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HSPH/Cancer > Molecular targeted Therapy > Flashcards

Molecular targeted Therapy Flashcards

1
Q

Alkylating agents

A

Cyclophosphamide
Melphalan
Chlorambucil

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2
Q

Antimetabolites

A

Methotrexate

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3
Q

Plant alkaloids

A

Taxanes

Vinca alkaloids

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4
Q

Hormones + antagonists

A

Anti-oestrogens

Anti-androgens

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5
Q

Targeted therapy

A

Monoclonal antibodies

Small TKIs

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6
Q

Breast cancer genetics

A

13-20% overexpress HER2

- HR2 Gene amplification

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7
Q

Breast cancer treatment

A

Trastuzumab

Lapantanib

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8
Q

Colorectal cancer genetics

A

35-50% overexpress EGFR
Polysomy or EGFR gene amplification + wild-type RAS only
Metastatic cancer in liver

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9
Q

Colorectal cancer

A

Combination of Cetuximab with Oxaliplatin-containing chemo

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10
Q

Lung cancer genetics

A

15% EGFR-positive- somatic mutations
some in TK domain
usually late diagnosis, poor prognosis

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11
Q

Lung cancer treatment

A

Afatinib (EGFR/HER2)
Erlotinib
Gefitinib
Bevacizumab

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12
Q

Melanoma genetics

A

> 50% with unresectable or metastatic melanoma have a mutation in the BRAF
20% patients don’t initially respond

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13
Q

Melanoma treatment

A

Vemurafenib
Dabrafenib
Trametinib

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14
Q

Antibody inhibitors of growth receptors

A

Bind to growth factor receptors and prevent growth signals

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15
Q

Antibody-drug conjugates

A

Antibody targets drug to tumour cells

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16
Q

TKI of growth receptors

A

Bind to growth receptors + prevent growth signals

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17
Q

Alemtuzumab (CLL)

A

Naked antibody

Activate immune system

18
Q

Pembrolizumab (melanoma)

A

Naked antibody

Target immune system checkpoints

19
Q

Herceptin (breast cancer)

A

Naked antibody

Inhibiting activity of antigen + prevent growth

20
Q

MOA monoclonal antibodies

A

Kill tumour directly
Kill tumour via an immune-mediated mechanism
Vascular or stromal ablation

21
Q

VEGF

A

Required for formation of nascent blood vessels
Protects endothelial cells from death via activation of PKC pathways + upregulation of anti-apoptotic proteins such as Bcl-2
Activity modified by TK receptors- VEGFR1 + VEGFR2
Most upregulated genes in cancer- survival of tumour cells

22
Q

Targetting VEGFR

A

Antibody target
Angiogenesis inhibited
Deprives tumours of nutrient-providing blood vessels

23
Q

TKI inhibitors targets

A

Inhibit intracellular TK enzymes to inhibit ATP binding
Target oncogene product
Inhibit signalling at key steps
Safer than chemo

24
Q

Side effects of targeted therapy

A 
Rash- EGFR
Hand foot syndrome- VEGF
High BP- VEGF
Slow wound healing/clotting- EGFR
Congestive HF- HER2
25
Q

-tinib

A

TKI

26
Q

-zomib

A

proteasome inhibitor

27
Q

-ciclib

A

cyclin-dependent kinase inhibitor

28
Q

-parib

A

poly ADP-ribose polymerase inhibitor

29
Q

EGFR Family TKRIs

Extracellular + Intracellular AAs

A

Extra- 630

Intra- 560

30
Q

target EGFR

A

Cetuximab

31
Q

target HER2

A

Trastuxumab

32
Q

target HER2/3

A

Pertuzumab

33
Q

target VEGFR

A

Bevacizumab

34
Q

Trastuzumab

A

Bind to domain IV on HER2

Suppresses ligand-independent HER2 signalling

35
Q

Pertuzumab

A

Binds to domain II on HER2

Supresses ligand-dependent HER2 signalling

36
Q

Fab in monoclonal antibody

A

selective monoclonal antibody targets tumour specific or tumour associated antigens

37
Q

Fc in monoclonal antibody

A

Has potent cytotoxic payload

38
Q

Tyrosine Kinases nomenclature

A

-tinib

39
Q

Mutations in TK domain of EGFR in lung cancer

A

exon 18,19,20,21

40
Q

Drug resistance

A

70% women don’t respond/resistant to trastuzumab

Most develop resistacne to TKI

41
Q

Trastuzamab

A

Cardiotoxicity

Decline in LV cardiac function

HSPH/Cancer (8 decks)

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