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Encorafenib is an oral small molecule BRAF kinase inhibitor.
Generic name : Encorafenib (Encorafenib)
Trade name : BRAFTOVI™
English name : Encorafenib Capsules
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.
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.
Active ingredient : Encorafenib (alaninib).
Excipients : Copovidone, poloxamer 188, microcrystalline cellulose, succinic acid, crospovidone, colloidal silica, plant-source magnesium stearate.
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.
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).
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).
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.
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%).
There are no absolute contraindications, but it is contraindicated in patients with wild-type BRAF.
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.
Save at 20°C-25°C (15°C-30°C allowed), sealed in the original bottle, moisture-proof (do not remove the desiccant).