3. Targeted therapy

Question 1

What is the problem with chemotherapy in cancer treatment?

Answer 1

Systemic nature of cytotoxicity
Is not selective for intrinsic anti-tumour factors
Anti-proliferative towards all cells rather than towards particular cancer cells
Host toxicity

Question 2

What is the problem with chemotherapy in cancer treatment?

Answer 2

Systemic nature of cytotoxicity
Is not selective for intrinsic anti-tumour factors
Anti-proliferative towards all cells rather than towards particular cancer cells
Host toxicity

Question 3

What is meant by ‘targeted cancer therapies’?

Answer 3

Drugs or other substances that block the growth and spread of cancer by interfering with specific molecules involved in tumour growth and progression

Question 4

What are the best type of targets in cancer therapies?

Answer 4

Those that are present mainly in cancer cells and only sparingly in normal cells - these parts of the normal cells then regenerate

Question 5

What are the two main types of targeted cancer therapies?

Answer 5

Monocloncal antibodies

Small molecules

Question 6

What are the majority of small molecules used in cancer therapies?

Answer 6

Tyrosine kinase inhibitors

Question 7

What effect do tyrosine kinase inhibitors have on cancer cells?

Answer 7

Inhibit signalling

Question 8

What is a SERM?

Answer 8

Selective oestrogen receptor modulator

Question 9

Name three common TKIs

Answer 9

Imatinib
Dasatinib
Nilotinib

Question 10

Name three common TKIs

Answer 10

Imatinib
Dasatinib
Nilotinib

Question 11

Name two SERMs

Answer 11

Tamoxifen

Toremifene

Question 12

What is an mAB?

Answer 12

Monoclonal antibody

Question 13

Why can mABs be used to treat cancer?

Answer 13

Specific, targetted treatment - delivery of anti-tumour agents - recognise and attach to specific agents produced by cells

Question 14

Give the structure of an antibody

Answer 14

Main heavy chain - the Fc portion
Then the diagonal lateral part is the light chains - Fab portion - at the end of the light chain is the antigen binding site

Question 15

Which region of the antibody is the most immune responsive?

Answer 15

Fc

Question 16

What is the ending of all the monoclonal antibody names?

Answer 16

-mab

Question 17

What is -umab?

Answer 17

Human (100%)

Question 18

What is -zumab?

Answer 18

Humanised (95%)

Question 19

What is -ximab?

Answer 19

Chimeric

Question 20

What is -omab?

Answer 20

Mouse

Question 21

What is -amba?

Answer 21

Rat

Question 22

What is -emab?

Answer 22

Hamster

Question 23

What is -imab?

Answer 23

Primate

Question 24

What is the most commonly up regulated antigen in cancer?

Answer 24

VEGF

Question 25

How can you block VEGF signalling?

Answer 25

Block the receptor
Inhibit tumour growth and metastasis
Deprive the tumour of nutrient-providing blood cells

Question 26

Why might you genetically engineer mABs?

Answer 26

To avoid the unwanted side effects

Question 27

What is B1?

Answer 27

A unique cell surface antigen of lymphoid malignancies of b-cell origin

Question 28

What is CD20?

Answer 28

Glycosylated phosphoprotein on the surface of B-cells suspected to act as a calcium channel
Is a target for therapeutic antibodies

Question 29

What are the two types of anti-CD20 antibodies and how do they differ?

Answer 29

Type 1 - prominent complement action and little/no direct cell death
Type 2 - no complement action and strong induction of direct cell death

Question 30

Why is Rituximab so significant?

Answer 30

This is the first therapeutic mAB - mouse-chimeric mAb and binds to CD20

Question 31

What is obinutuzumab?

Answer 31

-umab is human

Type II humanised CD20 antibody