BRAF Inhibitors Flashcards
What drugs are in the BRAF Inhibitors class?
Drugs in this class are:
- Dabrafenib
- Vemurafenib
- Encorafenib
What is the brand name of Dabrafenib?
The brand name of this generic drug is:
- Tafinlar
What is the brand name of Vemurafenib?
The brand name of this generic drug is:
- Zelboraf
What is the brand name of Encorafenib?
The brand name of this generic drug is:
- Braftovi
What is the generic of name of Tafinlar?
The generic name of this brand name drug is:
- Dabrafenib
What is the generic of name of Zelboraf?
The generic name of this brand name drug is:
- Vemurafenib
What is the generic of name of Braftovi?
The generic name of this brand name drug is:
- Encorafenib
What are the main indications for use of Dabrafenib?
The main indications of this drug are:
- Melanoma (with BRAFV6ooE or BRAFV6ooK mutation)
- Non-small cell lung cancer (with BRAF V6ooE mutation)
- Thyroid cancer (with BRAF V6ooE mutation)
What are the main indications for use of Vemurafenib?
The main indications of this drug are:
- Melanoma (with BRAFV6ooE or BRAFV6ooK mutation)
- Non-small cell lung cancer (with BRAF V6ooE mutation)
- Erdheim-Chester disease (with BRAF V6oo mutation)
What are the main indications for use of Encorafenib?
The main indications of this drug are:
- Melanoma (with BRAFV6ooE or BRAFV6ooK mutation)
- Colorectal cancer (with BRAF V6ooE mutation)
What is the class and MOA of Dabrafenib?
This drug in the following class:
- BRAF Inhibitors
This drug’s MOA is as follows:
- Selectively targets mutated forms BRAF kinase (V600-) and interferes with the mitogen-activated protein kinase (MAPK) signaling pathway that regulates the proliferation and survival of melanoma cells.
What is the class and MOA of Vemurafenib?
This drug in the following class:
- BRAF Inhibitors
This drug’s MOA is as follows:
- Selectively targets mutated forms BRAF kinase (V600-) and interferes with the mitogen-activated protein kinase (MAPK) signaling pathway that regulates the proliferation and survival of melanoma cells.
What is the class and MOA of Encorafenib?
This drug in the following class:
- BRAF Inhibitors
This drug’s MOA is as follows:
- Selectively targets mutated forms BRAF kinase (V600-) and interferes with the mitogen-activated protein kinase (MAPK) signaling pathway that regulates the proliferation and survival of melanoma cells.
What are the notable monitoring parameters for Vemurafenib?
The notable monitoring parameters for this drug are:
- See common parameters for class
- EKG at baseline. 15 days after initiation. then monthly for 3 months. then every 3 months thereafter (more frequently if clinically appropriate) and with dosage adjustments.
What are the notable/common monitoring parameters for the BRAF Inhibitors class?
The notable/common monitoring parameters for this drug class are:
- BRAFV6ooK or V6ooE mutation status prior to treatment
- Dermatologic evaluations prior to initiation, every 2 months during therapy, and for up to 6 months following discontinuation to assess for new cutaneous malignancies
What is the emetic potential of Dabrafenib?
The emetic potential of this drug is:
- Moderate - High
What is the emetic potential of Vemurafenib?
The emetic potential of this drug is:
- Minimal - Low
What is the emetic potential of Encorafenib?
The emetic potential of this drug is:
- Moderate - High
Describe the emetic potential of the BRAF Inhibitors class.
The emetic potential of this drug class is:
- All moderate-high except for Vemurafenib (minimal-low)
What drugs in the BRAF Inhibitors class have a moderate-high emetic potential?
Drugs in the class with a moderate-high emetic potential are:
- Dabrafenib
- Encorafenib
What drugs in the BRAF Inhibitors class have a minimal-low emetic potential?
Drugs in the class with a minimal-low emetic potential are:
- Vemurafenib
Describe the administration of Dabrafenib.
The administration of this drug is described as follows:
- Oral: Absorption decreased with a high fat meal (-1,000 calories: 58 to 75 grams of fat)
Describe the administration of Vemurafenib.
The administration of this drug is described as follows:
- Oral
Describe the administration of Encorafenib.
The administration of this drug is described as follows:
- Oral
Describe the metabolism of Dabrafenib.
The metabolism of this drug is as follows:
- Patients with moderate (bilirubin >1,5 to 3 times ULN and any AST) or severe (bilirubin >3 to 10 times ULN and any AST) hepatic impairment may have increased exposure to this drug
What are the notable ADRs of Vemurafenib?
The notable ADRs of this drug are:
- Secondary skin cancers
- QT prolongation
What are the notable/common ADRs of the BRAF Inhibitors class?
The notable/common ADRs of this drug class are:
- Secondary skin cancers
- QT prolongation with Vemurafenib
Describe the strategy and rationale for management of secondary skin cancers caused by BRAF inhibitors.
The strategy and rationale for management of this condition caused by this drug class are:
- Secondary cutaneous squamous cell cancers and keratoacanthomas are the result of compensatory RAF signaling seen with BRAF inhibition.
- The risk of these additional cancers is decreased with the addition of a MEK inhibitor.
- These cancers are typically localized and easily treated with surgical excision or topical fluorouracil cream.
- Regular skin assessments should be done throughout therapy with BRAF inhibitors.
Describe the half-life of Encorafenib.
The half-life of this drug is described as follows:
- This drug has a longer dissociation half-life than other BRAF inhibitors, allowing for sustained inhibition of BRAF (and thus tumor growth)
What are the clinical pearls of the BRAF Inhibitors class?
The clinical pearls of this drug class are as follows:
- Though the BRAF inhibitors were initially evaluated as single agents, combination therapy with a MEK inhibitor (ex: Trametinib) is now the recommended treatment regimen.
Describe the therapy selection process for BRAF Inhibitors?
The therapy selection process for this drug class is as follows:
- All metastatic tumors should be evaluated for the V6oo mutation.
- In V6ooE or V6ooK mutated tumors, the initial selection between BRAF inhibitors and immunotherapy is commonly done based on the aggressive nature of the tumor.
- Rapidly growing tumors that are symptomatic are treated with BRAF-directed therapy because it generates a higher rate of response that occurs quicker, while asymptomatic or more indolent tumors may be treated with immunotherapy.
Describe resistance among BRAF Inhibitors?
Resistance to this drug class is as follows:
- Though the BRAF inhibitors were initially evaluated as single agents, combination therapy with a MEK inhibitor (example: Trametinib) is now the recommended treatment regimen.
- This is due to the development of resistance to the single agent BRAF inhibitors after 6-7 months
- Combination therapy with both BRAF and MEK inhibitors may suppress the downstream resistance mechanism
Describe the symptoms of melanoma.
Symptoms of this condition are:
- ABCDE: asymmetry, border, color, diameter, and evolving
- A: Asymmetry - melanomas are often asymmetrical
- B: Border - melanomas often have an irregular border
- C: Color - melanomas often have more than one color or shade in the mole
- D: Diameter: melanomas are often larger than 6mm, or the size of a pencil eraser
- E: Evolving: melanomas tend to change over time while benign moles do not
