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Zelboraf Side Effects Center
Medical Editor: John P. Cunha, DO, FACOEP
Zelboraf (vemurafenib) is a kinase inhibitor used to treat patients with metastatic melanoma with BRAFV600E mutation that is unable to be removed by surgery. Common side effects of Zelboraf include joint pain, tiredness, nausea, hair loss, rash or itching, skin growths, blurred vision, or increased sensitivity of your eyes to light.
The recommended dose of Zelboraf is 960 mg (four 240 mg tablets) twice daily, 12 hours apart. Zelboraf may interact with blood thinners, cyclosporine, sirolimus, tacrolimus, digoxin, theophylline, ADHD medications, antibiotics, antidepressants, antifungals, cancer medicines, ergot drugs, cough medicines, pain medications, heart or blood pressure medications, heart rhythm medications, HIV/AIDS medicines, medicines to treat psychiatric disorders, or seizure medications. Tell your doctor all medications and supplements you use. Do not use Zelboraf if you are pregnant. It could harm the fetus. Use birth control, and tell your doctor if you become pregnant during treatment. It is unknown if this drug passes into breast milk or if it could harm a nursing baby. Breastfeeding is not recommended while you are using Zelboraf.
Our Zelboraf (vemurafenib) Side Effects Drug Center provides a comprehensive view of available drug information on the potential side effects when taking this medication.
This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
What is Patient Information in Detail?
Easy-to-read and understand detailed drug information and pill images for the patient or caregiver from Cerner Multum.
Zelboraf in Detail - Patient Information: Side Effects
Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficult breathing; swelling of your face, lips, tongue, or throat.
Stop using vemurafenib and call your doctor at once if you have a serious side effect such as:
- severe dizziness, fainting, fast or pounding heartbeats;
- white patches on your eyes;
- new or worsening skin lesions; or
- severe skin reaction -- fever, sore throat, swelling in your face or tongue, burning in your eyes, skin pain, followed by a red or purple skin rash that spreads (especially in the face or upper body) and causes blistering and peeling.
Less serious side effects may include:
- joint pain;
- tired feeling;
- hair loss;
- mild rash or itching;
- skin growths; or
- blurred vision, increased sensitivity of your eyes to light.
Read the entire detailed patient monograph for Zelboraf (Vemurafenib)
What is Prescribing information?
The FDA package insert formatted in easy-to-find categories for health professionals and clinicians.
Zelboraf FDA Prescribing Information: Side Effects
The following adverse reactions are discussed in greater detail in other sections of the label:
- New Primary Malignancies [see WARNINGS AND PRECAUTIONS]
- Hypersensitivity Reactions [see WARNINGS AND PRECAUTIONS]
- Dermatologic Reactions [see WARNINGS AND PRECAUTIONS]
- QT Prolongation [see WARNINGS AND PRECAUTIONS]
- Hepatotoxicity [see WARNINGS AND PRECAUTIONS]
- Photosensitivity [see WARNINGS AND PRECAUTIONS]
- Ophthalmologic Reactions [see WARNINGS AND PRECAUTIONS]
- Radiation Sensitization and Radiation Recall [see WARNINGS AND PRECAUTIONS]
- Renal Failure [see WARNINGS AND PRECAUTIONS]
Clinical 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.
This section describes adverse drug reactions (ADRs) identified from analyses of Trial 1 and Trial 2 [see Clinical Studies]. Trial 1 randomized (1:1) 675 treatment-naive patients with unresectable or metastatic melanoma to receive ZELBORAF 960 mg orally twice daily or dacarbazine 1000 mg/m² intravenously every 3 weeks. In Trial 2, 132 patients with metastatic melanoma and failure of at least one prior systemic therapy received treatment with ZELBORAF 960 mg orally twice daily.
Table 1 presents adverse reactions reported in at least 10% of 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.
Table 1 Adverse Reactions Reported in ≥ 10%
of Patients Treated with ZELBORAF*
|ADRs||Trial 1: Treatment-Naive Patients||Trial 2: Patients with Failure of at Least One Prior Systemic Therapy|
|All Grades (%)||Grade 3a (%)||All Grades (%)||Grade 3 (%)||All Grades (%)||Grade 3a (%)|
|Skin and subcutaneous tissue disorders|
|Rash maculo-papular||9||2||< 1||0||21||6|
|Rash papular||5||< 1||0||0||13||0|
|Musculoskeletal and connective tissue disorders|
|Myalgia||13||< 1||1||0||24||< 1|
|Pain in extremity||18||< 1||6||2||9||0|
|Musculoskeletal pain||8||0||4||< 1||11||0|
|Back pain||8||< 1||5||< 1||11||< 1|
|General disorders and administration site conditions|
|Edema peripheral||17||< 1||5||0||23||0|
|Pvrexia||19||< 1||9||< 1||17||2|
|Asthenia||11||< 1||9||< 1||2||0|
|Diarrhea||28||< 1||13||< 1||29||< 1|
|Nervous svstem disorders|
|Neoplasms benign, malignant and unspecified (includes cysts and polyps)|
|Skin papilloma||21||< 1||0||0||30||0|
|Cutaneous SCCT†#||24||22||< 1||< 1||24||24|
|Seborrheic keratosis||10||< 1||1||0||14||0|
|Metabolism and nutrition disorders|
|Decreased appetite||18||0||8||< 1||21||0|
|Respiratory, thoracic and mediastinal disorders|
|Injury, poisoning and procedural complications|
|*Adverse drug reactions, reported using MedDRA and graded
using NCI-CTC -AEv 4.0 (NCI common toxicity criteria) for assessment o f
a Grade 4 adverse reactions limited to gamma-glutamyltransferase increased ( < 1% in T rial 1 and 4% in T rial 2).
† Includes both squamous cell carcinoma o f the skin and keratoacanthoma.
# Cases o f cutaneous squamous cell carcinoma were required to be reported as Grade 3 per protocol.
Clinically relevant adverse reactions reported in < 10% of patients treated with ZELBORAF in the Phase 2 and Phase 3 studies include:
Musculoskeletal and connective tissue disorders: arthritis
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.
Table 2 : Change from Baseline to Grade 3/4 Liver
|Parameter||Change From Baseline to Grade 3/4|
|ZELBORAF (%)||Dacarbazine (%)|
|* For A L T , alkaline phosphatase, and bilirubin, there were no patients with a change to Grade 4 in either treatment arm.|
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.
Blood and lymphatic systems disorder: Neutropenia
Injury, poisoning and procedural complications: Radiation sensitization and recall [see WARNINGS AND PRECAUTIONS].
Gastrointestinal disorders: Pancreatitis
Read the entire FDA prescribing information for Zelboraf (Vemurafenib)
Additional Zelboraf Information
Report Problems to the Food and Drug Administration
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