Fitz - Targeted Therapy & Biologicals Flashcards

1
Q

occupies the ATP cofactor binding site on Bcr-Ab causing inhibition of phosphate transfer to tyrosine kinase

A

imatinib

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2
Q

resistance to imatinib

A

mutation in ATP binding pocket

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3
Q

can overcome imatibib resistance

A

dasatinib

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4
Q

tx: imatinib

A

CML, GIST

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5
Q

tx: basatinib

A

CML, ALL

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6
Q

receptors specific for GIST

A

c-kit, PDFR (membrane)

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7
Q

tx of imatinib-resistant GIST

A

sunitinib

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8
Q

membrane ass’d RTK inhibitors

A
  • gefitinib
  • erlotinib
  • lapatinib
  • sunitinib
  • sorafenib
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9
Q

RTK overexpression seen 25% of breast cancers

A

HER2

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10
Q

drugs that inhibit EGFR

A
  • gefitinib
  • erlotinib
  • lapatinib
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11
Q

drugs that inhibit HER2

A

lapatinib

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12
Q

drugs that inhibit PDFR and VEGFR

A
  • sunitinib

- sorafenib

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13
Q

tx: gefitinib, erlotinib

A

NSCLC

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14
Q

tx: sunitinib

A
  • GIST

- RCC

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15
Q

tx: sorafenib

A

RCC

HCC

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16
Q

tx: lapatinib

A

breast cancer

17
Q

inhibits mutant BRAF V600E

A

vemurafinib

18
Q

antibodies that target EGFR

A
  • cetuximab

- panitumab

19
Q

antibodies that target HER2R

A

trastuzumab

20
Q

antibodies that target VEGF ligand

A

bevacizumab

21
Q

tx: cetuximab

A

colorectal, H/N cancer (not KRAS mutants)

22
Q

tx: panitumumab

A

colorectal ca (not KRAS mutants)

23
Q

tx: bevacizumab

A

advanced solid tumors - RCC, colon, lung brain ca

24
Q

tx: trastuzumab

A

HER2+ breast ca

25
Q

target for rituxomab

A

CD20+ - B cell lymphomas