Encorafenib
Generic Name: encorafenib
Brand Names:
Braftovi
11 DESCRIPTION Encorafenib is a kinase inhibitor. The chemical name is methyl N -{(2 S )-1-[(4-{3-[5-chloro-2-fluoro-3-(methanesulfonamido)phenyl]-1-(propan-2-yl)-1 H -pyrazol-4-yl}pyrimidin-2-yl)amino]propan-2-yl}carbamate. The molecular formula is C 22 H 27 ClFN 7 O 4 S and the molecular weight is 540 daltons. The chemical structure of encorafenib is shown below: Encorafenib is a white to almost white powder.
Overview
11 DESCRIPTION Encorafenib is a kinase inhibitor. The chemical name is methyl N -{(2 S )-1-[(4-{3-[5-chloro-2-fluoro-3-(methanesulfonamido)phenyl]-1-(propan-2-yl)-1 H -pyrazol-4-yl}pyrimidin-2-yl)amino]propan-2-yl}carbamate. The molecular formula is C 22 H 27 ClFN 7 O 4 S and the molecular weight is 540 daltons. The chemical structure of encorafenib is shown below: Encorafenib is a white to almost white powder.
Uses
1 INDICATIONS AND USAGE BRAFTOVI is a kinase inhibitor indicated: Melanoma • in combination with binimetinib, for the treatment of patients with unresectable or metastatic melanoma with a BRAF V600E or V600K mutation, as detected by an FDA-authorized test. ( 1.1 , 2.1 ) Colorectal Cancer (CRC) • in combination with cetuximab and fluorouracil-based chemotherapy, for the treatment of adult patients with metastatic colorectal cancer (mCRC) with a BRAF V600E mutation, as detected by an FDA‑authorized test. ( 1.2 , 2.1 ) • in combination with cetuximab, for the treatment of adult patients with mCRC with a BRAF V600E mutation, as detected by an FDA-authorized test, after prior therapy.
Dosage
2 DOSAGE AND ADMINISTRATION Melanoma • Confirm the presence of BRAF V600E or V600K mutation in tumor specimens prior to the initiation of BRAFTOVI. ( 2.1 ) • The recommended dose is 450 mg orally once daily in combination with binimetinib. ( 2.2 ) CRC • Confirm the presence of BRAF V600E mutation in plasma or tumor specimens prior to the initiation of BRAFTOVI. ( 2.1 ) • The recommended dose is 300 mg orally once daily in combination with o biweekly cetuximab and mFOLFOX6 (fluorouracil, leucovorin and oxaliplatin) or cetuximab and FOLFIRI (fluorouracil, leucovorin and irinotecan) ( 2.3 ) o weekly cetuximab ( 2.3 ) NSCLC • Confirm the presence of BRAF V600E mutation in tumor or plasma specimens prior to initiating BRAFTOVI.
Side Effects
6 ADVERSE REACTIONS The following adverse reactions are described elsewhere in the labeling: • New Primary Malignancies [see Warnings and Precautions (5.1) ] • Tumor Promotion in BRAF Wild-Type Tumors [see Warnings and Precautions (5.2) ] • Cardiomyopathy [see Warnings and Precautions (5.3) ] • Hepatotoxicity [see Warnings and Precautions (5.4) ] • Hemorrhage [see Warnings and Precautions (5.5) ] • Uveitis [see Warnings and Precautions (5.6) ] • QT Prolongation [see Warnings and Precautions (5.7) ] • Embryo-Fetal Toxicity [see Warnings and Precautions (5.8) ] • Risks Associated with BRAFTOVI as a Single Agent [see Warnings and Precautions (5.9) ] • Risks Associated with Combination Treatment [see Warnings and Precautions (5.10) ] • Melanoma : Most common adverse reactions (≥25%) for BRAFTO...
Interactions
7 DRUG INTERACTIONS • Strong or moderate CYP3A4 inhibitors: Avoid coadministration. If unavoidable, reduce BRAFTOVI dosage. ( 2.6 , 7.1 ) • Strong CYP3A4 inducers: Avoid coadministration. ( 7.1 ) • Sensitive CYP3A4 substrates: Avoid coadministration with CYP3A4 substrates (including hormonal contraceptives) for which a decrease in plasma concentration may lead to reduced efficacy of the substrate. ( 7.2 ) • Transporters: Dose reductions of drugs that are substrates of OATP1B1, OATP1B3, or BCRP may be required when used concomitantly with BRAFTOVI.
