Synergistic Combinations of Small Molecule Kinase Inhibitors: Implications for Reducing Toxicities in Nasopharyngeal Carcinoma Treatment

2017 ◽  
Vol 4 (4) ◽  
Author(s):  
Heng Fong Seow
Keyword(s):  
Nasopharyngeal Carcinoma ◽  
Small Molecule ◽  
Kinase Inhibitors ◽  
Synergistic Combinations

scholarly journals Feasibility of Extrapolating Randomly Taken Plasma Samples to Trough Levels for Therapeutic Drug Monitoring Purposes of Small Molecule Kinase Inhibitors

2021 ◽  
Vol 14 (2) ◽  
pp. 119
Author(s):  
Ruben A. G. van Eerden ◽  
Esther Oomen-de Hoop ◽  
Aad Noordam ◽  
Ron H. J. Mathijssen ◽  
Stijn L. W. Koolen
Keyword(s):  
Therapeutic Drug Monitoring ◽  
Small Molecule ◽  
Trough Concentration ◽  
Drug Monitoring ◽  
Half Life ◽  
Kinase Inhibitors ◽  
Therapeutic Drug ◽  
Blood Samples ◽  
Elimination Half ◽  
Trough Levels

Small molecule kinase inhibitors (SMKIs) are widely used in oncology. Therapeutic drug monitoring (TDM) for SMKIs could reduce underexposure or overexposure. However, logistical issues such as timing of blood withdrawals hamper its implementation into clinical practice. Extrapolating a random concentration to a trough concentration using the elimination half-life could be a simple and easy way to overcome this problem. In our study plasma concentrations observed during 24 h blood sampling were used for extrapolation to trough levels. The objective was to demonstrate that extrapolation of randomly taken blood samples will lead to equivalent estimated trough samples compared to measured Cmin values. In total 2241 blood samples were analyzed. The estimated Ctrough levels of afatinib and sunitinib fulfilled the equivalence criteria if the samples were drawn after Tmax. The calculated Ctrough levels of erlotinib, imatinib and sorafenib met the equivalence criteria if they were taken, respectively, 12 h, 3 h and 10 h after drug intake. For regorafenib extrapolation was not feasible. In conclusion, extrapolation of randomly taken drug concentrations to a trough concentration using the mean elimination half-life is feasible for multiple SMKIs. Therefore, this simple method could positively contribute to the implementation of TDM in oncology.

scholarly journals FDA-approved small-molecule kinase inhibitors

2015 ◽  
Vol 36 (7) ◽  
pp. 422-439 ◽  
Author(s):  
Peng Wu ◽  
Thomas E. Nielsen ◽  
Mads H. Clausen
Keyword(s):  
Small Molecule ◽  
Kinase Inhibitors

Pyrimidoaminotropanes as Potent, Selective, and Efficacious Small Molecule Kinase Inhibitors of the Mammalian Target of Rapamycin (mTOR)

2013 ◽  
Vol 56 (7) ◽  
pp. 3090-3101 ◽  
Author(s):  
Anthony A. Estrada ◽  
Daniel G. Shore ◽  
Elizabeth Blackwood ◽  
Yung-Hsiang Chen ◽  
Gauri Deshmukh ◽  
...  
Keyword(s):  
Small Molecule ◽  
Kinase Inhibitors ◽  
Mammalian Target Of Rapamycin ◽  
Target Of Rapamycin

Inhibition of TGF-β Signaling in Tumor Cells by Small Molecule Src Family Kinase Inhibitors

2017 ◽  
Vol 17 (10) ◽  
Author(s):  
Tobias Bartscht ◽  
Benjamin Rosien ◽  
Dirk Rades ◽  
Roland Kaufmann ◽  
Harald Biersack ◽  
...  
Keyword(s):  
Tumor Cells ◽  
Small Molecule ◽  
Kinase Inhibitors ◽  
Src Family Kinase
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