Regorafenib for cancer

Expert Opinion on Investigational Drugs

Volumn 21, Issue 6, 2012, Pages 879-889

  Strumberg, Dirk ^a   Schultheis, Beate ^a  

^a RUHR UNIVERSITY BOCHUM   (Germany)

Author keywords

Colorectal cancer; Combination treatment; GIST; Regorafenib; Renal cell cancer; Tyrosine kinase inhibitor

Indexed keywords

BIOLOGICAL MARKER; FLUORODEOXYGLUCOSE F 18; IMATINIB; K RAS PROTEIN; ORPHAN DRUG; REGORAFENIB; SUNITINIB; VASCULOTROPIN RECEPTOR 2;

ANOREXIA; ANTINEOPLASTIC ACTIVITY; CANCER PATIENT; COLORECTAL CANCER; COMPUTER ASSISTED TOMOGRAPHY; DIARRHEA; DRUG DOSE ESCALATION; DRUG SAFETY; DRUG WITHDRAWAL; FATIGUE; FEVER; GASTROINTESTINAL STROMAL TUMOR; HOARSENESS; HUMAN; HYPERTENSION; HYPOPHOSPHATEMIA; KIDNEY CARCINOMA; LEUKOPENIA; MELANOMA; MUCOSA INFLAMMATION; MUTATIONAL ANALYSIS; NONHUMAN; OSTEOSARCOMA; OVARY CANCER; PAIN; PANCREAS CARCINOMA; PHASE 1 CLINICAL TRIAL (TOPIC); PHASE 2 CLINICAL TRIAL (TOPIC); POSITRON EMISSION TOMOGRAPHY; RANDOMIZED CONTROLLED TRIAL (TOPIC); RASH; REVIEW; SKIN MANIFESTATION; SQUAMOUS CELL CARCINOMA; TREATMENT RESPONSE;

ANIMALS; ANTINEOPLASTIC AGENTS; DRUG APPROVAL; HUMANS; MICE; NEOPLASMS; ORPHAN DRUG PRODUCTION; PHENYLUREA COMPOUNDS; PROTEIN KINASE INHIBITORS; PYRIDINES; UNITED STATES; UNITED STATES FOOD AND DRUG ADMINISTRATION;

EID: 84861038995     PISSN: 13543784     EISSN: 17447658     Source Type: Journal    
DOI: 10.1517/13543784.2012.684752     Document Type: Review

References (44)

