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What is Trametinib
Trametinib is a mitogen-activated extracellular signal-regulated kinase (MEK)1 and MEK2 inhibitor. It inhibits cell growth in BRAF V600 mutation-positive tumors by blocking MEK1 and MEK2 which are proteins activated in the BRAF pathway. Using an FDA-approved test, confirm the presence of the BRAF V600 mutation in tumor specimens prior to initiation of treatment.
Trametinib is indicated as single-agent therapy in patients with BRAF inhibitor-naive, BRAF V600E or V600K mutation-positive unresectable or metastatic melanoma.
In combination with dabrafenib, trametinib is used for the treatment of BRAF V600E or V600K mutation-positive unresectable or metastatic melanoma, as adjuvant therapy following complete resection in patients with BRAF V600E or V600K mutation-positive melanoma and lymph node involvement, for the treatment of BRAF V600E mutation-positive metastatic non-small cell lung cancer, and for the treatment of BRAF V600E mutation-positive locally advanced or metastatic anaplastic thyroid cancer (ATC) in patients with no satisfactory locoregional treatment options.
Venous thromboembolism and interstitial lung disease have been reported with trametinib therapy.
Brand Name
Mekinist
Indications
- malignant melanoma
- non-small cell lung cancer (NSCLC)
- thyroid cancer
Side Effects
- abdominal pain
- acneiform rash
- anemia
- anorexia
- arthralgia
- asthenia
- bleeding
- blurred vision
- bradycardia
- cardiomyopathy
- chills
- colitis
- cough
- dehydration
- diarrhea
- dizziness
- Drug Reaction with Eosinophilia and Systemic Symptoms (DRESS)
- dysgeusia
- dyspnea
- edema
- elevated hepatic enzymes
- epistaxis
- fatigue
- fever
- folliculitis
- GI bleeding
- GI perforation
- headache
- heart failure
- hematoma
- hemoptysis
- hemorrhoids
- hyperglycemia
- hypertension
- hypoalbuminemia
- hyponatremia
- hypophosphatemia
- hypotension
- hypoxia
- infection
- interstitial lung disease
- intracranial bleeding
- leukopenia
- lymphopenia
- macular edema
- maculopapular rash
- malaise
- melena
- musculoskeletal pain
- myalgia
- nausea
- neutropenia
- new primary malignancy
- ocular hemorrhage
- oral ulceration
- peripheral edema
- pleural effusion
- pneumonitis
- pruritus
- pulmonary embolism
- purpura
- QT prolongation
- rash
- renal failure (unspecified)
- retinal detachment
- rhabdomyolysis
- Stevens-Johnson syndrome
- stomatitis
- syncope
- thrombocytopenia
- thromboembolism
- thrombosis
- vaginal bleeding
- vesicular rash
- visual impairment
- vomiting
- xerophthalmia
- xerosis
- xerostomia
Monitoring Parameters
- echocardiogram
- ejection fraction
- multi-gated radionuclide angiography (MUGA)
- ophthalmologic exam
- pregnancy testing
- skin cancer screening exam
Contraindications
- bleeding
- breast-feeding
- cardiac arrhythmias
- cardiac disease
- cardiomyopathy
- children
- colitis
- contraception requirements
- dehydration
- diabetes mellitus
- fever
- geriatric
- GI bleeding
- GI perforation
- glaucoma
- heart failure
- hyperglycemia
- hypertension
- hypotension
- infants
- infection
- infertility
- inflammatory bowel disease
- intracranial bleeding
- male-mediated teratogenicity
- neonates
- new primary malignancy
- pleural effusion
- pneumonitis
- pregnancy
- pregnancy testing
- pulmonary disease
- QT prolongation
- renal failure
- reproductive risk
- retinal detachment
- serious rash
- thromboembolic disease
- ventricular dysfunction
Interactions
- Chloroquine
- Dasabuvir; Ombitasvir; Paritaprevir; Ritonavir
- Loperamide
- Loperamide; Simethicone
- Paclitaxel
- Sofosbuvir; Velpatasvir
- Sofosbuvir; Velpatasvir; Voxilaprevir
