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Restrict the search for
m sacubitril
to a specific field?
Status:
Investigational
Source:
NCT02043899: Phase 1/Phase 2 Interventional Completed Metastatic Neuroblastoma
(2014)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Source:
NCT00565721: Phase 2 Interventional Completed High-grade Glioma
(2007)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
FLUCICLATIDE F-18 is an 18F-radiolabelled synthetic cyclic peptide containing an RGD motif (Arg-Gly-Asp). It may be used as a tracer in positron emission tomography (PET) imaging. The RGD motif of FLUCICLATIDE F-18 selectively binds to the alpha-V/beta-3 integrin, upregulated on tumor cells and endothelial cells of tumor vasculature. Integrins play an important role in tumor angiogenesis and metastasis. Thus, FLUCICLATIDE F-18 is a potential biomarker of therapeutic response to antiangiogenic inhibitors.
Status:
Investigational
Source:
NCT01063907: Phase 1/Phase 2 Interventional Completed Multiple Myeloma
(2010)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
KW-2478 is a novel and potent non-ansamycin inhibitor of heat shock protein 90 designed to overcome the limitations, including low water solubility and hepatotoxicity, of 17-allylamino-17-demethoxygeldanamycin (17-AAG). KW-2478 exerts a strong antitumor activity against multiple myeloma (MM) cells with various chromosomal translocations. KW-2478 inhibits cell growth and apoptosis associated with Hsp90 client protein degradation. Recent study results have revealed that KW-2478 is able to deplete Hsp90 client Cdk9 and the phosphorylated 4E-BP1, a transcriptional kinase and a transcription inhibitor respectively, leading to reduced expression of FGFR3, c-Maf, and cyclin D1. KW-2478 suppresses tumor growth and induces the degradation of client proteins in tumors in NCI-H929 s.c. inoculated model at doses of 100 mg/kg or more. KW-2478 reduces both serum M protein and MM tumor burden in the bone marrow in OPM-2/GFP i.v. inoculated mouse model at doses of 100 mg/kg.
Status:
Investigational
Source:
NCT03721744: Phase 2/Phase 3 Interventional Recruiting Metastatic Pancreatic Cancer
(2018)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Napabucasin (BBI608) is an orally administered small molecule that blocks stem cell activity in cancer cells by targeting the signal transducer and activator of transcription 3 pathway, which is over-activated in many types of cancer and has been shown to be an important pathway in cancer stem cell-mediated propagation of cancer. Napabucasin has already shown promising efficacy on different cancer types, both as a monotherapy and in combination with conventional chemotherapeutic agents. Early-phase trials have shown promising anti-tumor efficacy when patients are treated with napabucasin in combination with standard chemotherapy agents, and preclinical results suggest that napabucasin can synergize with chemotherapy agents, such as paclitaxel, to potentially overcome drug resistance. Encouraging phase Ib/II trial results warrant further clinical study with napabucasin and paclitaxel combination therapy, especially in malignancies where there is an urgent and unmet need for effective therapeutics, such as in patients with advanced pancreatic adenocarcinoma.
Status:
Class (Stereo):
CHEMICAL (RACEMIC)
Carfluzepic Acid is benzodiazepine derivative with tranquilizing, anticonvulsant, and anxiolytic activity patented by pharmaceutical company C. M. Industries S. A.
Status:
Investigational
Source:
NCT02294266: Phase 1 Interventional Completed Amphetamine-Related Disorders
(2014)
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Mephedrone (4-methylmethcathinone) is a β-ketoamphetamine belonging to the family of synthetic cathinones, an emerging class of designer drugs known for their hallucinogenic and psychostimulant properties as well as for their abuse potential. Mephedrone is a stimulant of dopamine (DA) release and blocks its reuptake through its interaction with the dopamine transporter. Furthermore, it has some affinity for various 5-hydroxytryptamine (5-HT) receptor subtypes. Neurotoxic effect of mephedrone on 5-HT and DA systems remains controversial. Although some studies in animal models reported no damage to DA nerve endings in the striatum and no significant changes in brain monoamine levels, some others suggested a rapid reduction in 5-HT and DA transporter function. Persistent serotonergic deficits were observed after binge like treatment in a warm environment and in both serotonergic and dopaminergic nerve endings at high ambient temperature. Oxidative stress cytotoxicity and an increase in frontal cortex lipid peroxidation were also reported. Despite the re-classification of mephedrone as a Class B restricted substance by the United Kingdom and restrictive legislation by the United States, international policy regarding mephedrone control is still developing and interest in synthetic amphetamine-like drugs could drive the development of future mephedrone analogues.
Status:
Investigational
Source:
NCT04535193: Phase 1/Phase 2 Interventional Recruiting Cardiovascular Diseases
(2021)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Source:
NCT04628481: Phase 2 Interventional Active, not recruiting Recent Onset type1 Diabetes
(2021)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
LADARIXIN is a dual inhibitor of chemokine receptors CXCR1 and CXCR2. It inhibits human polymorphonuclear leukocyte (PMN) migration to chemokine CXCL8 in vitro and prevents PMN infiltration and tissue damage in several models of cerebral ischemia/reperfusion in vivo. It is under development for the treatment of type 1 diabetes.
Status:
Investigational
Source:
NCT03703882: Phase 3 Interventional Completed Muscular Dystrophy, Duchenne
(2018)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
CAT-1004 (Edasalonexent)is an orally administered small molecule designed to inhibit NF-κB, which is activated from infancy in Duchenne muscular dystrophy and is central to causing muscle damage and preventing muscle regeneration. Structurally CAT-1004 represents covalently links salicylic acid and docosahexaenoic acid -- two compounds known to inhibit NF-κB. . In a Phase 1 study in adults, NF-κB activity in peripheral mononuclear cells was inhibited following a single dose of edasalonexent but not by equimolar doses of salicylic acid and docosahexaenoic acid. Chronic activation of NF-κB is a key driver of muscle degeneration and suppression of muscle regeneration in Duchenne muscular dystrophy, which occurs early in the disease process and precedes loss of muscle function. Salicylic acid prevents NF-κB mediated muscle atrophy and decreases protein catabolism in muscle. Docosahexaenoic acid has been shown to upregulate anti-inflammatory pathways and suppress pro-inflammatory pathways via modulation of NF-κB activity. Edasalonexent is endocytosed and hydrolyzed by intracellular fatty acid amide hydrolase (FAAH) to release salicylic acid and DHA in the intracellular compartment, thus having a potential advantage of selectively delivering higher doses in target muscle cells where FAAH is abundant.
Status:
Investigational
Source:
NCT03194620: Not Applicable Interventional Completed Healthy
(2016)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
(-)-Epigallocatechin is a polyphenol, which occurs naturally in various plants, including green tea leaves. The compound was shown to have anti-cancer activity in vitro, with breast cancer, lung cancer, and colon cancer cells. The commercial preparation of Polyphenon E contains about 3% (-)-epigallocatechin as an impurity.