinoma
Dmitry A Nosov
Blokhin Oncology Research Center, Russia
J Clin Oncol 30:1678-85. 2012
..The antitumor activity and safety of tivozanib, which is a potent and selective vascular endothelial growth factor receptor-1, -2, and -3 inhibitor, was assessed in patients with advanced/metastatic renal cell carcinoma (RCC)...
- Sorafenib and radiation: a promising combination in colorectal cancer
Andrew W Suen
Department of Radiation Oncology, William Beaumont Hospital, Royal Oak, MI, USA
Int J Radiat Oncol Biol Phys 78:213-20. 2010
..To examine the combination of radiation and the multikinase inhibitor sorafenib in human colorectal cancer cell lines and xenografts...
- Sequential use of sorafenib and sunitinib in advanced renal-cell carcinoma (RCC): an Italian multicentre retrospective analysis of 189 patient cases
IRCCS San Matteo University Hospital Foundation, Pavia, Italy
BJU Int 108:E250-7. 2011
..To conduct a retrospective, multicentre, cohort analysis to assess the sequential use of the tyrosine kinase inhibitors (TKIs) sorafenib and sunitinib...
- Regorafenib monotherapy for previously treated metastatic colorectal cancer (CORRECT): an international, multicentre, randomised, placebo-controlled, phase 3 trial
Division of Medical Oncology, Mayo Clinic, Rochester, MN, USA
Lancet 381:303-12. 2013
..An international phase 3 trial was done to assess the multikinase inhibitor regorafenib in these patients...
- Toxicity of sorafenib: clinical and molecular aspects
Laboratoire de Pharmacologie Toxicologie, Service de Pharmacie, GH Cochin Saint Vincent de Paul, 75014 Paris, France
Expert Opin Drug Saf 9:275-87. 2010
..Despite its inherent selectivity, sorafenib can cause unusual adverse events whose the management represents a challenge for oncologists...
- Early skin toxicity as a predictive factor for tumor control in hepatocellular carcinoma patients treated with sorafenib
Department of Surgical and Oncological Sciences, Section of Medical Oncology Università di Palermo, Palermo, Italy, Via del Vespro 127, 90127 Palermo, Italy
Oncologist 15:85-92. 2010
..This study was conducted to assess the link between the antitumor efficacy of sorafenib and its early cutaneous side effects in advanced HCC patients...
- A phase I dose-escalation study of regorafenib (BAY 73-4506), an inhibitor of oncogenic, angiogenic, and stromal kinases, in patients with advanced solid tumors
Tumour Biology Center, University Hospital, Freiburg, Germany
Clin Cancer Res 18:2658-67. 2012
..This first-in-man, phase I dose-escalation study assessed the safety, pharmacokinetic, pharmacodynamic, and efficacy profiles of regorafenib in patients with advanced solid tumors...
- XZH-5 inhibits STAT3 phosphorylation and causes apoptosis in human hepatocellular carcinoma cells
Center for Childhood Cancer, Department of Pediatrics, College of Medicine, The Ohio State University, Columbus, 43205, USA
Apoptosis 16:502-10. 2011
..These results suggested that XZH-5 may serve as a lead compound for further development of STAT3 specific small molecule inhibitors for HCC therapy...
- Sorafenib overcomes TRAIL resistance of hepatocellular carcinoma cells through the inhibition of STAT3
Kuen Feng Chen
Department of Medical Research, National Taiwan University Hospital and National Taiwan University College of Medicine, Taipei, Taiwan
Clin Cancer Res 16:5189-99. 2010
..However, many hepatocellular carcinoma (HCC) cells show resistance to TRAIL-induced apoptosis. Here, we report that sorafenib improves the antitumor effect of TRAIL-related agents in resistant HCC...
- Phase II trial of sorafenib in patients with metastatic breast cancer previously exposed to anthracyclines or taxanes: North Central Cancer Treatment Group and Mayo Clinic Trial N0336
Division of Hematology Oncology, Mayo Clinic and Mayo Foundation, Jacksonville, FL 32224, USA
J Clin Oncol 27:11-5. 2009
..We conducted a cooperative group phase II study to assess antitumor activity and toxicity of sorafenib in patients with metastatic breast cancer (MBC) who had received prior treatment for their disease...
