Chemotherapeutics: Kinase Inhibitors and Monoclonal Antibodies Flashcards
-tinib suffix for
tyrosine kinase inhibitors
Gefitinib MOA
inhibits tyrosine kinase domain of EGFR
Gefitinib treats
NSCLC
gefitnib side effects
skin rash;acne syndome, diarrhea, anorexia
gefitinib cautions
metabolized by CYP3A4
CYP3A4 inhibited by
grapefruit juice and warfarin
gefitinib unique properties
monotherapy and related drug erlotinib
imatinib MOA
inhibits BCR-Abl kinase (tyrosine kinase)
imatinib treats
CML and GI stormal tumors (GIST)
imatinib side effects
fluid retention/CHF, n/v/d, prolong QT interval, hepatotoxicity, liver metabolism
lapatinib MOA
blocks tyrosine kinase actives of EGFR and HER2/neu
lapatinib treats
breast cancer
lapatinib side effects
n/d, rash, can prolong QT interval, dehydration
sunitinib MOA
inhibits VEGFRalpha, beta, 1,2,3 and c-kit
sunitinib treats
kidney and pancreatic cancer
sunitinib side effects
diarrhea, HTN, bleeding complications, CYP3A4
sorafenib MOA
inhibits VEGFR2,3, PDGFR and Raf kinases
sorafenib treats
kidney and liver cancers
sorafenib side effects
rash & skin problems/hand-foot syndrom, HTN, bleeding complications, CYP3A4
-xi
chimeric
-mab
monoclonal antibody
all Mabs can cause what kind of reaction
infusion reaction
Bevacizumab MOA
binds and blocks VEGF-A; prevents new angiogenesis
Bevacizumab treats
metastatic colorectal cancer
bevacizumab side effects
HTN, Arterial thombotic events, diarrhea, stomatitis, GI perforations
Cetuximab MOA
binds and inhibits EGFR signaling
cetuximab treats
colorectal cancer
cetuximab side effects
dyspnea, hypotension, interstitial lung dz, rash
cetuximab rash indicative of
positive response to therapy
rituximab MOA
antiCD20 mab, depletes B lymphocytes (attached by CD8)
rituximab treats
leukemias/lymphomas (NHL and CLL)
rituximab side effects
infusion reactions (some fatal), HTN, Brochospasm, angioedema, arrythimias, tumorlysis syndome can lead to kidney failure
trastuzumab MOA
Blnds/blocks HER2
trastuzumab treats
metastatic breast cancer
trastuzumab side effects
CHF, cardiomyopathy, flu-like symptoms, n/v
Denosumab MOA
targets RANK Ligand in osteoclasts, blocks bone resorption, prevents fractures
denosumab treats
prostate and breast cancers
denosumab side effects
osteonecrosis of the jaw and dermatological reactions
denosumab needs to be taken with
calcium and vit D
Pembrolizumab MOA
blocks PD1 (checkpoint inhibitor)