- Melanoma and other skin cancers
- Pancreatic, thyroid, and other endocrine cancers
- Respiratory and thoracic cancers
- Solid tumors
Melanoma and other skin cancers:
Indications for: MEKINIST
As monotherapy in BRAF-inhibitor treatment-naïve patients or in combination with dabrafenib for the treatment of unresectable or metastatic melanoma with BRAF V600E or V600K mutations, as detected by an FDA-approved test. In combination with dabrafenib for the adjuvant treatment of melanoma with BRAF V600E or V600K mutations, as detected by an FDA-approved test, and lymph node involvement, following complete resection.
Limitations of Use:
Not for treatment of colorectal cancer because of known intrinsic resistance to BRAF inhibition.
Adult Dosage:
Confirm presence of BRAF V600E or V600K mutation prior to initiation. Take at same time each day, at least 1hr before or 2hrs after a meal. Monotherapy or in combination with dabrafenib: 2mg once daily (approx. 24hrs apart); continue until disease progression or unacceptable toxicity. Adjuvant treatment with dabrafenib: 2mg once daily (approx. 24hrs apart); continue until disease recurrence or unacceptable toxicity for up to 1 year. Dose modifications: see full labeling.
Children Dosage:
Not established.
MEKINIST Warnings/Precautions:
See full labeling for dabrafenib prior to starting combination therapy. With dabrafenib: risk of new primary malignancies, cutaneous, and non-cutaneous; monitor and perform skin evaluation prior to initiation, every 2 months during therapy, and up to 6 months after discontinuation. Monitor for pulmonary embolism (permanently discontinue if life-threatening), colitis, GI perforations, skin toxicities and secondary infections. Withhold if uncomplicated deep vein thrombosis or pulmonary embolism occurs for up to 3wks. Permanently discontinue for all Grade 4 hemorrhagic events or any persistent Grade 3 events. Risk of cardiomyopathy; assess LVEF prior to initiation, after one month, and then at every 2–3 month intervals during treatment; withhold for up to 4wks if absolute LVEF decreases by ≥10% from baseline and is less than the lower limit of normal (LLN); permanently discontinue if symptomatic cardiomyopathy or absolute LVEF decrease of >20% from baseline that is below LLN. Perform eye exam periodically and at any time for visual disturbances; withhold for up to 3wks, if retinal pigment epithelial detachment is diagnosed. Permanently discontinue if documented retinal vein occlusion, interstitial lung disease or pneumonitis occurs. Withhold if fever ≥100.4°F, evaluate infection and assess renal function; prophylaxis with antipyretics when resuming or give steroids for subsequent pyrexia. Withhold if intolerable or severe skin toxicity occurs; permanently discontinue if unresolved after 3wks. Pre-existing diabetes or hyperglycemia; monitor serum glucose levels. Severe renal or moderate to severe hepatic impairment. Embryo-fetal toxicity. Advise females of reproductive potential to use effective contraception during and for 4 months after the last dose. Pregnancy: exclude status prior to initiation. Nursing mothers: not recommended (during and for 4 months after last dose).
MEKINIST Classification:
Kinase inhibitor.
Adverse Reactions:
Rash, diarrhea, lymphedema. In combination with dabrafenib: also pyrexia, chills, fatigue, nausea, vomiting, hypertension, peripheral edema, headache, arthralgia, myalgia, dry skin, decreased appetite, hemorrhage, cough, dyspnea, constipation, dermatitis acneiform, abdominal pain, paronychia.
Generic Drug Availability:
NO
How Supplied:
Tabs—30
Pancreatic, thyroid, and other endocrine cancers:
Indications for: MEKINIST
In combination with dabrafenib for the treatment of locally advanced or metastatic anaplastic thyroid cancer (ATC) with BRAF V600E mutation and with no satisfactory locoregional treatment options.
Limitations of Use:
Not for treatment of colorectal cancer because of known intrinsic resistance to BRAF inhibition.
Adult Dosage:
Confirm presence of BRAF V600E mutation prior to initiation. Take at same time each day, at least 1hr before or 2hrs after a meal. In combination with dabrafenib: 2mg once daily (approx. 24hrs apart); continue until disease recurrence or unacceptable toxicity. Dose modifications: see full labeling.
Children Dosage:
Not established.
