MEKTOVI® Dosage and Administration

(binimetinib)

2 DOSAGE AND ADMINISTRATION

2.1 Patient Selection

BRAF V600E or V600K Mutation-Positive Unresectable or Metastatic Melanoma

Confirm the presence of a BRAF V600E or V600K mutation in tumor specimens prior to initiating MEKTOVI [see Clinical Studies (14)]. Information on FDA-approved tests for the detection of BRAF V600E and V600K mutations in melanoma is available at: http://www.fda.gov/CompanionDiagnostics.

BRAF V600E Mutation-Positive Metastatic Non-Small Cell Lung Cancer (NSCLC)

Confirm the presence of a BRAF V600E mutation in tumor or plasma specimens prior to initiating MEKTOVI [see Clinical Studies (14.2)]. If no mutation is detected in a plasma specimen, test tumor tissue. Information on FDA-approved tests for the detection of BRAF V600E mutations in NSCLC is available at: http://www.fda.gov/CompanionDiagnostics.

2.2 Recommended Dosage and Administration

The recommended dosage of MEKTOVI is 45 mg orally taken twice daily, approximately 12 hours apart, in combination with encorafenib until disease progression or unacceptable toxicity. Refer to the encorafenib prescribing information for recommended encorafenib dosing information.

MEKTOVI may be taken with or without food [see Clinical Pharmacology (12.3)]. Do not take a missed dose of MEKTOVI within 6 hours of the next dose of MEKTOVI.

Do not take an additional dose if vomiting occurs after MEKTOVI administration but continue with the next scheduled dose.

2.3 Dosage Modifications for Adverse Reactions

If encorafenib is permanently discontinued, discontinue MEKTOVI.

Dose reductions for adverse reactions associated with MEKTOVI are presented in Table 1.

Table 1: Recommended Dose Reductions for MEKTOVI for Adverse Reactions
ActionRecommended Dose

First Dose Reduction

30 mg orally twice daily

Subsequent Modification

Permanently discontinue if unable to tolerate MEKTOVI 30 mg orally twice daily

Dosage modifications for adverse reactions associated with MEKTOVI are presented in Table 2.

Table 2: Recommended Dosage Modifications for MEKTOVI for Adverse Reactions
Severity of Adverse Reaction*Dose Modification for MEKTOVI
*
National Cancer Institute Common Terminology Criteria for Adverse Events (NCI CTCAE) version 4.03.
†
Dose modification of MEKTOVI when administered with encorafenib is not recommended for the following adverse reactions: palmar- plantar erythrodysesthesia syndrome (PPES), non-cutaneous RAS mutation-positive malignancies, and QTc prolongation.

Cardiomyopathy [see Warnings and Precautions (5.2)]

•
Asymptomatic, absolute decrease in LVEF of greater than 10% from baseline that is also below lower limit of normal (LLN)

Withhold MEKTOVI for up to 4 weeks, evaluate LVEF every 2 weeks.
Resume MEKTOVI at a reduced dose if the following are present:

•
LVEF is at or above the lower limit of normal and
•
Absolute decrease from baseline is 10% or less and
•
Patient is asymptomatic.

If the LVEF does not recover within 4 weeks permanently discontinue MEKTOVI.

•
Symptomatic congestive heart failure or absolute decrease in LVEF of greater than 20% from baseline that is also below LLN

Permanently discontinue MEKTOVI.

Venous Thromboembolism [see Warnings and Precautions (5.3)]

•
Uncomplicated deep venous thrombosis (DVT) or pulmonary embolism (PE)

Withhold MEKTOVI.

•
If improves to Grade 0-1, resume at a reduced dose.
•
If no improvement, permanently discontinue MEKTOVI.
•
Life threatening PE

Permanently discontinue MEKTOVI.

Serous Retinopathy [see Warnings and Precautions (5.4)]

•
Symptomatic serous retinopathy/Retinal pigment epithelial detachments

Withhold MEKTOVI for up to 10 days.

•
If improves and becomes asymptomatic, resume at same dose.
•
If not improved, resume at a lower dose level or permanently discontinue MEKTOVI.

Retinal Vein Occlusion (RVO) [see Warnings and Precautions (5.4)]

•
Any Grade

Permanently discontinue MEKTOVI.

Uveitis [see Warnings and Precautions (5.4)]

•
Grade 1-3

If Grade 1 or 2 does not respond to specific ocular therapy, or for Grade 3 uveitis, withhold MEKTOVI for up to 6 weeks.

•
If improved, resume at same or reduced dose.
•
If not improved, permanently discontinue MEKTOVI.
•
Grade 4

Permanently discontinue MEKTOVI.

Interstitial Lung Disease [see Warnings and Precautions (5.5)]

•
Grade 2

Withhold MEKTOVI for up to 4 weeks.

•
If improved to Grade 0-1, resume at a reduced dose.
•
If not resolved within 4 weeks, permanently discontinue MEKTOVI.
•
Grade 3 or Grade 4

Permanently discontinue MEKTOVI.

Hepatotoxicity [see Warnings and Precautions (5.6)]

•
Grade 2 AST or ALT increased

Maintain MEKTOVI dose.

