Monoclonal Antibody- Herecptin Flashcards
1
Q
Drug name of Herceptin?
A
Trastuzumab
2
Q
What does Herceptin treat
A
HER2+ breast cancer
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
4
Q
How is hereceptin metabolised
A
- intracellularly into peptides and amino acids
- Eliminated by IgG clearance through reticuloendothelial system
5
Q
What issues does Herecptin have
A
- Cardiotoxic
- Immune response to MAbs
- Expensive and laborious to make
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
7
Q
How does HER2 over expression cause uncontrolled proliferation
A
HER2 on cell surface carries signals inside and sidesteps CDK2 cell cycle checkpoint
8
Q
How does Herceptin stop HER2 mediated tumour growth
A
- Binds to EC portion of HER2
- Prevents homodimerisation
- Arrests cells in G1 phase
- Possibly through AKT inhibition
9
Q
What indirect ways does Herceptin reduce cancer growth
A
- Inhibits angiogenesis
- Activates p27 tumour suppressor
- Inhibits HER2 EC domain cleavage which can induce unregulated growth