Vemurafenib

ZELBORAF

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Pronunciation: vem-yoo-RAF-e-nib (ZEL-bor-raf)

Vemurafenib ballicule: receptor binding, kinetics and half-life diagram — Mechanism of action: Vemurafenib ballicule

What it isBRAF V600 kinase inhibitor; BRAF-mutant melanoma.

Why this oneRapid and often dramatic tumor regression within weeks.

What limits itSevere photosensitivity, and paradoxical squamous cell carcinomas in a quarter of patients. Resistance emerges within months unless a MEK inhibitor is added.

Vemurafenib molecular structure (skeletal formula) — Molecular structure: Vemurafenib

FDA-approved for

BRAF+ melanoma (2011)

FDA label

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FDA dosing	Population	Start	Target	Max
BRAF V600E-mutation melanoma (unresectable/metastatic) and Erdheim-Chester disease	Adults	960 mg BID (~12 h apart)	960 mg BID	960 mg BID

Renal Undefined

Hepatic Undefined

Missed dose may be taken up to 4 h before the next dose; do not take an extra dose after vomiting.

Instructions

Confirm BRAF V600E mutation before initiating
With or without a meal, ~12 h apart; do not crush or chew
A missed dose can be taken up to 4 h before the next dose; skip the extra dose if vomiting occurs
Unavoidable strong CYP3A4 inducer: increase dose by 240 mg as tolerated

Available strengths

tab 240 mg

Cautions

New primary cutaneous and non-cutaneous malignancies
Tumor promotion in BRAF wild-type melanoma
Serious hypersensitivity/anaphylaxis and DRESS
Severe dermatologic reactions (SJS/TEN)
QT prolongation (monitor ECG/electrolytes)
Hepatotoxicity
Photosensitivity
Ophthalmologic reactions (uveitis)
Embryo-fetal toxicity
Radiation sensitization and recall
Renal failure
Dupuytren's contracture and plantar fascial fibromatosis

Adverse reactions

Arthralgia
Rash
Alopecia
Fatigue
Photosensitivity reaction
Nausea
Pruritus
Skin papilloma

Pregnancy Can cause fetal harm based on mechanism; placental transfer reported.

Lactation Do not breastfeed during treatment and for 2 weeks after the final dose.

Cost

Vemurafenib (ZELBORAF)

Strength		#/mo	generic $/mo	CostPlus
240 mg	tab	60 BID		not offered

NADAC is a voluntary CMS survey of what retail community pharmacies pay for the drugs they stock. Vemurafenib is dispensed outside retail pharmacies, so it rarely appears on surveyed invoices.

Generic entry2032 est.

NO BOXED WARNINGS

Principal riskPhotosensitivity; paradoxical squamous carcinomas

Classes and tags

Clinical profile

Therapeutic safety burden3 / 4

Overdose danger2 / 4

Weight-gain liability0 / 4

Sedation liability0 / 4

QT / Torsades3 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk3 / 4

Legacy pregnancy categoryD

Defining liabilityMyelosuppression and agent-specific hepatic, cardiac, pulmonary, neurologic or reproductive toxicity require oncology monitoring.

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