Zelboraf Generic Name & Formulations
Legal Class
Rx
General Description
Vemurafenib 240mg; tabs.
Pharmacological Class
Kinase inhibitor.
How Supplied
Tabs—112, 120
Manufacturer
Generic Availability
NO
Zelboraf Indications
Indications
Erdheim-Chester Disease (ECD) with BRAF V600 mutation.
Zelboraf Dosage and Administration
Adult
Swallow whole. ≥18yrs: 960mg every 12hrs; continue until disease progression or unacceptable toxicity. Concomitant strong CYP3A4 inducer (if unavoidable): increase dose by 240mg as tolerated (see full labeling). Dose modifications for adverse reactions: see full labeling.
Children
<18yrs: not established.
Zelboraf Contraindications
Not Applicable
Zelboraf Boxed Warnings
Not Applicable
Zelboraf Warnings/Precautions
Warnings/Precautions
Risk of cutaneous squamous cell carcinoma (cuSCC): ≥65yrs, prior skin cancer, chronic sun exposure; if occurs, do excision and evaluate. Perform dermatologic evaluation before therapy, every 2 months during, and consider monitoring 6 months after discontinuation. Monitor for new non-cutaneous SCC and other malignancies. Long QT syndrome or QTc >500ms, uncorrectable electrolyte abnormalities, or concomitant drugs that prolong the QT interval: not recommended. Prior to and following initiation or after dose adjustment for QTc prolongation, evaluate ECG and electrolytes after 15 days, monthly during the 1st 3 months, then every 3 months thereafter, or more as clinically indicated. Severe hepatic or renal impairment. Monitor liver enzymes, bilirubin before initiating and monthly during treatment, or as needed. Measure SCr before initiating and periodically during treatment. Monitor for ophthalmologic reactions routinely. Avoid sun exposure. Embryo-fetal toxicity. Advise females of reproductive potential to use effective contraception during therapy and for at least 2 weeks after final dose. Pregnancy. Nursing mothers: not recommended (during and for 2 weeks after final dose).
Zelboraf Pharmacokinetics
See Literature
Zelboraf Interactions
Interactions
Avoid concomitant strong CYP3A4 inhibitors (eg, itraconazole); if unavoidable, consider dose reduction. Avoid concomitant strong CYP3A4 inducers (eg, phenytoin, carbamazepine, rifampin); use alternatives; if unavoidable, increase dose (see Adult). Avoid concomitant CYP1A2 (eg, tizanidine) and P-gp (eg, digoxin) substrates with narrow therapeutic indices; if unavoidable, consider dose reduction of substrates and monitor. Increased transaminase and bilirubin with concomitant ipilimumab. Concomitant or sequential administration with radiation treatment; monitor closely.
Zelboraf Adverse Reactions
Adverse Reactions
Arthralgia, rash, alopecia, fatigue, photosensitivity, nausea, pruritus, skin papilloma; severe hypersensitivity or dermatologic reactions (permanently discontinue if occur), QT prolongation, hepatotoxicity, uveitis, blurry vision, photophobia, other malignancies, radiation sensitization and recall, renal failure, Dupuytren's contracture (may be severe), plantar fascial fibromatosis.
Zelboraf Clinical Trials
See Literature
Zelboraf Note
Not Applicable
Zelboraf Patient Counseling
See Literature
Zelboraf Generic Name & Formulations
Legal Class
Rx
General Description
Vemurafenib 240mg; tabs.
Pharmacological Class
Kinase inhibitor.
How Supplied
Tabs—112, 120
Manufacturer
Generic Availability
NO
Zelboraf Indications
Indications
Treatment of unresectable or metastatic melanoma with BRAF V600E mutation as detected by an FDA-approved test.
Limitations of Use
Not for treatment of wild-type BRAF melanoma.
Zelboraf Dosage and Administration
Adult
Confirm BRAF V600E mutation-positive melanoma with FDA-approved test before initiating. Swallow whole. ≥18yrs: 960mg every 12hrs; continue until disease progression or unacceptable toxicity. Concomitant strong CYP3A4 inducer (if unavoidable): increase dose by 240mg as tolerated (see full labeling). Dose modifications for adverse reactions: see full labeling.
Children
<18yrs: not established.
Zelboraf Contraindications
Not Applicable
Zelboraf Boxed Warnings
Not Applicable
Zelboraf Warnings/Precautions
Warnings/Precautions
Risk of cutaneous squamous cell carcinoma (cuSCC): ≥65yrs, prior skin cancer, chronic sun exposure; if occurs, do excision and evaluate. Perform dermatologic evaluation before therapy, every 2 months during, and consider monitoring 6 months after discontinuation. Monitor for new non-cutaneous SCC and other malignancies. Long QT syndrome or QTc >500ms, uncorrectable electrolyte abnormalities, or concomitant drugs that prolong the QT interval: not recommended. Prior to and following initiation or after dose adjustment for QTc prolongation, evaluate ECG and electrolytes after 15 days, monthly during the 1st 3 months, then every 3 months thereafter, or more as clinically indicated. Severe hepatic or renal impairment. Monitor liver enzymes, bilirubin before initiating and monthly during treatment, or as needed. Measure SCr before initiating and periodically during treatment. Monitor for ophthalmologic reactions routinely. Avoid sun exposure. Embryo-fetal toxicity. Advise females of reproductive potential to use effective contraception during therapy and for at least 2 weeks after final dose. Pregnancy. Nursing mothers: not recommended (during and for 2 weeks after final dose).
Zelboraf Pharmacokinetics
See Literature
Zelboraf Interactions
Interactions
Avoid concomitant strong CYP3A4 inhibitors (eg, itraconazole); if unavoidable, consider dose reduction. Avoid concomitant strong CYP3A4 inducers (eg, phenytoin, carbamazepine, rifampin); use alternatives; if unavoidable, increase dose (see Adult). Avoid concomitant CYP1A2 (eg, tizanidine) and P-gp (eg, digoxin) substrates with narrow therapeutic indices; if unavoidable, consider dose reduction of substrates and monitor. Increased transaminase and bilirubin with concomitant ipilimumab. Concomitant or sequential administration with radiation treatment; monitor closely.
Zelboraf Adverse Reactions
Adverse Reactions
Arthralgia, rash, alopecia, fatigue, photosensitivity, nausea, pruritus, skin papilloma; severe hypersensitivity or dermatologic reactions (permanently discontinue if occur), QT prolongation, hepatotoxicity, uveitis, blurry vision, photophobia, other malignancies, radiation sensitization and recall, renal failure, Dupuytren's contracture (may be severe), plantar fascial fibromatosis.
Zelboraf Clinical Trials
See Literature
Zelboraf Note
Not Applicable
Zelboraf Patient Counseling
See Literature