trametinib(redirected from Mekinist)
Pregnancy Category: D
Pharmacologic: kinase inhibitors
Pharmacologic: kinase inhibitors
Treatment of metastatic/unresectable melanoma with the BRAF V660E or V600K mutation.
Inhibits the activity of kinases, enzymes that promote cellular proliferation
Decreased progression of melanoma.
Absorption: Well absorbed following oral administration
Protein Binding: 97.4%
Metabolism and Excretion: 50% metabolized, 80% eliminated in feces (metabolites and parent compound), 20% excreted in urine (mostly as metabolites).
Time/action profile (response)
|PO||1 mo||2 mo||5–7mos|
Contraindicated in: Obstetric: May cause fetal harm Lactation: Breastfeeding should be avoided
Use Cautiously in: Obstetric: Patients with child-bearing potential Pediatric: Safe and effective use in children has not been established
Adverse Reactions/Side Effects
Central nervous system
Ear, Eye, Nose, Throat
- blurred vision
- dry eyes
- retinal pigment epithelial detachment
- retinal vein occlusion
- interstitial lung disease/pneumonitis (life-threatening)
- cardiomyopathy (life-threatening)
- hypertension (most frequent)
- abdominal pain (most frequent)
- diarrhea (most frequent)
- ↑ liver enzymes (most frequent)
- stomatitis (most frequent)
- acneiform dermatitis (most frequent)
- rash (most frequent)
- skin toxicity (most frequent)
- dry skin
- palmar-plantar erythrodysesthesia syndrome
- bleeding (most frequent)
- lymphedema (most frequent)
Drug-Drug interactionNone noted
Oral (Adults) 2 mg daily continued until disease progression or unacceptable toxicity; dose modifications recommended for various levels of toxicity.
Tablets: 0.5 mg, 1 mg, 2 mg
- Assess left ventricular ejection fraction (LVEF) by echocardiogram or multigated acquisition (MUGA) scan before starting, after 1 month, and at 2–3 month intervals during therapy. If asymptomatic and absolute ↓ LVEF of ≥10% from baseline and below institutional lower limits of normal from pretreatment value, withhold for up to 4 wks. If LVEF improves to normal within 4 wks,resume trametinib at lower dose, ↓ by 0.5 mg, or discontinue in patients taking 1 mg daily. If symptomatic HF, absolute ↓ LVEF >20% of baseline that is below institutional lower limits of normal, or absolute ↓ LVEF ≥10% of baseline that is below institutional lower limits of normal that does not improve to normal within 4 wks following interruption of therapy, permanently discontinue trametinib.
- Perform ophthalmalogic evaluation at baseline; compare if patient reports visual disturbance. If Grade 2–3 retinal pigment epithelial detachment (RPED) occurs, withhold trametinib for up to 3 wks. If Grade 2–3 RPED improves to Grade 0–1 within 3 wks, resume trametinib at a lower dose (0.5 mg) or discontinue in patients taking 1 mg daily. If retinal vein occlusion occurs or if Grade 2–3 RPED does not improve to at least Grade 1 within 3 wks, permanently discontinue trametinib.
- Assess for signs and symptoms of interstitial lung disease (cough, dyspnea, hypoxia, pleural effusion, infiltrates). Permanently discontinue trametinib if these occur.
- Monitor for skin toxicities and secondary infections during therapy. If Grade 2 rash occurs, reduce dose by 0.5 mg or discontinue in patients taking 1 mg daily. If intolerable Grade 2 rash that does not improve within 3 wks following dose reduction or if Grade 3 or 4 rash occurs, withhold trametinib for up to 3 wks. If improved within 3 wks, resume trametinib at a lower dose (0.5 mg) or discontinue in patients taking 1 mg daily. If intolerable Grade 2 or Grade 3 or 4 rash that does not improve despite interruption of therapy for 3 wks, permanently discontinue trametinib.
- Monitor blood pressure periodically during therapy. May cause hypertension.
- Lab Test Considerations: May cause ↑ AST, ALT, and alkaline phosphatase.
- May cause hypoalbumemia.
- May cause anemia.
Potential Nursing DiagnosesImpaired skin integrity (Indications)
- Evidence of BRAF V600E or V600K mutations must be confirmed prior to starting therapy with trametinib.
- Oral: Administer twice daily about 12 hrs apart. Administer on an empty stomach at least 1 hr before or 2 hrs after a meal. Swallow tablets whole; do not break, crush, break, or chew.
- Instruct patient to take trametinib as directed at least 1 hr before or 2 hrs after meals. Take missed doses as soon as remembered unless within 12 hrs of next dose, then skip missed dose and take regularly scheduled dose.
- Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications.
- Inform patient of potential side effects. Advise patient to notify health care professional if signs and symptoms of heart failure (pounding or racing heart, shortness of breath, swelling of feet or ankles, lightheadedness), visual disturbances (blurred vision, loss of vision, seeing colored dots, seeing a blurred outline or halo around objects, other visual changes), dyspnea, progressive or intolerable rash (acne; redness, swelling, peeling, or tenderness of hands or feet), hypertension (severe headache, lightheadedness, dizziness) or severe diarrhea occur.
- Advise female patient to use a highly effective form of contraception during and for at least 4 months after treatment. Use a non-hormonal form of contraception; trametinib may decrease effectiveness of hormonal contraceptives. Advise patient to notify health care professional if pregnancy is suspected and to avoid breastfeeding. May impair fertility in females.
- Decrease in progression of malignant melanoma.
Drug Guide, © 2015 Farlex and Partners