TY  - JOUR
TT  - AN OVERVIEW TO IMATINIB EFFICACY AND RESISTANCE MECHANISMS
AU  - Kılıç, Pelin
PY  - 2017
DA  - February
JF  - The Turkish Journal Of Occupational / Environmental Medicine and Safety
JO  - turjoem
PB  - Engin TUTKUN
WT  - DergiPark
SN  - 2149-4711
SP  - 12
EP  - 12
VL  - Volume 2
IS  - İssue 1 (1)
KW  - AN OVERVIEW TO IMATINIB EFFICACY AND RESISTANCE MECHANISMS
N2  - Imatinib is a common therapy inthe clinical management of chronic myeloid leukemia (CML). Imatinib, a memberof the family of tyrosine kinase inhibitors, is a drug transporter subtrate. Itbinds expansively to plasma proteins, and can inhibit its own transporters andmetabolizing enzymes. The strongest drawback to imatinib treatment isresistance to such a treatment. Even tough response rates are high in imatinibtreatment, 70-90% of the patients may manifest nonresponse or diseaseprogression. This observed resistance may be a result of genetic mutations orgene amplifications of drug targets. Cancer cells can develop resistancetowards one one drug, to a group of cytotoxic agents or to a number of drugswhich are not from the same therapeutic group. There are other resistancemechanisms associated with MDR. One of the fundamental resistance mechanisms inCML patients is mutations in the BCR-ABL1 tyrosine kinase region. However,imatinib resistance may develop independently in some patients. The reason whyis the presence of additional factors required for formation of a completelydrug resistant phenotype. BCR-ABL positive cells increase the activity of theGLUT 1 glucose transporter thus increase glucose intake. Classical dose regimenduring imatinib treatment has revealed differences going up to 4-fold. Drugplasma level determination, and analysis of the impact of transporter proteinpolymorphic variants on drug levels in CML patients who are receiving imatinibtreatment, clinical evaluation of the effects of polymorphisms on imatinibefficacy and resistance development will help enlighten the individualmechanisms behind interindividual differences in imatinib pharmacokinetics.
CR  - Pelin KILIÇ
CR  - Turkish Medicines and Medical Devices Agency
UR  - https://dergipark.org.tr/tr/pub/turjoem/issue//303719
L1  - https://dergipark.org.tr/tr/download/article-file/290629
ER  -