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Encorafenib

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Encorafenib is an oral small molecule BRAF kinase inhibitor.

1. Drug name

Generic name : Encorafenib (Encorafenib)

Trade name : BRAFTOVI™

English name : Encorafenib Capsules

2. Indications

Applicable population : Used in combination with Binimetinib to treat unresectable or metastatic melanoma (BRAF V600E or V600K mutation, subject to FDA approval and testing confirmation).

Limitations : Not suitable for use in patients with wild-type BRAF melanoma.

3. Specifications and characteristics

Specifications :

50 mg capsule: orange cap printed with "A", beige body printed with "LGX 50mg".

75 mg capsule: beige cap printed with "A" and white body printed with "LGX 75mg".

Characteristics : Hard gelatin capsule, the content is white to off-white powder.

4. Main ingredient

Active ingredient : Encorafenib (alaninib).

Excipients : Copovidone, poloxamer 188, microcrystalline cellulose, succinic acid, crospovidone, colloidal silica, plant-source magnesium stearate.

5. Usage and Dosage

Regular dosage : 450 mg orally, once a day (combined with bimetinib 45 mg, twice a day), before or after a meal.

Missed dose of : If you miss a dose, take it within 12 hours; if it exceeds 12 hours, skip it and do not double the dose.

Vomiting : There is no need to take additional doses after vomiting, just take the next dose as originally planned.

6. Dose adjustment

Adverse reaction adjustment :

Reduce the dose to 300 mg/day for the first time and to 200 mg/day for the second time. If the drug is still not tolerated, discontinue the drug permanently.

Specific toxicities (such as QTc prolongation, uveitis) require suspension or permanent discontinuation (see Table 2 for details).

Drug interaction :

CYP3A4 strong/moderate inhibitor : reduce the dose to 1/3 (strong inhibitor) or 1/2 (moderate inhibitor).

7. Medication precautions

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

Monitor :

It is necessary to monitor electrocardiogram (QT interval), electrolytes, liver function, skin lesions and vision changes before and during medication.

Contraindications : There are no clear contraindications, but you need to be alert to the risks of combined medication (such as CYP3A4 inducers).

8. U200c for special groups

Pregnant women : may cause fetal harm, so non-hormonal contraception must be used (hormonal contraceptives may be ineffective).

Lactation period : Avoid breastfeeding during treatment and within 2 weeks of stopping the drug.

Children : Safety has not been established.

Hepatic/renal insufficiency : No adjustment is required for mild to moderate; no recommended dosage for severe.

9. Adverse reactions

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

Severe :

Squamous cell carcinoma/basal cell carcinoma of the skin (2.6%), bleeding (19%), QT prolongation, uveitis (4%).

The risk of skin toxicity is higher when used alone (such as palmoplantar erythema syndrome 51%).

10. Contraindications

There are no absolute contraindications, but it is contraindicated in patients with wild-type BRAF.

11. Drug interactions

CYP3A4 inhibitor/inducer : Avoid combined use of strong/moderate inducers; the dosage of inhibitors needs to be adjusted.

QT prolonging drug : Avoid concomitant use (such as antiarrhythmic drugs).

Hormonal contraceptive : may be ineffective and you need to switch to non-hormonal contraception.

12. Storage method

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