Brand Name
Mektovi
Generic Name
Binimetinib
View Brand Information FDA approval date: January 30, 2017
Form: Tablet
What is Mektovi (Binimetinib)?
MEKTOVI is a kinase inhibitor indicated: in combination with encorafenib, for the treatment of patients with unresectable or metastatic melanoma with a BRAF V600E or V600K mutation, as detected by an FDA-approved test.
Approved To Treat
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Brand Information
MEKTOVI (BINIMETINIB)
1DOSAGE FORMS AND STRENGTHS
Tablets: 15 mg, yellow/dark yellow, unscored biconvex oval film-coated tablets debossed with a stylized "A" on one side and "15" on the other side.
2CONTRAINDICATIONS
None.
3ADVERSE REACTIONS
The following adverse reactions are described elsewhere in the labeling:
- New Primary Malignancies
- Cardiomyopathy
- Venous Thromboembolism
- Ocular Toxicities
- Interstitial Lung Disease
- Hepatotoxicity
- Rhabdomyolysis
- Hemorrhage
- Embryo-Fetal Toxicity
- Risks Associated with Combination Treatment
3.1Clinical Trials Experience
Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.
The data described in WARNINGS AND PRECAUTIONS reflect exposure of 192 patients with
The pooled safety population described in the WARNINGS AND PRECAUTIONS also reflect exposure of 98 patients with
BRAF V600E or V600K Mutation-Positive Unresectable or Metastatic Melanoma
The data described below reflect exposure of 192 patients with
The COLUMBUS trial
The most common (≥25%) adverse reactions in patients receiving MEKTOVI in combination with encorafenib were fatigue, nausea, diarrhea, vomiting, and abdominal pain.
Adverse reactions leading to dose interruptions of MEKTOVI occurred in 33% of patients receiving MEKTOVI in combination with encorafenib; the most common were left ventricular dysfunction (6%) and serous retinopathy (5%). Adverse reactions leading to dose reductions of MEKTOVI occurred in 19% of patients receiving MEKTOVI in combination with encorafenib; the most common were left ventricular dysfunction (3%), serous retinopathy (3%), and colitis (2%). Five percent (5%) of patients receiving MEKTOVI in combination with encorafenib experienced an adverse reaction that resulted in permanent discontinuation of MEKTOVI. The most common adverse reactions resulting in permanent discontinuation of MEKTOVI were hemorrhage in 2% and headache in 1% of patients.
Table 3 and Table 4 present adverse drug reactions and laboratory abnormalities, respectively, identified in COLUMBUS. The COLUMBUS trial was not designed to demonstrate a statistically significant difference in adverse reaction rates for MEKTOVI in combination with encorafenib, as compared to vemurafenib, for any specific adverse reaction listed in Table 3.
Other clinically important adverse reactions occurring in <10% of patients who received MEKTOVI in combination with encorafenib were:
Gastrointestinal disorders:
Skin and subcutaneous tissue disorders:
Immune system disorders:
BRAF V600E Mutation-Positive Metastatic Non-Small Cell Lung Cancer (NSCLC)
The safety of MEKTOVI in combination with encorafenib is described in 98 patients with
The PHAROS trial
The most common (≥25%) adverse reactions in patients receiving MEKTOVI were fatigue, nausea, diarrhea, musculoskeletal pain, vomiting, abdominal pain, visual impairment, constipation, dyspnea, rash, and cough.
Adverse reactions leading to dose interruptions of MEKTOVI occurred in 62% of patients receiving MEKTOVI; the most common (≥5%) were diarrhea (17%); nausea (15%); fatigue (9%); AST increased (7%); ALT increased, anemia, musculoskeletal pain, vomiting (6% each); and acute kidney injury, hemorrhage, and LV dysfunction/cardiomyopathy (5% each). Adverse reactions leading to dose reductions of MEKTOVI occurred in 33% of patients receiving MEKTOVI; the most common (≥5%) were diarrhea (8%), nausea (6%), and AST increased (5%). A total of 17% of patients receiving MEKTOVI experienced an adverse reaction that resulted in permanent discontinuation of MEKTOVI; the most common (≥2%) were diarrhea (3.1%); musculoskeletal pain, LV dysfunction/cardiomyopathy, fatigue, nausea, rash, visual impairment, and vomiting (2% each). None of the other adverse reactions leading to permanent discontinuation of MEKTOVI occurred in more than 1 patient.
Serious adverse reactions occurred in 38% of patients who received MEKTOVI in combination with encorafenib. Serious adverse reactions in ≥2% of patients included hemorrhage (6%); diarrhea (4.1%); anemia, dyspnea, pneumonia (3.1% each); arrhythmia, device related infection, edema, myocardial infarction, and pleural effusion (2% each). Fatal adverse reactions occurred in 2% of patients who received MEKTOVI (45 mg twice-daily) in combination with encorafenib, including intracranial hemorrhage and myocardial infarction (1% each).
Table 5 and Table 6 present adverse drug reactions and laboratory abnormalities, respectively, identified in PHAROS.
Other clinically important adverse reactions occurring in <10% of patients who received MEKTOVI in combination with encorafenib were:
Nervous system disorders:
Gastrointestinal disorders:
Skin and subcutaneous tissue disorders:
Immune system disorders:
4DRUG INTERACTIONS
No clinically important drug interactions have been observed with MEKTOVI.
5OVERDOSAGE
Since binimetinib is 97% bound to plasma proteins, hemodialysis is likely to be ineffective in the treatment of overdose with MEKTOVI.
6DESCRIPTION
Binimetinib is a kinase inhibitor. The chemical name is 5-[(4-bromo-2-fluorophenyl)amino]-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzimidazole-6-carboxamide. The molecular formula is C
Binimetinib is a white to slightly yellow powder. In aqueous media, binimetinib is slightly soluble at pH 1, very slightly soluble at pH 2, and practically insoluble at pH 4.5 and higher.
MEKTOVI (binimetinib) tablets for oral use contain 15 mg of binimetinib with the following inactive ingredients: lactose monohydrate, microcrystalline cellulose, croscarmellose sodium, magnesium stearate (vegetable source), and colloidal silicon dioxide. The coating contains polyvinyl alcohol, polyethylene glycol, titanium dioxide, talc, ferric oxide yellow, and ferrosoferric oxide.
7HOW SUPPLIED/STORAGE AND HANDLING
MEKTOVI (binimetinib) is supplied as 15 mg yellow/dark yellow, unscored biconvex oval film-coated tablets debossed with a stylized "A" on one side and "15" on the other side, available in bottles of 180 tablets (NDC 70255-010-02).
8PATIENT COUNSELING INFORMATION
Advise the patient to read the FDA-approved patient labeling (Medication Guide).
Inform patients of the following:
9PRINCIPAL DISPLAY PANEL - 15 mg Tablet Bottle Label
NDC 70255-010-02
MEKTOVI
15 mg
Rx only
180 Tablets
10PRINCIPAL DISPLAY PANEL - 15 mg Tablet Bottle Carton
NDC 70255-010-02
MEKTOVI
15 mg
Rx only
180 Tablets
