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Zelboraf

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Zelboraf

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 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;
  • nausea;
  • hair loss;
  • mild rash or itching;
  • skin growths; or
  • blurred vision, increased sensitivity of your eyes to light.

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.

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
(Adverse Reactions)

SIDE EFFECTS

The following adverse reactions are discussed in greater detail in other sections of the label:

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
ZELBORAF
n=336
Dacarbazine
n=287
ZELBORAF
n=132
All Grades (%) Grade 3a (%) All Grades (%) Grade 3 (%) All Grades (%) Grade 3a (%)
Skin and subcutaneous tissue disorders
Rash 37 8 2 0 52 7
Photosensitivity reaction 33 3 4 0 49 3
Alopecia 45 < 1 2 0 36 0
Pruritus 23 1 1 0 30 2
Hyperkeratosis 24 1 < 1 0 28 0
Rash maculo-papular 9 2 < 1 0 21 6
Actinic keratosis 8 0 3 0 17 0
Dry skin 19 0 1 0 16 0
Rash papular 5 < 1 0 0 13 0
Erythema 14 0 2 0 8 0
Musculoskeletal and connective tissue disorders
Arthralgia 53 4 3 < 1 67 8
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
Fatigue 38 2 33 2 54 4
Edema peripheral 17 < 1 5 0 23 0
Pyrexia 19 < 1 9 < 1 17 2
Asthenia 11 < 1 9 < 1 2 0
Gastrointestinal disorders
Nausea 35 2 43 2 37 2
Diarrhea 28 < 1 13 < 1 29 < 1
Vomiting 18 1 26 1 26 2
Constipation 12 < 1 24 0 16 0
Nervous system disorders
Headache 23 < 1 10 0 27 0
Dysgeusia 14 0 3 0 11 0
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
Investigations
Gamma-glutamyltransferase increased 5 3 1 0 15 6
Metabolism and nutrition disorders
Decreased appetite 18 0 8 < 1 21 0
Respiratory, thoracic and mediastinal disorders
Cough 8 0 7 0 12 0
Injury, poisoning and procedural complications
Sunburn 10 0 0 0 14 0
*Adverse drug reactions, reported using MedDRA and graded using NCI-CTC-AE v 4.0 (NCI common toxicity criteria) for assessment of toxicity.
aGrade 4 adverse reactions limited to gamma-glutamyltransferase increased ( < 1% in Trial 1 and 4% in Trial 2).
† Includes both squamous cell carcinoma of the skin and keratoacanthoma.
#Cases of 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:

Skin and subcutaneous tissue disorders: palmar-plantar erythrodysesthesia syndrome, keratosis pilaris, erythema nodosum, Stevens-Johnson syndrome, toxic epidermal necrolysis

Musculoskeletal and connective tissue disorders: arthritis

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.

Table 2 : Change From Baseline to Grade 3/4 Liver Laboratory Abnormalities*

Parameter Change From Baseline to Grade 3/4
ZELBORAF (%) Dacarbazine (%)
GGT 11.5 8.6
AST 0.9 0.4
ALT 2.8 1.9
Alkaline phosphatase 2.9 0.4
Bilirubin 1.9 0
* For ALT, alkaline phosphatase, and bilirubin, there were no patients with a change to Grade 4 in either treatment arm.

Postmarketing Experience

The following adverse reactions have been identified during postapproval 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 a pre-existing chronic myelomonocytic leukemia with NRAS mutation.

Skin and Subcutaneous Tissue Disorders: Drug reaction with eosinophilia and systemic symptoms (DRESS syndrome).

Read the entire FDA prescribing information for Zelboraf (Vemurafenib) »

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