1. Escudier B, Eisen T, Stadler WM, et al. Sorafenib in advanced clear-cell renal-cell carcinoma. N Engl J Med 2007;356:125-34 (Pubitemid 46089673)
2. Llovet JM, Ricci S, Mazzaferro V, et al. Sorafenib in advanced hepatocellular carcinoma. N Engl J Med 2008;359:378-90
3. Strumberg D. Preclinical and clinical development of the oral multikinase inhibitor sorafenib in cancer treatment. Drugs Today (Barc) 2005;41:773-84 (Pubitemid 43333354)
4. Dhillon AS, Hagan S, Rath O, Kolch W. MAP kinase signalling pathways in cancer. Oncogene 2007;26:3279-90 (Pubitemid 46763021)
5. 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;129:245-55
6. Wilhelm SM, Carter C, Tang L, et al. 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. Cancer Res 2004;64:7099-109 (Pubitemid 39331023)
7. Hedbom S, Steinbild S, Frost A, et al. Phase I study of BAY 73-4506, a multikinase inhibitor, administered for 21 days on/7 days off in patients with advanced solid tumors [abstract]. J Clin Oncol 2007;25:3593
8. Mross K, Frost A, Steinbild S, et al. 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. Clin Cancer Res 2012;published online; doi:1078-0432. CCR-11-1900 [pii];10.1158/1078-0432. CCR-11-1900 [doi]
9. Shimizu T, Tolcher AW, Patnaik A, et al. Phase I dose-escalation study of continuously administered regorafenib (BAY 73-4506), an inhibitor of oncogenic and angiogenic kinases, in patients with advanced solid tumors [abstract]. J Clin Oncol 2010;28:3035 .
10. Kies MS, Blumenschein GR Jr, Christensen O, et al. Phase I study of regorafenib (BAY 73-4506), an inhibitor of oncogenic and angiogenic kinases, administered continuously in patients (pts) with advanced refractory non-small cell lung cancer (NSCLC) [abstract]. J Clin Oncol 2010;28:7585
11. Lipworth AD, Robert C, Zhu AX. Hand-foot syndrome (hand-foot skin reaction, palmar-plantar erythrodysesthesia): focus on sorafenib and sunitinib. Oncology 2009;77:257-71
12. Izzedine H, Ederhy S, Goldwasser F, et al. Management of hypertension in angiogenesis inhibitor-treated patients. Ann Oncol 2009;20:807-15
13. Gurevich F, Perazella MA. Renal effects of anti-angiogenesis therapy: update for the internist. Am J Med 2009;122:322-8
14. Izzedine H, Massard C, Spano JP, et al. VEGF signalling inhibition-induced proteinuria: mechanisms, significance and management. Eur J Cancer 2010;46:439-48
15. Torino F, Corsello SM, Longo R, et al. Hypothyroidism related to tyrosine kinase inhibitors: an emerging toxic effect of targeted therapy. Nat Rev Clin Oncol 2009;6:219-28
16. Bellmunt J, Eisen T, Fishman M, Quinn D. Experience with sorafenib and adverse event management. Crit Rev Oncol Hematol 2011;78:24-32
17. Strumberg D, Clark JW, Awada A, et al. Safety, pharmacokinetics, and preliminary antitumor activity of sorafenib: a review of four phase I trials in patients with advanced refractory solid tumors. Oncologist 2007;12:426-37 (Pubitemid 46698720)
18. Eisen T, Joensuu H, Nathan P, et al. Phase II study of BAY 73-4506, a multikinase inhibitor, in previously untreated patients with metastatic or unresectable renal cell cancer [abstract]. J Clin Oncol 2009;27:5033
19. Eisen T, Joensuu H, Nathan P, et al. Phase II trial of the oral multikinase inhibitor BAY 73-4506 as 1st-line therapy in patients with metastatic or unresectable renal cell cancer (RCC) [abstract]. Eur J Cancer 2009;7:424
20. Eisen T, Joensuu H, Nathan P, et al. Phase II trial of the oral multikinase inhibitor regorafenib (BAY 73-4506) as first-line therapy in patients with metastatic or unresectable renal cell carcinoma (RCC) [abstract]. Eur J Cancer 2011;47:7141
21. Jeffers M, Quinn D, Joensuu H, et al. Identification of plasma biomarkers for the multikinase inhibitor regorafenib (BAY 73-4506) in patients (pts) with renal cell cancer (RCC) [abstract and poster update]. Ann Oncol 2010;21:1238
22. Bolondi L, Tak WY, Gasbarrini A, et al. Phase II safety study of the oral multikinase inhibitor regorafenib (BAY 73-4506) as second-line therapy in patients with hepatocellular carcinoma [abstract]. Eur J Cancer 2011;7:6576
23. Frost A, Buechert M, Unger C, et al. Phase I study of BAY 73-4506, an inhibitor of oncogenic and angiogenic kinases, in patients with advanced solid tumors: final results of a dose-escalation study [abstract]. J Clin Oncol 2008;26:2558
24. Strumberg D, Scheulen ME, Schultheis B, et al. Regorafenib (BAY 73-4506) in advanced colorectal cancer: a phase I study. Br J Cancer 2012; in press
