BIOLOGICS

Question 1

cetuximab

Answer 1

Cetuximab is a chimeric (mouse/human) Mab that
binds to and inhibits EGFR (HER1)

Question 2

trastuzumab

Answer 2

humanised Mab targeting HER2

Question 3

bevacizumab

Answer 3

binds to vascular endothelial growth
factor (VEGF-a) preventing it from binding to its
receptor

Question 4

moa of trastuzumab (inhibition of tumour proliferation)

Answer 4

Binding of Trastuzumab to HER2 prevents it dimerising
and signalling
* Stimulates HER2 receptor downregulation by promoting
its endocytosis and proteolysis limiting the signal for
further cell growth

Question 6

moa of trastuzumab (prevention of activation)

Answer 6

Prevents shedding of the extracellular portion of the receptor by inhibiting the action of
metalloproteinases

Question 7

types of her 1 receptor tki

Answer 7

gefitinib
afatinib
osimertinib

Question 8

gefitinib

Answer 8

1st generation reversible binding
to wildtype and mutated receptors

Question 9

afatinib

Answer 9

2nd generation irreversible binding
to wildtype and mutated receptors

Question 10

osimertinib

Answer 10

• 3rd generation irreversible
  binding to receptors with the resistance
  mutation T790M

Question 11

types of kinase inhibitors

Answer 11

vemurafenib
trametinib

Question 12

vemurafenib

Answer 12

B-RAF kinase inhibitor with selectivity for the
ATP binding site with the V600E mutation
(constitutively active) inhibiting the kinase
activity
* CYP1A2 inhibitor; CYP3A4 inducer

Question 13

trametinib

Answer 13

Reversible MEK1 and MEK2 kinase inhibitor
* Binds to S218 in the activation loop of the
enzyme preventing phosphorylation by RAF at
this residue

Question 14

what are types of cancer immunotherapy

Answer 14

rituximab
blimatumomab
ipilimumab
nivolumab
atezolizumab

Question 15

rituximab (chimeric)

Answer 15

Directed against CD20 expressed on B cells
* Recruits macrophages, natural killer cells, complement
proteins for cell destruction

Question 16

Ofatumumab (human)

Answer 16

Directed against CD20 expressed on B cells
* Recruits macrophages, natural killer cells, complement
proteins for cell destruction

Question 17

blinatumomab (human)

Answer 17

A bi-specific antibody composed of 2 variable regions which
recognise CD19 (B cell) and CD3 (CD8+ T cell )
* Tethers the cancerous B cells to cytotoxic T cells promoting
their destruction

Question 18

ipilimumab (human)

Answer 18

binds to CTLA-4.
* CTLA-4 is an inhibitory protein expressed on the surface of
activated T cells. It binds to C80/86 to downregulate T cell
function

Question 19

nivolumab (human)

Answer 19

binds to PD-1 preventing PD-1L binding
to it

Question 20

atezolizumab (humanised)

Answer 20

binds to PD-1L
* PD-1 limits the activation of immune cells. When PD-1L binds to
PD-1 it triggers prompt apoptosis of the T cell
* Checkpoint inhibitors act to increase the immune response.

Question 21

types of Poly ADP Ribose Polymerase (PARP)
Inhibitors

Answer 21

Poly ADP ribose polymerase (PARP) inhibitors e.g. Olaparib and Niraparib
* Inhibit repair of single strand breaks in DNA