U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS
This repository is under review for potential modification in compliance with Administration directives.

Showing 1 - 10 of 35 results

Status:
US Approved Rx (2020)
First approved in 2020

Class (Stereo):
CHEMICAL (ACHIRAL)



TUCATINIB (ONT-380 or ARRY-380) is an orally active, reversible and selective small-molecule HER2 inhibitor invented by Array and licensed to Cascadian Therapeutics (previously named Oncothyreon) for development, manufacturing and commercialization. ...
Status:
US Approved Rx (2018)
First approved in 2018

Class (Stereo):
CHEMICAL (ACHIRAL)



Dacomitinib is an oral, once-daily, pan-HER inhibitor. It is an irreversible inhibitor of HER-1 (EGFR), HER-2 and HER-4 tyrosine kinases. Dacomtinib is being evaluated in phase 3 clinical trials against nonsmall-cell lung cancer. Direct comparison wi...
Status:
US Approved Rx (2017)
First approved in 2017

Class (Stereo):
CHEMICAL (ACHIRAL)



Neratinib (HKI-272) is a pan-HER inhibitor, this irreversible tyrosine kinase inhibitor binds and inhibits the tyrosine kinase activity of epidermal growth factor receptors, EGFR (or HER1), HER2 and HER4, which leads to reduced phosphorylation and ac...
Status:
US Approved Rx (2024)
First approved in 2007

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Lapatinib is a small molecule and a member of the 4-anilinoquinazoline class of kinase inhibitors. It is present as the monohydrate of the ditosylate salt (trade name TYKERB). Lapatinib is dual inhibitor of the EGFR (epidermal growth factor receptor...
Status:
Investigational

Class (Stereo):
CHEMICAL (ACHIRAL)



Canertinib or CI-1033 (N-[4-[N-(3-Chloro-4-fluorophenyl)amino]-7-[3-(4-morpholinyl)propoxy]quinazolin-6-yl]acrylamide) is a pan-erbB tyrosine kinase inhibitor. It selectively inhibits erbB1 (epidermal growth factor receptor), erbB2, erbB3, and erbB4 ...
Status:
Investigational

Class (Stereo):
CHEMICAL (ACHIRAL)



AST-1306, also known as Allitinib, is an orally active potent, selective, irreversible inhibitor of the HER family of receptor tyrosine kinases. AST-1306 inhibits the enzymatic activities of wild-type epidermal growth factor receptor (EGFR) and ErbB2...
Status:
Investigational

Class (Stereo):
CHEMICAL (ABSOLUTE)



BMS-690514 is a potent, reversible oral inhibitor of epidermal growth factor receptor (EGFR/HER-1), HER-2 and -4, and vascular endothelial growth factor receptors (VEGFRs)-1 to -3 offering targeted inhibition of tumour growth and vascularisation in a...
Status:
Investigational

Class (Stereo):
CHEMICAL (ACHIRAL)



Tesevatinib (EXEL-7647 or XL647) was optimized as an inhibitor of a spectrum of growth-promoting and angiogenic receptor tyrosine kinases (RTKs) to simultaneously block tumor growth and vascularization. In particular, Tesevatinib potently inhibits th...
Status:
Investigational

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

CP 724714 is an orally bioavailable, quinazoline-based, selective small molecule inhibitor of the HER2/erbB2 receptor tyrosine kinase. The compound could have particular potential in the treatment of women with metastatic breast cancer, of which 25-3...
Status:
Investigational

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

HKI-357 is a potent, dual irreversible inhibitor of ErbB2 (HER2) and EGFR. HKI-357 suppresses ligand-induced EGFR autophosphorylation and cell proliferation in NCI-H1975 cells containing L858R and T790M mutations.