Select therapeutic use:

Colorectal and other GI cancers:

Indications for BRAFTOVI:

In combination with cetuximab for the treatment of metastatic colorectal cancer (CRC) with a BRAF V600E mutation, as detected by an FDA-approved test, after prior therapy.

Limitations of Use:

Not for treatment of wild-type BRAF CRC.

Adult:

Confirm BRAF V600E mutation prior to initiation. 300mg once daily with cetuximab until disease progression or unacceptable toxicity. Discontinue Braftovi if cetuximab is discontinued. Dose modifications for adverse reactions, concomitant strong or moderate CYP3A4 inhibitors: see full labeling. Also, refer to cetuximab labeling for dosing.

Children:

Not established.

Warnings/Precautions:

Monitor for new primary malignancies (cutaneous, non-cutaneous). Perform dermatologic exams prior to initiating, every 2 months during, and up to 6 months following treatment discontinuation. Discontinue if RAS-mutation (+) non-cutaneous malignancies develop. Uveitis: assess for visual symptoms at each visit; perform ophthalmologic exams regularly and for new or worsening visual disturbances. Long QT syndromes, significant bradyarrhythmias, severe or uncontrolled heart failure, concomitant drugs associated with QT prolongation; monitor. Correct hypokalemia and hypomagnesemia prior to and during treatment. Withhold, reduce or permanently discontinue dose if QTc >500ms. Increased risk of certain adverse reactions with Braftovi monotherapy; reduce dose if binimetinib interrupted or discontinued; see full labeling. Moderate to severe hepatic or severe renal impairment. Embryo-fetal toxicity. Advise females of reproductive potential to use effective contraception (non-hormonal methods) during and for 2 weeks after final dose. Pregnancy: exclude status prior to initiation. Nursing mothers: not recommended (during and for 2 weeks after final dose).

Pharmacologic Class:

Kinase inhibitor.

Interactions:

Potentiated by strong or moderate CYP3A4 inhibitors (including grapefruit juice); avoid; reduce dose if unavoidable. Antagonized by strong or moderate CYP3A4 inducers; avoid. May antagonize hormonal contraceptives; avoid. May affect sensitive CYP3A4 substrates. Avoid concomitant drugs known to prolong QT/QTc interval.

Adverse Reactions:

Fatigue, nausea, abdominal pain, arthralgia; hemorrhage (discontinue if Grade 4 reaction reoccurs), potential male infertility. In combination with binimetinib: also vomiting. In combination wtih cetuximab: also diarrhea, dermatitis acneiform, decreased appetite, rash.

Metabolism:

CYP3A4 (primarily), CYP2C19, CYP2D6.

Elimination:

Fecal, renal. Half-life: 3.5 hours.

Generic Availability:

NO

How Supplied:

Caps 75mg—2x60, 2x90

Pricing for BRAFTOVI

2 bottles of capsules of 75mg carton (Qty: 1)
Appx. price $13333
GoodRx

Melanoma and other skin cancers:

Indications for BRAFTOVI:

In combination with binimetinib for the treatment of unresectable or metastatic melanoma with a BRAF V600E or V600K mutation, as detected by an FDA-approved test.

Limitations of Use:

Not for treatment of wild-type BRAF melanoma.

Adult:

Confirm BRAF V600E or V600K mutation prior to initiation. 450mg once daily with binimetinib until disease progression or unacceptable toxicity. Dose modifications for adverse reactions, concomitant strong or moderate CYP3A4 inhibitors: see full labeling. Also, refer to binimetinib labeling for dosing.

Children:

Not established.

Warnings/Precautions:

Monitor for new primary malignancies (cutaneous, non-cutaneous). Perform dermatologic exams prior to initiating, every 2 months during, and up to 6 months following treatment discontinuation. Discontinue if RAS-mutation (+) non-cutaneous malignancies develop. Uveitis: assess for visual symptoms at each visit; perform ophthalmologic exams regularly and for new or worsening visual disturbances. Long QT syndromes, significant bradyarrhythmias, severe or uncontrolled heart failure, concomitant drugs associated with QT prolongation; monitor. Correct hypokalemia and hypomagnesemia prior to and during treatment. Withhold, reduce or permanently discontinue dose if QTc >500ms. Increased risk of certain adverse reactions with Braftovi monotherapy; reduce dose if binimetinib interrupted or discontinued; see full labeling. Moderate to severe hepatic or severe renal impairment. Embryo-fetal toxicity. Advise females of reproductive potential to use effective contraception (non-hormonal methods) during and for 2 weeks after final dose. Pregnancy: exclude status prior to initiation. Nursing mothers: not recommended (during and for 2 weeks after final dose).

Pharmacologic Class:

Kinase inhibitor.

Interactions:

Potentiated by strong or moderate CYP3A4 inhibitors (including grapefruit juice); avoid; reduce dose if unavoidable. Antagonized by strong or moderate CYP3A4 inducers; avoid. May antagonize hormonal contraceptives; avoid. May affect sensitive CYP3A4 substrates. Avoid concomitant drugs known to prolong QT/QTc interval.

Adverse Reactions:

Fatigue, nausea, abdominal pain, arthralgia; hemorrhage (discontinue if Grade 4 reaction reoccurs), potential male infertility. In combination with binimetinib: also vomiting. In combination wtih cetuximab: also diarrhea, dermatitis acneiform, decreased appetite, rash.

Metabolism:

CYP3A4 (primarily), CYP2C19, CYP2D6.

Elimination:

Fecal, renal. Half-life: 3.5 hours.

Generic Availability:

NO

How Supplied:

Caps 75mg—2x60, 2x90

Pricing for BRAFTOVI

2 bottles of capsules of 75mg carton (Qty: 1)
Appx. price $13333
GoodRx