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Restrict the search for
beta carotene
to a specific field?
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
TAS-116 is a highly potent oral HSP90 inhibitor with unique tissue distribution properties. TAS-116 has the potential to demonstrate antitumor activity, while being designed to limit certain adverse events by unique tissue distribution. Phase-II clinical trials in gastrointestinal stromal tumours are ongoing in Japan.
Status:
Investigational
Source:
INN:lanifibranor [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
IVA-337 (LANIFIBRANOR), an indole sulfonamide derivative, is a pan peroxisome proliferator-activated receptor (PPAR) agonist. It is under investigation in Phase 2 clinical trials for non-alcoholic steatohepatitis, non-alcoholic fatty liver disease, and type 2 diabetes.
Status:
Investigational
Source:
NCT01358981: Phase 1 Interventional Completed Diabetes Mellitus, Type 2
(2011)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Status:
Investigational
Source:
NCT00838084: Phase 1 Interventional Completed Alzheimer's Disease
(2008)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
LY2811376 is a non-peptide inhibitor of BACE1 selective over BACE2. It showed robust central reduction of amyloid-β in humans.
Status:
Investigational
Source:
NCT01580644: Phase 1 Interventional Completed Healthy
(2012)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
GLPG0187 is a compound that belongs to the class of organic compounds known as naphthyridines, and has been studied as a potential drug in the treatment of solid tumors. GLPG0187 is a broad spectrum integrin receptor antagonist that inhibits αvβ1 integrin. In vitro, this compound was found to diminish the size of the aldehyde dehydrogenase high subpopulation of prostate cancer cells dose-dependently. It also significantly reduced tumor cell migration and cell proliferation. In vivo, it reduced metastatic tumor growth, and inhibited the progression of bone metastases as well as the formation of new bone metastases. Phase I studies have been completed to study safety and drug tolerance of GLPG0187. The drug was well tolerated, but continuous infusion of GLPG0187 did not show signs of monotherapy efficacy.
Status:
Investigational
Source:
NCT03507790: Phase 2 Interventional Active, not recruiting Mild to Moderate Alzheimer's Disease
(2018)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Source:
NCT02933372: Phase 2 Interventional Completed Parkinson's Disease
(2015)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Status:
Investigational
Source:
NCT00868790: Phase 2 Interventional Terminated Type 2 Diabetes Mellitus
(2009)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
MK 3577 is an orally active glucagon receptor antagonist which was under development by Merck & Co for the treatment of type 2 diabetes mellitus. MK 3577 demonstrate activity in cellular models and preclinical trials. In phase II clinical trials MK 3577 shows good efficacy and acceptable level of adverse events, but no further development reports were published.
Status:
Investigational
Class (Stereo):
CHEMICAL (ABSOLUTE)
Status:
Investigational
Source:
NCT01915576: Phase 1 Interventional Completed Neoplasms
(2013)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
BAY-1125976 is an orally bioavailable inhibitor of the serine/threonine protein kinase AKT (protein kinase B) isoforms 1 and 2 (AKT1/2) with potential antineoplastic activity. AKT1/2 inhibitor BAY1125976 selectively binds to and inhibits the phosphorylation and activity of AKT1/2 in a non-ATP competitive manner, which may result in the inhibition of the phosphatidylinositol 3 (PI3K)/AKT/mammalian target of rapamycin (mTOR) signaling pathway. This may lead to both the reduction of cell proliferation and the induction of cell apoptosis in AKT-overexpressing tumor cells. The AKT signaling pathway is often deregulated in cancer and is associated with tumor cell proliferation, survival, and migration. BAY 1125976 is equally potent against Akt1 and Akt2 isoforms and up to 86 fold less potent against Akt3 It inhibits the Akt1 and Akt2 by binding into an allosteric binding pocket formed by kinase and PH domain. It inhibits cell proliferation in a broad panel of human cancer cell lines, particularly in breast and prostate cancer cell lines expressing estrogen or androgen receptors. It effectively blocks Akt signaling by inhibiting the phosphorylation of Akt and the downstream effectors, including eukaryotic translation initiation factor 4E binding protein 1 (4E-BP1), glycogen synthase kinase 3 beta (GSK3s), proline-rich Akt substrate 40 kDa (PRAS40), S6 ribosomal protein (S6RP), and 70 kDa ribosomal protein S6 kinase 1 (70S6K). BAY 1125976 exhibits strong in vivo efficacy in both cell line and patient-derived xenograft models such as the KPL4 breast cancer model (PIK3CAH1074R mutant), the MCF7 and HBCx-2 breast cancer models, and the AktE17K mutant driven prostate cancer (LAPC-4) and anal cancer (AXF 984) models.
