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Biological & Targeted Agents - Cancer Drug List for FRCR CO1 > ErbB TKI Inhbitiors > Flashcards

ErbB TKI Inhbitiors Flashcards

1
Q

What is the MoA of Afatinib?

A

Irreversibly inhbits ErbB family of TKIs
- EGFR
- HER2 and 4 (also some HER3 activity)

Downregulates ERbB signalling which reduces tumour cell proliferation and vascularisation

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2
Q

How long does it take Afatinib to reach peak levels?

A

2-5 hours

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3
Q

How long does it take Afatanib to reach steady state?

A

8 days

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4
Q

Is Afatinib affected by food?

A

Yes - 50% exposure reduction with food

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5
Q

What is the distribution of Afatinib?

A

Binds to albumin and haemoglobin
Accumulates in retina and skin

95% Plasma protein bound
Some BBB crossing

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6
Q

How is Afatinib metaboloised?

A

Michael addition reactions resulting in adducnt formation to proteins and molecules

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7
Q

How is Afatinib eliminated?

A

Faeces

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8
Q

What is the half-life of afatinib?

A

37 hours

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9
Q

What is the indication for Afatinib?

A

NSCLC

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10
Q

What are the adverse effects of Afatinib?

A
  • Dry skin
  • alopecia
  • Rash
  • Diarrhoea
  • N&V
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11
Q

What are the drug-drug interactions of Afatinib?

A

Careful of antivirals, verapamil, antibiotics

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12
Q

What is the mechanism og action of Erlotinib?

A

Inhibits EGFR

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13
Q

What is the Bioavailability of Erlotinib?

A

60%
Increased with smoking food

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14
Q

How long to reach peak plasma levels erlotinib?

A

4 hours

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15
Q

Steady state for erlotinib is reached

A

7 days

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16
Q

What is the distribution of Erlotinin? (PPB and BBB)

A

95% PPB
BBB yes

17
Q

How is Erlotinib metabolised?

A

CYP3A4

18
Q

How is Erlotibin excreted?

A

Faeces

19
Q

What are the indictions for Erlotinib?

A

NSCLC - EGFR

20
Q

What are the adverse effects of Erlotinib?

A
  • Rash
  • Anorexia
  • Diarrhoea
  • Fatigue
  • N&V
21
Q

What drug drug interactions for erlotinib?

A

CYP3A4
Warfarin
Anti-acids
Statins
Cigarettes

22
Q

What is the mechanism of action of osimertinib?

A

Irreversible injbitor of EGFR

23
Q

What is the bioavailability of osimertinib?

A

70%

24
Q

What is the time to reach steady state of osimertinib?

A

15 days

25
Q

How long does it take for osimertinib to reach peak plasma levels?

A

6 hours

26
Q

What is the plasma protein binding of osimertinib?

A

95%

27
Q

How is osimertinib metabolised?

A

CYP3A4 and 3A5

28
Q

How is osimertinib excreted?

A

Faeces

29
Q

What is the half life of osimertinib?

A

44 hours

30
Q

What is the indication for osimertinib?

A

NSCLC

31
Q

What are the adverse effetcs of osimertinib?

A
  • Dry skin
  • Prolonged QT
  • Nails and rash
  • Diarrhoea
  • mucositis
32
Q

What is the mechanism of action of cetuximab?

A

Binds to EGFR to prevent EGF binding

33
Q

What tumours won’t respond to cetuximab?

A

KRAS mutations

34
Q

What is the half life of cetuximab?

A

120 hours

35
Q

What are the indications for cetuximab?

A
  • Colorectal
  • Head and neck cancer
36
Q

What are the adverse effects of cetuximab?

A
  • Rash
  • Constipation
  • Anorexia
  • Mg
  • Neuropathy
  • Cough, SOB

Biological & Targeted Agents - Cancer Drug List for FRCR CO1 (3 decks)

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