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Restrict the search for
telotristat ethyl
to a specific field?
Status:
Investigational
Source:
NCT03592472: Phase 3 Interventional Recruiting Renal Cell Carcinoma
(2018)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Abexinostat (PCI-24781) is a novel, second-generation phenyl hydroxamic acid–based, orally bioavailable HDAC inhibitor that has previously been shown to have activity in vitro and in vivo against a broad array of cancers, including hematopoietic malignancies and bone and soft-tissue sarcomas. Abexinostat is a pan-HDAC inhibitor mostly targeting HDAC1 with Ki of 7 nM, modest potent to HDACs 2, 3, 6, and 10 and greater than 40-fold selectivity against HDAC8. Abexinostat exhibits potent antitumor activity against a variety of tumor cell lines with GI50 ranging from 0.15 uM to 3.09 uM. PCI-24781 also has an antiproliferative effect on HUVEC endothelial cells with GI50 of 0.43 uM. Abexinostat treatment causes dose-dependent accumulation of both acetylated histones and acetylated tubulin in HCT116 or DLD-1 cells, induces expression of p21, and leads to PARP cleavage and accumulation of the γH2AX. It has also shown good tolerability and activity in Phase I and II clinical trials against lymphoma, as well as against solid tumors in Phase-I trials. Additionally, it acts as a potent radiosensitizing agent and is synergistic with cytotoxic chemotherapy, such as doxorubicin in preclinical models.
Status:
Investigational
Source:
NCT00843518: Phase 2 Interventional Completed Alzheimer's Disease
(2009)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Mibampator, also known as LY451395, is a potent and highly selective an AMPA receptor potentiator, which plays a role in the regulation of the glutamatergic system. The AMPA system also has important functions in the regulation of synapses, synaptic regeneration, and neuroprotection and is therefore a good therapeutic target for treatments aiming to improve cognition and function or alter disease progression. Mibampator was in the phase II clinical trial for the treatment of agitation and aggression in Alzheimer's disease (AD).
Status:
Investigational
Source:
NCT01091454: Phase 2 Interventional Completed Triple-negative Breast Cancer
(2010)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Brostallicin is a DNA minor groove binder which has shown very promising preclinical activity against a variety of human tumors both in vitro and in vivo. Brostallicin shows potent in vitro cytotoxic activity against tumor cells with IC50 values in the low nanomolar range, circumvents resistance to alkylating agents and camptothecins. Brostallicin has broad antitumor activity in animal models. A clear therapeutic gain is observed in preclinical models when brostallicin is combined with anticancer agents such as cisplatin, doxorubicin, and taxotere.
Status:
Investigational
Source:
NCT02743026: Not Applicable Interventional Completed HIV
(2015)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Source:
NCT01308164: Not Applicable Interventional Completed Type 1 Diabetes
(2011)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Source:
NCT00525213: Phase 2 Interventional Completed Rheumatoid Arthritis
(2007)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Rabeximod is an indolo[2,3-b]quinoxaline derivative patented by OxyPharma AB as anti-inflammatory agent useful for the treatment of autoimmune disease. Rabeximod impaired monocyte differentiation into monocyte-derived dendritic cells and pro-inflammatory allostimulated macrophages. Monocyte-derived dendritic cells that were treated with Rabeximod resulted in a significant decrease in their ability to pinocytose antigens, while no effect was exerted by the drug on the ability of allostimulated macrophages and anti-inflammatory macrophages to phagocytose. Rabeximod reduces the severity of arthritis in rodent models of rheumatoid arthritis and multiple sclerosis. Rabeximod efficiently prevented arthritis during the time window when TLR2 or TLR4 ligands activate inflammatory macrophages.
Status:
Investigational
Source:
NCT01561690: Phase 2 Interventional Completed Asthma
(2012)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Status:
Investigational
Source:
NCT01448954: Phase 2 Interventional Completed Atopic Asthma
(2011)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Class (Stereo):
CHEMICAL (RACEMIC)
Soterenol [(+)-1-(3-methanesulphonamido, 4-hydroxyphenyl)-2-isopropylaminoethanol, MJ 1992] is a directly acting sympathomimetic amine which has been shown to display Beta2-adrenoceptor selectivity. Soterenol, a methanesulfonamido-phenethanolamine related structurally to isoproterenol, was a highly effective bronchodilator agent in several animal species by various routes of administration. The bronchodilator potency of soterenol was equivalent to, or greater than, that of isoproterenol. Soterenol also had potent stimulant action on the alpha-receptor of the smooth muscle.
Status:
Investigational
Source:
NCT01271270: Phase 1 Interventional Completed Age-Related Macular Degeneration
(2010)
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
RES-529 (previously named Palomid 529, P529) is a phosphoinositide 3-kinase (PI3K)/AKT/mechanistic target of rapamycin (mTOR) pathway inhibitor that interferes with the pathway through both mTOR complex 1 (mTORC1) and mTOR complex 2 (mTORC2) dissociation. P529 inhibits tumor growth, angiogenesis, and vascular permeability. It retains the beneficial aspects of tumor vascular normalization that rapamycin boasts. This compound is currently being developed in oncology and ophthalmology. The oncology focus is for the treatment of glioblastoma, where it has received orphan designation by the US Food and Drug Administration, and prostate cancer.
