Monoclonal Antibody- Herecptin Flashcards

1
Q

Drug name of Herceptin?

A

Trastuzumab

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2
Q

What does Herceptin treat

A

HER2+ breast cancer

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3
Q

Why is it Herceptin significant drug

A

1/5 BCs over express HER2, tend to be more aggressive
3 million lives saved since 1998

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4
Q

How is hereceptin metabolised

A
  1. intracellularly into peptides and amino acids
  2. Eliminated by IgG clearance through reticuloendothelial system
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5
Q

What issues does Herecptin have

A
  1. Cardiotoxic
  2. Immune response to MAbs
  3. Expensive and laborious to make
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6
Q

How does HER2 pathway promote cancer growth

A

Initiates MAPK pathway and PI3/AKT pathway activating NF-KB pathway all of which are tumorigenic

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7
Q

How does HER2 over expression cause uncontrolled proliferation

A

HER2 on cell surface carries signals inside and sidesteps CDK2 cell cycle checkpoint

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8
Q

How does Herceptin stop HER2 mediated tumour growth

A
  1. Binds to EC portion of HER2
  2. Prevents homodimerisation
  3. Arrests cells in G1 phase
  4. Possibly through AKT inhibition
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9
Q

What indirect ways does Herceptin reduce cancer growth

A
  1. Inhibits angiogenesis
  2. Activates p27 tumour suppressor
  3. Inhibits HER2 EC domain cleavage which can induce unregulated growth
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