VEMURAFENIB

Targeted Cancer Therapy

Brand names: ZELBORAF

Oral

Mechanism of Action

12.1 Mechanism of Action Vemurafenib is a low molecular weight, orally available inhibitor of some mutated forms of BRAF serine- threonine kinase, including BRAF V600E. Vemurafenib also inhibits other kinases in vitro such as CRAF, ARAF, wild-type BRAF, SRMS, ACK1, MAP4K5, and FGR at similar concentrations. Some mutations in the BRAF gene including V600E result in constitutively activated BRAF proteins, which can cause cell proliferation in the absence of growth factors that would normally be required for proliferation. Vemurafenib has anti-tumor effects in cellular and animal models of melanomas with mutated BRAF V600E.

Indications

2.1 ) ZELBORAF ® is indicated for the treatment of patients with Erdheim- Chester Disease with BRAF V600 mutation. ( 1.2

2.1 ) Limitation of Use: ZELBORAF is not indicated for treatment of patients with wild-type BRAF melanoma ( 2.1

Contraindications

• 4 CONTRAINDICATIONS None. None

FDA Warnings

5 WARNINGS AND PRECAUTIONS New Primary Cutaneous Malignancies: Perform dermatologic evaluations prior to initiation of therapy, every 2 months while on therapy, and for up to 6 months following discontinuation of ZELBORAF
Serious Hypersensitivity Reactions including anaphylaxis and Drug Reaction with Eosinophilia and Systemic Symptoms (DRESS Syndrome): Discontinue ZELBORAF for severe hypersensitivity reactions
Correct electrolyte abnormalities and control for cardiac risk factors for QT prolongation
7 ) Serious Ophthalmologic Reactions: Monitor for signs and symptoms of uveitis

Known Side Effects

11 documented side effects by frequency

Rash

>10%

Joint Pain

1-10%

Fatigue

1-10%

Diarrhea

1-10%

Nausea

1-10%

Fever

1-10%

Hair Loss

0.1-1%

Decreased Appetite

0.1-1%

Vomiting

0.1-1%

Sun Sensitivity

0.1-1%

Itching

0.1-1%

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Compare With

14 available comparisons

Formulations

Dosage Forms

Tablet

Route

Oral