Targeted Therapy Flashcards
Name the 5 basic classes of antineoplastic drugs
Alkylating agents Antimetabolites Plant alkaloids Hormone and antagonists Targeted Therapy
Name 3 alkylating agents
Melphalan
Chlorambucil
Cyclophosphamide
Name an antimetabolite
Methotrexate
Name 2 plant alkaloids
Taxanes
Vinca alkaloids
Name 2 hormones and antagonists
Anti-oestrogens
Anti-androgens
Name 2 targeted therapies
Monoclonal antibodies
Small tyrosine kinase inhibitors
What are the 2 best targets for cancer therapy
1- found in cancer cells but not normal
2- more targets in cancer than normal (eg gene amplification)
Define targeted cancer therapies
Drugs or other substances that block the growth and spread of cancer by interfering with specific molecules involved in tumour growth and progression
Name 2 intracellular pathways signalled by tyrosine kinases
P13 kinase pathway
MAPK pathway
Describe the action of antibodu of inhibitors of growth receptors
Bind to growth factors receptor and prevent growth signal
Describe the action of antibody-drug conjugatres
Targets drug to tumour cells
What syllable do all monoclonal antibodies end in
mab
What does it mean if the next to last syllable of a mab is u
Human
What does it mean if the next to last syllable of a mab is zu
Humanised
What does it mean if the next to last syllable is xi
Chimeric
What does it mean if the next to last syllable is o, a, e and u
o= mouse a= rat e= hampster i= primate
How do drugs that target growth factor receptors work?
Inhibits growth factor signalling that is mediated with tyrosine kinase
Results in arrest in tumour growth
Name 2 drugs that target epidermal growth factor receptor
Cetuximab
Panitumumab
Name a drug that targets HER2 (ErbB2)
Trastuzumab
Name a drug that targets HER3
Pertuzumab
Name a drug that targets vascular endothelial growth factor receptor
Bevacizumab
How do antibodies access tumour cells
Vessels are leaky so small and large molecules can access tissue
Tumour tissue doesn’t have lymphatic drainage so macromolecules are retained
How do some monoclonal antibodies kill the tumour cell directly
Signalling blocked
Apoptosis induced
Possible delivery of toxic payload
How do monocloonal antibodies kill tumour cells via immune mediated mechanism
Induce phagocytosis
Complement dependent cytotoxicity
Antibody dependent cell cytotoxicity
How do monoclonal antibodies work by vascular or stromal ablation
Possible delivery of toxic payload
VEGF antagonism
In what percentage of breast cancers overexpress HER2
15%