【藥品庫存】 本藥品為臨時採購藥品，經院長核可後，限定特定科別、病人使用。

Melanoma:

Adjuvant treatment of melanoma (in combination with dabrafenib) in patients with BRAF V600E or BRAF V600K mutations (as detected by an approved test), and lymph node involvement, following complete resection.

Treatment of unresectable or metastatic melanoma in patients with BRAF V600E or BRAF V600K mutations (as detected by an approved test), either as a single-agent (in BRAF inhibitor treatment-naive patients) or in combination with dabrafenib.

Non-small cell lung cancer (metastatic): Treatment of metastatic non-small cell lung cancer in patients with BRAF V600E mutation as detected by an approved test (in combination with dabrafenib).

Thyroid cancer, anaplastic, locally advanced or metastatic: Treatment of locally advanced or metastatic anaplastic thyroid cancer (in combination with dabrafenib) in patients with BRAF V600E mutation and with no satisfactory locoregional treatment options.

Antineoplastic Agent, MEK Inhibitor

Absorption: Rapid; decreased with a high-fat, high-calorie meal (~1,000 calories)
Distribution: 214 L
Protein binding: ~97% to plasma proteins
Metabolism: Predominantly deacetylation (via hydrolytic enzymes) alone or with mono-oxygenation or in combination with glucuronidation
Bioavailability: 72%
Half-life elimination: ~4 to 5 days
Time to peak: 1.5 hours; delayed with a high-fat, high-calorie meal (~1,000 calories)
Excretion: Feces (>80%); urine (<20% with <0.1% as unchanged drug)

There are no contraindications listed in the manufacturer's US labeling.

Based on its mechanism of action and on findings in animal reproduction studies, in utero exposure to trametinib may cause fetal harm.

It is not known if trametinib is present in breast milk.
Due to the potential for serious adverse reactions in the breastfed infant, breastfeeding is not recommended by the manufacturer during trametinib treatment and for 4 months after the last trametinib dose.

Cardiovascular: Edema (including peripheral edema: ?32%), hypertension (15%)

Dermatologic: Acneiform eruption (19%), skin rash (57%), xeroderma (11%)

Endocrine & metabolic: Hypoalbuminemia (42%)

Gastrointestinal: Abdominal pain (13%), diarrhea (43%), stomatitis (15%; grades 3/4: 2%)

Hematologic & oncologic: Anemia (38%; grades 3/4: 2%), hemorrhage (13%; grades 3/4: <1%), lymphedema (?32%; grades 3/4: 1%)

Hepatic: Increased serum alanine aminotransferase (39%), increased serum alkaline phosphatase (24%), increased serum aspartate aminotransferase (60%)

Melanoma, adjuvant treatment (with BRAF V600E or BRAF V600K mutations): Oral: 2 mg once daily (in combination with dabrafenib); continue for ?1 year in the absence of disease progression or unacceptable toxicity.
Melanoma, metastatic or unresectable (with BRAF V600E or BRAF V600K mutations): Oral: 2 mg once daily (either as a single-agent or in combination with dabrafenib), continue until disease progression or unacceptable toxicity.
Non-small cell lung cancer, metastatic (with BRAF V600E mutation): Oral: 2 mg once daily (in combination with dabrafenib); continue until disease progression or unacceptable toxicity.
Thyroid cancer, anaplastic, locally advanced or metastatic (with BRAF V600E mutation): Oral: 2 mg once daily (in combination with dabrafenib); continue until disease progression or unacceptable toxicity.

Mild to moderate impairment (GFR ?30 mL/minute/1.73 m2): No dosage adjustment necessary.
Severe impairment (GFR <30 mL/minute/1.73 m2): There are no dosage adjustments provided in the manufacturer's labeling

Mild impairment (bilirubin ? ULN and AST > ULN or bilirubin >1 to 1.5 times ULN with any AST): No dosage adjustment necessary.
Moderate (bilirubin >1.5 to 3 times ULN and any AST) to severe (bilirubin >3 to 10 times ULN and any AST) impairment: There are no dosage adjustments provided in the manufacturer's labeling