Fancy cancer drugs Flashcards
Gefitinib
- use
- MOA
- side effects main
Lung cancer- adenoca with EGFR mutation positive
Tyrosine kinase domain of EGFR inhibited
ACne skin rash,
Diarrhoea, N and V
ILD rare but severe
Erlotinib
- use
- MOA
- side effects main
Lung cancer- adenoca with EGFR mutation positive
Tyrosine kinase domain of EGFR inhibited
ACne skin rash,
Diarrhoea, N and V
ILD rare but severe
hepatotoxicity and hepatorenal syndrome
Crizotinib
- use
- MOA
- side effects main
Lung cancer- mostly seen in adenoCa. Need to have AML-4-ALK fusion
Inhibits ALK and ROS1 and cMET. Causes cell arrest at G1/S
oral therapy GI mild-mod pneumonitis can be severe Bradycardia and long QTc Mild visual disturbance
Ceritinib
Lung cancer- mostly seen in adenoCa. Need to have AML-4-ALK fusion
Inhibits ALK and ROS1 and cMET. Causes cell arrest at G1/S
20 x more potent than crizotinib- used when progress on crizotinib
Nivolumab
Anti-PD-1 Antibody
Prevents binding of cancer PD-L1 to downregulate T cell response–>increase immune response against cancer
Works in melanoma
Works in lung ca irrespective of PDL1 status of tumour
Pertuzumab
HER2 positive breast cancer
New study shows best treatment for metastatic HER2 positive cancer is Trastuzumab + pertuzumab + docetaxel
oral small molecule TKI
Unlike Herceptin can get into the CNS
Binds to the dimerisation domain of HER2 receptor, blocks binding with self and other EGFR
Trastuzumab
HER2 positive breast cancer
Also in HER2 positive stomach cancer!
Lapatanib
small oral molecule used in HER2 positive breast cancer where they have progressed quickly following trastuzumab
binding to the ATP-binding pocket of the EGFR/HER2 protein kinase domain, preventing self-phosphorylation and subsequent activation of the signal mechanism.
rash, diarrhea, nausea
Exemastane
In ER/PR positive breast cancer use in metastatic disease once has progressed on nonsteroidal AI (like anastrozole or letrozole)
Sunitinib
Multi-TKI
Renal clear cell first line
hypertension, hand foot syndrome, diarrhoea, haem tox, thyroid dysfunction
Pazopanib
VEGF-i
Renal clear cell first line
hypertension, diarrhea, anorexia, LFT, hair colour
Temsirolimus
Can be first line in renal clear cell
hyperglucaemia, hyperlipidaemia, rash, periph oedema
Cannot access on PBS
PNEUMONITIS- CAN DIE- MUST STOP DRUG
Everolimus good if progress on VEGF therapy quickly
Axitinib
VEGF-i
Used in renal cell clear
second line preferred agent
Dabrafenib
BRAF inhibitor in presence of V600E mutation in melanoma
50% response rate
fatigue, arthralgia, rash, SCC, hyperkeratosis, other non-BRAF melanomas.
Trametinib
Used in melanoma with the BRAF inhibitors (Dabrafenib/Vemurafenib)- eventually if block BRAF receptor, the downstream MEK pathway will mutate and become autonomous. Hence better response if from the start give a MEK inhibitor with BRAF inhibitor.
