Binimetinib is an oral inhibitor targeting MEK1/2 kinase, mainly used to treat melanoma and non-small cell lung cancer carrying BRAFV600E/K mutations. This drug needs to be used in combination with Conafenib to inhibit tumor growth by blocking the MAPK signaling pathway, but attention should be paid to adverse reactions such as cardiomyopathy and liver toxicity.

1. Indications and mechanisms of action

Bimetinib combined with Conafenib is suitable for:

(1) Melanoma

The treatment of unresectable or metastatic melanoma with BRAFV600E/K mutation requires FDA approved testing to confirm the mutation.

(2) Non small cell lung cancer

For metastatic NSCLC with BRAFV600E mutation, mutation testing confirmation is also required.

2 Usage and dosage specifications

The standard dose is 45mg orally, once every 12 hours, until disease progression or intolerable toxicity occurs. Please note:

(1) Dose adjustment

Reduce the dosage to 30mg/time for patients with moderate liver damage; If a grade ≥ 3 adverse reaction occurs, the medication should be suspended and reduced or permanently discontinued after recovery.

(2) Administration method

Swallow the whole tablet and avoid taking it with high-fat meals (which may delay absorption). If missed, make-up can be taken within 6 hours, otherwise it will be skipped.

3 Special precautions

(1) Cardiovascular monitoring

Echocardiography should be performed every 3 months before and during treatment, and treatment should be interrupted when LVEF decreases by more than 10% with symptoms.

(2) Reproductive toxicity

Women of childbearing age should use contraception for 30 days after the last dose, and it should be avoided during pregnancy (which may cause fetal malformation).

4 Resistance Mechanisms

Tumors may activate escape inhibition through pathways such as BRAF amplification and NRAS mutations. Combination therapy can delay drug resistance, but it is necessary to monitor the decrease in efficacy.