Tyrosine Kinase Inhibitors Flashcards

1
Q

Imatinib

A
  1. First generation TKI
  2. Recommended initial dose = 400 mg once daily for CP-CML
  3. Recommended initial dose = 600 mg once daily for AP-CML and BP- CML
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Imatinib DDI w/ Antidepressants

A

Minor increase in exposure; Monitor QTc monitoring

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Imatinib DDI w/ Cardiovascular Meds

A

Increase in exposure; strongly consider alternative cardiac medication or TKI dose adjustment

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Imatinib DDI w/ Anti-infectives

A

Increase in exposure

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Imatinib Side Effects

A

~ fluid retention
~ GI upset
~ Muscle cramps
~ rash

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Nilotinib Dosing : newly diagnosed CP-CML

A

300 mg twice daily

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Nilotinib Dosing: resistant or intolerant CP-CML and AP-CML

A

400 mg twice daily

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Nilotinib Dosing: BP-CML

A

400 mg twice daily

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Nilotinib prolongs the…

A

QT interval
ECGs should be obtained at baseline, 7 days after initiation, and periodically thereafter, as well as following any dose adjustments

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Nilotinib DDI w/ PPIs

A

decrease in exposure

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Nilotinib DDI w/ H2RAs

A

decrease in exposure; AVOID; if absolutely necessary consider once daily H2RA greater than or equal to 2 hours after or greater than 10 hours before taking nilotinib

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Nilotinib DDI w/ Antacids

A

decrease in exposure if concomitant; use antacids at least 2 hours before or at least 2 hours after taking

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Nilotinib DDI w/ antidepressants

A

AVOID d/t cumulative QTc prolongation risk

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Nilotinib DDI w/ CV Medications

A

increase in exposure and arrhythmia risk; AVOID

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Nilotinib DDI w/ anti-infectives (azole antifungals, clarithromycin, telithromycin, ritonavir)

A

increase in exposure

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Nilotinib Dosing Considerations

A

avoid food 2 hours before and 1 hour after taking

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

Omacetaxine Dosing: Resistant or Intolerant CP- CML and AP-CML

A

Induction: 1.25 mg/m2 twice daily for 14 days of a 28 day cycle
Maintenance: 1.25 mg/m2 twice daily for 7 days of a 28 day cycle

18
Q

Omacetaxine Non Hematologic Toxicity

A

grade 3 or 4 hyperglycemia

19
Q

Ponatinib Dosing: CP -CML

A

45 mg once daily with a reduction to 15 mg once daily upon achievement of BCR::ABL1 less than 1%

20
Q

Ponatinib Adverse Reactions

A

~ arterial occlusive events and venous thromboembolic events
~ heart failure
~ hepatotoxicity
~ CV risk
~ skin rash
~ pancreatitis

21
Q

Ponatinib DDI w/ PPIs

A

minor decrease in exposure

22
Q

Ponatinib DDI w/ antidepressants

A

minor increase in exposure; monitor QTc monitoring

23
Q

Ponatinib DDI w/ CV Medications

A

increase in exposure

24
Q

Ponatinib DDI w/ anti-infectives (azole antifungals, clarithromycin, telithromycin, ritonavir)

A

increase in exposure

25
Q

Asciminib Dosing: CP- CML (previously treated with more than 2 TKIs)

A

80 mg once daily or 40 mg twice daily

26
Q

Asciminib Dosing: CP-CML with T315I mutation

A

200 mg twice daily

27
Q

Asciminib Administration Pearls

A

should be taken orally without food. Avoid food 2 hours before and 1 hour after taking

28
Q

Asciminib DDI w/ anti-infectives (azole antifungals, clarithromycin, telithromycin, ritonavir)

A

Increase in exposure

29
Q

Asciminib Drug Interactions

A

~ strong CYP3A4 inhibitors
~ CYP3A4 substrates
~ CYP2C9 substrates
~ P-glycoprotein substrates

30
Q

Dasatinib Dosing: CP-CML

A

100 mg once daily

31
Q

Dasatinib Dosing: AP-CML and BP-CML

A

140 mg once daily

32
Q

Dasatinib Rare but Serious Toxicity

A

Pulmonary arterial hypertension

33
Q

Dasatinib Adverse Events

A

fluid retention
pleural/pericardial effusion
GI upset
rash

34
Q

Dasatinib DDI w/ PPIs

A

decrease in exposure

35
Q

Dasatinib DDI w/ H2RAs

A

decrease in exposure; AVOID; if absolutely necessary consider once daily H2RA greater than 2 hours after taking

36
Q

Dasatinib DDI w/ antacids

A

decrease in exposure; use antacids at least 2 hours before or at least 2 hours after taking dasatinib

37
Q

Dasatinib DDI w/ antidepressants

A

minor increase in exposure; monitor QTc

38
Q

Dasatinib DDI w/ CV Medications

A

increase in exposure

39
Q

Dasatinib DDI w/ anti-infectives (azole antifungals, clarithromycin, telithromycin, ritonavir)

A

increase in exposure

40
Q

Dasatinib DDI w/ fluoroquinolones

A

QTc monitoring