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Bimetinib, with its unique mechanism of action, precisely targets the RAS/RAF/MEK/ERK signaling pathway to treat BRAF carriers. New hope for cancer patients with V600E or V600K gene mutations.
1. Generic name : Binimetinib (Binimetinib)
2. Trade name : MEKTOVI®
3. Dosage form : Oral tablets
4. Main ingredients :Each tablet contains bimetinib 15mg
5. Excipients :lactose monohydrate, microcrystalline cellulose, croscarmellose sodium, magnesium stearate (plant source), colloidal silicon dioxide; coating contains polyvinyl alcohol, polyethylene glycol, titanium dioxide, talc, iron oxide yellow, ferric tetroxide.
Melanoma : Used in combination with encorafenib to treat patients with unresectable or metastatic melanoma with BRAF V600E or V600K mutations confirmed by FDA-approved testing.
1. Specifications : 15 mg/tablet, yellow/dark yellow biconvex oval film-coated tablet, with "A" printed on one side and "15" printed on the other side.
2. Characteristics : The tablets have the appearance of opaque hard capsules and are packaged at 180 tablets per bottle.
1. Basic dose of : 45 mg orally, twice a day (about 12 hours apart), combined with encofenib until disease progression or intolerable toxicity.
2. Taking requirements : Can be taken with food or on an empty stomach; if you miss a dose, you can take it again if it is more than 6 hours before the next dose, otherwise skip it; there is no need to take it after vomiting.
3. Dose adjustment :
(1). Hepatic insufficiency : The recommended dose for patients with moderate or severe liver damage (total bilirubin >1.5×ULN) is 30 mg twice a day.
(2) Adverse reaction adjustment : Suspend, reduce the dose or permanently discontinue the drug according to the toxicity level (if the first LVEF drops >10% and is lower than the lower limit of normal value, it needs to be suspended).
1. Monitoring requirements :
Check left ventricular ejection fraction (LVEF), liver function, CPK level and visual acuity regularly before and during treatment.
Seek medical attention immediately if you experience visual disturbances, difficulty breathing, myalgia, or bleeding.
2. Concomitant use of is contraindicated: Avoid combined use with strong or moderate CYP3A4 inhibitors.
3. Dietary recommendations : No special dietary restrictions are required, but grapefruit juice needs to be avoided (it may affect metabolism).
1. Pregnant women : Contraindicated, may cause fetal malformations (animal data show embryotoxicity).
2. Lactation : Breastfeeding is prohibited during treatment and within 3 days after the last dose.
3. Children : Safety has not been established.
4. U200c for the elderly: No dose adjustment is required, but liver and kidney function need to be closely monitored.
1. Common (≥25%) :
Fatigue (43%), nausea (41%), diarrhea (36%), vomiting (30%), and abdominal pain (28%).
2. Severe but rare :
Cardiomyopathy (7%), venous thrombosis (6%), retinopathy (20%), hepatotoxicity (6% ALT elevation), rhabdomyolysis (0.1%).
Bleeding events (19%, of which 3.2% were grade ≥3).
There are no clear contraindications, but patients with moderate to severe liver damage need to adjust the dose.
1. CYP3A4 inhibitor : It may significantly increase the exposure of bimetinib, so combined use should be avoided.
2. Encofenib combined with : There is no need to adjust the dose of bimetinib, but the interaction of encofenib needs to be considered.
Save at room temperature (20-25°C), avoid moisture and light, and keep the bottle cap tightly closed.
Note : If you experience persistent visual disturbances, chest pain, or unexplained muscle pain during medication, you need to seek medical attention immediately. Specific medication must be taken as directed by your doctor and combined with Encofenib’s prescription information.