[HTML][HTML] Selective estrogen receptor modulators (SERMs) and selective estrogen receptor degraders (SERDs) in cancer treatment

HK Patel, T Bihani - Pharmacology & therapeutics, 2018 - Elsevier
Breast cancer is the most frequently diagnosed cancer in women, with estrogen receptor
positive (ER+) breast cancer making up approximately 75% of all breast cancers diagnosed …

Clinically relevant concentrations of anticancer drugs: a guide for nonclinical studies

DR Liston, M Davis - Clinical cancer research, 2017 - AACR
Approved and marketed drugs are frequently studied in nonclinical models to evaluate the
potential application to additional disease indications or to gain insight about molecular …

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

MP Goetz, K Sangkuhl, HJ Guchelaar… - Clinical …, 2018 - Wiley Online Library
Tamoxifen is biotransformed by CYP2D6 to 4‐hydroxytamoxifen and 4‐hydroxy N‐
desmethyl tamoxifen (endoxifen), both with greater antiestrogenic potency than the parent …

[HTML][HTML] Endocrine resistance in hormone receptor positive breast cancer–from mechanism to therapy

A Rani, J Stebbing, G Giamas, J Murphy - Frontiers in endocrinology, 2019 - frontiersin.org
The importance and role of the estrogen receptor (ER) pathway has been well-documented
in both breast cancer (BC) development and progression. The treatment of choice in women …

Tamoxifen: a most unlikely pioneering medicine

VC Jordan - Nature reviews Drug discovery, 2003 - nature.com
For more than 25 years, tamoxifen has been the gold standard for the endocrine treatment of
all stages of oestrogen-receptor-positive breast cancer, and the World Health Organization …

Polymorphism of human cytochrome P450 enzymes and its clinical impact

SF Zhou, JP Liu, B Chowbay - Drug metabolism reviews, 2009 - Taylor & Francis
Pharmacogenetics is the study of how interindividual variations in the DNA sequence of
specific genes affect drug response. This article highlights current pharmacogenetic …

The discovery and development of selective estrogen receptor modulators (SERMs) for clinical practice

PY Maximov, TM Lee… - Current clinical …, 2013 - ingentaconnect.com
Selective estrogen receptor modulators (SERMs) are structurally different compounds that
interact with intracellular estrogen receptors in target organs as estrogen receptor agonists …

Influence of cytochrome P450 polymorphisms on drug therapies: pharmacogenetic, pharmacoepigenetic and clinical aspects

M Ingelman-Sundberg, SC Sim, A Gomez… - Pharmacology & …, 2007 - Elsevier
The polymorphic nature of the cytochrome P450 (CYP) genes affects individual drug
response and adverse reactions to a great extent. This variation includes copy number …

CYP2D6 genotype, antidepressant use, and tamoxifen metabolism during adjuvant breast cancer treatment

Y Jin, Z Desta, V Stearns, B Ward, H Ho… - Journal of the …, 2005 - academic.oup.com
Background: The efficacy of tamoxifen therapy for the treatment of breast cancer varies
widely among individuals. Plasma concentrations of the active tamoxifen metabolite …

Association between CYP2D6 polymorphisms and outcomes among women with early stage breast cancer treated with tamoxifen

W Schroth, MP Goetz, U Hamann, PA Fasching… - Jama, 2009 - jamanetwork.com
Context The growth inhibitory effect of tamoxifen, which is used for the treatment of hormone
receptor–positive breast cancer, is mediated by its metabolites, 4-hydroxytamoxifen and …