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 drugsDrugsMetabolitesClearanceAccelerating Metabolite Identification Mass Spectrometry Technology Drives Metabolite Identification Studies Forward
NASSAR A. Accelerating Metabolite Identification Mass Spectrometry Technology Drives Metabolite Identification Studies Forward. 2022, 267-302. DOI: 10.1002/9781119851042.ch8.Peer-Reviewed Original ResearchDrug candidatesDrug discoveryLC-MSLiquid chromatography-mass spectrometryChromatography-mass spectrometryMetabolite identification studiesSuccessful drug candidatesFlight mass spectrometryDrug discovery effortsMass spectrometry technologyTriple quadrupoleADMET studiesStructural assignmentMass spectrometryMetabolite characterizationLead compoundsSpectrometry technologyIon trapDiscovery effortsOverall safety profileHuman-specific metabolitesSpectrometryDrug development processMetabolism issuesMetabolite profilingRole of Structural Modifications of Drug Candidates to Enhance Metabolic Stability
Nassar A. Role of Structural Modifications of Drug Candidates to Enhance Metabolic Stability. 2022, 303-322. DOI: 10.1002/9781119851042.ch9.Peer-Reviewed Original ResearchDrug candidatesStructural modificationsMetabolic stabilityDrug discovery processADME propertiesMetabolite characterizationDrug designDrug discoveryBalance of propertiesToxicity relationshipsExcretion studiesMetabolic instabilityDiscovery processHuman patientsStabilityPropertiesSuccess rateModificationDrugsCandidatesCharacterizationAbsorptionPatientsChemical 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
Structural Modifications of Drug Candidates: How Useful Are They in Improving Metabolic Stability of New Drugs? Part I: Enhancing Metabolic Stability
Nassar A. Structural Modifications of Drug Candidates: How Useful Are They in Improving Metabolic Stability of New Drugs? Part I: Enhancing Metabolic Stability. 2010, 1-16. DOI: 10.1002/9780470571224.pse109.Peer-Reviewed Original ResearchMinimizing 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
2008
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. 2008, 283-306. DOI: 10.1002/9780470439265.ch12.Peer-Reviewed Original ResearchStructural Modifications of Drug Candidates: How Useful Are They in Improving PK Parameters of New Drugs? Part II: Drug Design Strategies
Nassar A. Structural Modifications of Drug Candidates: How Useful Are They in Improving PK Parameters of New Drugs? Part II: Drug Design Strategies. 2008, 269-281. DOI: 10.1002/9780470439265.ch11.Peer-Reviewed Original ResearchStructural Modifications of Drug Candidates: How Useful Are They in Improving Metabolic Stability of New Drugs? Part I: Enhancing Metabolic Stability
Nassar A. Structural Modifications of Drug Candidates: How Useful Are They in Improving Metabolic Stability of New Drugs? Part I: Enhancing Metabolic Stability. 2008, 253-268. DOI: 10.1002/9780470439265.ch10.Peer-Reviewed Original Research