Encorafenib

What is Encorafenib?

• Encorafenib (Braftovi) is a kinase inhibitor used for the treatment of certain melanomas.

What are the uses of this medicine?

This medicine is used: in combination with a medicine called binimetinib to treat people with a type of skin cancer called melanoma:

• that has spread to other parts of the body or cannot be removed by surgery, and
• that has a certain type of abnormal "BRAF" gene

in combination with a medicine called cetuximab, for the treatment of adults with cancer of your colon or rectum (colorectal cancer):

• that has been previously treated, and
• that has spread to other parts of the body, and
• that has a certain type of abnormal "BRAF" gene

How does this medicine work?

• Encorafenib blocks certain proteins made by the mutated BRAF gene, which may help keep cancer cells from growing and may kill them. It is a type of kinase inhibitor and a type of targeted therapy.
• Encorafenib is a kinase inhibitor that targets BRAF V600E, as well as wild-type BRAF and CRAF in in vitro cell-free assays with IC50 values of 0.35, 0.47, and 0.3 nM, respectively.
• Mutations in the BRAF gene, such as BRAF V600E, can result in constitutively activated BRAF kinases that may stimulate tumor cell growth.
• Encorafenib was also able to bind to other kinases in vitro including JNK1, JNK2, JNK3, LIMK1, LIMK2, MEK4, and STK36 and reduce ligand binding to these kinases.

Who Should Not Use this medicine ?

• This medicine have no usage limittations.

What drug interactions can this medicine cause?

• Avoid coadministration of Braftovi with strong or moderate CYP3A4 inhibitors, including grapefruit juice. If coadministration is unavoidable, reduce the Braftovi dose.
• Avoid coadministration of Braftovi with strong or moderate CYP3A4 inducers.
• Avoid coadministration of Braftovi with hormonal contraceptives.
• Avoid coadministration of Braftovi with drugs known to prolong the QT/QTc interval.

Is this medicine FDA approved?

• It was approved for use in the United States in 2018.

How should this medicine be used?

Melanoma

• Confirm the presence of BRAF V600E or V600K mutation in tumor specimens prior to the initiation of Braftovi.

Mutation-Positive Metastatic Colorectal Cancer (CRC)

• Confirm the presence of BRAF V600E mutation in tumor specimens prior to the initiation of Braftovi

Recommended Dosage

Recommended Dosage for BRAF V600E or V600K Mutation-Positive Unresectable or Metastatic Melanomaː

• The recommended dosage of Braftovi is 450 mg (six 75 mg capsules) orally once daily in combination with binimetinib until disease progression or unacceptable toxicity.

Recommended Dosage for BRAF V600E Mutation-Positive Metastatic Colorectal Cancer (CRC)ː The recommended dosage of Braftovi is 300 mg (four 75 mg capsules) orally once daily in combination with cetuximab until disease progression or unacceptable toxicity.

Administration

• Take Braftovi exactly as your healthcare provider tells you. Do not change your dose or stop taking Braftovi unless your healthcare provider tells you to.
• Your healthcare provider may change your dose of Braftovi, temporarily stop, or completely stop your treatment with Braftovi if you develop certain side effects.
• For melanoma, take Braftovi in combination with binimetinib by mouth one time each day.
• For colorectal cancer, take Braftovi by mouth one time each day. You will also receive cetuximab through a vein in your arm (intravenously) given by your healthcare provider.
• Braftovi may be taken with or without food.
• Avoid grapefruit during treatment with Braftovi. Grapefruit products may increase the amount of Braftovi in your body.
• If you miss a dose of Braftovi, take it as soon as you remember. If it is within 12 hours of your next scheduled dose, take your next dose at your regular time. Do not make up for the missed dose.
• Do not take an extra dose if you vomit after taking your scheduled dose. Take your next dose at your regular time.
• If you stop treatment with binimetinib or cetuximab, talk to your healthcare provider about your Braftovi treatment. Your Braftovi dose may need to be changed or stopped.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Capsules: 75 mg

This medicine is available in fallowing brand namesː

• Braftovi

What side effects can this medication cause?

The most common side effects of this medicine include: The most common side effects of Braftovi when taken in combination with binimetinib, include:

• fatigue
• nausea
• vomiting
• abdominal pain
• pain or swelling of your joints (arthralgia)

The most common side effects of Braftovi when taken in combination with cetuximab, include:

• fatigue
• nausea
• diarrhea
• acne-like rash (dermatitis acneiform)
• abdominal pain
• decreased appetite
• pain or swelling of your joints (arthralgia)
• rash

Braftovi may cause serious side effects, including:

• Risk of new skin cancers
• Bleeding problems
• Eye problems
• Changes in the electrical activity of your heart called QT prolongation

What special precautions should I follow?

• New primary malignancies, cutaneous and non-cutaneous, have been observed in patients treated with BRAF inhibitors and can occur with Braftovi. Monitor for malignancies and perform dermatologic evaluations prior to, while on therapy, and following discontinuation of treatment.
• Increased cell proliferation can occur with BRAF inhibitors.
• Major hemorrhagic events can occur with Braftovi.
• Uveitis, including iritis and iridocyclitis, has been reported in patients treated with Braftovi in combination with binimetinib. Perform ophthalmologic evaluation at regular intervals and for any visual disturbances.
• Braftovi is associated with dose-dependent QTc interval prolongation in some patients.Monitor electrolytes before and during treatment. Correct electrolyte abnormalities and control for cardiac risk factors for QT prolongation. Withhold Braftovi for QTc of 500 ms or greater.
• Braftovi Can cause fetal harm. Advise females with reproductive potential of potential risk to the fetus and to use effective non-hormonal method of contraception.

What to do in case of emergency/overdose?

Management for overdosage:

• Since encorafenib is 86% bound to plasma proteins, hemodialysis is likely to be ineffective in the treatment of overdose with Braftovi.

Can this medicine be used in pregnancy?

• Based on its mechanism of action, Braftovi can cause fetal harm when administered to a pregnant woman .
• There are no available clinical data on the use of Braftovi during pregnancy.

Can this medicine be used in children?

• The safety and effectiveness of Braftovi have not been established in pediatric patients.

What are the active and inactive ingredients in this medicine?

• Active ingredient: encorafenib
• Inactive ingredients: copovidone, poloxamer 188, microcrystalline cellulose, succinic acid, crospovidone, colloidal silicon dioxide, and magnesium stearate of vegetable origin
• Capsule shell: gelatin, titanium dioxide, iron oxide red, iron oxide yellow, ferrosoferric oxide, monogramming ink (pharmaceutical glaze, ferrosoferric oxide, propylene glycol)

Who manufactures and distributes this medicine?

Distributed by: Array BioPharma Inc., a wholly owned subsidiary of Pfizer Inc. Boulder, Colorado 80301. Braftovi® is a registered trademark of Array BioPharma Inc. in the United States and various other countries.

What should I know about storage and disposal of this medication?

• Store Braftovi at room temperature between 68°F to 77°F (20°C to 25°C).
• Store Braftovi in the original bottle.
• Keep the Braftovi bottle tightly closed and protect it from moisture.
• Braftovi comes with a desiccant packet in the bottle to help protect your medicine from moisture. Do not remove the desiccant packet from the bottle.
• Keep Braftovi and all medicines out of the reach of children.

• Dailymed label info on Encorafenib
• FDA Encorafenib

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