Encorafenib is an oral small molecule BRAF kinase inhibitor.

1. Drug name

Common name: Encorafenib

Product Name: BRAFTOVI ™

English name: Encorafenib Capsules

2. Indications

Applicable population: Used in combination with Binimetinib for the treatment of unresectable or metastatic melanoma (BRAF V600E or V600K mutations, subject to FDA approved testing confirmation).

Restriction: Not applicable to patients with wild-type BRAF melanoma.

3. Specifications and characteristics

Specifications:

50mg capsules: Orange cap print "A", beige body print "LGX 50mg".

75mg capsules: beige cap print "A", white body print "LGX 75mg".

Appearance: Hard gelatin capsule, with contents ranging from white to off white powder.

4. Main components

Active ingredient: Encorafenib (alanine aminotransferase).

Auxiliary materials: copolypyrrolidone, poloxamer 188, microcrystalline cellulose, succinic acid, cross-linked polyvinylpyrrolidone, colloidal silica, plant-based magnesium stearate.

5. Usage and dosage

Conventional dose: 450 mg orally, once daily (in combination with Bimetinib 45 mg twice daily), before or after meals.

Omission: If missed, take a replacement within 12 hours; If it exceeds 12 hours, skip and do not double the dosage.

Vomiting: No need to take additional medication after vomiting, follow the original plan for the next dose.

6. Dose adjustment

Adverse reaction adjustment:

The first dose is reduced to 300 mg/day, and the second dose is reduced to 200 mg/day. If intolerance persists, the medication will be permanently discontinued.

Specific toxicities (such as QTc prolongation and uveitis) require temporary or permanent discontinuation of medication (see Table 2 for details).

Drug interactions:

CYP3A4 strong/medium acting inhibitors: Reduce the dosage to 1/3 (strong inhibitors) or 1/2 (medium acting inhibitors) of the original dosage.

7. Medication precautions

Diet: No need to fast, but avoid grapefruit (which may increase blood drug concentration).

Monitoring:

Monitor electrocardiogram (QT interval), electrolytes, liver function, skin lesions, and changes in vision before and during medication.

Contraindications: There are no clear contraindications, but caution should be exercised regarding the risk of concomitant medication (such as CYP3A4 inducers).

8. Medication for special populations

Pregnant women: may cause fetal harm and require the use of non hormonal contraception (hormonal contraceptives may be ineffective).

Breastfeeding period: Avoid breastfeeding during treatment and within 2 weeks of discontinuing medication.

Children: Safety has not been established.

Liver/kidney dysfunction: mild to moderate without adjustment; No recommended dosage for severe cases.

9. Adverse reactions

Common (≥ 25%): fatigue, nausea, vomiting, abdominal pain, joint pain.

Serious:

Skin squamous cell carcinoma/basal cell carcinoma (2.6%), bleeding (19%), QT prolongation, uveitis (4%).

The risk of skin toxicity is higher when used alone (such as 51% for palmar and plantar erythema syndrome).

10. Contraindications

There are no absolute contraindications, but wild-type BRAF patients are contraindicated.

11. Drug interactions

CYP3A4 inhibitors/inducers: avoid using strong/medium acting inducers in combination; The dosage of the inhibitor needs to be adjusted.

QT prolongation drugs: Avoid combination therapy (such as antiarrhythmic drugs).

Hormonal contraceptive pills: may fail, non hormonal contraception should be used instead.

12. Storage method

Store at 20 ° C-25 ° C (15 ° C-30 ° C allowed), sealed in the original bottle, moisture-proof (do not remove desiccant).

Encorafenibinformation