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Chemotherapeutic Agents > Targeted Cancer therapies and immunotherapies > Flashcards

Targeted Cancer therapies and immunotherapies Flashcards

1
Q

What are the two elements of personalized medicine?

A

Targeted therapeutic
Companion diagnostic

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2
Q

What enzyme breaks down 5-FU?

A

Dihydropyrimidine dehydrogenase

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3
Q

What is Chronic Myeloid Leukaemia?

A

Myeloproliferative disorder characterized by clonal expansion of pleuripotent hematopoetic stem cells

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4
Q

What is CML’s MoA?

A

Proto-oncogene activation by chromosomal translocation
3’ ABL fused to 5’ BCR -> chimeric oncogene
Retains ABL protein kinase activity
BCR alters expression

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5
Q

What is a protein-kinase inhibitor?

A

Imatinib mesylate (Gleevac)
Tyrosine-kinase inhibitor of BCR-ABL

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6
Q

What is Imatinib MoA?

A

Binds close to ATP binding site (blocks ATP)
Locking it in closed conformation
Prevents substrate tyrosine phosphorylation and signalling

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7
Q

What is Imatinib’s clinical uses?

A

GIT stromal tumours

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8
Q

What are the side effects of Imatinib?

A

GIT disturbances
fatigue
Headaches
Rashes

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9
Q

What are mechanisms of resistance to Imatinib?

A

Reactivation of BCR-ABL kinase activity

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10
Q

What are 2 examples of cancer immunotherapies?

A

IFN-a2 - hairy cell leukemia then advanced melanoma
IL-2 - mRCC and advanced melanoma

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11
Q

How are tumours invisible to the immune system?

A

Do not have co-stimulatory molecules

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12
Q

What is the target on engineered tumours?

A

B7 co-stimulatory molecules

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13
Q

What is a key immunotherapy ICT mechanism?

A

Blocking CTLA-4 which activates TCR
Remobilizes T cells

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14
Q

What is an example of a CTLA-4 inhibitor?

A

Ipilimumab

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15
Q

What are adverse effects of ipilimumab?

A

Colitis
hepatitis
some autoimmune diseases
fatal heart attack

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16
Q

What is the MoA of Programmed death 1 (PD1)?

A

Induced on tumour cells by interferon gamma
Exhausts tumour fighting T cells

17
Q

What is a PD-1 inhibitor?

A

Nivolumab

18
Q

What is Nivolumab’s MoA?

A

When bound by PD-L1 and PD-L2 a T cell response is triggered
Unlocks T cell

19
Q

What is Nivolumab’s clinical uses?

A

Melanoma
Non-small-cell lung cancer
Renal cell carcinoma
cervical cancer

20
Q

What are 4 big problems with immunotherapies?

A

Varying response rates
Resistance
Cost
health Inequalities

21
Q

What is a key feature of a ‘cold’ tumour?

A

Not many immune cells present

22
Q

What is the result of combining immunotherapies?

A

Improve survival
Greater inhibitory effects

Chemotherapeutic Agents (14 decks)

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