Literature DB >> 25714002

Evaluation of CYP2D6 enzyme activity using a 13C-dextromethorphan breath test in women receiving adjuvant tamoxifen.

Stephanie L Safgren1, Vera J Suman, Matthew L Kosel, Judith A Gilbert, Sarah A Buhrow, John L Black, Donald W Northfelt, Anil S Modak, David Rosen, James N Ingle, Matthew M Ames, Joel M Reid, Matthew P Goetz.   

Abstract

BACKGROUND: In tamoxifen-treated patients, breast cancer recurrence differs according to CYP2D6 genotype and endoxifen steady-state concentrations (Endx Css). The ¹³C-dextromethorphan breath test (DM-BT), labeled with ¹³C at the O-CH3 moiety, measures CYP2D6 enzyme activity. We sought to examine the ability of the DM-BT to identify known CYP2D6 genotypic poor metabolizers and examine the correlation between DM-BT and Endx Css.
METHODS: DM-BT and tamoxifen pharmacokinetics were obtained at baseline, 3, and 6 months following tamoxifen initiation. Potent CYP2D6 inhibitors were prohibited. The correlation between baseline DM-BT with CYP2D6 genotype and Endx Css was determined. The association between baseline DM-BT (where values ≤0.9 is an indicator of poor in vivo CYP2D6 metabolism) and Endx Css (using values≤11.2 known to be associated with poorer recurrence free survival) was explored.
RESULTS: A total of 91 patients were enrolled and 77 were eligible. CYP2D6 genotype was positively correlated with baseline, 3, and 6 months DM-BT (r ranging from 0.457-0. 60; P<0.001). Both CYP2D6 genotype (r=0.47, 0.56, P<0.0001), and baseline DM-BT (r=0.60, 0.54, P<0.001) were associated with 3 and 6 months Endx Css, respectively. Seven (78%) of nine patients with low (≤11.2 nmol/l) 3 month Endx Css also had low DM-BT (≤0.9) including 2/2 CYP2D6 PM/PM and 5/5 IM/PM. In contrast, one (2%) of 48 patients with a low DM-BT had Endx Css more than 11.2 nmol/l.
CONCLUSION: In patients not taking potent CYP2D6 inhibitors, DM-BT was associated with CYP2D6 genotype and 3 and 6 months Endx Css but did not provide better discrimination of Endx Css compared with CYP2D6 genotype alone. Further studies are needed to identify additional factors which alter Endx Css.

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Year:  2015        PMID: 25714002      PMCID: PMC4356640          DOI: 10.1097/FPC.0000000000000121

Source DB:  PubMed          Journal:  Pharmacogenet Genomics        ISSN: 1744-6872            Impact factor:   2.089


  16 in total

1.  Dextromethorphan as a phenotyping test to predict endoxifen exposure in patients on tamoxifen treatment.

Authors:  Anne-Joy M de Graan; Sebastiaan F Teunissen; Filip Y F L de Vos; Walter J Loos; Ron H N van Schaik; Felix E de Jongh; Aad I de Vos; Robbert J van Alphen; Bronno van der Holt; Jaap Verweij; Caroline Seynaeve; Jos H Beijnen; Ron H J Mathijssen
Journal:  J Clin Oncol       Date:  2011-07-18       Impact factor: 44.544

2.  Activity levels of tamoxifen metabolites at the estrogen receptor and the impact of genetic polymorphisms of phase I and II enzymes on their concentration levels in plasma.

Authors:  T E Mürdter; W Schroth; L Bacchus-Gerybadze; S Winter; G Heinkele; W Simon; P A Fasching; T Fehm; M Eichelbaum; M Schwab; H Brauch
Journal:  Clin Pharmacol Ther       Date:  2011-03-30       Impact factor: 6.875

3.  Tamoxifen metabolite concentrations, CYP2D6 genotype, and breast cancer outcomes.

Authors:  L Madlensky; L Natarajan; S Tchu; M Pu; J Mortimer; S W Flatt; D M Nikoloff; G Hillman; M R Fontecha; H J Lawrence; B A Parker; A H B Wu; J P Pierce
Journal:  Clin Pharmacol Ther       Date:  2011-03-23       Impact factor: 6.875

4.  Comparative contribution to dextromethorphan metabolism by cytochrome P450 isoforms in vitro: can dextromethorphan be used as a dual probe for both CTP2D6 and CYP3A activities?

Authors:  A Yu; R L Haining
Journal:  Drug Metab Dispos       Date:  2001-11       Impact factor: 3.922

5.  Active tamoxifen metabolite plasma concentrations after coadministration of tamoxifen and the selective serotonin reuptake inhibitor paroxetine.

Authors:  Vered Stearns; Michael D Johnson; James M Rae; Alan Morocho; Antonella Novielli; Pankaj Bhargava; Daniel F Hayes; Zeruesenay Desta; David A Flockhart
Journal:  J Natl Cancer Inst       Date:  2003-12-03       Impact factor: 13.506

6.  Tamoxifen for prevention of breast cancer: report of the National Surgical Adjuvant Breast and Bowel Project P-1 Study.

