Is vemurafenib a tyrosine kinase inhibitor?
Vemurafenib inhibits a serine-threonine protein kinase that is called B-RAF. The RAF kinases are serine/threonine protein kinases. Vemurafenib also inhibits tyrosine kinases, such as KIT and c-RET, and thus this drug is also a tyrosine kinase inhibitor (TKI).
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.
Are BRAF inhibitors immunotherapy?
Specifically, two types of therapies, BRAF targeted therapy (TT), which target the constitutively active mitogen activated protein kinase (MAPK) pathway resulting from oncogenic BRAF mutations present in 40–50% of patients, and immunotherapy, which target the human immune system to enhance anti-tumor immunity, have …
What is vemurafenib used for?
Vemurafenib is used to treat certain types of melanoma (a type of skin cancer) that cannot be treated with surgery or that has spread to other parts of the body. It is also used to treat a certain type of Erdheim-Chester disease (ECD; a disease that causes an overproduction of a type of white blood cells).
What is Braftovi and Mektovi?
BRAFTOVI (braf-TOE-vee) + MEKTOVI (mek-TOE-vee) is a targeted oral combination therapy used to treat people with melanoma that has spread to other parts of the body (metastatic) or cannot be removed by surgery (unresectable) and has a certain type* of abnormal BRAF gene.
What is the difference between targeted therapy and immunotherapy?
These targeted therapy medications tend to be in the form of pills, taken orally. In contrast, immunotherapy drugs don’t attack cancer cells directly; instead, they stimulate the patient’s own immune system to recognize cancer cells as foreign bodies and attack these cancer cells.
How do BRAF inhibitors 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.
What kind of enzyme inhibitor is PLX4032?
PLX4032, also known as Vemurafenib, RG7204, RO5185426 and Zelboraf, is a highly selective B-Raf enzyme inhibitor with an IC50 of 44 nM against V600E-mutant BRAF. J Virol. 2020 Feb 14;94 (5):e01791-19.
How is PLX4032 used to treat colon cancer?
PLX4032 is highly effective in the treatment of melanoma, for its ability of inhibiting B-RAF V600E. However, PLX4032 displays limited effect in colon cancer patients that also carrying B-RAF V600E oncoprotein.
What kind of melanoma does vemurafenib treat?
Vemurafenib is a small-molecule BRAF inhibitor approved by the Food and Drug Administration (FDA) to treat patients with nonoperable metastatic melanoma with a BRAF (V600E) mutation [71].
What are the most common side effects of vemurafenib?
The BRIM-2 trial investigated 132 patients; the most common adverse events were arthralgia in 58% of patients, skin rash in 52%, and photosensitivity in 52%. In order to better manage side effects some form of dose modification was necessary in 45% of patients.