Vemurafenib

Drug #2253

Vemurafenib is a low molecular weight, orally available antineoplastic agent, inhibitor of BRAF serine-threonine kinase. Vemurafenib is indicated for BRAF V600 mutation-positive unrescectable or metastatic melanoma. Mutations in the BRAF gene which substitute the valine at amino acid position 600 results in constitutively activated BRAF proteins, which can cause cell proliferation in the absence of growth factors that would normally be required for proliferation.

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Primary Characteristics

It is classified in Antineoplastic pharmacological group.

Non-proprietary name: Vemurafenib.

Pharmacokinetics

Distribution: Vemurafenib has a plasma protein binding is 99%.

Elimination: it is metabolised via hepatic, plasma half-life is 51.6 hours, renal excretion is <1%, 94% in feaces, unchanged in bile.

Indications

Vemurafenib is primarily indicated in conditions like Malignant melanoma.

Contraindications

Vemurafenib is contraindicated in conditions like Hypersensitivity.

Dosage

Vemurafenib's dosage details are as follows:

Dose	Single Dose	Frequency	Route	Instructions
Adult Dosage
720 mg	720 mg	Every 2h	PO	It can be taken with or without food. Missed doses can be taken 4 hours prior to the next dose. QTc prolongation may require dose reduction (i.e. 480mg)
Paediatric Dosage (20kg)
No data.
Neonatal Dosage (3kg)
No data.

Drug Interactions

13 interactions

Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.

Side Effects

Vemurafenib in overdosage may give rise to further complications which include Epidermal necrolysis , Photosensitivity , Uveitis, Hypersensitivity reactions .

Vemurafenib produces potentially life-threatening effects which include Stevens Johnson syndrome, QT prolongation. Careful monitoring is needed with proper medical management.

Vemurafenib is known to cause more or less tolerable side effects which are usually transient. These include Alopecia, Anorexia , Arthralgia, Asthenia , Back pain, Constipation , Cough , Diarrhea, Dry skin, Dysgeusia, Erythema, Fatigue, Folliculitis, Headache, Hypotension , Maculopapular rash, Musculoskeletal pain , Myalgia, Nausea, Pain in upper & lower extremities, Peripheral neuropathy, Pruritus , Pyrexia , Vasculitis, Vomiting .

Warnings / Precautions

Patient must have BRAF V600 mutation-positive tumor status. Discontinue if hypersensitivity, dermatologic reactions occur. it is not recommended in patients with electrolyte abnormalities, QTc prolongation. Patients with moderate-severe renal/hepatic impairment requires close monitoring. Women of child bearing potential should recieve an effective means of contraception. Patients should be aware of possible fatigue or eye problem.

Available Brands

None recorded.

Storage Conditions

Vemurafenib should be stored .