Fitz- CML Module Flashcards

1
Q

What is the general MOA for STIs?

A

They bind to to the ATP binding site of TK

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2
Q

What are the general SE of STIs?

A

Generally have fewer SE than conventional therapies because they are target toward the specific defect of a particular cancer.

CAN cause CHF and MYOCARDIAL INFARCTION
TERATOGENIC

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3
Q

Why is Imatinib so successful?

A

Targets a genetic defect that is perfectly selective to cancer cells

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4
Q

What are the TUs for imatinib?

A

Complete hematological/cytological response in 85-95% of pts w/ chronic CML

Delay death in 25% of pts in blast crisis

Gastroinstestinal stormal tumors expressing c-kit

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5
Q

Where does imatinib act?

A

Competitive antagonist at the ATP binding site of:

BCR-ABL
c-KIT–altered in GIST
PDGF

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6
Q

What does DASTAINIB specifically target?

A

SRC

A TK whose expression is up-regulated in several types of cancer

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7
Q

What are common toxicities associated w/ imatinib?

A

edema

BMS

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8
Q

What are the therapeutic uses for gefitinib and erolotinib? What is weird about it in terms of efficacy?

A

Metastatic non-small cell lung cancer after failure of standard chemotherapies

different populations experience varying efficacies–> having the right mutation means the diff between a cure and a response

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9
Q

What is the MOA for efitinib and erolotinib? what does it commonly target?

A

competitive antagonists of ATP binding site of EGFR TK

EGFR TK is overexpressed in epithelial derived cancers

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10
Q

Interstitial pneumonia is associated w/ what drugs?

A

Erlotinib and gefitinib

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11
Q

How does imatinib compare to the conventional therapy for the treatment of CML?

A

STIs are MOST successful at promoting remission, but don’t cure the underlying cause of cancer.

They generally have LOWER toxicity and GREATER differential selectivity.

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