BIGBEAR
PHARMACEUTICALS
Encorafenib is an oral, highly selective BRAF V600 mutant kinase inhibitor, often used in combination with MEK inhibitors for enhanced efficacy.
AuthenticGuaranteeFast DeliveryPrivacy Encorafenib acts precisely on the BRAF V600 mutation site in the MAPK signaling pathway, inhibiting the proliferation and survival of tumor cells. It is often used in combination with MEK inhibitors or EGFR monoclonal antibodies in clinical practice to improve anti‑tumor efficacy.
Encorafenib in combination with cetuximab is indicated for the treatment of adult patients with BRAF V600E-mutant metastatic colorectal cancer (CRC) who have received prior systemic therapy.
Therapy should be initiated under the supervision of a physician experienced in the treatment of cancer.
Prior to initiation of treatment with encorafenib in combination with cetuximab, patients must be confirmed to have BRAF V600E mutation-positive disease using a test approved by the National Medical Products Administration (NMPA).
Treatment is not indicated for patients with wild-type BRAF colorectal cancer (CRC).
The recommended dose of encorafenib is 300mg (four 75mg capsules) once daily.
Encorafenib should be administered in combination with cetuximab until disease progression or unacceptable toxicity occurs.
For oral use. Swallow capsules whole with water.
Encorafenib may be taken with or without food.
Grapefruit juice should be avoided during treatment with encorafenib.
If a dose of encorafenib is missed, the missed dose should be taken only if more than 12 hours remain before the next scheduled dose.
If vomiting occurs after taking encorafenib, no replacement dose should be given; the next dose should be taken at the scheduled time.
Pregnancy
No clinical data are available on the use of encorafenib in pregnant women.
Animal studies have shown reproductive toxicity of encorafenib.
The use of encorafenib is not recommended in pregnant women or women of childbearing potential not using effective contraception.
If encorafenib is used during pregnancy, or if the patient becomes pregnant while receiving encorafenib, the patient should be informed of the potential hazard to the fetus.
Lactation
It is unknown whether encorafenib or its metabolites are excreted in human milk.
Therefore, a risk to the breastfed newborn/infant cannot be excluded.
A decision must be made whether to discontinue breastfeeding or to discontinue encorafenib, taking into account the benefit of breastfeeding for the infant and the benefit of therapy for the mother.
Females of Reproductive Potential/Contraception
Females of reproductive potential should use effective contraception during treatment with encorafenib and for at least 1 month after the last dose.
Encorafenib may reduce the effectiveness of hormonal contraceptives.
Therefore, female patients using hormonal contraceptives are advised to use an additional or alternative contraceptive method, such as barrier contraception (e.g., condoms), during treatment and for at least 1 month after the last dose.
Fertility
No data are available on the effect of encorafenib on human fertility.
Results from animal studies indicate that encorafenib may impair fertility in male animals of reproductive potential.
As the clinical relevance is unknown, male patients should be advised of the potential risk of impaired spermatogenesis.
The safety and efficacy of encorafenib in children and adolescents have not been established. No relevant data are available.
No dose adjustment is required in patients aged 65 years and older.
The incidence of adverse reactions leading to dose interruption of encorafenib in patients treated with encorafenib in combination with cetuximab was 33%; the most common adverse reactions included vomiting (4%), fatigue (4%), nausea (4%), pyrexia (3%), and diarrhea (3%).
The incidence of adverse reactions leading to dose reduction of encorafenib was 9%; the most common adverse reactions were fatigue (2%), arthralgia (2%), and peripheral neuropathy (2%).
The incidence of adverse reactions leading to permanent discontinuation of encorafenib was 10%.
Hypersensitivity to the active substance or to any of the excipients.
Encorafenib is intended for administration in combination with cetuximab in patients with BRAF V600E‑mutant metastatic colorectal cancer.
For more information on the warnings and precautions related to cetuximab therapy, refer to the cetuximab prescribing information.
Bleeding events, including major bleeding events, may occur in patients during encorafenib treatment.
Concomitant use of anticoagulants and antiplatelet therapy may increase the risk of hemorrhage.
If a patient experiences a Grade ≥3 bleeding event, dosing should be interrupted or discontinued, and managed according to clinical guidance.
Ocular toxicities reported with encorafenib monotherapy in melanoma patients include uveitis, iritis, and iridocyclitis.
Patients should be evaluated for new or worsening symptoms of visual disturbance at each visit.
