Oncology Biologics Flashcards
Nib or Mab?
Mab
What are the two mechanisms of MABs?
- Recruit other things like NK, Macrophages, Complex proteins which all are toxic to the cancer cell and promote cell death
- Blocking the receptor signaling- This is not a toxic effect often times need to administer other toxins to kill the cells
Transtuzumab/ HER2
What is overexpressed?
Strategy?
- HER2 is overexpressed and this causes initiation of various hallmark cascades
- Block the receptor
Trastuzumab
What type of drug?
MOA?
Selectivity?
Resistance?
- Humanized Monoclonal protein (from mice)
- Binds to the HER2 receptor –> Blocks the receptor sites–> Interupts the growth signal
- Overexpression of the receptor
- If used as single agent there is resistance but it needs to be used in combination so it isnt static and becomes cidal
Tratuzumab is mainly used for what cancers?
- Breast cancer is the most common treatment
- Heart monitoring is important
Bevacizumab
Inhibitor of?
VEGF
Originally approved for breast cancer but there was no improvement of QOL so it was taken off
Cetuximab Panitumumab
Approved for the treatment of EGFR-expressing metastic colorectal cancer with no?
With no KRAS mutation
Why is it so important that we know what drugs dont work with what mutations?
Because if you have something like KRAS and you just simply block the receptor nothing with happen because downstream mutations are what are causing the proliferation fo hallmarks
ADC?
Antibody drug conjugate
Kadcyla-ada-trastuzumab emtasine
DM1? MOA if given alone?
Trastuzumab is given for what reason?
- DM1 Mertansin- Mitosis inhibitor, and is too toxic to be given alone
- Trastuzumab is employed as a delivery system to target cell with overexpressed HER2
Brentuximab Vedotin
General structure?
MAB target?
MMAE?
- MAB, Linker, Warhead
- Targets CD30 protein expressed in hodgkin and large cell lymphomas
- MMAE- Antimitotis agent inhibitd polymerization
