Vemurafenib

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.

Brands
Adult Dose
Dose: 480 to 960 mg
Single Dose: 720 (720)
Frequency: 2 hourly
Route: PO
Instructions: 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)
Neonatal
Paedriatic
Characteristics
It belongs to Antineoplastic pharmacological group.
Contraindications
Vemurafenib is contraindicated in conditions like Hypersensitivity.
Effects
The severe or irreversible adverse effects of Vemurafenib, which give rise to further complications include Photosensitivity, Epidermal necrolysis, Hypersensitivity reactions, Uveitis.Vemurafenib produces potentially life-threatening effects which include Stevens Johnson syndrome, QT prolongation. which are responsible for the discontinuation of Vemurafenib therapy.The symptomatic adverse reactions produced by Vemurafenib are more or less tolerable and if they become severe, they can be treated symptomatically, these include Headache, Fatigue, Nausea, Vomiting, Alopecia, Anorexia, Diarrhea, Myalgia, Constipation, Maculopapular rash, Pruritus, Erythema, Hypotension, Cough, Asthenia, Arthralgia, Dry skin, Peripheral neuropathy, Folliculitis, Pyrexia, Vasculitis, Musculoskeletal pain, Dysgeusia, Pain in upper & lower extremities, Back pain.
Indications
Vemurafenib is primarily indicated in conditions like Malignant melanoma.
Interactions
Vemurafenib is known to interact with other drugs, the details of drug interactions is as follows:DrugDetailsSeverityOnsetManagementAtazanavirAtazanavir inhibits P-gp, glucuronidation and CYP3A4, and increases plasma concentration of Vemurafenib.CarbamazepineCarbamazepine induces P-gp and CYP3A4.KetoconazoleKetoconazole inhibits P-gp, glucuronidation and CYP3A4, and increases plasma concentration of Vemurafenib.Nefazodone (HCl)Nefazodone inhibits P-gp, glucuronidation and CYP3A4, and increases plasma concentration of Vemurafenib.Phenytoin (Na)Phenytoin induces P-gp and CYP3A4.RifabutinRifabutin induces P-gp and CYP3A4.RifampicinRifampin induces P-gp and CYP3A4.RitonavirRitonavir inhibit P-gp, glucuronidation and CYP3A4, and increases plasma concentration of Vemurafenib.SaquinavirSaquinavir inhibits P-gp, glucuronidation and CYP3A4, and increases plasma concentration of Vemurafenib.St.Johns Wort ExtractSt.Johns Wort induces P-gp and CYP3A4.TelithromycinTelithromycin inhibits P-gp, glucuronidation and CYP3A4, and increases plasma concentration of Vemurafenib.VORICONAZOLEStrong CYP3A4 inhibitors may increase levels of vemurafenib. Monitor concomitant therapy closely.Warfarin (Na)Vemurafenib increases the plasma concentration of Warfarin. These interactions are sometimes beneficial and sometimes may pose threats to life. Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.
Interfrence
Risks
Drug should not be given to Paediatrics, Pregnant Mothers, patients suffering from Kidney dysfunction, and patients suffering from Liver Malfunction.If prescribing authority justifies the benefits of the drug against the possible damages he/she should reevaluate them and consult the reference material and previous studies.
Storage
Store . Protect from Moisture.
Warnings
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.
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