Brand Name
Zelboraf
Generic Name
Vemurafenib
View Brand Information FDA approval date: August 17, 2011
Classification: Kinase Inhibitor
Form: Tablet
What is Zelboraf (Vemurafenib)?
ZELBORAF ® is a kinase inhibitor indicated for the treatment of patients with unresectable or metastatic melanoma with BRAF V600E mutation as detected by an FDA-approved test.
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Brand Information
ZELBORAF (Vemurafenib)
1DOSAGE FORMS AND STRENGTHS
Tablet: 240 mg.
2CONTRAINDICATIONS
None.
3ADVERSE REACTIONS
The following adverse reactions are discussed in greater detail in other sections of the label:
- New Primary Malignancies
- Hypersensitivity Reactions
- Dermatologic Reactions
- QT Prolongation
- Hepatotoxicity
- Photosensitivity
- Ophthalmologic Reactions
- Radiation Sensitization and Radiation Recall
- Renal Failure
- Dupuytren's Contracture and Plantar Fascial Fibromatosis
3.1Clinical Trials Experience
Because clinical studies are conducted under widely varying conditions, adverse reaction rates observed in the clinical studies of a drug cannot be directly compared to rates in the clinical studies of another drug and may not predict the rates observed in a broader patient population in clinical practice.
Unresectable or Metastatic Melanoma with BRAF V600E Mutation This section describes adverse drug reactions (ADRs) identified from analyses of Trial 1 and Trial 2
Table 1 presents adverse reactions reported in at least 10% of unresectable or metastatic melanoma patients treated with ZELBORAF. The most common adverse reactions of any grade (≥ 30% in either study) in ZELBORAF-treated patients were arthralgia, rash, alopecia, fatigue, photosensitivity reaction, nausea, pruritus, and skin papilloma. The most common (≥ 5%) Grade 3 adverse reactions were cuSCC and rash. The incidence of Grade 4 adverse reactions was ≤ 4% in both studies.
The incidence of adverse events resulting in permanent discontinuation of study medication in Trial 1 was 7% for the ZELBORAF arm and 4% for the dacarbazine arm. In Trial 2, the incidence of adverse events resulting in permanent discontinuation of study medication was 3% in ZELBORAF-treated patients. The median duration of study treatment was 4.2 months for ZELBORAF and 0.8 months for dacarbazine in Trial 1, and 5.7 months for ZELBORAF in Trial 2.
Clinically relevant adverse reactions reported in < 10% of unresectable or metastatic melanoma patients treated with ZELBORAF in the Phase 2 and Phase 3 studies include:
Skin and subcutaneous tissue disorders: palmar-plantar erythrodysesthesia syndrome, keratosis pilaris, panniculitis, erythema nodosum, Stevens-Johnson syndrome, toxic epidermal necrolysis
Musculoskeletal and connective tissue disorders: arthritis, Dupuytren's contracture
Nervous system disorders: neuropathy peripheral, VIIth nerve paralysis
Neoplasms benign, malignant and unspecified (includes cysts and polyps): basal cell carcinoma, oropharyngeal squamous cell carcinoma
Infections and infestations: folliculitis
Eye disorders: retinal vein occlusion
Vascular disorders: vasculitis
Cardiac disorders: atrial fibrillation
Table 2 shows the incidence of worsening liver laboratory abnormalities in Trial 1 summarized as the proportion of patients who experienced a shift from baseline to Grade 3 or 4.
3.2Postmarketing Experience
The following adverse reactions have been identified during post approval use of ZELBORAF. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure.
Neoplasms benign, malignant and unspecified (incl. cysts and polyps): Progression of pre-existing chronic myelomonocytic leukemia with NRAS mutation [see .
Skin and subcutaneous tissue disorders: Drug reaction with eosinophilia and systemic symptoms (DRESS syndrome) [see .
Blood and lymphatic systems disorder: Neutropenia
Injury, poisoning and procedural complications: Radiation sensitization and recall [see
Gastrointestinal disorders: Pancreatitis
Renal and urinary disorders: Acute interstitial nephritis, acute tubular necrosis [see
Musculoskeletal and connective tissue disorders: Dupuytren's contracture and plantar fascial fibromatosis [see
4OVERDOSAGE
There is no information on overdosage of ZELBORAF.
5DESCRIPTION
ZELBORAF (vemurafenib) is a kinase inhibitor available as 240 mg tablets for oral use. Vemurafenib has the chemical name propane-1-sulfonic acid {3-[5-(4-chlorophenyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl]- 2,4-difluoro-phenyl}-amide. It has the molecular formula C
Vemurafenib is a white to off-white crystalline solid. It is practically insoluble in aqueous media.
Tablets of ZELBORAF are for oral administration. Each tablet contains 240 mg of vemurafenib.
The inactive ingredients of ZELBORAF are:
6HOW SUPPLIED/STORAGE AND HANDLING
ZELBORAF (vemurafenib) is supplied as 240 mg film-coated tablets with VEM debossed on one side. The following packaging configurations are available:
NDC 50242-090-01 single bottle of 120 count
NDC 50242-090-02 single bottle of 112 count
7PATIENT COUNSELING INFORMATION
Advise the patient to read the FDA-approved patient labeling (
Healthcare providers should advise patients of the potential benefits and risks of ZELBORAF and instruct their patients to read the
- Evidence of BRAF V600E mutation in the tumor specimen with an FDA approved test is necessary to identify patients with melanoma for whom treatment with ZELBORAF is indicated
- ZELBORAF increases the risk of developing new primary cutaneous malignancies. Advise patients of the importance of contacting their healthcare provider immediately for any changes in their skin
- Anaphylaxis and other serious hypersensitivity reactions can occur during treatment and upon re- initiation of treatment with ZELBORAF. Advise patients to stop taking ZELBORAF and to seek immediate medical attention for symptoms of anaphylaxis or hypersensitivity
- Severe dermatologic reactions can occur in patients receiving ZELBORAF. Advise patients to stop taking ZELBORAF and to contact their health-care provider for severe dermatologic reactions
- ZELBORAF can prolong QT interval, which may result in ventricular arrhythmias. Advise patients of the importance of monitoring of their electrolytes and the electrical activity of their heart (via an ECG) during ZELBORAF treatment
- Liver injury leading to functional hepatic impairment, including coagulopathy or other organ dysfunction, can occur with ZELBORAF. Advise patients of the importance of laboratory monitoring of their liver during ZELBORAF treatment and to contact their health-care provider for relevant symptoms
- ZELBORAF can cause mild to severe photosensitivity. Advise patients to avoid sun exposure, wear protective clothing, and use a broad spectrum UVA/UVB sunscreen and lip balm (SPF ≥ 30) when outdoors to help protect against sunburn
- Ophthalmologic reactions can occur in patients treated with ZELBORAF. Advise patients to contact their health-care provider immediately for ophthalmologic symptoms
8PRINCIPAL DISPLAY PANEL - 240 mg Tablet Bottle Carton
NDC 50242-090-02
Zelboraf
(vemurafenib)
tablets
(vemurafenib)
tablets
240 mg
Do not crush or chew tablet.
Rx only
Attention Pharmacist: Dispense the
112 tablets
Genentech | Daiichi Sankyo, Inc.
10210025
