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Restrict the search for
beta carotene
to a specific field?
Status:
Investigational
Source:
USAN:LANABECESTAT CAMSYLATE [USAN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Status:
Investigational
Source:
INN:razuprotafib [INN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Status:
Investigational
Source:
INN:olitigaltin [INN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
TD139 is a highly potent, specific inhibitor of the galactoside binding pocket of galectin-3. TD139 is formulated for inhalation, which enables direct targeting the fibrotic tissue in the lungs, while minimizing systemic exposure. TD139 was initially developed by a team of scientists from Lund University, Sweden, and Edinburgh University, the UK. TD-139 is in phase I/II clinical trials for the treatment of idiopathic pulmonary fibrosis.
Status:
Investigational
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Conditions:
ICI-118,551 is a selective subtype β2 adrenergic receptor (adrenoreceptor) antagonist. ICI-118,551 binds to the β2 subtype with at least 100 times greater affinity than to other subtypes of the beta adrenoceptor β1 or β3. Pharmacological experiments proved that the right shift of the norepinephrine dose-response curve by ICI-118,551 was mediated via a beta(2)-adrenoceptor/G(i/o) protein-dependent pathway enhancing NO production in the endothelium. These results were corroborated in beta-adrenoceptor and endothelial NO synthase knockout mice where ICI had no effect. ICI-118,551 increased vascular lumen diameter in lung sections and reduced pulmonary arterial pressure under normoxia and under hypoxia in the isolated perfused lung model. These effects were found to be physiologically relevant, because ICI-118,551 specifically decreased pulmonary but not systemic blood pressure in vivo. Thus, it has been suggested that ICI-118,551 is a pulmonary arterial-specific vasorelaxant and might be a potential novel therapeutic agent for the treatment of pulmonary arterial hypertension. It was also demonstrated that systemic topical administration of ICI 118,551 results in decreased intraocular pressure in both eyes of rabbits, indicating that at least part of the ocular hypotensive effect of topical ICI 118,551 is mediated through systemic absorption. However, ICI 118,551 did not lower blood pressure in hypertensive patients known to respond to therapy with atenolol or propranolol.
Status:
Investigational
Source:
NCT01168752: Phase 1 Interventional Completed Cancer
(2010)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
CUDC-305, is a novel heat shock protein 90 (HSP90) inhibitor with strong affinity for HSP90 alpha/beta, high oral bioavailability and potent anti-proliferative activity against a broad range of cancer cell lines (with a mean IC50 of 220 nmol/L), including many non-small cell lung cancer (NSCLC) cell lines which are resistant to standard-of-care (SOC) agents. In both laboratory and animal testing, CUDC-305 demonstrated high potency in vitro and/or in vivo across a wide range of cancers. Most notably, Curis scientists observed complete tumor regression following oral administration of CUDC-305 in a mouse xenograft model of acute myelogenous leukemia (AML). Tumor regression has also been observed after treatment of CUDC-305 in mouse xenograft models of breast, non-small cell lung, gastric cancer and glioblastoma brain cancers. In this preclinical testing, the compound also demonstrated an ability to effectively cross the blood brain barrier, and demonstrated an ability to extend survival in an intracranial glioblastoma model. Early stage toxicity studies suggest that CUDC-305 appears to have a better therapeutic window than several leading Hsp90 inhibitors in clinical development.
Status:
Investigational
Source:
INN:vactosertib [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
EW-7197 is an orally bioavailable inhibitor of the serine/threonine kinase, transforming growth factor (TGF)-beta receptor type 1 (TGFBR1), also known as activin receptor-like kinase 5 (ALK5), with potential antineoplastic activity. EW-7197 is in phase I clinical trials for the treatment of solid tumors. Also, EW-7197 has a strong potential as an anti-fibrosis therapeutic agent.
Status:
Investigational
Source:
NCT04469998: Phase 2 Interventional Completed Posterior Blepharitis
(2020)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
GW-870086 (now known as GSK 870086) was developed by GlaxoSmithKline as a glucocorticoid receptor agonist. Repeat inhaled doses of GW-870086 was studied in phase II clinical trial in patients with asthma. In addition, phase II clinical trial was investigated to determine the efficacy of GW-870086 ream formulation in subjects with moderate to severe atopic dermatitis. However, the development of this drug appears to have been discontinued.
Status:
Investigational
Source:
NCT01972672: Phase 2 Interventional Completed Hepatocellular Carcinoma (HCC)
(2013)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Icaritin is a monoprenylated favonol with 4′-methoxyl from Epimedium Genus. It has been documented to have osteoblastic and neuroprotective activities. It can reduce the incidence of steroid-associated oesteonecrosis in rabbit with inhibition of both intravascular thrombosis and extravascular lipid deposition for maintaining the integrity of intraosseous vasculature. Icaritin shows anti-infammatory activity and inhibitory activities against cancer cells. The phase III clinical trial is planned for the treatment of Hepatocellular carcinoma.
Status:
Investigational
Source:
NCT02258555: Phase 1 Interventional Terminated Follicular Lymphoma
(2015)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Status:
Investigational
Source:
INN:samotolisib [INN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
LY3023414, an investigational drug, is a small molecule that that demonstrates activity against PI3K, mTOR, and DNA-PK in tumor cells, thereby inducing cell-cycle effects and inhibiting cancer cell viability. As shown in vitro LY3023414 inhibits the ability of PI3K and mTOR to phosphorylate substrates in the PI3K/mTOR pathway, one of the most frequently mutated pathways in cancer, leading to cancer progression and resistance to existing treatments. Downstream target inhibition by LY3023414 occurs rapidly via an intermittent “on/off” mechanism that may enhance the drug's clinical tolerability, which may in turn allow LY3023414 to overcome some of the toxicities associated with PI3K/mTOR inhibitors and potentially reduce the emergence of feedback mechanisms leading to resistance. The physicochemical and absorption properties of LY3023414 are favorable, as evidenced by the molecule's high solubility across a wide pH range and high oral bioavailability. On the basis of these findings, LY3023414 is currently being evaluated in clinical trials in patients with advanced cancer such as metastatic prostate cancer and non-small cell lung cancer in combination with other chemotherapeutic agents and in endometrial cancer as a monotherapy.