- Sorafenib: a review of its use in advanced hepatocellular carcinoma
Gillian M Keating
Wolters Kluwer Health mid R Adis, Auckland, New Zealand
Drugs 69:223-40. 2009
- Clinical responses observed with imatinib or sorafenib in melanoma patients expressing mutations in KIT
Peter MacCallum Cancer Centre, East Melbourne, Victoria, Australia
Br J Cancer 102:1219-23. 2010
..Mutations in KIT are more frequent in specific melanoma subtypes, and response to KIT inhibition is likely to depend on the identified mutation...
- Synergistic antitumor activity of sorafenib in combination with epidermal growth factor receptor inhibitors in colorectal and lung cancer cells
Dipartimento Medico Chirurgico di Internistica Clinica e Sperimentale F Magrassi e A Lanzara, Seconda Universita degli Studi di Napoli, Napoli, Italy
Clin Cancer Res 16:4990-5001. 2010
..Cancer cell survival, invasion, and metastasis depend on cancer cell proliferation and on tumor-induced angiogenesis. We evaluated the efficacy of the combination of sorafenib and erlotinib or cetuximab...
- Sorafenib induces growth inhibition and apoptosis in human synovial sarcoma cells via inhibiting the RAF/MEK/ERK signaling pathway
Chang Liang Peng
Musculoskeletal Tumor Center, Peking University Peoples Hospital, Beijing, China
Cancer Biol Ther 8:1729-36. 2009
..In conclusion, our findings demonstrate that sorafenib is effective for growth inhibition of synovial sarcoma cell lines in vitro and suggest that sorafenib may be a new therapeutic option for patients with synovial sarcoma...
- Phase II evaluation of sorafenib in advanced and metastatic squamous cell carcinoma of the head and neck: Southwest Oncology Group Study S0420
Stephen K Williamson
University of Kansas Cancer Center, Hematology Oncology Division, Westwood, KS 66205, USA
J Clin Oncol 28:3330-5. 2010
..The primary end point was response probability (ie, confirmed complete and partial response [PR])...
- Sorafenib inhibits signal transducer and activator of transcription-3 signaling in cholangiocarcinoma cells by activating the phosphatase shatterproof 2
Boris R A Blechacz
Division of Gastroenterology and Hepatology, Miles and Shirley Fiterman Center for Digestive Diseases, College of Medicine, Mayo Clinic, Rochester, MN 55905, USA
Hepatology 50:1861-70. 2009
..In this in vivo model, sorafenib also decreased tumor Tyr(705) STAT3 phosphorylation and increased tumor cell apoptosis...
- Renal cell carcinoma
Brian I Rini
Cleveland Clinic Taussig Cancer Center, Cleveland, Ohio, USA
Curr Opin Oncol 20:300-6. 2008
..This study is intended to update prognostic and therapeutic decision-making data and provide perspective on advances in understanding the molecular biology of this disease...
- Safety and feasibility of using sorafenib in recurrent hepatocellular carcinoma after orthotopic liver transplantation
Department of Gastrointestinal Oncology, Taussig Cancer Center, Cleveland Clinic, Cleveland, Ohio 44195, USA richard kim moffitt org
Oncology 79:62-6. 2010
..However, 10-15% of patients will have reoccurrence after OLT. Currently, sorafenib is available for advanced HCC. The safety and efficacy of sorafenib in this population has not been reported...
- Multikinase inhibitor sorafenib exerts cytocidal efficacy against Non-Hodgkin lymphomas associated with inhibition of MAPK14 and AKT phosphorylation
Department of Haematology and Oncology, Georg August University Goettingen, Germany
Br J Haematol 152:401-12. 2011
..In conclusion, sorafenib has significant in vitro efficacy against aggressive B- and T-cell lymphoma cells, associated with inhibition of MAPK14 and panAKT...