How many Encorafenib pills do you take a day and what are the effects
The daily dosage of Encorafenib should be determined according to the indications, usually a single oral dose of 450mg (melanoma/NSCLC) or 300mg (colorectal cancer), and the efficacy is determined by the combination therapy. It has high bioavailability and minimal food impact, and can reach a steady state concentration within 15 days.
1 Standard Dose Protocol
(1) Melanoma/non-small cell lung cancer: 450mg once daily (approximately 3 150mg capsules), to be used in combination with Bimetinib.
(2) Colorectal cancer: 300mg once daily (approximately 2 150mg capsules), to be used in combination with cetuximab.
(3) Medication time: Oral administration at a fixed time. When taken with a high-fat meal, the peak concentration decreases by 36% but does not affect total absorption.
2 Pharmacodynamic characteristics
(1) Effective time: Peak plasma concentration is reached 2 hours after oral administration, steady state is reached 15 days, and half-life is 3.5 hours.
(2) Exposure level: 50-700mg. Single dose administration shows dose proportionality, but after repeated administration, the excessive increase and decrease are observed.
(3) Metabolic pathway: Mainly metabolized by CYP3A4, with 47% excreted through feces and urine.
3 Principles of Dose Adjustment
(1) Adverse reaction reduction: melanoma reduced to 300mg/day for the first time, and colorectal cancer reduced to 225mg/day.
(2) Abnormal liver function: Child Pugh A grade does not require adjustment, and there is no recommended dose for B/C grade.
(3) Drug interactions: When combined with strong CYP3A4 inhibitors, the dosage should be reduced to 150mg/day.
4 Clinical efficacy data
(1) Melanoma: Median PFS of 14.9 months and ORR of 63% when combined with bimetinib.
(2) Colorectal cancer: When used in combination with cetuximab monotherapy, the median OS was 9.3 months and DCR was 67%.
(3) Drug resistance management: If RAS mutations occur, medication should be discontinued, and treatment can continue for skin malignancies.
5 Medication precautions
(1) Omission treatment: Do not take the medication within 12 hours of the next dose, and do not take the dose after vomiting.
(2) Storage conditions: Store below 25 ℃, with a shelf life of 24 months.
(3) Dosage form specification: Capsules are commonly taken at 150mg per capsule and should be swallowed whole.
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