U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 231 - 240 of 1679 results

Status:
Investigational
Source:
NCT00784290: Phase 1/Phase 2 Interventional Completed Hepatocellular Carcinoma
(2003)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Orantinib (SU-6668) is an orally bioavailable receptor tyrosine kinase inhibitor. Orantinib binds to and inhibits the autophosphorylation of vascular endothelial growth factor receptor 2 (VEGFR2), platelet-derived growth factor receptor (PDGFR), and fibroblast growth factor receptor (FGFR), thereby inhibiting angiogenesis and cell proliferation. Orantinib also inhibits the phosphorylation of the stem cell factor receptor tyrosine kinase c-kit, often expressed in acute myelogenous leukemia cells. Orantinib was in phase II clinical trials for the treatment of breast cancer. It was also in phase III clinical trials for the treatment of hepatocellular carcinoma. However, this research was terminated in 2014. The compound was originally developed by Sugen (subsidiary of Pfizer). In 1998, a co-development agreement took place between Sugen and Taiho for the compound.
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 single agent. Bristol-Myers Squibb was developing BMS 690514, as an oral treatment for cancer. BMS-690514 had being in phase II for the treatment of breast cancer; non-small cell lung cancer, but later these studies were discontinued.
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 the EGF/ErbB2, VEGF, and ephrin RTK families. The drug is being developed by Kadmon Corporation under licence from Symphony Evolution (Symphony Capital Partners). Kadmon is developing tesevatinib for the treatment of autosomal polycystic kidney disease and solid cancers.
SU-14813 is an oral, multitargeted tyrosine kinase inhibitor (TKI) targeting vascular endothelial growth factor receptors (VEGFR), platelet-derived growth factor receptors (PDGFR), KIT, and fms-like tyrosine kinase 3 (FLT-3). SU-14813 was developed as a next-generation TKI agent following sunitinib (SU-11248) designed to demonstrate optimized pharmacokinetic (PK) and tolerability profiles. SU14813 demonstrated broad and potent antitumor activity equivalent to that of sunitinib, which resulted in tumor regression, growth arrest, growth delay, and prolonged survival in established xenograft cancer models in mice. A phase II trial of SU-14813 in patients with breast cancer was completed. However, according to the Pfizer pipeline development has been discontinued.
Status:
Investigational
Source:
NCT02173457: Phase 3 Interventional Completed Type 2 Diabetes
(2014)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT02870582: Phase 3 Interventional Completed Metastatic Colorectal Cancer
(2016)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Donafenib (CM-4307) is a derivative of sorafenib, where [1H] hydrogens on the terminal methyl group are substituted by deuterium. The drug was developed by the Chinese company Suzhou Zelgen Biopharmaceuticals. Upon oral administration, donafenib binds to and blocks the activity of Raf kinase, and inhibits Raf-mediated signal transduction pathways. This inhibits cell proliferation in Raf-expressing tumor cells. In addition, donafenib may inhibit unidentified RTKs, and thus may further block tumor cell proliferation in susceptible tumor cells. Donafenib is being investigated in phase 3 clinical trials for the treatment of 131I-refractory differentiated thyroid cancer, advanced hepatocellular carcinoma, and metastatic colorectal cancer.
Status:
Investigational
Source:
NCT02260947: Phase 1 Interventional Completed Healthy
(2014)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

PF-06273340 is a brain penetrant, orally available and potent tropomyosin-related kinase (Trk) inhibitor. PF-06273340 has a low metabolic turnover in Human liver microsomes and hepatocytes is a good substrate for efflux transporters P-glycoprotein and Breast cancer resistance protein (BCRP) and have moderate passive permeability. PF-06273340 was investigated in Phase I clinical trials for the treatment acute and chronic pain. However clinical development has been discontinued.
Status:
Investigational
Source:
NCT00676299: Phase 1 Interventional Completed Protein Kinase Inhibitors
(2006)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
NCT03920254: Phase 2/Phase 3 Interventional Terminated Ulcerative Colitis (UC)
(2020)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)