Bimetinib, with its unique mechanism of action, precisely targets the RAS/RAF/MEK/ERK signaling pathway, bringing new hope to cancer patients carrying BRAF V600E or V600K gene mutations.

1、 Drug name and main ingredients

1. Common name: Binimetinib

2. Product Name: MEKTOVI ®

3. Dosage form: Oral tablets

4. Main ingredients: Each tablet contains 15mg of Bimetinib

5. Accessories: lactose monohydrate, microcrystalline cellulose, cross-linked carboxymethyl cellulose sodium, magnesium stearate (plant source), colloidal silica; The coating contains polyvinyl alcohol, polyethylene glycol, titanium dioxide, talc powder, iron oxide yellow, and ferric oxide.

2、 Indications

Melanoma: Used in combination with encorafenib to treat patients with BRAFV600E or V600K mutations confirmed by FDA approved testing for unresectable or metastatic melanoma.

3、 Specifications and characteristics

1. Specification: 15mg/tablet, yellow/dark yellow double convex elliptical film coated tablet, with "A" printed on one side and "15" printed on the other side.

2. Appearance: The tablet has an opaque hard capsule appearance and is packaged as 180 tablets per bottle.

4、 Usage and dosage

1. Basic dose: 45mg orally, twice a day (with an interval of about 12 hours), in combination with enrofloxacin, until disease progression or intolerable toxicity occurs.

2. Usage requirements: Can be taken with food or on an empty stomach; If there is a missed dose and it is more than 6 hours before the next dose, it can be taken again. Otherwise, it will be skipped; No need to take additional medication after vomiting.

3. Dose adjustment:

(1) Liver dysfunction: For moderate or severe liver injury (total bilirubin>1.5 × ULN), the recommended dose is 30mg twice a day.

(2) Adverse reaction adjustment: Suspend, reduce, or permanently discontinue medication based on toxicity level (if the initial LVEF decrease is>10% and below the lower limit of normal, pause).

5、 Medication precautions

1. Monitoring requirements:

Regularly check left ventricular ejection fraction (LVEF), liver function, CPK levels, and vision before and during treatment.

Seek medical attention immediately when symptoms of visual impairment, difficulty breathing, muscle pain, or bleeding occur.

2. Taboo combination: Avoid co administration with potent or moderate CYP3A4 inhibitors.

3. Dietary advice: No special dietary restrictions are needed, but grapefruit juice should be avoided (which may affect metabolism).

6、 Medication for special populations

1. Pregnant women: Prohibited, may cause fetal malformation (animal data shows embryotoxicity).

2. Breastfeeding period: Breastfeeding is prohibited during the treatment period and within 3 days after the last dose.

3. Children: Safety has not been established.

4. Elderly individuals: No need to adjust dosage, but close monitoring of liver and kidney function is necessary.

7、 Adverse reactions

1. Common (≥ 25%):

Fatigue (43%), nausea (41%), diarrhea (36%), vomiting (30%), and abdominal pain (28%).

2. Serious but rare:

Cardiomyopathy (7%), venous thrombosis (6%), retinopathy (20%), hepatotoxicity (6% elevated ALT), rhabdomyolysis (0.1%).

Bleeding events (19%, of which 3.2% were ≥ grade 3).

8、 Contraindications

There are no clear contraindications, but patients with moderate to severe liver injury need to adjust the dosage.

9、 Drug interactions

1. CYP3A4 inhibitors: may significantly increase exposure to bimertinib and should be avoided in combination.

2. Enkaempferol combination therapy: No need to adjust the dosage of bimetinib, but reference should be made to the interactions of Enkaempferol.

10、 Storage method

Store at room temperature (20-25 ° C), avoid moisture and light, and keep the bottle cap tightly sealed.

Note: If you experience persistent visual impairment, chest pain, or unexplained muscle pain during medication, seek medical attention immediately. Specific medication should be taken according to the doctor's advice and combined with the prescription information of Enkafenib.

Binimetinibinformation