Vemurafenib

DEA Class; Rx

Common Brand Names; Zelboraf

• Antineoplastics, BRAF Kinase Inhibitor

Indicated for treatment of unresectable or metastatic melanoma with BRAF-V600E mutation as detected by an FDA-approved test

Indicated for the treatment of Erdheim-Chester Disease (ECD) with BRAF V600 mutation

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• Arthralgia (82%)
• Maculopapular rash (59%)
• Alopecia (55%) Fatigue (55%)
• Skin papilloma (55%)
• QT prolongation (55%)
• Hyperkeratosis (50%)
• Diarrhea (50%)
• Dry skin (45%)
• Seborrheic keratosis (41%)
• Photosensitivity reaction (41%)
• Palmar-plantar erythrodysesthesia syndrome (41%)
• Pruritus (36%) SCC of skin (36%)
• Peripheral sensory neuropathy (36%)
• Cough (36%) Hypertension (36%)
• Nausea (32%)
• Actinic keratosis (32%)
• Keratosis pilaris (32%)
• Rash papular (23%)
• Vomiting (23%)
• Melanocytic nevus (23%)
• Sunburn (23%)
• Keratoacanthoma (<20%)
• Dupuytren’s contracture (<20%)

Anaphylaxis and other serious hypersensitivity reactions reported during treatment and upon reinitiation, including generalized rash and erythema, hypotension, and drug reaction with eosinophilia and systemic symptoms (DRESS syndrome); permanently discontinue

Severe dermatologic reactions, including Stevens-Johnson syndrome and toxic epidermal necrolysis reported; discontinue treatment

Elevated liver enzymes may occur; monitor liver enzymes and bilirubin before treatment initiation and then monthly or as clinically indicated

Liver injury leading to functional hepatic impairment, including coagulopathy or other organ dysfunction, can occur with vemurafenib

Mild-to-moderate photosensitivity reported; advise patients to avoid sun exposure and wear protective clothing and use a broad spectrum UVA/UVB sunscreen and lip balm (SPF >30) when outdoors

Serious ophthalmologic reactions, including uveitis, iritis, blurry vision, photophobia, and retinal vein occlusion reported

Based on mechanism of action, can cause fetal harm when administered to pregnant women; avoid use during pregnancy and use effective contraception (see Pregnancy

Severe cases of radiation sensitization and recall reported

Renal failure, including acute interstitial nephritis and acute tubular necrosis reported; measure serum creatinine before initiation of therapy and periodically during treatment

Dupuytren’s contracture and plantar fascial fibromatosis reported; majority of cases, mild to moderate, but severe disabling cases of Dupuytren’s contracture also reported

There are no available data on the use of vemurafenib in pregnant women to determine the drug-associated risk

There is no information available regarding presence of vemurafenib in human milk, effects on breastfed infant, or effects on milk production

Vemurafenib 

tablet

• 240mg