Vemurafenib

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Vemurafenib

ZELBORAF

نام تجاری

Hoffmann-La Roche Inc.

شرکت تولید کننده

Inhibitor of some mutated forms of BRAF serine-threonine kinase, including BRAF-V600E

Also inhibits other kinases in vitro (eg, CRAF, ARAF, wild-type BRAF, SRMS, ACK1, MAP4K5, FGR

مکانیسم اثر

FDA : On August 17, 2011 approved vemurafenib tablets for the treatment of patients with unresectable or metastatic melanoma with the BRAFV600E mutation as detected by an FDA-approved test.

تأییدات بین المللی

(FDA, NICE,…..)

late-stage or unresectable melanoma

اندیکاسیون ها دوز دارو و فواصل تجویز

Roche Molecular Systems, Inc.

international randomized open-label trial in patients with previously untreated metastatic or unresectable melanoma with the BRAFV600E mutation as detected by the cobas 4800 BRAF V600 Mutation Test

 

 

مطالعاتی که بر اساس آن تائیدیه گرفته است

۹۶۰ mg, orally twice daily administered approximately 12 hours apart, with or without a meal

نحوه‌ی تجویز

Film coated tablet: 240 mg

اشکال دارویی

 

قیمت

۳۰%: arthralgia, rash, alopecia, fatigue, photosensitivity reaction, and nausea.

۲۴%: Cutaneous squamous cell carcinomas (cuSCC), including squamous cell carcinomas of the skin and keratoacanthomas

 

Arthralgia (53-67%), Fatigue (38-54%), Rash (37-52%), Photosensitivity (33-49%), Alopecia (36-45%), Nausea (35-37%), Pruritus (23-30%), Skin papilloma (21-30%), Diarrhea (28-29%), Hyperkeratosis (24-28%), Headache (23-27%), Vomiting (18-26%), Cutaneous squamous cell, carcinoma (24%), Myalgia (13-24%), Peripheral edema (17-23%), Decreased appetite (18-21%), Maculopapular rash (9-21%), Pyrexia (17-19%), Dry skin (16-19%), Pain in extremity (9-18%), Actinic keratosis (8-17%), Constipation (12-16%), Increased gamma-glutamyltrasferase [GGT] (5-15%), Dysgeusia (11-14%), Sunburn (10-14%), Erythema (8-14%), Papular rash (5-13%), Cough (8-12%), Musculoskeletal and back pain (8-11%), Asthenia (2-11%)

عوارض شایع

hypersensitivity, Stevens-Johnson syndrome, toxic epidermal necrolysis, uveitis, QT prolongation, and liver enzyme laboratory abnormalities

عوارض شدید

None

کنترااندیکاسیون

۱- BRAF mutation test required to confirm eligibility for treatment; has not been studied with wild-type BRAF melanoma

۲- Discontinue in patients who experience severe hypersensitivity reactions, Stevens-Johnson syndrome and toxic epidermal necrolysis reported

۳-QT prolongation:

Monitor ECG and electrolytes before treatment initiation and after dose modification

Monitor ECGs at day 15, monthly during the first 3 months of treatment, and then q3Months thereafter, or more often as clinically indicated

If the QTc exceeds 500 ms, temporarily interrupt treatment, correct electrolyte abnormalities, and control for cardiac risk factors for QT prolongation (see Dose Modifications)

•Permanent discontinuation recommended if after correction of associated risk factors, QTc increase meets values of both > 500 ms and > 60 ms change from pre-treatment values

۴- Elevated liver enzymes:

monitor liver enzymes and bilirubin before treatment initiation and then monthly or as clinically indicated

۵-Mild-to-moderate photosensitivity:

avoid sun exposure and wear protective clothing and use a broad spectrum UVA/UVB sunscreen and lip balm (SPF >30) when outdoors

۵-Avoid in pregnancy

موارد احتیاط

Based on in vitro data, vemurafenib is a substrate of CYP3A4, and therefore, concomitant administration of strong CYP3A4 inhibitors or inducers may alter vemurafenib concentrations. Strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, clarithromycin, atazanavir, nefazodone, saquinavir, telithromycin, ritonavir, indinavir, nelfinavir, voriconazole) and inducers (e.g., phenytoin, carbamazepine, rifampin, rifabutin, rifapentine, phenobarbital) should be used with caution when coadministered with ZELBORAF.

تداخل دارویی

 

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