Warnings
5 WARNINGS AND PRECAUTIONS • New Primary Malignancies, cutaneous and noncutaneous : Can occur. Monitor for malignancies and perform dermatologic evaluations prior to, while on therapy, and following discontinuation of treatment. ( 5.1 ) • Tumor Promotion in BRAF Wild-Type Tumors : Increased cell proliferation can occur with BRAF inhibitors. ( 5.2 ) • Cardiomyopathy : Assess left ventricular ejection fraction (LVEF) before initiating treatment with BRAFTOVI and binimetinib, and after one month of treatment, then every 2 to 3 months thereafter. The safety of BRAFTOVI in combination with binimetinib has not been established in patients with LVEF below 50%. 4 CONTRAINDICATIONS None. None. ( 4 )
Pregnancy
8.1 Pregnancy Risk Summary Based on its mechanism of action, BRAFTOVI can cause fetal harm when administered to a pregnant woman [see Clinical Pharmacology (12.1) ] . There are no available clinical data on the use of BRAFTOVI during pregnancy.
Storage
Store at 20°C to 25°C (68°F to 77°F); excursions permitted between 15°C and 30°C (59°F and 86°F) [see USP Controlled Room Temperature]. Do not use if safety seal under cap is broken or missing. Dispense in original bottle. Do not remove desiccant. Protect from moisture. Keep container tightly closed.
Frequently Asked Questions
What is Encorafenib used for?▼
1 INDICATIONS AND USAGE BRAFTOVI is a kinase inhibitor indicated: Melanoma • in combination with binimetinib, for the treatment of patients with unresectable or metastatic melanoma with a BRAF V600E or V600K mutation, as detected by an FDA-authorized test. ( 1.1 , 2.1 ) Colorectal Cancer (CRC) • in combination with cetuximab and fluorouracil-based chemotherapy, for the treatment of adult patients with metastatic colorectal cancer (mCRC) with a BRAF V600E mutation, as detected by an FDA‑authorized test. ( 1.2 , 2.1 ) • in combination with cetuximab, for the treatment of adult patients with mCRC with a BRAF V600E mutation, as detected by an FDA-authorized test, after prior therapy.
What are the side effects of Encorafenib?▼
6 ADVERSE REACTIONS The following adverse reactions are described elsewhere in the labeling: • New Primary Malignancies [see Warnings and Precautions (5.1) ] • Tumor Promotion in BRAF Wild-Type Tumors [see Warnings and Precautions (5.2) ] • Cardiomyopathy [see Warnings and Precautions (5.3) ] • Hepatotoxicity [see Warnings and Precautions (5.4) ] • Hemorrhage [see Warnings and Precautions (5.5) ] • Uveitis [see Warnings and Precautions (5.6) ] • QT Prolongation [see Warnings and Precautions (5.7) ] • Embryo-Fetal Toxicity [see Warnings and Precautions (5.8) ] • Risks Associated with BRAFTOVI as a Single Agent [see Warnings and Precautions (5.9) ] • Risks Associated with Combination Treatment [see Warnings and Precautions (5.10) ] • Melanoma : Most common adverse reactions (≥25%) for BRAFTO...
Can I take Encorafenib during pregnancy?▼
8.1 Pregnancy Risk Summary Based on its mechanism of action, BRAFTOVI can cause fetal harm when administered to a pregnant woman [see Clinical Pharmacology (12.1) ] . There are no available clinical data on the use of BRAFTOVI during pregnancy.
What are the important warnings for Encorafenib?▼
5 WARNINGS AND PRECAUTIONS • New Primary Malignancies, cutaneous and noncutaneous : Can occur. Monitor for malignancies and perform dermatologic evaluations prior to, while on therapy, and following discontinuation of treatment. ( 5.1 ) • Tumor Promotion in BRAF Wild-Type Tumors : Increased cell proliferation can occur with BRAF inhibitors. ( 5.2 ) • Cardiomyopathy : Assess left ventricular ejection fraction (LVEF) before initiating treatment with BRAFTOVI and binimetinib, and after one month of treatment, then every 2 to 3 months thereafter. The safety of BRAFTOVI in combination with binimetinib has not been established in patients with LVEF below 50%. 4 CONTRAINDICATIONS None. None. ( 4 )
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Medical Disclaimer
This drug information is for educational purposes only and should not replace professional medical advice. Drug information is sourced from the FDA National Drug Code Directory and Structured Product Labeling. Always consult with a healthcare provider before starting, stopping, or changing any medication.