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Flashcards in Clinical Correlation Cancer Deck (21):

What do the tyrosine kinase inhibitors and monoclonal antibodies differ in terms of route of administration and half-life?

TKIs = short half life, taken orally

Monoclonal Abs = long halflife, given IV


What drug is the prototypical VEGF monoclonal antibody and how does it work?

bevacizumab - the beverage lady

Works by binding the VEGF ligands to prevent downstream signalling and impede angiogenesis to tumors


What tumors is bevacizumab used for?

Colorectal and lung cancers


What pathways does bevacizumab inhibit by binding VEGF ligand?

Ras/MAPK pathway and PI3-kinase / Atk
(protein kinase B) pathway

Decreased functional vasculature to tumors


What are the adverse effects of bevacizumab?

Bleeding (blood on beverage lady's shirt)
Hypertension (increases peripheral vascular resistance)
Proteinuria (altered kidney blood flow)


What drug is a VEGF tyrosine kinase inhibitor? What type of cancer does it primarily treat?

-tinibs are tyrosine kinase inhibitors (nib of pen)

Sunitinib (sun outside the building with VEGF vegetables in the field) - binds into TK active site and inhibits phosphorylation

Treats renal cell cancer (flank crab buckles on farmer)


What other cancers does sunitinib treat and how?

Gastrointestinal stromal tumors -> crossreactive with platelet-derived growth factor receptor (PDGFR) and c-KIT


What are the common toxicities of sunitinib?

Hypertension (like bevacizumab)
Hypothyroidism (mechanism unknown)


What drug is an EGFR 1 monoclonal antibody? EGFR tyrosine kinase inhibitor?

EGFR 1 monoclonal antibody - cetuximab - think tusks of elephant with GiRaFeE on his saddle

EGFR tyrosine kinase inhibitor - erlotinib - think Earl of Tinib with Geoffrey on his head


What cancers is cetuximab useful for?

Colorectal adenocarcinomas and head and neck squamous cell cancers


What type of pathology must be present to effectively treat cancer with cetuximab?

Normal KRas/NRas biology -> if mutated, EGFR receptor will not be driving pathology, and it will not be effective


What are the toxicities of cetuximab?

Rash - in almost all patients (think of red spots on the giraffe)
Hypersensitivity - think of elephant sicking serum sickness cup (chimeric antibody)


What cancer type is erlotinib used for?

EGFR-mutated non-small cell lung cancers (exons 19 and 21)


What are the toxicities of erlotinib?

Rash (think of the Earl's rash)
Diarrhea (think of his soiled pants)


What is the important EGFR2 antibody and what are its mechanisms?

Trastuzumab - Think of tapestry

Activity against HER2 receptor -> think of her two kids in the tyrosine kinase wheel

Also has ADCC activity - antibody-directed cell-mediated cytotoxicity


What cancers is trastuzumab useful for?

Breast cancer (think of breast cancer crabs on her bobs)

Some GI cancers


What is the unique toxicity of trastuzumab?

Cardiotoxicity - think of hearts hanging from her tapestry


What drug is the prototype Antibody-drug conjugate and when is it used?

Trastuzumab (tapestry) with emtansine

Emtansine is a mitotic spindle inhibitor to breast cancer

Used in advanced HER2 positive breast cancer (her 2 kids)


What drug is an anti-PD-1 monoclonal antibody and how does it work?

Nivolumab - binds the PD-1 receptor on T-cells so it cannot bind the PD-L1 of cancer cells which will induce apoptosis of that T cell line


What is nivolumab used to treat?

Melanoma, lung cancer, and kidney cancer


What are the toxicities of nivolumab?

Everything related to overactive T cells (since reactive ones cannot be easily apoptosed)


Lung, liver, and colon inflammation