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www.MedChemE
MedChemExpress
Antibody-DrugConjugates(ADCs)Handbook
ToimprovetheSpecificityofBioactiveMoleculestoTumorCells
MCE
MasterofBioactiveMolecules
Antibody-DrugConjugates(ADCs)
Antibody-DrugConjugate(ADC)isapotentbiopharmaceuticalcancer-targeteddrugscomprisedofahumanizedorhumanmonoclonalantibodyconjugatedwithcytotoxicdrugs(payloads)viaachemicallinker[1].
ADCsexhibithighselectivityandtoxicitytothetumor,andbecomeoneofthefastest-growingclassesoftherapeutics.TheADCsaremulticomponentmolecules.Theselectionoftargetantigen,antibody,payload,linker,andconjugationstrategiesisofvitalimportanceinthedesignofADCs.
Exceptforspecificantigensandantibodies,linkersandpayloadsarealsoveryimportantfactorsfortheefficacyofADCs.
ADCCytotoxin
Destroyscancercells
ADCLinker
Joinsantibodyanddrug
Antibody
Targetscancercells
Figure1.SchematicstructureofADCs.
www.MedChemE
Inhibitors ? ScreeningLibraries ? Proteins
ADCsExpandtheTherapeuticWindow
ADCscanincreaseefficacyandreducethetoxicityofpayloadscomparedwithtraditionalcytotoxicdrugs.Theselectivedeliveryofcytotoxicdrugstotumorcellsincreasesthepercentageofcytotoxicmoleculesthatreachthetumor,thusbroadeningthetherapeuticwindow.Nevertheless,thetherapeuticwindowremainednarrowforsecond-generationADCs.Thisisduetooff-targettoxicity,competitionwithunconjugatedantibodiesandaggregationorfastclearance.
Withthecomingofnewtechnology,thediscoveryofthepayloads,theoptimizationoftheantibody,thelinkerandconjugationchemistryplaysakeyroleinimprovingthetherapeuticwindowofthird-generationADCs[2].
Chemotherapies Second-generationADCs Third-generationADCs
Drugdose
Maximumtolerateddose
Minimumeffectivedose
TherapeuticWindow
Maximumtolerateddose
MMAEorMMAF;DM1orDM4
ConjugatedvialysineonmAb
Reducedhingecysteineconjugation
Minimumeff
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