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Tyler's Cards > BCR-ABL TKIs > Flashcards

BCR-ABL TKIs Flashcards

1
Q

What drugs are in the BCR-ABL TKIs class?

A

Drugs in this class are:
- Bosutinib
- Dasatinib
- lmatinib
- Nilotinib
- Ponatinib
- Asciminib

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2
Q

What is the brand name of Bosutinib?

A

The brand name of this generic drug is:
- Bosulif

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3
Q

What is the brand name of Dasatinib?

A

The brand name of this generic drug is:
- Sprycel

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4
Q

What is the brand name of lmatinib?

A

The brand name of this generic drug is:
- Gleevec

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5
Q

What is the brand name of Nilotinib?

A

The brand name of this generic drug is:
- Tasigna

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6
Q

What is the brand name of Ponatinib?

A

The brand name of this generic drug is:
- Iclusig

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7
Q

What is the brand name of Asciminib?

A

The brand name of this generic drug is:
- Scemblix

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8
Q

What is the generic of name of Bosulif?

A

The generic name of this brand name drug is:
- Bosutinib

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9
Q

What is the generic of name of Sprycel?

A

The generic name of this brand name drug is:
- Dasatinib

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10
Q

What is the generic of name of Gleevec?

A

The generic name of this brand name drug is:
- lmatinib

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11
Q

What is the generic of name of Tasigna?

A

The generic name of this brand name drug is:
- Nilotinib

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12
Q

What is the generic of name of Iclusig?

A

The generic name of this brand name drug is:
- Ponatinib

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13
Q

What is the generic of name of Scemblix?

A

The generic name of this brand name drug is:
- Asciminib

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14
Q

What are the main indications for use of Bosutinib?

A

The main indications of this drug are:
- Chronic Myeloid Leukemia

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15
Q

What are the main indications for use of Dasatinib?

A

The main indications of this drug are:
- Chronic Myeloid Leukemia
- Acute lymphoblastic Leukemia
- Gastrointestinal stromal tumors

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16
Q

What are the main indications for use of lmatinib?

A

The main indications of this drug are:
- Chronic Myeloid Leukemia
- Acute lymphoblastic Leukemia
- Gastrointestinal stromal tumors

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17
Q

What are the main indications for use of Nilotinib?

A

The main indications of this drug are:
- Chronic Myeloid Leukemia
- Acute lymphoblastic Leukemia
- Gastrointestinal stromal tumors

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18
Q

What are the main indications for use of Ponatinib?

A

The main indications of this drug are:
- Chronic Myeloid Leukemia
- Acute lymphoblastic Leukemia

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19
Q

What are the main indications for use of Asciminib?

A

The main indications of this drug are:
- Chronic Myeloid Leukemia

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20
Q

What are the main/common indications of the BCR-ABL TKIs class?

A

The main/common indications of this drug class are:
- Chronic Myeloid Leukemia
- Acute lymphoblastic Leukemia
- Gastrointestinal stromal tumors

21
Q

What is the class and MOA of Bosutinib?

A

This drug in the following class:
- BCR-ABL TKIs

This drug’s MOA is as follows:
- Inhibits BCR-ABL tyrosine kinase - the abnormal gene product of the Philadelphia chromosome in chronic myeloid leukemia

22
Q

What is the class and MOA of Dasatinib?

A

This drug in the following class:
- BCR-ABL TKIs

This drug’s MOA is as follows:
- Inhibits BCR-ABL tyrosine kinase - the abnormal gene product of the Philadelphia chromosome in chronic myeloid leukemia

23
Q

What is the class and MOA of lmatinib?

A

This drug in the following class:
- BCR-ABL TKIs

This drug’s MOA is as follows:
- Inhibits BCR-ABL tyrosine kinase - the abnormal gene product of the Philadelphia chromosome in chronic myeloid leukemia

24
Q

What is the class and MOA of Nilotinib?

A

This drug in the following class:
- BCR-ABL TKIs

This drug’s MOA is as follows:
- Inhibits BCR-ABL tyrosine kinase - the abnormal gene product of the Philadelphia chromosome in chronic myeloid leukemia

25
Q

What is the class and MOA of Ponatinib?

A

This drug in the following class:
- BCR-ABL TKIs

This drug’s MOA is as follows:
- Inhibits BCR-ABL tyrosine kinase - the abnormal gene product of the Philadelphia chromosome in chronic myeloid leukemia

26
Q

What is the class and MOA of Asciminib?

A

This drug in the following class:
- BCR-ABL TKIs

This drug’s MOA is as follows:
- Inhibits BCR-ABL tyrosine kinase - the abnormal gene product of the Philadelphia chromosome in chronic myeloid leukemia
- This drug is a novel first in class STAMP (Specifically Targeting the ASL Myristoyl Pocket) inhibitor. This drug potently inhibits ABL1 kinase activity of the BCR-ABL1 fusion protein via allosteric binding to the ASL myristoyl pocket.

27
Q

What are the notable/common monitoring parameters for the BCR-ABL TKIs class?

A

The notable/common monitoring parameters for this drug class are:
- CBC weekly for first month, biweekly for the second month, then periodically thereafter
- Liver function tests (at baseline and monthly)
- In patients who discontinue therapy after a sustained molecular response, monitor BCR-ABL transcript levels and CBC with differential monthly for 1 year, then every 6 weeks for the second year, and every 12 weeks thereafter

28
Q

What is the emetic potential of Bosutinib?

