2022
Drug Design Strategies: Role of Structural Modifications of Drug Candidates to Improve PK Parameters of New Drugs
NASSAR A. Drug Design Strategies: Role of Structural Modifications of Drug Candidates to Improve PK Parameters of New Drugs. 2022, 323-343. DOI: 10.1002/9781119851042.ch10.Peer-Reviewed Original ResearchDrug candidatesSuccessful drug designDrug metabolism scientistsDrug designDrug discoveryStructural modificationsMetabolic stabilityDiverse propertiesActive metabolitePass metabolismToxicity relationshipsSoft drugsReactive metabolitesInhibition/inductionMetabolism studiesPharmacokinetic issuesRenal clearanceSafe drugPK parametersMetabolic clearanceMetabolic inactivationNew drugsDrugsMetabolitesClearanceChemical Structural Alert and Reactive Metabolite Concept as Applied in Medicinal Chemistry to Minimize the Toxicity of Drug Candidates
NASSAR A. Chemical Structural Alert and Reactive Metabolite Concept as Applied in Medicinal Chemistry to Minimize the Toxicity of Drug Candidates. 2022, 345-372. DOI: 10.1002/9781119851042.ch11.Peer-Reviewed Original ResearchAryl hydroxamic acidsDrug candidatesMedicinal chemistryChemical groupsQuinone methideChemical structural alertsReactive metabolitesArylpropionic acidsStructural alertsLarge clinical trialsHydroxamic acidPreclinical safety studiesToxicity problemsToxicity warningExamples of drugsPotential toxicityAdverse reactionsClinical trialsMedium-chain fatty acidsSide effectsStable metaboliteAcidHuman drugsSafety studiesNitroaromatics
2010
Minimizing the Potential for Drug Bioactivation of Drug Candidates to Success in Clinical Development
Nassar A. Minimizing the Potential for Drug Bioactivation of Drug Candidates to Success in Clinical Development. 2010, 1-24. DOI: 10.1002/9780470571224.pse111.Peer-Reviewed Original ResearchDrug candidatesIdiosyncratic drug reactionsNew drug candidatesReactive metabolitesDrug discoveryDrug bioactivationDrug-metabolizing enzymesHuman drug-metabolizing enzymesPotential toxicitySafety profileDrug reactionsClinical developmentPreclinical phaseSubtle evidenceReactionRecent effortsToxicityMetabolitesCandidates