CYP2D6 genotyping in breast cancer patients by liquid chromatography-electrospray ionization mass spectrometry

Author(s):  
Beate Beer ◽  
Sabine Plattner ◽  
Michael Hubalek ◽  
Anne Oberguggenberger ◽  
Monika Sztankay ◽  
...  

AbstractThe application of cytochrome P450 2D6 (CYP2D6) genotyping to allow a personalized treatment approach for breast cancer patients undergoing endocrine therapy has been repeatedly discussed. However, the actual clinical relevance of the CYP2D6 genotype in the endocrine treatment of breast cancer still remains to be elucidated. A major prerequisite for the successful and valid evaluation of the CYP2D6 genotype with regard to its pharmacokinetic and clinical relevance is the availability of a comprehensive, accurate and cost-effective CYP2D6 genotyping strategy. Herein we present a CYP2D6 genotyping assay employing polymerase chain reaction (PCR)-ion pair reversed-phase high-performance liquid chromatography-electrospray ionization time-of-flight mass spectrometry (ICEMS). The genotyping strategy involves the simultaneous amplification of nine variable regions within the CYP2D6 gene by a two-step PCR protocol and the direct analysis of the generated PCR amplicons by ICEMS. The nucleotide composition profiles generated by ICEMS enable the differentiation of 37 of the 80 reported CYP2D6 alleles. The assay was applied to type the CYP2D6 gene in 199 Austrian individuals including 106 breast cancer patients undergoing tamoxifen treatment. The developed method turned out to be a highly applicable, robust and cost-effective approach, enabling an economical CYP2D6 testing for large patient cohorts.

2016 ◽  
Vol 452 ◽  
pp. 18-26 ◽  
Author(s):  
Takahiro Takayama ◽  
Haruhito Tsutsui ◽  
Ippei Shimizu ◽  
Tatsuya Toyama ◽  
Nobuyasu Yoshimoto ◽  
...  

Cancers ◽  
2019 ◽  
Vol 11 (9) ◽  
pp. 1353 ◽  
Author(s):  
Jemal Hussien Ahmed ◽  
Eyasu Makonnen ◽  
Alan Fotoohi ◽  
Abraham Aseffa ◽  
Rawleigh Howe ◽  
...  

Tamoxifen displays wide inter-individual variability (IIV) in its pharmacokinetics and treatment outcome. Data on tamoxifen pharmacokinetics and pharmacogenetics from black African breast cancer patient populations is lacking. We investigated the pharmacokinetic and pharmacogenetic profile of tamoxifen and its major active metabolite, endoxifen, in Ethiopian breast cancer patients. A total of 81 female breast cancer patients on adjuvant tamoxifen therapy were enrolled. Tamoxifen (Tam) and its major metabolites, N-desmethyltamoxifen (NDM), 4-hydroxy-tamoxifen (4-HT), and (Z)-endoxifen (E) were quantified using LC-MS/MS. Genotyping for CYP2D6, CYP2C9, CYP2C19, CYP3A5, POR, and ABCB1 and UGT2B15 and copy number variation for CYP2D6 were done. The proportion of patients with low endoxifen level (<5.9 ng/mL) was 35.8% (median concentration 7.94 ng/mL). The allele frequency of CYP2D6 gene deletion (*5) and duplication (*1×N or *2×N) was 4.3% and 14.8%, respectively. Twenty-six percent of the patients carried duplicated or multiplicated CYP2D6 gene. An increase in CYP2D6 activity score was associated with increased endoxifen concentration and MRE/NDM (p < 0.001). The IIV in endoxifen concentration and MRE/NDM was 74.6% and 59%, respectively. CYP2D6 diplotype explained 28.2% and 44% of the variability in absolute endoxifen concentration and MRE/NDM, respectively. The explanatory power of CYP2D6 diplotype was improved among ABCB1c.4036G carriers (43% and 65.2%, respectively for endoxifen concentration and MRE/NDM) compared to A/A genotype. CYP2C9, CYP2C19, and CYP3A5 genotypes had no significant influence on endoxifen concentration or MRE/NDM. In conclusion, we report a high rate of low endoxifen level as well as large IIV in tamoxifen and its metabolite concentrations. CYP2D6 is significant predictor of plasma endoxifen level in a gene-dose dependent manner.


2018 ◽  
Author(s):  
M Banys-Paluchowski ◽  
K Milde-Langosch ◽  
T Fehm ◽  
I Witzel ◽  
L Oliveira-Ferrer ◽  
...  

Biomarkers ◽  
2008 ◽  
Vol 13 (4) ◽  
pp. 435-449 ◽  
Author(s):  
Antje Frickenschmidt ◽  
Holger Fröhlich ◽  
Dino Bullinger ◽  
Andreas Zell ◽  
Stefan Laufer ◽  
...  

Sign in / Sign up

Export Citation Format

Share Document