Regorafenib (BAY 73-4506) in advanced colorectal cancer: A phase I study

British Journal of Cancer

Volumn 106, Issue 11, 2012, Pages 1722-1727

  Strumberg, D ^a   Scheulen, M E ^b   Schultheis, B ^a   Richly, H ^b   Frost, A ^c   Buchert M ^d   Christensen, O ^e   Jeffers, M ^e   Heinig, R ^f   Boix, O ^f   Mross, K ^c  

^a RUHR UNIVERSITY BOCHUM   (Germany)

^b UNIVERSITY HOSPITAL ESSEN   (Germany)

^c UNIVERSITY OF FREIBURG   (Germany)

^d UNIVERSITY OF FREIBURG   (Germany)

^e BAYER CORPORATION   (United States)

^f BAYER PHARMA AG   (Germany)

Author keywords

colorectal cancer; KRAS; multi kinase inhibitor; regorafenib; tumour angiogenesis

Indexed keywords

BAY 75 7495; BAY 81 8752; DRUG METABOLITE; K RAS PROTEIN; REGORAFENIB; UNCLASSIFIED DRUG;

ADULT; ADVANCED CANCER; AGED; ALOPECIA; ANOREXIA; ANTINEOPLASTIC ACTIVITY; AREA UNDER THE CURVE; ARTICLE; CANCER CHEMOTHERAPY; CANCER CONTROL; CANCER SIZE; CANCER SURVIVAL; CLINICAL ARTICLE; COHORT ANALYSIS; COLORECTAL CANCER; DESQUAMATION; DIARRHEA; DRUG BLOOD LEVEL; DRUG DOSE ESCALATION; DRUG EFFICACY; DRUG ELIMINATION; DRUG ERUPTION; DRUG HALF LIFE; DRUG SAFETY; DRUG TOLERABILITY; DRUG WITHDRAWAL; DRY SKIN; DUODENUM ULCER; FATIGUE; FEMALE; HAND FOOT SYNDROME; HEARING DISORDER; HUMAN; HYPERTENSION; MALE; MAXIMUM PLASMA CONCENTRATION; MULTIPLE CYCLE TREATMENT; MUTATIONAL ANALYSIS; MYALGIA; NEONATAL WEIGHT LOSS; ORAL MUCOSITIS; PHASE 1 CLINICAL TRIAL; PRIORITY JOURNAL; PROGRESSION FREE SURVIVAL; SIDE EFFECT; STEADY STATE; THROMBOCYTOPENIA; TREATMENT DURATION; TREATMENT RESPONSE; VOICE CHANGE; WEIGHT REDUCTION; XEROSTOMIA;

ADULT; AGED; AGED, 80 AND OVER; ANTINEOPLASTIC AGENTS; COLORECTAL NEOPLASMS; DISEASE-FREE SURVIVAL; DOSE-RESPONSE RELATIONSHIP, DRUG; FEMALE; HUMANS; KAPLAN-MEIER ESTIMATE; MALE; MIDDLE AGED; PHENYLUREA COMPOUNDS; PYRIDINES;

EID: 84861459479     PISSN: 00070920     EISSN: 15321827     Source Type: Journal    
DOI: 10.1038/bjc.2012.153     Document Type: Article

References (17)