MEKINIST Warnings/Precautions:
See full labeling for dabrafenib prior to starting combination therapy. With dabrafenib: risk of new primary malignancies, cutaneous, and non-cutaneous; monitor and perform skin evaluation prior to initiation, every 2 months during therapy, and up to 6 months after discontinuation. Monitor for pulmonary embolism (permanently discontinue if life-threatening), colitis, GI perforations, skin toxicities and secondary infections. Withhold if uncomplicated deep vein thrombosis or pulmonary embolism occurs for up to 3wks. Permanently discontinue for all Grade 4 hemorrhagic events or any persistent Grade 3 events. Risk of cardiomyopathy; assess LVEF prior to initiation, after one month, and then at every 2–3 month intervals during treatment; withhold for up to 4wks if absolute LVEF decreases by ≥10% from baseline and is less than the lower limit of normal (LLN); permanently discontinue if symptomatic cardiomyopathy or absolute LVEF decrease of >20% from baseline that is below LLN. Perform eye exam periodically and at any time for visual disturbances; withhold for up to 3wks, if retinal pigment epithelial detachment is diagnosed. Permanently discontinue if documented retinal vein occlusion, interstitial lung disease or pneumonitis occurs. Withhold if fever ≥100.4°F, evaluate infection and assess renal function; prophylaxis with antipyretics when resuming or give steroids for subsequent pyrexia. Withhold if intolerable or severe skin toxicity occurs; permanently discontinue if unresolved after 3wks. Pre-existing diabetes or hyperglycemia; monitor serum glucose levels. Severe renal or moderate to severe hepatic impairment. Embryo-fetal toxicity. Advise females of reproductive potential to use effective contraception during and for 4 months after the last dose. Pregnancy: exclude status prior to initiation. Nursing mothers: not recommended (during and for 4 months after last dose).
MEKINIST Classification:
Kinase inhibitor.
Adverse Reactions:
Rash, diarrhea, lymphedema. In combination with dabrafenib: also pyrexia, chills, fatigue, nausea, vomiting, hypertension, peripheral edema, headache, arthralgia, myalgia, dry skin, decreased appetite, hemorrhage, cough, dyspnea, constipation, dermatitis acneiform, abdominal pain, paronychia.
Generic Drug Availability:
NO
How Supplied:
Tabs—30
Respiratory and thoracic cancers:
Indications for: MEKINIST
In combination with dabrafenib for the treatment of metastatic non-small cell lung cancer (NSCLC) with BRAF V600E mutation, as detected by an FDA-approved test.
Limitations of Use:
Not for treatment of colorectal cancer because of known intrinsic resistance to BRAF inhibition.
Adult Dosage:
Confirm presence of BRAF V600E mutation prior to initiation. Take at same time each day, at least 1hr before or 2hrs after a meal. In combination with dabrafenib: 2mg once daily (approx. 24hrs apart); continue until disease recurrence or unacceptable toxicity. Dose modifications: see full labeling.
Children Dosage:
Not established.
MEKINIST Warnings/Precautions:
See full labeling for dabrafenib prior to starting combination therapy. With dabrafenib: risk of new primary malignancies, cutaneous, and non-cutaneous; monitor and perform skin evaluation prior to initiation, every 2 months during therapy, and up to 6 months after discontinuation. Monitor for pulmonary embolism (permanently discontinue if life-threatening), colitis, GI perforations, skin toxicities and secondary infections. Withhold if uncomplicated deep vein thrombosis or pulmonary embolism occurs for up to 3wks. Permanently discontinue for all Grade 4 hemorrhagic events or any persistent Grade 3 events. Risk of cardiomyopathy; assess LVEF prior to initiation, after one month, and then at every 2–3 month intervals during treatment; withhold for up to 4wks if absolute LVEF decreases by ≥10% from baseline and is less than the lower limit of normal (LLN); permanently discontinue if symptomatic cardiomyopathy or absolute LVEF decrease of >20% from baseline that is below LLN. Perform eye exam periodically and at any time for visual disturbances; withhold for up to 3wks, if retinal pigment epithelial detachment is diagnosed. Permanently discontinue if documented retinal vein occlusion, interstitial lung disease or pneumonitis occurs. Withhold if fever ≥100.4°F, evaluate infection and assess renal function; prophylaxis with antipyretics when resuming or give steroids for subsequent pyrexia. Withhold if intolerable or severe skin toxicity occurs; permanently discontinue if unresolved after 3wks. Pre-existing diabetes or hyperglycemia; monitor serum glucose levels. Severe renal or moderate to severe hepatic impairment. Embryo-fetal toxicity. Advise females of reproductive potential to use effective contraception during and for 4 months after the last dose. Pregnancy: exclude status prior to initiation. Nursing mothers: not recommended (during and for 4 months after last dose).