Authors:  B Fisher; J P Costantino; D L Wickerham; C K Redmond; M Kavanah; W M Cronin; V Vogel; A Robidoux; N Dimitrov; J Atkins; M Daly; S Wieand; E Tan-Chiu; L Ford; N Wolmark
Journal:  J Natl Cancer Inst       Date:  1998-09-16       Impact factor: 13.506

7.  Comprehensive evaluation of tamoxifen sequential biotransformation by the human cytochrome P450 system in vitro: prominent roles for CYP3A and CYP2D6.

Authors:  Zeruesenay Desta; Bryan A Ward; Nadia V Soukhova; David A Flockhart
Journal:  J Pharmacol Exp Ther       Date:  2004-05-24       Impact factor: 4.030

8.  Evaluation of a [13C]-dextromethorphan breath test to assess CYP2D6 phenotype.

Authors:  J Steven Leeder; Robin E Pearce; Andrea Gaedigk; Anil Modak; David I Rosen
Journal:  J Clin Pharmacol       Date:  2008-09       Impact factor: 3.126

9.  The tamoxifen metabolite, endoxifen, is a potent antiestrogen that targets estrogen receptor alpha for degradation in breast cancer cells.

Authors:  Xianglin Wu; John R Hawse; Malayannan Subramaniam; Matthew P Goetz; James N Ingle; Thomas C Spelsberg
Journal:  Cancer Res       Date:  2009-02-24       Impact factor: 12.701

10.  Quantification of tamoxifen and three metabolites in plasma by high-performance liquid chromatography with fluorescence detection: application to a clinical trial.

Authors:  Kyung-Hoon Lee; Bryan A Ward; Zeruesenay Desta; David A Flockhart; David R Jones
Journal:  J Chromatogr B Analyt Technol Biomed Life Sci       Date:  2003-07-05       Impact factor: 3.205

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  7 in total

Review 1.  Endoxifen, an Estrogen Receptor Targeted Therapy: From Bench to Bedside.

Authors:  Swaathi Jayaraman; Joel M Reid; John R Hawse; Matthew P Goetz
Journal:  Endocrinology       Date:  2021-12-01       Impact factor: 5.051

Review 2.  Stable isotope biomarker breath tests for human metabolic and infectious diseases: a review of recent patent literature.

Authors:  Graham S Timmins
Journal:  Expert Opin Ther Pat       Date:  2016-08-10       Impact factor: 6.674

3.  Clinical Pharmacogenetics Implementation Consortium (CPIC) Guideline for CYP2D6 and Tamoxifen Therapy.

Authors:  Matthew P Goetz; Katrin Sangkuhl; Henk-Jan Guchelaar; Matthias Schwab; Michael Province; Michelle Whirl-Carrillo; W Fraser Symmans; Howard L McLeod; Mark J Ratain; Hitoshi Zembutsu; Andrea Gaedigk; Ron H van Schaik; James N Ingle; Kelly E Caudle; Teri E Klein
Journal:  Clin Pharmacol Ther       Date:  2018-01-31       Impact factor: 6.875

Review 4.  European guideline on indications, performance and clinical impact of 13 C-breath tests in adult and pediatric patients: An EAGEN, ESNM, and ESPGHAN consensus, supported by EPC.

Authors:  Jutta Keller; Heinz F Hammer; Paul R Afolabi; Marc Benninga; Osvaldo Borrelli; Enrique Dominguez-Munoz; Dan Dumitrascu; Oliver Goetze; Stephan L Haas; Bruno Hauser; Daniel Pohl; Silvia Salvatore; Marc Sonyi; Nikhil Thapar; Kristin Verbeke; Mark R Fox
Journal:  United European Gastroenterol J       Date:  2021-06-14       Impact factor: 4.623

5.  First-in-Human Phase I Study of the Tamoxifen Metabolite Z-Endoxifen in Women With Endocrine-Refractory Metastatic Breast Cancer.

Authors:  Matthew P Goetz; Vera J Suman; Joel M Reid; Don W Northfelt; Michael A Mahr; Andrew T Ralya; Mary Kuffel; Sarah A Buhrow; Stephanie L Safgren; Renee M McGovern; John Black; Travis Dockter; Tufia Haddad; Charles Erlichman; Alex A Adjei; Dan Visscher; Zachary R Chalmers; Garrett Frampton; Benjamin R Kipp; Minetta C Liu; John R Hawse; James H Doroshow; Jerry M Collins; Howard Streicher; Matthew M Ames; James N Ingle
Journal:  J Clin Oncol       Date:  2017-08-30       Impact factor: 50.717

6.  Predicting steady-state endoxifen plasma concentrations in breast cancer patients by CYP2D6 genotyping or phenotyping. Which approach is more reliable?

Authors:  Milena Gusella; Felice Pasini; Barbara Corso; Laura Bertolaso; Giovanni De Rosa; Cristina Falci; Yasmina Modena; Carmen Barile; Donatella Da Corte Z; AnnaPaola Fraccon; Silvia Toso; Elisabetta Cretella; Antonella Brunello; Caterina Modonesi; Romana Segati; Cristina Oliani; Nadia Minicuci; Roberto Padrini
Journal:  Pharmacol Res Perspect       Date:  2020-10

Review 7.  Generating a Precision Endoxifen Prediction Algorithm to Advance Personalized Tamoxifen Treatment in Patients with Breast Cancer.

Authors:  Thomas Helland; Sarah Alsomairy; Chenchia Lin; Håvard Søiland; Gunnar Mellgren; Daniel Louis Hertz
Journal:  J Pers Med       Date:  2021-03-13
  7 in total

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