Drug reference

Encorafenib

Tyrosine Kinase Inhibitor · Antineoplastic

Tyrosine Kinase InhibitorAntineoplastic

CDSCO approvedSchedule H

EXCRETION

—

not curated

INTERACTIONS

12 major

SEVERE in our sources

PREGNANCY

Manufacturer advises avoid—toxicity in

FDA category + note

Top interactionssee all 12 →

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Mechanism

Encorafenib is a highly selective small molecule inhibitor of BRAF V600E and V600K mutations. These mutations lead to constitutive activation of BRAF kinase, which in turn activates downstream signaling pathways crucial for cell growth and proliferation in melanoma. By inhibiting BRAF kinase, encorafenib blocks this pathway and thus inhibits tumor cell growth.

Indications

Metastatic melanoma with BRAF V600E or V600K mutationUnresectable or metastatic melanoma with a BRAF V600 mutation (in combination with binimetinib)unresectable metastatic melanoma with BRAF mutations (in combination with binimetinib)metastatic colorectal cancer with a BRAF V600E mutation (in combination with cetuximab)melanomas that harbor a mutation at position 600 in BRAF

Dosing

Adult: l INDICATIONS AND DOSE Unresectable or metastatic melanoma with a BRAF V600 mutation (in combination with encorafenib) (specialist use only) ▶ BY MOUTH ▶ Adult: 45 mg twice daily, for dose adjustments due to side-effects, consult product literature IMPORTANT SAFETY INFORMATION RISKS OF INCORRECT DOSING OF ORAL ANTI-CANCER MEDICINES See Cytotoxic drugs p. 938.…
Renal adjustment: Dosage adjustment is recommended in patients with mild to moderate renal or hepatic impairment.
Hepatic adjustment: Dosage adjustment is recommended in patients with mild to moderate renal or hepatic impairment.

Pharmacokinetics

Half-life

3.5 h (elimination)

Metabolism

CYP3A4 (mostly)

Contraindications

Recent active gastro-intestinal bleeding
Untreated brain metastases

Side effects

Common

AlopeciaAnaemiaAppetite decreasedArthralgiaAstheniaConstipationCoughDehydrationDiarrhoeaDizzinessDysphoniaDyspnoeaElectrolyte imbalanceGastrointestinal discomfortGastrointestinal disordersHeadacheHyperthyroidismHypothyroidismMucositisMyalgiaNauseafatiguediarrheaacneiform dermatitisabdominal painpyrexiaarthralgiashyperproliferative skin lesions (e.g., squamous cell skin cancers)

Serious