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Biological & Targeted Agents - Cancer Drug List for FRCR CO1 > ALK TKI inhbitors > Flashcards

ALK TKI inhbitors Flashcards

1
Q

What is the mechanism of action of Alectanib?

A
  • Highly selective ALK and RET TKI
  • Inhbits ALK phosphorylation
  • Inhbits downstream STAT and PI3K/AKT
  • Active against mutant forms of the ALK enzyme
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2
Q

What does ALK stand for?

A

Anaplastic Lymphoma Kinase

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3
Q

What is the Bioavailability of Alectanib?

A

37%

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4
Q

How long does it take for alectanib to reach max dose?

A

4-6 hours

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5
Q

How long does it take for Alectanib to reach steady state?

A

7 days

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6
Q

Effects with food

A

3x exposure after high fat/calorie food

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7
Q

What is the distribution of Alectanib? Does it cross the BBB?

A

99% plasma protein bound
Crosses BBB

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8
Q

How is Alectanib metabolised?

A

CYP3A4

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9
Q

How is Alectanib eliminated?

A

98% faeces

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10
Q

What is the indication for Alectanib?

A

NSCLC

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11
Q

What are the adverse effects of Alectanib?

A
  • Brady
  • Skin
  • Constipation
  • Oedema
  • Fatigue
  • Anaemia
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12
Q

What are the drug-drug interactions of Alectanib?

A
  • CYP2A5
  • Drugs that cause bradycardia
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13
Q

What is the mechanism of action of Crizotinib?

A

Inhbits ALK

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14
Q

What is the bioavailability of Crizotinib?

A

50%

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15
Q

When is peak plasma level of crizotinib reached?

A

4 hours

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16
Q

How long does it take Crizotonib to reach a steady state?

A

15 days

17
Q

How does food affect Crizotinib?

A

14% BA reduction with high fat meal

18
Q

How is Crizotonib distributed?

A

91% PPB
Extensive tissue

19
Q

How is Crizotinib eliminated?

A

65% Faeces
25% Urine

20
Q

What is the half life of Crizotinib?

A

2 days
(42 hours)

21
Q

What are the indications of Crizotinib?

A

NSCLC
- ALK positive
- ROS1 positive

22
Q

What are the adverse events of Crizotinib?

A
  • Bradycardia
  • Constipation, diarrhoea, abdo pain, loss of appetite, reflux, N&V
  • Fatigue
  • Oedema
  • Fever
  • LFTs
  • Myelosuppression
23
Q

What are the drug drug interactions of Crizotinib?

A

CYP3A4
Drugs that make stomach less acidic
Cardiac

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

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