4 Precision Drug Targets Flashcards
How are drug targets identified
Accredited, validated diagnostic test
What are some issues with cytotoxic chemotherapy (4)
Low specificity
Low therapeutic indices
Affects both normal and malignant cells
Mainly IV administration
What are some pros of molecular targeted drugs (4)
Monoclonal antibodies (mabs) and small molecule inhibitors (ibs)
Highly target specific, not 100% tumour selective
Improved therapeutic index
Short bolus iv administration
What are some patient specific questions
Dose to use Reach tumour Side effects Response Right time
What does DNA topoisomerase I do (4)
Resolves torsional stress in DNA strands when double helices are unravelled during replication, transcription and recombination
Relaxes supercoils generated during transcription
Cuts one strand to enable replication
Re-anneals strands
What happens if re-ligation is inhibited
ssDNA breaks/mutates which is detected and leads to apoptosis
What are some uracil analogudes
5FU
Capecitabine
What is an analogue of cytidine
Gemcitabine
What are the 3 main metabolits of 5FU
FdUMP
FdUTP
FUTP
What are microtubules comprised of
Polymerised ab-tubulin
What are microtubules critical for (5)
Cell division Vesicle transport Signalling Cell shape Polarity
What are two taxanes
Paclitaxel
Docetaxel
What toxicities are involved with taxels
Hypersensitivity
Neutropenia
Sensory neuropathy
What toxicities are involved with vinca alkaloids
Standard chemo toxicity
Hair loss, penia, fatigue and hypersensitivity
MOA of taxanes (3)
1) Bind to interior surface of b-subunit of microtubuke
2) Stabilise microtubule and increase polymerisation
3) Prevent microtubule disassembly
