protein-targeted therapies- TKIs Flashcards
how do protein-targeted therapies work?
target intracellular pathways
Types of protein-targeted therapies
Tyrosine kinase inhibitors
mTOR inhibitor
proteasome inhibitor
Common side effects of protein-targeted therapies
skin rashes, cardiotoxicity, GI symptoms (n,v,d,anorexia)
Types of Tyrosine Kinase Inhibitors
Erlotinib (Tarceva) Gefitinib (Iressa) Imatinib (Gleevec) Sorafenib (Nexavar) Sunitinib (Sutent)
Indications for Tyrosine Kinase inhibitors
Erlotinib (Tarceva)-NSCLC, pancreatic
Gefitinib (Iressa)-NSCLC
Imatinib (Gleevec)-(Ph)CML, (Ph) ALL, GIST, MDS
Sorafenib (Nexavar)-renal, liver
Sunitinib (Sutent)-GIST, renal pancreatic neuroendocrine
Erlotinib (Tarceva)
NSCLC, Pancreatic
Interactions: take on empty stomach with full glass of water. Sensitive to CYP3A4 inhibitors and inducers
Gefitinib (Iressa)
NSCLC
Interactions: dissolve tablets in water and follow with full glass of water. Barbiturates increase toxicity
Imatinib (Gleevec)
(Ph)CML, (Ph) ALL, GIST, MDS
Interactions: take with meal and glass of water. Can be dissolved in water or apple juice. Sensitive to CYP3A4 inhibitors and inducers
Sorafenib (Nexavar)
renal, liver
Interactions: take on empty stomach. Sensitive to CYP3A4 inducers (decrease activity)
Sunitinib (Sutent)
GIST, renal pancreatic neuroendocrine
Interactions: take with or without food. Sensitive to CYP3A4 inhibitors and inducers
Other TKI’s –> Axitinib (Inlyta)
PO
Sensitive to CYP3A4 inhibitors and inducers
Other TKI’s –> Dasatinib (sprycel)
PO
Sensitive to CYP3A4 inhibitors and inducers. Do not crush or cut drug.
Other TKI’s –> Lapatinib (Tykerb)
PO
CYP3A4 inhibitors increase drug activity. Do not crush or cut drug
Other TKI’s –> Nilotinib (Tasigna)
PO
CYP3A4 inhibitors increase drug activity.
Contains lactose, may need lactase enzymes
Regorafenib (Stivarga)
PO
High fat meals alter absorption. Take with low fat meal that contains less than 30 g fat
