EGFR Inhibitors Flashcards

1
Q

What drugs are in the EGFR Inhibitors class?

A

Drugs in this class are (not all inclusive):
- Gefitinib
- Erlotinib
- Osimertinib
- Afatinib

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2
Q

What is the brand name of Gefitinib?

A

The brand name of this generic drug is:
- Iressa

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3
Q

What is the brand name of Erlotinib?

A

The brand name of this generic drug is:
- Tarceva

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4
Q

What is the brand name of Osimertinib?

A

The brand name of this generic drug is:
- Tagrisso

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5
Q

What is the brand name of Afatinib?

A

The brand name of this generic drug is:
- Gilotrif

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6
Q

What is the generic of name of Iressa?

A

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

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7
Q

What is the generic of name of Tarceva?

A

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

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8
Q

What is the generic of name of Tagrisso?

A

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

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9
Q

What is the generic of name of Gilotrif?

A

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

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10
Q

What are the main indications for use of Gefitinib?

A

The main indications of this drug are:
- Non-Small Cell Lung Cancer with EGFR mutation

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11
Q

What are the main indications for use of Erlotinib?

A

The main indications of this drug are:
- Non-Small Cell Lung Cancer with EGFR mutation
- Pancreatic Cancer with EGFR mutation

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12
Q

What are the main indications for use of Osimertinib?

A

The main indications of this drug are:
- Non-Small Cell Lung Cancer with EGFR mutation, T790M EGFR-mutation positive, or brain/leptomeningeal metastases

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13
Q

What are the main indications for use of Afatinib?

A

The main indications of this drug are:
- Non-Small Cell Lung Cancer with EGFR mutation

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14
Q

What are the main/common indications of the EGFR Inhibitors class?

A

The main/common indications of this drug class are:
- Certain cancers (such as Non-Small Cell Lung Cancer) with EGFR mutation

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15
Q

What is the class and MOA of Gefitinib?

A

This drug in the following class:
- EGFR Inhibitors

This drug’s MOA is as follows:
- EGFR inhibitors are highly selective tyrosine kinase inhibitors that covalently bind to epidermal growth factor receptors and irreversibly inhibit tyrosine kinase phosphorylation and downregulate EGFR signaling preventing cell growth.

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16
Q

What is the class and MOA of Erlotinib?

A

This drug in the following class:
- EGFR Inhibitors

This drug’s MOA is as follows:
- EGFR inhibitors are highly selective tyrosine kinase inhibitors that covalently bind to epidermal growth factor receptors and irreversibly inhibit tyrosine kinase phosphorylation and downregulate EGFR signaling preventing cell growth.

17
Q

What is the class and MOA of Osimertinib?

A

This drug in the following class:
- EGFR Inhibitors

This drug’s MOA is as follows:
- EGFR inhibitors are highly selective tyrosine kinase inhibitors that covalently bind to epidermal growth factor receptors and irreversibly inhibit tyrosine kinase phosphorylation and downregulate EGFR signaling preventing cell growth.

18
Q

What is the class and MOA of Afatinib?

A

This drug in the following class:
- EGFR Inhibitors

This drug’s MOA is as follows:
- EGFR inhibitors are highly selective tyrosine kinase inhibitors that covalently bind to epidermal growth factor receptors and irreversibly inhibit tyrosine kinase phosphorylation and downregulate EGFR signaling preventing cell growth.

19
Q

What are the notable/common monitoring parameters for the EGFR Inhibitors class?

A

The notable/common monitoring parameters for this drug class are:
- Confirm EGFR mutation positive before beginning therapy

20
Q

Describe the emetic potential of the EGFR Inhibitors class.

A

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

21
Q

Describe the administration of Gefitinib.

A

The administration of this drug is described as follows:
- Oral

22
Q

Describe the administration of Erlotinib.

A

The administration of this drug is described as follows:
- Oral
- Absorption is ~60% on an empty stomach, increases to ~100% with food

23
Q

Describe the administration of Osimertinib.

A

The administration of this drug is described as follows:
- Oral

24
Q

Describe the administration of Afatinib.

A

The administration of this drug is described as follows:
- Oral
- Absorption is decreased with high-fat meals

25
Q

Describe the metabolism of EGFR Inhibitors.

A

The metabolism of this drug class is as follows:
- Primarily hepatic with the exception of Afatinib (minimal enzymatic metabolism)

26
Q

What are the notable/common ADRs of the EGFR Inhibitors class?

A

The notable/common ADRs of this drug class are:
- Acneiform Rash
- N/V/D
- Skin/nail changes
- Dry mouth
- Decreased appetite
- Hepatic dysfunction
- Disease flare (after discontinuation)

27
Q

Describe the strategy and rationale for management of Acneiform Rash caused by EGFR Inhibitors.

A

The strategy and rationale for management of this condition caused by this drug are:
- This is a common side effect of this class.
- EGFR is expressed in many different tissues, including epithelial tissue, skin, hair follicles, and the gastrointestinal tract.
- During treatment with EGFR inhibitors cutaneous adverse events occur in 65-90% of patients. This rash usually develops in the first 1-2 weeks, peaks at 3-4 weeks of therapy, and its intensity decreases after 2 weeks but can often persist over some months.
- Management:
- Mild Rash: patients may not require any form of intervention. Consider topical hydrocortisone cream or clindamycin gel.
- Moderate Rash: hydrocortisone cream or clindamycin gel plus doxycycline 100 mg oral twice daily or minocycline 100 mg oral twice daily.
- Studies have found that the development of a rash seems to be associated with an increased likelihood of tumor response and/or survival in NSCLC.

28
Q

What are the clinical pearls of the EGFR Inhibitors class?

A

The clinical pearls of this drug class are as follows:
- For patients with asymptomatic progression on a TKI, continuation of EGFR-TKI therapy can be considered
- For patients who have not received osimertinib, recommend testing for the T790M mutation at time of progression.
- If positive, osimertinib therapy is indicated.
- For patients with symptomatic progression on a TKI, options include:
- Continuing with an EGFR inhibitor
- Switching to osimertinib if T790M mutation positive
- Switching to systemic chemotherapy
- EGFR mutations are present in 10-15% of non-small cell lung cancers and typically occur more commonly in women, Asian ethnicities, and never-smokers.
- K-RAS and EGFR mutations are mutually exclusive. Meaning that if a patient has a K-RAS mutation, they will not respond to EGFR inhibitors.

29
Q

Describe resistance among EGFR Inhibitors?

A

Resistance to this drug class is as follows:
- The T790M mutation is the most common EGFR resistance mechanism (seen in 50-60% of patients) and can be present at diagnosis or develop during treatment.
- This mutation increases affinity of kinase to ATP and decreases affinity to erlotinib and gefitinib.
- Patients with the T790M mutation should be switched to osimertinib as is a third-generation EGFR-TKI that is selective for both EGFR-TKI-sensitizing and T790M resistance mutations.