The role of metabolic activation in drug-induced hepatotoxicity

BK Park, NR Kitteringham, JL Maggs… - Annu. Rev …, 2005 - annualreviews.org
▪ Abstract The importance of reactive metabolites in the pathogenesis of drug-induced
toxicity has been a focus of research interest since pioneering investigations in the 1950s …

Antiestrogens and selective estrogen receptor modulators as multifunctional medicines. 2. Clinical considerations and new agents

VC Jordan - Journal of medicinal chemistry, 2003 - ACS Publications
The critical step in the development of novel approaches to prevent disease is the
translation of laboratory concepts to clinically useful interventions. The expanding database …

Role of reactive metabolites in drug-induced hepatotoxicity

A Srivastava, JL Maggs, DJ Antoine, DP Williams… - Adverse drug …, 2010 - Springer
Drugs are generally converted to biologically inactive forms and eliminated from the body,
principally by hepatic metabolism. However, certain drugs undergo biotransformation to …

Understanding the genotoxicity of tamoxifen?

DH Phillips - Carcinogenesis, 2001 - academic.oup.com
Tamoxifen is an anti-oestrogenic drug widely used for adjuvant therapy of breast cancer. Its
use has caused an increased incidence of endometrial cancer and it is also a potent …

Hepatotoxicity: a scheme for generating chemical categories for read-across, structural alerts and insights into mechanism (s) of action

M Hewitt, SJ Enoch, JC Madden… - Critical reviews in …, 2013 - Taylor & Francis
The ability of a compound to cause adverse effects to the liver is one of the most common
reasons for drug development failures and the withdrawal of drugs from the market. Such …

Metabolism of lamotrigine to a reactive arene oxide intermediate

JL Maggs, DJ Naisbitt, JNA Tettey… - Chemical research in …, 2000 - ACS Publications
Lamotrigine [3, 5-diamino-6-(2, 3-dichlorophenyl)-1, 2, 4-triazine] is an antiepileptic drug
associated with hypersensitivity reactions which are thought to be an immunological …

Molecular mechanisms involved in the protective actions of Selective Estrogen Receptor Modulators in brain cells

E Baez-Jurado, MA Rincón-Benavides… - Frontiers in …, 2019 - Elsevier
Synthetic selective modulators of the estrogen receptors (SERMs) have shown to protect
neurons and glial cells against toxic insults. Among the most relevant beneficial effects …

Identification of human CYP forms involved in the activation of tamoxifen and irreversible binding to DNA

DJ Boocock, K Brown, AH Gibbs, E Sanchez… - …, 2002 - academic.oup.com
This study investigates which CYP forms are responsible for the conversion of tamoxifen to
its putative active metabolite α-hydroxytamoxifen and irreversible binding to DNA. We have …

Breast cancer chemoprevention: risk-benefit effects of the antioestrogen tamoxifen

K Brown - Expert opinion on drug safety, 2002 - Taylor & Francis
The anti-oestrogen tamoxifen, which is widely used as adjuvant therapy for breast cancer, is
undergoing evaluation as a chemopreventive agent in women at increased risk of …

Chemoprevention of breast cancer by tamoxifen: risks and opportunities

LL Smith, K Brown, P Carthew, CK Lim… - Critical reviews in …, 2000 - Taylor & Francis
The antiestrogen tamoxifen is widely used in the adjuvant therapy of breast cancers in
women and helps to prevent the occurrence of breast tumors in healthy women. However …