A

The emetic potential of this drug is:
- Minimal-Low if <400 mg/day
- Moderate-High if >400 mg/day

29
Q

What is the emetic potential of Dasatinib?

A

The emetic potential of this drug is:
- Minimal-Low

30
Q

What is the emetic potential of lmatinib?

A

The emetic potential of this drug is:
- Minimal-Low if <400 mg/day
- Moderate-High if >400 mg/day

31
Q

What is the emetic potential of Nilotinib?

A

The emetic potential of this drug is:
- Minimal-Low

32
Q

What is the emetic potential of Ponatinib?

A

The emetic potential of this drug is:
- Minimal-Low

33
Q

What is the emetic potential of Asciminib?

A

The emetic potential of this drug is:
- Minimal-Low

34
Q

Describe the emetic potential of the BCR-ABL TKIs class.

A

The emetic potential of this drug class is:
- Most are Minimal-Low
- Bosutinib and Imatinib are Moderate-High if >400 mg/day

35
Q

What drugs in the BCR-ABL TKIs class have a moderate-high emetic potential?

A

Drugs in the class with a moderate-high emetic potential are:
- Bosutinib and Imatinib if >400 mg/day

36
Q

What drugs in the BCR-ABL TKIs class have a minimal-low emetic potential?

A

Drugs in the class with a low emetic potential are:
- All of them except if >400 mg/day for Bosutinib and Imatinib (Moderate-High)

37
Q

Describe the administration of Bosutinib.

A

The administration of this drug is described as follows:
- Once Daily

38
Q

Describe the administration of Dasatinib.

A

The administration of this drug is described as follows:
- Once Daily

39
Q

Describe the administration of lmatinib.

A

The administration of this drug is described as follows:
- Usually Once Daily - select regimens are Twice Daily

40
Q

Describe the administration of Nilotinib.

A

The administration of this drug is described as follows:
- Twice Daily (may influence adherence)

41
Q

Describe the administration of Ponatinib.

A

The administration of this drug is described as follows:
- Once Daily

42
Q

Describe the administration of Asciminib.

A

The administration of this drug is described as follows:
- Usually Once Daily - select regimens are Twice Daily

43
Q

Describe the general techniques for administration of the BCR-ABL TKIs class.

A

The general techniques for administration of this drug class is described as follows:
- All are once daily except for Nilotinib and select regimens of Imatinib and Asciminib (twice daily)

44
Q

What are the notable/common ADRs of the BCR-ABL TKIs class?

A

The notable/common ADRs of this drug class are:
- Edema
- Thrombocytopenia
- Neutropenia
- Bleeding

45
Q

What are the clinical pearls of the BCR-ABL TKIs class?

A

The clinical pearls of this drug class are as follows:
- Food and/or medications may enhance or decrease absorption
- Neither dasatinib, nilotinib or bosutinib have shown improved overall survival or progression free survival rates compared to imatinib, so choice of first-line therapy should be individualized.
- The following should be considered when choosing an agent:
- toxicity profile
- patient’s age and ability to tolerate therapy
- adherence/ease of administration
- comorbid conditions
- drug interactions
- cost
- feasibility of treatment discontinuation
- In patients with disease progression, the selection of an alternative agent in this class is based on prior therapy, concurrent disease states, and/or mutational testing.

46
Q

Describe considerations for discontinuation of BCR-ABL TKIs.

A

Considerations for discontinuation of agents in this class are as follows:
- The management of CML as a chronic disease requires long-term therapy which can cause both adverse effects and a financial burden.
- Discontinuation of TKI may be feasible in selected patients and with careful monitoring.
- Discontinuation of TKI therapy may be considered only in patients who met all of the following criteria:
- Chronic phase -CML with no history of accelerated phase or blast crisis
- Have been on TKI therapy for at least 3 years with no history of resistance
- Had stable molecular response for >2 years on at least 4 tests performed at least 3 months apart
- Patients who do quality for TKI discontinuation must have monthly molecular monitoring for the first year following discontinuation, then every 6 weeks during the second year, and quarterly thereafter if still in a major molecular response.
- If a patient loses their molecular response, they must have prompt resumption of therapy within 4 weeks.

47
Q

Describe considerations for resistance to BCR-ABL TKIs.

A

Considerations for resistence to agents in this class are as follows:
- Point mutations in the ABL kinase domain are the most frequent mechanism of secondary resistance to these drugs.
- Among mutations in the ABL domain, the presence of the T315i mutation is the most common and displays resistance to all currently available agents except ponatinib and asciminib.
- T315i mutation is also associated with disease progression and poorer survival.
- Asciminib binds allosterically to the ABL pocket and is less susceptible to mutations that drive resistance. It has demonstrated activity against wild-type BCR-ABL1 and several mutant forms (including T315i), even showing activity in heavily pretreated patients.
- Consider performing BCR-ABL kinase domain mutational analysis in patients who fail to achieve the response milestones, patients with any loss of response, or patients who experience disease progression to accelerated phase-CML or blast crisis-CML.

48
Q

Describe considerations for interactions with BCR-ABL TKIs.

A

Considerations for interactions with agents in this class are as follows:
- Dasatinib, Bosutinib, and Ponatinib require an acidic environment for absorption.
- Avoid the use of proton pump inhibitors and separate H2-antagonists by at least two hours.

49
Q

Describe considerations for CNS penetration of BCR-ABL TKIs.

A

Considerations for CNS penetration of agents in this class are as follows:
- Of the available agents, dasatinib crosses blood-brain barrier to the greatest extent.

Tyler's Cards (37 decks)

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