Tamoxifen Dose Escalation in CYP2D6 Poor Metabolizer Breast Cancer
Patients and Associated Side Effects
Abstract
Aims CYP2D6 is a key enzyme for metabolizing tamoxifen into active
metabolites, but polymorphisms in this enzyme lead to varying metabolic
capacities. Increasing the tamoxifen dose in patients with deficient
CYP2D6 metabolism can elevate endoxifen levels to those of patients with
normal phenotypes. This study examines the impact of increasing the dose
of tamoxifen on toxicity in poor metabolizers of the CYP2D6 enzyme.
Methods Eighty-six breast cancer patients treated with tamoxifen were
classified by CYP2D6 metabolizer phenotype according to Clinical
Pharmacogenetics Implementation Consortium guidelines. All patients
started with a 20 mg/day dose of tamoxifen, with poor metabolizers
having their doses increased to 60 mg/day. Side effects, including
osteoarticular pain, hot flashes, asthenia, and uterine changes, were
analyzed using Kaplan-Meier analysis and the Cox proportional hazards
regression model to assess the relationship between CYP2D6 metabolizer
type and these side effects. Results Significant differences were found
only in uterine changes among CYP2D6 metabolizer types in both the
overall cohort and a subgroup selected via Propensity Score Matching
(PSM). Rapid metabolizers exhibited a lower incidence of uterine changes
(p < 0.001 in Kaplan-Meier analysis; HR 0.195, 95% CI: 0.07 -
0.52, p = 0.001) in the complete cohort. In the PSM cohort, Kaplan-Meier
analysis showed a p-value of 0.001 with an HR of 0.07 (95% CI: 0.01 -
0.54, p = 0.011). Conclusion Tamoxifen dose scalation in patients with
poor CYP2D6 metabolism may increase the occurrence of uterine changes
but does not significantly affect the incidence of osteoarticular pain,
hot flashes, or asthenia.