Zelboraf

— THERAPEUTIC CATEGORIES —
  • Leukemias, lymphomas, and other hematologic cancers
  • Melanoma and other skin cancers

Zelboraf Generic Name & Formulations

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

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