Linked Life Data

20020275

Source:http://linkedlifedata.com/resource/pubmed/id/20020275

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
196
pubmed:dateCreated
2009-12-18
pubmed:abstractText
A large body of circumstantial evidence suggests that metabolic activation of drug candidates to chemically reactive electrophilic metabolites that are capable of covalently modifying cellular macromolecules may result in acute and/or immune system-mediated idiosyncratic toxicities in humans. Thus, minimizing the potential for metabolic activation of new drug candidates during the drug discovery and lead optimization stage represents a prudent strategy to help discover and develop the next generation of safe and effective therapeutic agents. In the present chapter, we discuss the scientific methodologies that currently are available to industrial pharmaceutical scientists for assessing and minimizing metabolic activation during drug discovery, their attributes and limitations, and future scientific directions that have the potential to help advance progress in this field. We also propose a roadmap that should help utilize the armamentarium of available scientific tools in a logical way and contribute to addressing metabolic activation issues in the drug discovery-setting in a rapid, scientifically appropriate, and resource-conscious manner.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:status
MEDLINE
pubmed:issn
0171-2004
pubmed:author
pubmed:issnType
Print
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
511-44
pubmed:meshHeading
pubmed:year
2010
pubmed:articleTitle
Approaches for minimizing metabolic activation of new drug candidates in drug discovery.
pubmed:affiliation
Department of Drug Metabolism and Pharmacokinetics, Merck Research Laboratories, Rahway, New Jersey, USA. sanjeev_kumar@merck.com
pubmed:publicationType
Journal Article, Review