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Novel Tyrosine Kinase Inhibitors in the Treatment of Cancer
被引:19
作者:
Ocana, Alberto
[1
,2
,3
]
Serrano, Rosario
[2
]
Calero, Raul
[2
]
Pandiella, Atanasio
[3
]
机构:
[1] Princess Margaret Hosp, Drug Dev Program, Toronto, ON M4X 1K9, Canada
[2] Albacete Univ Hosp Spain, AECC Canc Res Unit, Albacete, Spain
[3] Univ Salamanca, CSIC, Ctr Invest Canc, E-37008 Salamanca, Spain
关键词:
LUNG-CANCER;
MUTATIONS;
RESISTANCE;
GEFITINIB;
THERAPY;
D O I:
10.2174/138945009788488378
中图分类号:
R9 [药学];
学科分类号:
1007 ;
摘要:
In summary, multi-TK inhibitors are being designed to target multiple activated kinases. The future design plan for these compounds should take into consideration the activated array of kinases in a given tumor. This undoubtedly will increase the efficacy, also avoiding toxicity. Furthermore, irreversible TK inhibitors show more efficacy than reversible ones, with a similar toxicity profile, thereby presenting these inhibitors as attractive alternatives to reversible inhibitors. In addition, irreversible inhibitors may offer advantages with respect to their ability to be more efficacious to fight avoid resistance due to secondary mutations. The development of multikinase, reversible, irreversible, and other allosteric inhibitors of tyrosine kinases is clearly widening the armamentarium to fight neoplastic diseases, and will allow better targeting of the tumoral cells, improved toxicological properties, and more favourable responses by preventing drug resistance.
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页码:575 / 576
页数:2
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