Is vemurafenib a BRAF inhibitor?

Vemurafenib is a BRAF kinase inhibitor indicated for the treatment of patients with unresectable or metastatic melanoma with the BRAF V600E variant, as detected by an FDA-approved test. It was one of the first molecularly targeted agents to receive FDA approval for advanced melanoma (3).

How does vemurafenib bind to BRAF?

Vemurafenib (PLX4032) was developed as a low molecular weight molecule for the inhibition of the mutated serine threonine kinase BRAF, and it selectively binds to the ATP-binding site of BRAF-V600E kinase and inhibits its activity.

When was Dabrafenib approved by the FDA?

FDA approves dabrafenib plus trametinib for anaplastic thyroid cancer with BRAF V600E mutation. On May 4, 2018, the Food and Drug Administration approved dabrafenib (TAFINLAR®, Novartis Pharmaceuticals Corp.) and trametinib (MEKINIST®, Novartis Pharmaceuticals Corp.)

Is Tafinlar FDA approved?

The U.S. Food and Drug Administration approved Tafinlar (dabrafenib) and Mekinist (trametinib), administered together, for the treatment of anaplastic thyroid cancer (ATC) that cannot be removed by surgery or has spread to other parts of the body (metastatic), and has a type of abnormal gene, BRAF V600E (BRAF V600E …

What is the mechanism of action of vemurafenib?

Vemurafenib is the first molecularly targeted therapy to be licensed in the US and Europe for treatment of advanced melanoma. Its mechanism of action involves selective inhibition of the mutated BRAF V600E kinase that leads to reduced signalling through the aberrant mitogen-activated protein kinase (MAPK) pathway.

Is Tafinlar chemotherapy?

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

What type of therapy is vemurafenib?

Generic name: 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. It is an oral BRAF kinase inhibitor – (For more detail, see “How this drug works,” below.)

How much does Zelboraf cost?

The cost for Zelboraf oral tablet 240 mg is around $5,608 for a supply of 112 tablets, depending on the pharmacy you visit. Prices are for cash paying customers only and are not valid with insurance plans.

Does vemurafenib interrupt the B-Raf/MEK pathway?

Vemurafenib interrupts the B-Raf/MEK step on the B-Raf/MEK/ERK pathway − if the B-Raf has the common V600E mutation. Vemurafenib only works in melanoma patients whose cancer has a V600E BRAF mutation (that is, at amino acid position number 600 on the B-Raf protein, the normal valine is replaced by glutamic acid ).

What is the mechanism of action of BRAF inhibitors?

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. In addition to their molecularly targeted activity, BRAF inhibitors have immunomodulatory effects.

What is the PMID for vemurafenib for BRAF-mutant cancer?

PMID 9689060. ^ a b c Bollag G, Tsai J, Zhang J, Zhang C, Ibrahim P, Nolop K, Hirth P (November 2012). “Vemurafenib: the first drug approved for BRAF-mutant cancer”. Nature Reviews.

What is the PNAS Bibcode for vemurafenib?

Bibcode: 1998PNAS…95.9214C. doi: 10.1073/pnas.95.16.9214. PMC 21318. PMID 9689060. ^ a b c Bollag G, Tsai J, Zhang J, Zhang C, Ibrahim P, Nolop K, Hirth P (November 2012). “Vemurafenib: the first drug approved for BRAF-mutant cancer”.