•
If no improvement within 2 weeks, withhold MEKTOVI until improved to Grade 0-1 or to pretreatment/baseline levels and then resume at the same dose.
•
Grade 3 or 4 AST or ALT increased

See Other Adverse Reactions.

Rhabdomyolysis or Creatine Phosphokinase (CPK) elevations [see Warnings and Precautions (5.7)]

•
Grade 4 asymptomatic CPK elevation or
•
Any Grade CPK elevation with symptoms or with renal impairment

Withhold MEKTOVI dose for up to 4 weeks.

•
If improved to Grade 0-1 resume at a reduced dose.
•
If not resolved within 4 weeks, permanently discontinue MEKTOVI.

Dermatologic [other than palmar plantar erythrodysesthesia syndrome (PPES)] [see Adverse Reactions (6.1)]

•
Grade 2

If no improvement within 2 weeks, withhold MEKTOVI until Grade 0-1. Resume at same dose if first occurrence or reduce dose if recurrent.

•
Grade 3

Withhold MEKTOVI until Grade 0-1. Resume at same dose if first occurrence or reduce dose if recurrent.

•
Grade 4

Permanently discontinue MEKTOVI.

Other Adverse Reactions (including Hemorrhage) [see Warnings and Precautions (5.8), Adverse Reactions (6.1)]†

•
Recurrent Grade 2 or
•
First occurrence of any Grade 3

Withhold MEKTOVI for up to 4 weeks.

•
If improves to Grade 0-1 or to pretreatment/baseline levels, resume at reduced dose.
•
If no improvement, permanently discontinue MEKTOVI.
•
First occurrence of any Grade 4

Permanently discontinue MEKTOVI, or
Withhold MEKTOVI for up to 4 weeks.

•
If improves to Grade 0-1 or to pretreatment/baseline levels, then resume at a reduced dose.
•
If no improvement, permanently discontinue MEKTOVI.
•
Recurrent Grade 3

Consider permanently discontinuing MEKTOVI.

•
Recurrent Grade 4

Permanently discontinue MEKTOVI.

Refer to the encorafenib prescribing information for dose modifications for adverse reactions associated with encorafenib.

2.4 Dosage Modifications for Moderate or Severe Hepatic Impairment

For patients with moderate (total bilirubin greater than 1.5 and less than or equal to 3 × ULN and any AST) or severe (total bilirubin levels greater than 3 × ULN and any AST) hepatic impairment, the recommended dosage is 30 mg orally taken twice daily [see Use in Specific Populations (8.6), Clinical Pharmacology (12.3)].

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Dosage and Administration

2 DOSAGE AND ADMINISTRATION

2.1 Patient Selection

BRAF V600E or V600K Mutation-Positive Unresectable or Metastatic Melanoma

Confirm the presence of a BRAF V600E or V600K mutation in tumor specimens prior to initiating MEKTOVI [see Clinical Studies (14)]. Information on FDA-approved tests for the detection of BRAF V600E and V600K mutations in melanoma is available at: http://www.fda.gov/CompanionDiagnostics.

BRAF V600E Mutation-Positive Metastatic Non-Small Cell Lung Cancer (NSCLC)

Confirm the presence of a BRAF V600E mutation in tumor or plasma specimens prior to initiating MEKTOVI [see Clinical Studies (14.2)]. If no mutation is detected in a plasma specimen, test tumor tissue. Information on FDA-approved tests for the detection of BRAF V600E mutations in NSCLC is available at: http://www.fda.gov/CompanionDiagnostics.

2.2 Recommended Dosage and Administration

The recommended dosage of MEKTOVI is 45 mg orally taken twice daily, approximately 12 hours apart, in combination with encorafenib until disease progression or unacceptable toxicity. Refer to the encorafenib prescribing information for recommended encorafenib dosing information.

MEKTOVI may be taken with or without food [see Clinical Pharmacology (12.3)]. Do not take a missed dose of MEKTOVI within 6 hours of the next dose of MEKTOVI.

Do not take an additional dose if vomiting occurs after MEKTOVI administration but continue with the next scheduled dose.

2.3 Dosage Modifications for Adverse Reactions

If encorafenib is permanently discontinued, discontinue MEKTOVI.

Dose reductions for adverse reactions associated with MEKTOVI are presented in Table 1.

Table 1: Recommended Dose Reductions for MEKTOVI for Adverse Reactions
ActionRecommended Dose

First Dose Reduction

30 mg orally twice daily

Subsequent Modification

Permanently discontinue if unable to tolerate MEKTOVI 30 mg orally twice daily

Dosage modifications for adverse reactions associated with MEKTOVI are presented in Table 2.

Table 2: Recommended Dosage Modifications for MEKTOVI for Adverse Reactions
Severity of Adverse Reaction*Dose Modification for MEKTOVI
*
National Cancer Institute Common Terminology Criteria for Adverse Events (NCI CTCAE) version 4.03.
†
Dose modification of MEKTOVI when administered with encorafenib is not recommended for the following adverse reactions: palmar- plantar erythrodysesthesia syndrome (PPES), non-cutaneous RAS mutation-positive malignancies, and QTc prolongation.

