What type of inhibitor is vemurafenib?

An orally bioavailable, ATP-competitive, small-molecule inhibitor of BRAF(V600E) kinase with potential antineoplastic activity.

Who manufactures vemurafenib?

Roche (SIX: RO, ROG; OTCQX: RHHBY) today announced that the U.S. Food and Drug Administration (FDA) approved Zelboraf (vemurafenib) for the treatment of BRAF V600E mutation-positive, inoperable or metastatic melanoma, as determined by an FDA-approved test.

How is vemurafenib administered?

The recommended dose of ZELBORAF is 960 mg (four 240 mg tablets) orally every 12 hours with or without a meal. A missed dose can be taken up to 4 hours prior to the next dose. Treat patients with ZELBORAF until disease progression or unacceptable toxicity occurs.

How much does vemurafenib cost?

Vemurafenib, the first drug in this class, costs $13,000 per month ($207,000 for a patient with median survival).

How does BRAF inhibitor work?

The BRAF inhibitors vemurafenib, dabrafenib and encorafenib are used in the treatment of patients with BRAF-mutant melanoma. They selectively target BRAF kinase and thus interfere with the mitogen-activated protein kinase (MAPK) signalling pathway that regulates the proliferation and survival of melanoma cells.

How effective is vemurafenib?

Vemurafenib has prolonged efficacy in patients with BRAF V600–mutant NSCLC (n = 62), as demonstrated by a 37% overall response rate. Response rates were similar in previously treated and untreated patients.

Is vemurafenib chemotherapy?

Generic name: Vemurafenib Zelboraf® is the trade name for the generic chemotherapy drug vemurafenib. In some cases, health care professionals may use the generic name vemurafenib when referring to the trade name Zelboraf®. Drug type: Zelboraf® is a targeted therapy.

Is BRAF inhibitor chemotherapy?

We previously found that BRAF inhibition prevents activation of the DNA-damage repair (DDR) pathway in colorectal cancer thus potentiating the effect of chemotherapy.

What is the function of BRAF?

Normal Function The BRAF gene provides instructions for making a protein that helps transmit chemical signals from outside the cell to the cell’s nucleus. This protein is part of a signaling pathway known as the RAS/MAPK pathway, which controls several important cell functions.

Is Zelboraf an immunotherapy?

The U.S. Food and Drug Administration (FDA) has approved the immunotherapy Tecentriq (atezolizumab), in combination with Cotellic (cobimetinib) and Zelboraf (vemurafenib), for the treatment of BRAF V600 mutation-positive advanced melanoma.

Which is the best BRAF inhibitor for melanoma?

Abstract Treatment with BRAF inhibitors such as vemurafenib or dabrafenib in patients with advanced BRAFV600 mutated melanoma has shown objective tumor responses in approximately half of the patients.

How is vemurafenib used to treat brafv600-mutant gliomas?

Vemurafenib demonstrated evidence of durable antitumor activity in some patients with BRAFV600-mutant gliomas, although efficacy seemed to vary qualitatively by histologic subtype. Additional study is needed to determine the optimal use of vemurafenib in patients with primary brain …

How is vemurafenib used in the VE basket study?

Patients and methods: The VE-BASKET study was an open-label, nonrandomized, multicohort study for BRAFV600-mutant nonmelanoma cancers. Patients with BRAFV600-mutant glioma received vemurafenib 960 mg twice per day continuously until disease progression, withdrawal, or intolerable adverse effects.

Can a BRAF and MEK inhibitor be used in combination therapy?

BRAF and MEK inhibitors in combination with immunotherapy. While response rates up to 70% have been observed with BRAF and MEK inhibitors in clinical trials, given the limited durability of responses, there has been interest in combination with checkpoint inhibitors such as anti-cytotoxic T lymphocyte antigen-4…