25. Christensen O, Buechert M, Fasol U, et al. Analysis of plasma biomarkers, DCE-MRI, and KRAS mutations in patients (pts) with advanced colorectal carcinoma (CRC) treated with the multikinase inhibitor regorafenib [abstract]. Ann Oncol 2010;21(Suppl 8):619P
26. NCT01103323. Patients with metastatic colorectal cancer treated with regorafenib or placebo after failure of standard therapy. Available from: http://clinicaltrials.gov 2011
27. Chu E. An update on the current and emerging targeted agents in metastatic colorectal cancer. Clin Colorectal Cancer 2011;published online; doi:S1533-0028 (11)00044-2 [pii];10.1016/j.clcc.2011.05.005 [doi]
28. Grothey A, Sobrero AF, Siena S, et al. Results of a phase III randomized, double-blind, placebo-controlled, multicenter trial (CORRECT) of regorafenib plus best supportive care (BSC) versus placebo plus BSC in patients (pts) with metastatic colorectal cancer (mCRC) who have progressed after standard therapies [abstract]. J Clin Oncol 2012;30:LBA 385
29. Schultheis B, Folprecht G, Kuhlmann J, et al. Phase I study of regorafenib sequentially administered with either FOLFOX or FOLFIRI in patients with first-/second line colorectal cancer [abstract]. J Clin Oncol 2011;29:3585
30. NCT01289821. First Line Treatment of Metastatic Colorectal Cancer With mFOLFOX6 in Combination With Regorafenib. Available from: http://clinicaltrials. gov 2011
31. Dagher R, Cohen M, Williams G, et al. Approval summary: imatinib mesylate in the treatment of metastatic and/or unresectable malignant gastrointestinal stromal tumors. Clin Cancer Res 2002;8:3034-8 (Pubitemid 35155011)
32. Demetri GD. Differential properties of current tyrosine kinase inhibitors in gastrointestinal stromal tumors. Semin Oncol 2011;38(Suppl 1):S10-19
33. Demetri GD, van Oosterom AT, Garrett CR, et al. Efficacy and safety of sunitinib in patients with advanced gastrointestinal stromal tumour after failure of imatinib: a randomised controlled trial. Lancet 2006;368:1329-38 (Pubitemid 44528723)
34. Wiebe L, Kasza KE, Maki RG, et al. Activity of sorafenib (SOR) in patients (pts) with imatinib (IM) and sunitinib (SU)-resistant gastrointestinal stromal tumors (GIST): a phase II trial of the University of Chicago phase II consortium [abstract]. J Clin Oncol 2008;26:10502
35. George S, von Mehren M, Heinrich MC, et al. A multicenter phase II study of regorafenib in patients (pts) with advanced gastrointestinal stromal tumor (GIST), after therapy with imatinib (IM) and sunitinib (SU) [abstract and update from presentation]. J Clin Oncol 2011;29:10007
36. Van den Abbeele AD, Tanaka Y, Locascio T, et al. Assessment of regorafenib activity with FDG-PET/CT in a multicenter phase II study in patients (pts) with advanced gastrointestinal stromal tumor (GIST) following failure of standard therapy (Rx) [abstract]. J Clin Oncol 2011;29:10050
37. NCT01271712. Study of Regorafenib as a 3rd-line or Greater Treatment for Gastrointestinal Stromal Tumors (GIST). Available from: http://clinicaltrials. gov 2011
38. NCT01187615. Determination of Safety, Efficacy, and Pharmacokinetics of Regorafenib Combined with Pemetrexed and Cisplatin in Patients with Nonsquamous Non-Small Cell Lung Cancer. Available from: http://clinicaltrials.gov 2011
39. Bergmann L, Eisen T, Joensuu H, et al. Phase II trial of regorafenib (BAY 73-4506) a novel oral multikinase inhibitor as 1st-line therapy in patients with metastatic or unresectable renal cell cancer (RCC) [abstract V459]. Onkologie 2010;33:128
40. NCT01298570. Regorafenib + FOLFIRI Versus Placebo + FOLFIRI as 2nd Line Tx in K-RAS/BRAF Mutant Metastatic Colorectal Cancer. Available from: http://clinicaltrials.gov 2011
41. NCT01003015. Safety Study of BAY73-4506 in Patients With Hepatocellular Carcinoma. Available from: http://clinicaltrials.gov 2011
42. Roberts PJ, Stinchcombe TE, Der CJ, Socinski MA. Personalized medicine in non-small-cell lung cancer: is KRAS a useful marker in selecting patients for epidermal growth factor receptor-targeted therapy? J Clin Oncol 2010;28:4769-77
43. O'Connor JP, Jackson A, Parker GJ, et al. Dynamic contrast-enhanced MRI in clinical trials of antivascular therapies. Nat Rev Clin Oncol 2012;9:167-77
44. Mross K, Fasol U, Frost A, et al. DCE-MRI assessment of the effect of vandetanib on tumor vasculature in patients with advanced colorectal cancer and liver metastases: a randomized phase I study. J Angiogenes Res 2009;1:5