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Flashcards in Fancy cancer drugs Deck (20)
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1
Q

Gefitinib

  • use
  • MOA
  • side effects main
A

Lung cancer- adenoca with EGFR mutation positive
Tyrosine kinase domain of EGFR inhibited

ACne skin rash,
Diarrhoea, N and V
ILD rare but severe

2
Q

Erlotinib

  • use
  • MOA
  • side effects main
A

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

3
Q

Crizotinib

  • use
  • MOA
  • side effects main
A

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
4
Q

Ceritinib

A

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

5
Q

Nivolumab

A

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

6
Q

Pertuzumab

A

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

7
Q

Trastuzumab

A

HER2 positive breast cancer

Also in HER2 positive stomach cancer!

8
Q

Lapatanib

A

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

9
Q

Exemastane

A

In ER/PR positive breast cancer use in metastatic disease once has progressed on nonsteroidal AI (like anastrozole or letrozole)

10
Q

Sunitinib

A

Multi-TKI
Renal clear cell first line
hypertension, hand foot syndrome, diarrhoea, haem tox, thyroid dysfunction

11
Q

Pazopanib

A

VEGF-i
Renal clear cell first line
hypertension, diarrhea, anorexia, LFT, hair colour

12
Q

Temsirolimus

A

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

13
Q

Axitinib

A

VEGF-i
Used in renal cell clear
second line preferred agent

14
Q

Dabrafenib

A

BRAF inhibitor in presence of V600E mutation in melanoma
50% response rate
fatigue, arthralgia, rash, SCC, hyperkeratosis, other non-BRAF melanomas.

15
Q

Trametinib

A

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.

16
Q

Difference between Dabrafenib and Vemurafenib?

A

acts against BRAF mutations in melanoma
For vemurafenib, has to be V600E
Dabrafenib any.

17
Q

When are mTOR inhibitors used in cancer

A

temsirolimus and everolimus in renal cell cancer

Also used in ER/PR + positive breast cancer that has become resistant to hormonal agents.

18
Q

Bevacizumab

A
VEGF inhibitor
Used in colon cancer metastatic
Hypertension, GI perforation
Impaired wound healing
Tumour associated haemorrhage
2 x increase arterial thromboembolic events.
19
Q

Cetuximab

A

Colorectal cancer in kRAS wild type patients
An EGFR inhibitor
Note histological over expression of EGFR often seen but does not correlate with effect
Get rash, which is good, and get Diarrhoea and hypomagnesaemia.

20
Q

Panitumumab

A

Ab against EGFR
Used in colorectal Ca with kras wild type
Rash, diarrhoea