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Mektovi Generic Name & Formulations
Legal Class
General Description
Pharmacological Class
How Supplied
Manufacturer
Generic Availability
Mechanism of Action
Binimetinib is a reversible inhibitor of mitogen-activated extracellular signal regulated kinase 1 (MEK1) and MEK2 activity. In vitro, binimetinib inhibited extracellular signal-related kinase (ERK) phosphorylation in cell-free assays as well as viability and MEK-dependent phosphorylation of BRAF-mutant human melanoma cell lines. Binimetinib also inhibited in vivo ERK phosphorylation and tumor growth in BRAF-mutant murine xenograft models.
Mektovi Indications
Indications
Mektovi Dosage and Administration
Adult
Confirm presence of a BRAF V600E or V600K mutation prior to initiation. 45mg twice daily (approx. 12hrs apart) with encorafenib until disease progression or unacceptable toxicity. Moderate or severe hepatic impairment: 30mg twice daily. Dose modifications for adverse reactions: see full labeling. Refer to encorafenib labeling for dosing. Discontinue if encorafenib is permanently discontinued.
Children
Mektovi Contraindications
Not Applicable
Mektovi Boxed Warnings
Not Applicable
Mektovi Warnings/Precautions
Warnings/Precautions
Monitor for new primary malignancies (cutaneous, noncutaneous). Cardiomyopathy: assess ejection fraction by echocardiogram or MUGA scan prior to initiating, 1 month after, and then every 2–3 months during treatment. Baseline ejection fraction <50% or below institutional LLN: not established. Cardiovascular risk factors; monitor closely. Venous thromboembolism (DVT & PE). Ocular toxicities (serious retinopathy, retinal vein occlusion [RVO], uveitis): assess for visual symptoms at each visit; perform ophthalmologic exams regularly and for new or worsening visual disturbances (esp. within 24hrs for RVO). Assess new or progressive unexplained pulmonary symptoms or for possible interstitial lung disease. Hepatotoxicity: monitor LFTs before initiation, monthly during treatment, and as clinically indicated. Rhabdomyolysis: monitor CPK and creatinine prior to initiating, periodically during, and as clinically indicated. Embryo-fetal toxicity. Advise females of reproductive potential to use effective contraception during and for ≥30 days after the last dose. Pregnancy: exclude status prior to initiation. Nursing mothers: not recommended (during and for 3 days after the last dose).
Mektovi Pharmacokinetics
Absorption
After oral administration, at least 50% of the dose was absorbed with a median time to maximum concentration of 1.6 hours.
Distribution
Mean apparent volume of distribution: 92 L. Plasma protein bound: 97%.
Elimination
Fecal (62%), fecal (31%). Half-life: 3.5 hours. Apparent clearance (CL/F): 20.2 L/h.
Mektovi Interactions
Not Applicable
Mektovi Adverse Reactions
Adverse Reactions
In combination with encorafenib: fatigue, nausea, diarrhea, vomiting, abdominal pain, musculoskeletal pain, visual impairment, constipation, dyspnea, rash, cough; hemorrhage.
Mektovi Clinical Trials
See Literature
Mektovi Note
Not Applicable
Mektovi Patient Counseling
See Literature
Mektovi Generic Name & Formulations
Legal Class
General Description
Pharmacological Class
How Supplied
Manufacturer
Generic Availability
Mechanism of Action
Binimetinib is a reversible inhibitor of mitogen-activated extracellular signal regulated kinase 1 (MEK1) and MEK2 activity. In vitro, binimetinib inhibited extracellular signal-related kinase (ERK) phosphorylation in cell-free assays as well as viability and MEK-dependent phosphorylation of BRAF-mutant human melanoma cell lines. Binimetinib also inhibited in vivo ERK phosphorylation and tumor growth in BRAF-mutant murine xenograft models.
Mektovi Indications
Indications
In combination with encorafenib for the treatment of metastatic non-small cell lung cancer (NSCLC) with a BRAF V600E mutation, as detected by an FDA-approved test.
Mektovi Dosage and Administration
Adult
Confirm presence of a BRAF V600E mutation prior to initiation. 45mg twice daily (approx. 12hrs apart) with encorafenib until disease progression or unacceptable toxicity. Moderate or severe hepatic impairment: 30mg twice daily. Dose modifications for adverse reactions: see full labeling. Refer to encorafenib labeling for dosing. Discontinue if encorafenib is permanently discontinued.
Children
Mektovi Contraindications
Not Applicable
Mektovi Boxed Warnings
Not Applicable
Mektovi Warnings/Precautions
Warnings/Precautions
Monitor for new primary malignancies (cutaneous, noncutaneous). Cardiomyopathy: assess ejection fraction by echocardiogram or MUGA scan prior to initiating, 1 month after, and then every 2–3 months during treatment. Baseline ejection fraction <50% or below institutional LLN: not established. Cardiovascular risk factors; monitor closely. Venous thromboembolism (DVT & PE). Ocular toxicities (serious retinopathy, retinal vein occlusion [RVO], uveitis): assess for visual symptoms at each visit; perform ophthalmologic exams regularly and for new or worsening visual disturbances (esp. within 24hrs for RVO). Assess new or progressive unexplained pulmonary symptoms or for possible interstitial lung disease. Hepatotoxicity: monitor LFTs before initiation, monthly during treatment, and as clinically indicated. Rhabdomyolysis: monitor CPK and creatinine prior to initiating, periodically during, and as clinically indicated. Embryo-fetal toxicity. Advise females of reproductive potential to use effective contraception during and for ≥30 days after the last dose. Pregnancy: exclude status prior to initiation. Nursing mothers: not recommended (during and for 3 days after the last dose).
Mektovi Pharmacokinetics
Absorption
After oral administration, at least 50% of the dose was absorbed with a median time to maximum concentration of 1.6 hours.
Distribution
Mean apparent volume of distribution: 92 L. Plasma protein bound: 97%.
Elimination
Fecal (62%), fecal (31%). Half-life: 3.5 hours. Apparent clearance (CL/F): 20.2 L/h.
Mektovi Interactions
Not Applicable
Mektovi Adverse Reactions
Adverse Reactions
In combination with encorafenib: fatigue, nausea, diarrhea, vomiting, abdominal pain, musculoskeletal pain, visual impairment, constipation, dyspnea, rash, cough; hemorrhage.
Mektovi Clinical Trials
See Literature
Mektovi Note
Not Applicable
Mektovi Patient Counseling
See Literature
