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Pharm Ch38

Cancer - Signal Transduction

QuestionAnswer
MOA of Gefitinib, Erlotinib, Cetuximab, Trastuzumab EGFR Antagonists
Reversible inhibitor of tyrosine kinase, PO; Tx: NSCLCs Gefitinib
2nd or 3rd line Tx: NSCLC, colon, pancreatic, H&N cancer, glioblastoma Erlotinib
binds EGFR (ErbB1), Tx: H&N cancer, ADR: skin rash, diarrhea Cetuximab
binds ErbB2 (HER-2) Tx: breast cancer, ADR: cardiotoxicity Trastuzumab
MOA of Imatinib mesylate inhibits ABL kinase (targeted therapeutic)
Tx: CML (BCR-ABL), GIST (C-KIT), systemic mastocytosis, idiopathic hypereosinophilic syndrome (PDGFRA), ADR: edema, N/D, cramps, rash Imatinib mesylate
MOA of Sorafenib B-RAF inhibitor (MAP Kinase Pathway Inhibition)
Tx: melanoma, RCC Sorafenib
MOA of Rapamycin (Sirolimus) binds to FKBP12 (mTOR Inhibitor) which causes immunosuppression, promotes cell cycle inhibition, apoptosis and angiogenesis inhibition
MOA of Bortezomib Proteasome Inhibitor: targets N-terminal threonine residue of 20S subunit
Tx: refractory multiple myeloma, ADR: neuropathy, thrombocytopenia, neutropenia Bortezomib
MOA of Bevacizumab Anti-VEGF-A Antibody
Tx: refractory RCC, ADR: proteinuria, HTN, thrombosis, bleeding Bevacizumab
MOA of Sunitinib inhibits VEGFR-1, 2, PDGFR
synthetic glutamic acid derivative (IMiD), inhibits TNF-a, bFGF Tx: ENL, multiple myeloma, ADR: teratogenic, phocomelia, thrombosis, neuropathy Thalidomide
synthetic second-gen IMiD, Tx: refractory multiple myeloma, MDS (del 5q), ADRs: myelosuppression, thrombocytopenia Lenalidomide
anti-CD20 IgG1, Tx: B-cell NHL, ADRs: immunosuppression, hypersensitivity Rituximab
Created by: fmuralid
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