Cardiomyopathy [see Warnings and Precautions (5.2)]

•
Asymptomatic, absolute decrease in LVEF of greater than 10% from baseline that is also below lower limit of normal (LLN)

Withhold MEKTOVI for up to 4 weeks, evaluate LVEF every 2 weeks.
Resume MEKTOVI at a reduced dose if the following are present:

•
LVEF is at or above the lower limit of normal and
•
Absolute decrease from baseline is 10% or less and
•
Patient is asymptomatic.

If the LVEF does not recover within 4 weeks permanently discontinue MEKTOVI.

•
Symptomatic congestive heart failure or absolute decrease in LVEF of greater than 20% from baseline that is also below LLN

Permanently discontinue MEKTOVI.

Venous Thromboembolism [see Warnings and Precautions (5.3)]

•
Uncomplicated deep venous thrombosis (DVT) or pulmonary embolism (PE)

Withhold MEKTOVI.

•
If improves to Grade 0-1, resume at a reduced dose.
•
If no improvement, permanently discontinue MEKTOVI.
•
Life threatening PE

Permanently discontinue MEKTOVI.

Serous Retinopathy [see Warnings and Precautions (5.4)]

•
Symptomatic serous retinopathy/Retinal pigment epithelial detachments

Withhold MEKTOVI for up to 10 days.

•
If improves and becomes asymptomatic, resume at same dose.
•
If not improved, resume at a lower dose level or permanently discontinue MEKTOVI.

Retinal Vein Occlusion (RVO) [see Warnings and Precautions (5.4)]

•
Any Grade

Permanently discontinue MEKTOVI.

Uveitis [see Warnings and Precautions (5.4)]

•
Grade 1-3

If Grade 1 or 2 does not respond to specific ocular therapy, or for Grade 3 uveitis, withhold MEKTOVI for up to 6 weeks.

•
If improved, resume at same or reduced dose.
•
If not improved, permanently discontinue MEKTOVI.
•
Grade 4

Permanently discontinue MEKTOVI.

Interstitial Lung Disease [see Warnings and Precautions (5.5)]

•
Grade 2

Withhold MEKTOVI for up to 4 weeks.

•
If improved to Grade 0-1, resume at a reduced dose.
•
If not resolved within 4 weeks, permanently discontinue MEKTOVI.
•
Grade 3 or Grade 4

Permanently discontinue MEKTOVI.

Hepatotoxicity [see Warnings and Precautions (5.6)]

•
Grade 2 AST or ALT increased

Maintain MEKTOVI dose.

•
If no improvement within 2 weeks, withhold MEKTOVI until improved to Grade 0-1 or to pretreatment/baseline levels and then resume at the same dose.
•
Grade 3 or 4 AST or ALT increased

See Other Adverse Reactions.

Rhabdomyolysis or Creatine Phosphokinase (CPK) elevations [see Warnings and Precautions (5.7)]

•
Grade 4 asymptomatic CPK elevation or
•
Any Grade CPK elevation with symptoms or with renal impairment

Withhold MEKTOVI dose for up to 4 weeks.

•
If improved to Grade 0-1 resume at a reduced dose.
•
If not resolved within 4 weeks, permanently discontinue MEKTOVI.

Dermatologic [other than palmar plantar erythrodysesthesia syndrome (PPES)] [see Adverse Reactions (6.1)]

•
Grade 2

If no improvement within 2 weeks, withhold MEKTOVI until Grade 0-1. Resume at same dose if first occurrence or reduce dose if recurrent.

•
Grade 3

Withhold MEKTOVI until Grade 0-1. Resume at same dose if first occurrence or reduce dose if recurrent.

•
Grade 4

Permanently discontinue MEKTOVI.

Other Adverse Reactions (including Hemorrhage) [see Warnings and Precautions (5.8), Adverse Reactions (6.1)]†

•
Recurrent Grade 2 or
•
First occurrence of any Grade 3

Withhold MEKTOVI for up to 4 weeks.

•
If improves to Grade 0-1 or to pretreatment/baseline levels, resume at reduced dose.
•
If no improvement, permanently discontinue MEKTOVI.
•
First occurrence of any Grade 4

Permanently discontinue MEKTOVI, or
Withhold MEKTOVI for up to 4 weeks.

•
If improves to Grade 0-1 or to pretreatment/baseline levels, then resume at a reduced dose.
•
If no improvement, permanently discontinue MEKTOVI.
•
Recurrent Grade 3

Consider permanently discontinuing MEKTOVI.

•
Recurrent Grade 4

Permanently discontinue MEKTOVI.

Refer to the encorafenib prescribing information for dose modifications for adverse reactions associated with encorafenib.

2.4 Dosage Modifications for Moderate or Severe Hepatic Impairment

For patients with moderate (total bilirubin greater than 1.5 and less than or equal to 3 × ULN and any AST) or severe (total bilirubin levels greater than 3 × ULN and any AST) hepatic impairment, the recommended dosage is 30 mg orally taken twice daily [see Use in Specific Populations (8.6), Clinical Pharmacology (12.3)].
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