Drug reference

Vemurafenib

Tyrosine Kinase Inhibitor · Antineoplastic agent

Tyrosine Kinase InhibitorAntineoplastic agent

CDSCO approvedSchedule H

EXCRETION

—

not curated

INTERACTIONS

12 major

SEVERE in our sources

PREGNANCY

Manufacturer advises avoid unless

FDA category + note

Top interactionssee all 12 →

AbarelixSevereDatabaseDDInter
AbirateroneSevereDatabaseDDInter
AdenosineSevereDatabaseDDInter
AlfuzosinSevereDatabaseDDInter

Mechanism

BRAF mutations lead to constitutive activation of BRAF kinase, which in turn activates downstream signaling pathways involved in cell growth and proliferation. Vemurafenib is a highly selective small molecule inhibitor of BRAF V600E and V600K mutations, thereby inhibiting these activated pathways.

Indications

Metastatic melanoma (with BRAF V600E and V600K mutations)BRAF V600 mutation-positive unresectable or metastatic melanoma (in combination with cobimetinib)melanoma in patients whose tumors express the mutant BRAF V600Eother tumors (e.g., thyroid cancer, hairy cell leukemia) that express BRAF V600Esystemic therapy of thyroid cancers with BRAF V600E driver mutationredifferentiation therapy to induce radioiodine uptake in non–iodine-avid thyroid cancers with BRAF V600Emetastatic melanoma harboring activating BRAF (V600E/K) mutationsErdheim-Chester disease (rare blood cancer)melanomas that harbor a mutation at position 600 in BRAFChemotherapy-refractory Hairy Cell LeukemiaBRAF V600E mutated Langerhans Cell Histiocytosis

Dosing

Adult: l INDICATIONS AND DOSE Treatment of BRAF V600 mutation-positive unresectable or metastatic melanoma (in combination with vemurafenib) (specialist use only) ▶ BY MOUTH ▶ Adult: 60 mg once daily for 21 days; subsequent cycles repeated after a 7-day interval, for dose adjustment due to side-effects—consult product literature IMPORTANT SAFETY INFORMATION RISKS OF INCORRECT DOSING OF ORAL ANTI-CANCER M…

Pharmacokinetics

Half-life

57 h (elimination)

Metabolism

CYP3A4 (substrate)

Contraindications

patients with melanoma carrying wild-type BRAF

Side effects

Common

cutaneous events (30%–60% of patients)arthralgiafatiguenauseaincreased photosensitivity reactionsheadachepyrexiaarthralgiashyperproliferative skin lesions (e.g., squamous cell skin cancers)

Serious