MEKINIST Classification:
Kinase inhibitor.
Adverse Reactions:
Rash, diarrhea, lymphedema. In combination with dabrafenib: also pyrexia, chills, fatigue, nausea, vomiting, hypertension, peripheral edema, headache, arthralgia, myalgia, dry skin, decreased appetite, hemorrhage, cough, dyspnea, constipation, dermatitis acneiform, abdominal pain, paronychia.
Generic Drug Availability:
NO
How Supplied:
Tabs—30
Solid tumors:
Indications for: MEKINIST
In combination with dabrafenib, for the treatment of unresectable or metastatic solid tumors in adult and pediatric patients with BRAF V600E mutation who have progressed following prior treatment and have no satisfactory alternative treatment options.
Limitations of Use:
Not for treatment of colorectal cancer because of known intrinsic resistance to BRAF inhibition.
Adult Dosage:
Confirm presence of BRAF V600E mutation prior to initiation. Swallow whole. Take at least 1hr before or 2hrs after a meal. In combination with dabrafenib: ≥18yrs: 2mg once daily (approx. 24hrs apart); continue until disease progression or unacceptable toxicity. Dose modifications: see full labeling.
Children Dosage:
<6yrs or <26kg: not established. Confirm presence of BRAF V600E mutation prior to initiation. Swallow whole. Take at least 1hr before or 2hrs after a meal. In combination with dabrafenib: 6–17yrs (26–37kg): 1mg once daily (approx. 24hrs apart); (38–50kg): 1.5mg once daily; (≥51kg): 2mg once daily; continue until disease progression or unacceptable toxicity. Dose modifications: see full labeling.
MEKINIST Warnings/Precautions:
See full labeling for dabrafenib prior to starting combination therapy. With dabrafenib: risk of new primary malignancies, cutaneous, and non-cutaneous; monitor and perform skin evaluation prior to initiation, every 2 months during therapy, and up to 6 months after discontinuation. Monitor for pulmonary embolism (permanently discontinue if life-threatening), colitis, GI perforations, skin toxicities and secondary infections. Withhold if uncomplicated deep vein thrombosis or pulmonary embolism occurs for up to 3wks. Permanently discontinue for all Grade 4 hemorrhagic events or any persistent Grade 3 events. Risk of cardiomyopathy; assess LVEF prior to initiation, after one month, and then at every 2–3 month intervals during treatment; withhold for up to 4wks if absolute LVEF decreases by ≥10% from baseline and is less than the lower limit of normal (LLN); permanently discontinue if symptomatic cardiomyopathy or absolute LVEF decrease of >20% from baseline that is below LLN. Perform eye exam periodically and at any time for visual disturbances; withhold for up to 3wks, if retinal pigment epithelial detachment is diagnosed. Permanently discontinue if documented retinal vein occlusion, interstitial lung disease or pneumonitis occurs. Withhold if fever ≥100.4°F, evaluate infection and assess renal function; prophylaxis with antipyretics when resuming or give steroids for subsequent pyrexia. Withhold if intolerable or severe skin toxicity occurs; permanently discontinue if unresolved after 3wks. Pre-existing diabetes or hyperglycemia; monitor serum glucose levels. Severe renal or moderate to severe hepatic impairment. Embryo-fetal toxicity. Advise females of reproductive potential to use effective contraception during and for 4 months after the last dose. Pregnancy: exclude status prior to initiation. Nursing mothers: not recommended (during and for 4 months after last dose).
MEKINIST Classification:
Kinase inhibitor.
Adverse Reactions:
Rash, diarrhea, lymphedema. In combination with dabrafenib: also pyrexia, chills, fatigue, nausea, vomiting, hypertension, peripheral edema, headache, arthralgia, myalgia, dry skin, decreased appetite, hemorrhage, cough, dyspnea, constipation, dermatitis acneiform, abdominal pain, paronychia.
Generic Drug Availability:
NO
How Supplied:
Tabs—30
