Monoclonal antibodies/small molecule Flashcards
Trastuzumab
- MECH OF ACTION:
–> Binds to extracellular portion of receptor HER-2 and BLOCKS HER-2 mediated signaling
–> can induce antibody dependent cytotoxicity
- TX for HER-2 overexpressing metastatic breast cancer
- ADVERSE: CARDIAC TOXICITY
Cetuximab
- Mech of Action:
–> monoclonal antibody that binds to EGFR and blocks signaling
- TX of EGFR-expressing colorectal tumors
- RESISTANCE:
- Activating mutations in RAS leads to resistance
Bevacizumab
- monocolonal antibody that binds VEGF
–> prevents VEGF from activating VEGF receptors causing inhibiton of angiogenesis
- ADVERSE EFFECTS:
–> HYPERTENSION
Lapatinib
- MECH of ACTION
–> small molecule that inhibits both EGFR and HER-2 KINASE ACTIviTY
- TX of HER-2 amplfieed, trastuzumab-refractory breast cancer
Erlotinib
- EGFR-inhibitor
–> ATP competitive inhibitor
- TX of Metastatic nonsmall cell lung carcinoma
Imatinib
- MECH OF ACTION:
–> small molecular inhibitor of BCR-ABL
- TX for Chronic myelogenous leukemia (CML) –> caused by philadelphia chromosome translocation
- RESISTANCE
–> point mutations in BCR-ABL cause a reduced affinity for imatinib
ASPARAGINASE
- Mech of action;
- Hydrolyzes plasma L-asparagine into L-aspartate (normal cells can produce L-asparagine, tumor cells cannot)
–> starves the tumor cells of L-asparagine
- TX for childhood acute lymphoblastic leukemia (ALL)
- ADVERSE = Hypersensitivity reaction
Bortezomib
- Mech of action:
–> inhibits proteasome causing increased levels of p53
–> also reduces levels of protein that normally inhibits apoptosis called NK-kappaB
- TX for Multiple myelomas
- ADVERSE = Peripheral neuropathy
Temsirolimus
- Mech of Action:
–> Inhibition of mTOR complex 1 –> reduces protein translation, promotes cell cycle inhibiton and promotes apoptosis
- TX for renal cell carcinoma
