Agerafenib is a selective multi-kinase inhibitor. It is undergoing a trial to test its ability to treatmalignant tumors in humans. It is effective in doses ranging between 30 milligrams and 100 milligrams. It is also known as CEP-32496 and RXDX 105. It is a strong inhibitor of theBRAF gene that is commonly found in cancerous cells.
Agerafenib was originally discovered by a company calledDaiichi Sankyo (then called Ambit Biosciences) andTeva Pharmaceuticals (then called Cephalon) during a research program.[1] The chemical was originally named "CEP-32496" before being renamed to "RXDX 105" in 2015.[1] It is currently undergoing a clinical trial to test its effectiveness against cancer in humans.[2]
The chemical is a strong inhibitor of the BRAF gene, which is present in around 7% of all malignant tumors.[7] It does this due to its strongcytotoxicity to cells containing it.[7] Agerafenib also inhibitsphosphorylation inmitogen-activated protein kinase (an enzyme that causes certain cellular responses).[8] The drug is shown to be most effective in humans in doses between 30 milligrams and 100 milligrams.[9]
^Purich, Daniel (2017).The Inhibitor Index: A Desk Reference on Enzyme Inhibitors, Receptor Antagonists, Drugs, Toxins, Poisons, Biologics, and Therapeutic Leads. London:CRC Press. p. 1989.ISBN978-1-351-73067-9.
