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Oncology PCOL

Exam 1

DrugClassMOATarget(s)ADRs
Gefitinib TK Inhibitor - EGFR Antagonist Reversible inhibitor of EGFR EGFR Secondary resistance, Liver function effects, Interstitial lung disease
Lapatinib TK Inhibitor - EGFR Antagonist Reversible inhibitor of EGFR + HER-2 EGFR + HER2 BW for Hepatotoxicity
Tucatinib TK Inhibitor - EGFR Antagonist Reversible HER-2 inhibitor HER2 Diarrhea + Hepatotoxicity
Afatinib TK Inhibitor - EGFR Antagonist Irreversible inhibitor of EGFR + HER2 + HER4 EGFR + HER2 + HER4
Osimertinib TK Inhibitor - EGFR Antagonist Irreversible EGFR inhibitor (including for variants L858R + exon 19 deletion) EGFR Interstitial lung disease, Pneumonia, Pulmonary embolism
Cetuximab TK Inhibitor - EGFR Antagonist High specificity Chimeric mouse/human IgG1 against EGFR (must evaluate for KRAS) EGFR Rash = Tumor response BW for Infusion reactions + Cardiopulmonary arrest
Panitumumab TK Inhibitor - EGFR Antagonist Human kappa monoclonal antibody against EGFR EGFR BW for dermatologic reactions
Trastuzumab TK Inhibitor - EGFR Antagonist Humanized monoclonal antibody against HER2; Downregulates HER2 and induces antibody-dependent cellular cytotoxicity HER2 BW for Cardiomyopathy, Infusion reactions, Pulmonary toxicity, Embryo-fetal toxicity *DI with Warfarin
Ado-trastuzumab emtansine TK Inhibitor - EGFR Antagonist Trastuzumab linked to small molecule cytotoxin (DM1) which binds to HER2 and is released to interrupt the cell cycle and causes apoptosis HER2 BW for Hepatotoxicity, Cardiotoxicity, Embryo-fetal toxicity
fam-trastuzumab deruxtecan-nxki TK Inhibitor - EGFR Antagonist Trastuzumab attached to Dxd (topoisomerase I inhibitor) which is released and causes DNA damage/apoptosis HER2 BW for Interstitial lung disease, Embryo-fetal toxicity
Pertuzumab TK Inhibitor - EGFR Antagonist Humanized monoclonal antibody targeting EHR2 *Used with trastuzumab to target different regions on HER2 receptor HER2 BW for Left ventricular dysfunction and Embryo-fetal toxicity
Crizotinib TK Inhibitor - ALK Inhibitor Binds to intracellular ALK, preventing phosphorylation ALK + ROS1 + MET Secondary resistance, Interstitial lung disease, Hepatotoxicity, QT prolongation, Bradycardia
Alectinib TK Inhibitor - ALK Inhibitor 2nd gen ALK inhibitor (better BBB penetration) ALK + RET Visual disturbances, Photo sensitivity, Fetal harm
Brigatinib TK Inhibitor - ALK Inhibitor 2nd gen ALK inhibitor (better BBB penetration) ALK + ROS1 + FLT3 + EGFR Variants Visual disturbances, Photo sensitivity, Fetal harm
Ensartinib TK Inhibitor - ALK Inhibitor 2nd gen ALK inhibitor (better BBB penetration) ALK + ROS1 + MET Visual disturbances, Photo sensitivity, Fetal harm
Lorlatinib TK Inhibitor - ALK Inhibitor 3rd gen ALK inhibitor (efficacious against ALK-resistant mutations) ALK + ROS1 Fetal harm
Midostaurin TK Inhibitor - FLT3 Inhibitor Inhibits FLT3, including ITD and TKD variants FLT3 Fetal harm
Quizartinib TK Inhibitor - FLT3 Inhibitor Inhibits FLT3, more potent for ITD FLT3 BW for QT prolongation, TdP and Cardiac arrest *CI in hypokalemia, hypomagnesemia, long QT
Entrectinib TK Inhibitor - TRK Inhibitor Inhibitor of TRKs, ROS1, ALK kinases TRK + ROS1 + ALK
Larotrectinib TK Inhibitor - TRK Inhibitor Inhibitor of TRK kinases TRK Neurotoxicity, Hepatotoxicity
Repotrectinib TK Inhibitor - TRK Inhibitor 2nd gen inhibitor of TRKs and ROS2 (better efficacy) TRK + ROS1
Pralsetinib TK Inhibitor - RET Inhibitor Inhibits RET RET
Selpercatinib TK Inhibitor - RET Inhibitor Inhibits RET, plus VEGFR and FGFRs RET + VEGFR + FGFR Impaired wound healing, Hepatotoxicity, QTc prolongation
Amivantamab-vmjw TK Inhibitor - MET Inhibitor Bispecific antibody that targets EGFR and MET; Stops signaling from receptors and kills targeted cells by antibody-dependent cellular cytotoxicity MET + EGFR Fetal harm
Capmantinib TK Inhibitor - MET Inhibitor MET Kinase inhibitor MET Peripheral edema
Tepotinib TK Inhibitor - MET Inhibitor MET Kinase inhibitor MET Peripheral edema
Acalabrutinib TK Inhibitor - BTK Inhibitor 2nd gen Irreversible BTK inhibitor (less CV effects) BTK Myelosuppression, Hemorrhaging **Better ADR profile than Zanubrutinib
Zanubrutinib TK Inhibitor - BTK Inhibitor 2nd gen Irreversible BTK inhibitor (less CV effects) BTK Myelosuppression, Hemorrhaging
Created by: merandaharker
 

 



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