If new or worsening visual disturbances are identified, including reduced central visual acuity, blurred vision, or visual loss, prompt ophthalmological evaluation is recommended.
QT interval prolongation has been observed in patients treated with BRAF inhibitors.
A comprehensive QT study to evaluate the potential for encorafenib to prolong the QT interval has not been conducted.
Overall, available data suggest that encorafenib monotherapy may cause a mild increase in heart rate and a small prolongation of the QTc interval.
Insufficient data exist to exclude a clinically relevant, exposure‑dependent QTc prolongation.
Due to the potential risk of QT prolongation, serum electrolyte abnormalities (including magnesium and potassium) should be corrected prior to initiation and during treatment, and risk factors for QT prolongation (e.g., congestive heart failure, bradyarrhythmia) should be managed.
ECG evaluation is recommended prior to initiation of encorafenib, 1 month after initiation, and approximately every 3 months during treatment, or more frequently as clinically indicated.
QTc prolongation may be managed by dose reduction, interruption, or discontinuation, in addition to correcting electrolyte abnormalities and controlling risk factors.
New primary malignancies (cutaneous and non‑cutaneous) have occurred in patients treated with BRAF inhibitors and may occur during encorafenib treatment.
Cutaneous malignancies such as cutaneous squamous cell carcinoma (cuSCC), including keratoacanthoma, and new primary melanoma have been reported in patients treated with BRAF inhibitors including encorafenib (see Adverse Reactions).
Dermatological evaluation is recommended prior to initiation of encorafenib, every 2 months during treatment, and for 6 months after treatment discontinuation.
Suspected cutaneous lesions should be managed with skin excision and histopathological assessment.
Patients should be instructed to promptly notify their physician if new skin lesions develop; encorafenib may be continued without dose adjustment.
Based on its mechanism of action, encorafenib may promote malignancies associated with RAS activation via mutation or other mechanisms.
Patients receiving encorafenib should undergo head and neck examination, chest/abdominal CT, anus and pelvic examination (females), and complete blood count at baseline, during treatment, and at the end of treatment as clinically indicated.
Permanent discontinuation should be considered in patients who develop RAS mutation‑positive non‑cutaneous malignancies.
Benefit‑risk should be carefully considered prior to administering encorafenib to patients with previous or concurrent RAS mutation‑associated cancers.
Hepatic laboratory test abnormalities, including elevations in AST and ALT, have occurred in patients during encorafenib treatment.
Hepatic laboratory values should be monitored prior to initiation, at least monthly for the first 6 months of treatment, and as clinically indicated thereafter.
Hepatic laboratory test abnormalities may be managed by dose interruption, reduction, or discontinuation.
As encorafenib is primarily metabolized and eliminated by the liver, exposure may be increased in patients with mild to severe hepatic impairment within the range of intersubject variability.
In the absence of clinical data, the use of encorafenib is not recommended in patients with moderate or severe hepatic impairment.
Encorafenib should be used with caution in patients with mild hepatic impairment (300 mg once daily dosing regimen).
Close monitoring for encorafenib‑related toxicity, including clinical and liver function tests, and ECG assessment as clinically indicated during treatment, is recommended in patients with mild hepatic impairment.
No data are available in patients with severe renal impairment.
Encorafenib should be used with caution in patients with severe renal impairment.
Increased creatinine has been frequently reported in patients receiving encorafenib monotherapy or in combination with cetuximab.
Reported cases of renal failure (including acute kidney injury and renal impairment) were generally associated with vomiting and dehydration.
Other contributing factors include diabetes mellitus and hypertension.
Serum creatinine should be monitored as clinically indicated, and increased creatinine managed by dose adjustment or discontinuation.
Patients should ensure adequate fluid intake during treatment.
Concomitant use of strong CYP3A4 inhibitors should be avoided during encorafenib treatment.
If a strong CYP3A4 inhibitor must be co‑administered, patients should be closely monitored for safety.
Concomitant use of moderate CYP3A4 inhibitors should be undertaken with caution during encorafenib treatment.
Encorafenib has a minor effect on the ability to drive and use machines.
Visual disturbances have been reported in some patients treated with encorafenib during clinical trials.
Patients who experience visual disturbances or any other adverse reactions that may affect their ability to drive or operate machinery should be advised not to drive or use machines.
For more detailed drug information, please consult the official package leaflet.
If any issues arise, please contact us immediately.
Email:haiousales@gmail.com
Copyright2024@ BIGBEAR All right reserved BIGBEAR
