Characteristics
Year of discovery: 2006
Year of introduction: 2020
Discovered by: Array BioPharma
Developed by: Array BioPharma
Primary targets: HER2
Binding type: I/II
Class: receptor tyrosine kinase
Treatment: HER2-positive breast cancer
Other names: ONT-380, ARRY-380
Oral bioavailability = not reported
Elimination half-life = 5.4 hours
Protein binding = 97%
Uses
N6-(4,5-Dihydro-4,4-dimethyl-2-oxazolyl)-N4-[3-methyl-4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)phenyl]-4,6-quinazolinediamine is a novel?diarylamine ErbB inhibitor.
Side effects
Tukysa (tucatinib) is a brand-name prescription medication. The Active ingredient is tucatinib. Serious side effects can include diarrhoea, liver damage, and allergic reactions. Mild side effects can occur with Tukysa use. This list doesn’t include all possible mild side effects of the drug. Mild side effects that have been reported with Tukysa include nausea and vomiting, fatigue, reduced appetite, weight loss, joint pain; peripheral neuropathy (nerve damage that causes tingling, numbness, or weakness in your arms, hands, legs, or feet); abdominal pain; headache; skin rash; nosebleeds; anemia (low level of red blood cells); stomatitis; hand-foot syndrome.
Mode of action
Tucatinib binds to tyrosine kinase (an enzyme) of HER2, reducing PI3-kinase and MAP-kinase signaling. In vitro, tucatinib inhibits phosphorylation of HER2 and HER3, resulting in inhibition of downstream MAPK and AKT signaling and cell proliferation, and showed anti-tumor activity in HER2 expressing tumor cells. In vivo, tucatinib inhibited the growth of HER2 expressing tumors. The combination of tucatinib and trastuzumab showed increased anti-tumor activity in vitro and in vivo compared to either drug alone.
