N- (2- (4- ((3- chloro- 4- (3- (trifluoromethyl)phenoxy)phenyl)amino)- 5H- pyrrolo(3,2- d)pyrimidin- 5- yl)ethyl)- 3- hydroxy- 3- methylbutanamide

02/14/2012 - "Phase I first-in-human study of TAK-285, a novel investigational dual HER2/EGFR inhibitor, in cancer patients."
02/01/2014 - "Patients with advanced, histologically confirmed solid tumors and Eastern Cooperative Oncology Group performance status ≤2 received daily oral TAK-285; daily dose was escalated within defined cohorts until MTD and recommended phase 2 dose (RP2D) were determined. "
01/01/2014 - "These results suggest that HER2 and HER3 mainly regulate cancer cell growth in TAK-285-sensitive cells and that phospho-HER3 could be used as a potential molecular marker to select patients most likely to respond to TAK-285. "
01/01/2013 - "In mouse and rat xenograft tumor models, TAK-285 showed antitumor activity against cancers that expressed HER2 or EGFR. "
01/20/2015 - "HER2 and HER3 cooperatively regulate cancer cell growth and determine sensitivity to the novel investigational EGFR/HER2 kinase inhibitor TAK-285. "

03/10/2012 - "On the basis of substantial brain penetration of unbound TAK-285, it is concluded that TAK-285 might have the potential in the treatment of brain metastases of HER2 over-expressing metastatic breast cancer. "
01/01/2013 - "Our studies suggest that investigational drugs such as TAK-285 that have strong antitumor activity and are not Pgp substrates may be useful in the development of agents with the potential to treat brain metastases. "
01/01/2014 - "We recently reported that TAK-285, an orally bioavailable small molecule inhibitor of HER kinases, is not a p-glycoprotein substrate and penetrates the blood-brain barrier, suggesting favorable activity for the treatment of brain metastases. "
01/01/2013 - "TAK-285 was examined in a model of breast cancer brain metastasis using direct intracranial injection of BT-474-derived luciferase-expressing cells and showed greater inhibition of brain tumor growth compared to animals treated with lapatinib. "

03/10/2012 - "TAK-285, an investigational, orally active HER2/EGRF inhibitor is in clinical development for potential use in HER2 over-expressing metastatic breast cancer. "
03/10/2012 - "On the basis of substantial brain penetration of unbound TAK-285, it is concluded that TAK-285 might have the potential in the treatment of brain metastases of HER2 over-expressing metastatic breast cancer. "
03/08/2021 - "This is in accordance with experimental findings that showed the tak-285 inhibitor has increased activity relative to lapatinib in breast cancer cell lines."
01/01/2013 - "TAK-285 was as effective as lapatinib in antitumor activity in a mouse subcutaneous BT-474 breast cancer xenograft model. "
01/01/2014 - "To identify the determinants of sensitivity to TAK-285, we examined the relationship between the IC50 values of TAK-285 for cell growth inhibition and the expression of candidate genes that are involved in the HER family signaling pathway and trastuzumab resistance in a panel of human breast cancer cell lines, other types of cancer cells, and non-transformed cells in vitro. "

01/01/2013 - "Antitumor Activity of TAK-285, an Investigational, Non-Pgp Substrate HER2/EGFR Kinase Inhibitor, in Cultured Tumor Cells, Mouse and Rat Xenograft Tumors, and in an HER2-Positive Brain Metastasis Model."
01/01/2013 - "TAK-285 was examined in a model of breast cancer brain metastasis using direct intracranial injection of BT-474-derived luciferase-expressing cells and showed greater inhibition of brain tumor growth compared to animals treated with lapatinib. "

12/01/2023 - "Development of new TAK-285 derivatives as potent EGFR/HER2 inhibitors possessing antiproliferative effects against 22RV1 and PC3 prostate carcinoma cell lines."