Brivanib alaninate for cancer

被引:37
作者
Diaz-Padilla, Ivan [1 ]
Siu, Lillian L. [1 ]
机构
[1] Princess Margaret Hosp, Toronto, ON M4X 1K9, Canada
关键词
angiogenesis; brivanib; colorectal cancer; dynamic contrast-enhanced magnetic resonance (DCE-MRI); hepatocellular carcinoma; GROWTH-FACTOR RECEPTOR-1; PHASE-I; DUAL INHIBITOR; DISCOVERY; VEGF; AMPLIFICATION; VALIDATION; EXPRESSION; RESISTANCE; MUTATIONS;
D O I
10.1517/13543784.2011.565329
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Areas covered: This review provides an updated summary of preclinical and clinical experience with brivanib in cancer. Data presented in abstract form from international conferences or journal articles found with a PubMed search of published literature up to December 2010 are described in this review. Expert opinion: Brivanib appears tolerable and exhibits favorable pharmacokinetic and pharmacodynamic profiles with evidence of target inhibition in surrogate tissues. Clinical and pharmacodynamic data support an oral once daily administration at 800 mg. Brivanib shows promising activity as single agent in hepatocellular carcinoma and in combination with cetuximab in colorectal cancer. Further evaluations with cytotoxic chemotherapy and in other solid tumors are currently ongoing.
引用
收藏
页码:577 / 586
页数:10
相关论文
共 54 条
[11]  
*BRIST MYERS SQUIB, PHAS 2 STUD BRIV BMS
[12]  
*BRIST MYERS SQUIB, STUD BRIV BMS 582664
[13]  
*BRIST MYERS SQUIB, PHAS 3 TRANS ART CHE
[14]  
*BRIST MYERS SQUIB, COMB BRIV 5 FLUOR LE
[15]  
*BRIST MYERS SQUIB, COMP BRIV BEST SUPP
[16]   Validation of 70-gene prognosis signature in node-negative breast cancer [J].
Bueno-de-Mesquita, J. M. ;
Linn, S. C. ;
Keijzer, R. ;
Wesseling, J. ;
Nuyten, D. S. A. ;
van Krimpen, C. ;
Meijers, C. ;
de Graaf, P. W. ;
Bos, M. M. E. M. ;
Hart, A. A. M. ;
Rutgers, E. J. T. ;
Peterse, J. L. ;
Halfwerk, H. ;
de Groot, R. ;
Pronk, A. ;
Floore, A. N. ;
Glas, A. M. ;
van't Veer, L. J. ;
van de Vijver, M. J. .
BREAST CANCER RESEARCH AND TREATMENT, 2009, 117 (03) :483-495
[17]   Discovery of brivanib alaninate ((S)-((R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan-2-yl)2-aminopropanoate), a novel prodrug of dual vascular endothelial growth factor receptor-2 and fibroblast growth factor receptor-1 kinase inhibitor (BMS-540215) [J].
Cai, Zhen-Wei ;
Zhang, Yongzheng ;
Borzilleri, Robert M. ;
Qian, Ligang ;
Barbosa, Stephanie ;
Wei, Donna ;
Zheng, Xiaoping ;
Wu, Lawrence ;
Fan, Junying ;
Shi, Zhongping ;
Wautlet, Barri S. ;
Mortillo, Steve ;
Jeyaseelan, Robert, Sr. ;
Kukral, Daniel W. ;
Kamath, Amrita ;
Marathe, Punit ;
D'Arienzo, Celia ;
Derbin, George ;
Barrish, Joel C. ;
Robl, Jeffrey A. ;
Hunt, John T. ;
Lombardo, Louis J. ;
Fargnoli, Joseph ;
Bhide, Rajeev S. .
JOURNAL OF MEDICINAL CHEMISTRY, 2008, 51 (06) :1976-1980
[18]   Frequent activating mutations of FGFR3 in human bladder and cervix carcinomas [J].
Cappellen, D ;
De Oliveira, C ;
Ricol, D ;
de Medina, SGD ;
Bourdin, J ;
Sastre-Garau, X ;
Chopin, D ;
Thiery, JP ;
Radvanyi, F .
NATURE GENETICS, 1999, 23 (01) :18-20
[19]   Drug resistance by evasion of antiangiogenic targeting of VEGF signaling in late-stage pancreatic islet tumors [J].
Casanovas, O ;
Hicklin, DJ ;
Bergers, G ;
Hanahan, D .
CANCER CELL, 2005, 8 (04) :299-309
[20]   Dynamic Contrast-Enhanced MRI in Oncology Drug Development [J].
Cheng, Hai-Ling Margaret .
CURRENT CLINICAL PHARMACOLOGY, 2007, 2 (02) :111-122