1. Akbulut H, Icli F, Yalcin B, Demirkazik A, Onur H, Buyukcelik A, Utkan G (2004) Activity of irinotecan, cisplatin and dacarbazine (CPD) combination in previously treated patients with advanced colorectal carcinoma. Exp Oncol 26: 149-152
2. Bitossi R, Sculli CM, Tampellini M, Alabiso I, Brizzi MP, Ferrero A, Ottone A, Bellini E, Gorzegno G, Berruti A, Dogliotti L (2008) Gemcitabine and protracted 5-fluorouracil infusion as third-line chemotherapy in refractory colorectal cancer patients. Anticancer Res 28: 3055-3060
3. Cercek A, Saltz L (2010) Evolving treatment of advanced colorectal cancer. Curr Oncol Rep 12: 153-159
4. Dressman D, Yan H, Traverso G, Kinzler KW, Vogelstein B (2003) Transforming single DNA molecules into fluorescent magnetic particles for detection and enumeration of genetic variations. Proc Natl Acad Sci USA 100: 8817-8822 (Pubitemid 36899181)
5. Eisen T, Joensuu H, Nathan P, Harper P, Wojtukiewicz M, Nicholson S, Bahl B, Tomczak P, Wagner A, Quinn D (2011) Phase II trial of the oral multikinase inhibitor regorafenib (BAY 73-4506) as first-line therapy in patients with metastatic or unresectable renal cell cancer (RCC) Eur J Cancer 47(Suppl): Abstract 7. 141
6. Eisenhauer EA, Therasse P, Bogaerts J, Schwartz LH, Sargent D, Ford R, Dancey J, Arbuck S, Gwyther S, Mooney M, Rubinstein L, Shankar L, Dodd L, Kaplan R, Lacombe D, Verweij J (2009) New response evaluation criteria in solid tumours: revised RECIST guideline (version 1.1). Eur J Cancer 45: 228-247
7. Food and Drug Administration (2001) Guidance for Industry. Bioanalytical Method Validation. Food and Drug Administration: Silver Spring, MD, USA
8. Hamilton J, Grem J (1998) Lower gastrointestinal tract cancer. In Current Cancer Therapeutics, Kirkwood JM, Lotze MT, Yasko JM (eds) 3rd edn, pp 156-160. Churchill Livingstone, Current Medicine Inc.: Philadelphia, PA, USA
9. Hurwitz H, Fehrenbacher L, Novotny W, Cartwright T, Hainsworth J, Heim W, Berlin J, Baron A, Griffing S, Holmgren E, Ferrara N, Fyfe G, Rogers B, Ross R, Kabbinavar F (2004) Bevacizumab plus irinotecan, fluorouracil, and leucovorin for metastatic colorectal cancer. N Engl J Med 350: 2335-2342 (Pubitemid 38702844)
10. Mross K, Fasol U, Frost A, Benkelmann R, Kuhlmann J, Büchert M, Unger C, Blum H, Hennig J, Milenkova TP, Tessier J, Krebs AD, Ryan AJ, Fischer R (2009) 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 1: 5
11. Mross K, Frost A, Steinbild S, Hedborn S, Büchert M, Fasol U, Unger C, Kraetzschmar J, Heinig R, Boix O, Christensen O (2012) 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; e-pub ahead of print 20 April 2012
12. National Comprehensive Cancer Network (2011) NCCN Clinical Practice Guidelines in Oncology. National Comprehensive Cancer Network: Fort Washington, PA, USA
13. Parkin DM, Bray F, Ferlay J, Pisani P (2005) Global cancer statistics, 2002. CA Cancer J Clin 55: 74-108 (Pubitemid 40372904)
14. Van Cutsem E, Siena S, Humblet Y, Canon JL, Maurel J, Bajetta E, Neyns B, Kotasek D, Santoro A, Scheithauer W, Spadafora S, Amado RG, Hogan N, Peeters M (2008) An open-label, single-arm study assessing safety and efficacy of panitumumab in patients with metastatic colorectal cancer refractory to standard chemotherapy. Ann Oncol 19: 92-98
15. Van Cutsem E, Peeters M, Siena S, Humblet Y, Hendlisz A, Neyns B, Canon JL, Van Laethem JL, Maurel J, Richardson G, Wolf M, Amado RG (2007) Open-label phase III trial of panitumumab plus best supportive care compared with best supportive care alone in patients with chemotherapy-refractory metastatic colorectal cancer. J Clin Oncol 25: 1658-1664 (Pubitemid 46797944)
16. Wilhelm SM, Dumas J, Adnane L, Lynch M, Carter CA, Schütz G, Thierauch KH, Zopf D (2011) 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 129: 245-255
17. Zopf D, Heinig R, Thierauch K-H, Hirth-Dietrich C, Hafner F-T, Christensen O, Lin T, Wilhelm S, Radtke M (2010) Regorafenib (BAY 73-4506): preclinical pharmacology and clinical identification and quantification of its major metabolites (17-21 April) (2010) At the American Association for Cancer Research 101st Annual Meeting, Washington, DC, USA