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Restrict the search for
angiotensin ii
to a specific field?
Status:
Investigational
Source:
NCT00972322: Phase 1 Interventional Completed Type 2 Diabetes Mellitus
(2009)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Merck was developing MK 8245, an orally active inhibitor of stearoyl CoA desaturase for the treatment of type-2 diabetes mellitus. MK-8245 is a liver-targeting inhibitor of stearoyl-CoA desaturase (SCD) with IC50 of 1 nM for human SCD1 and 3 nM for both rat SCD1 and mouse SCD1, with anti-diabetic and anti-dyslipidemic efficacy. It is in Phase 2 clinical studies for type 2 diabetes mellitus.
Status:
Investigational
Source:
NCT00055926: Phase 1 Interventional Completed Breast Cancer
(2003)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
CP 724714 is an orally bioavailable, quinazoline-based, selective small molecule inhibitor of the HER2/erbB2 receptor tyrosine kinase. The compound could have particular potential in the treatment of women with metastatic breast cancer, of which 25-30% over express HER2/erbB2. CP 724714 was in preclinical development with Pfizer.
Status:
Investigational
Source:
NCT00612118: Phase 2 Interventional Completed Allergic Rhinitis
(2008)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
GSK-256066 is a PDE4B inhibitor which was developed by GlaxoSmithKline and tested in phase II of clinical trials for the treatment of COPD, Asthma and Seasonal allergic rhinitis. According to the GSK pipeline, development of GSK-256066 was terminated. There are studies that describes the possibility of repurposing of the drug as antitrypanosomal agents, because it inhibits PDEB1 of Trypanosoma brucei.
Status:
Investigational
Source:
NCT03397134: Phase 3 Interventional Completed Negative Symptoms of Schizophrenia
(2017)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
CYR-101 (MIN-101) is a cyclic amide derivative that has high equipotent affinities for 5-HT2A and sigma-2 receptors (Ki of 7.53 nM and 8.19 nM for 5-HT2A and sigma-2, respectively). MIN-101 also shows binding affinity for a1-adrenergic receptors but low or no affinity for muscarinic, cholinergic, and
histaminergic receptors. MIN-101 demonstrated statistically significant efficacy in reducing negative symptoms and good tolerability in stable schizophrenia patients. The drug is in phase II clinical trials for the treatment of Schizophrenia.
Status:
Investigational
Source:
NCT01802320: Phase 2 Interventional Completed Colon Mucinous Adenocarcinoma
(2013)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
MK-2206 is an oral selective allosteric inhibitor of Akt that targets all three isoforms of human Akt (Akt-1, Akt-2 and Akt-3). In a phase I study of solid tumors, MK-2206 demonstrated evidence of target modulation and anti-proliferative activity as a single agent and in combination with other agents. Current ongoing trials of MK-2206 include monotherapy and combination therapy in breast cancer, colorectal cancer, haematological malignancies, non-small cell lung cancer and other. Detected treatment-related adverse event are: rash, fatigue, hyperglycemia.
Status:
Investigational
Source:
NCT01564459: Phase 2 Interventional Completed Diabetic Neuropathy, Painful
(2012)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Filorexant (MK-6096) is a novel, structurally distinct dual orexin receptor antagonist, conclusively validates orexin signalling mechanism as a specific and effective target for the treatment of insomnia and potentially other disorders in which sleep/wake dysregulation occurs. Also, it is being investigated as a possible agent against diabetic neuropathies, major depressive disorder and for the a migraine prophylaxis. Detected adverse events are: sleep-onset paralysis, excessive daytime sleepiness. As of May 2015, filorexant is no longer listed on Merck's online development pipeline.
Status:
Investigational
Source:
NCT03417739: Phase 2 Interventional Active, not recruiting Uveal Melanoma
(2018)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
BVD-523 potently and selectively inhibits ERK1 and ERK2 kinases in a reversible, ATP-competitive fashion. Consistent with its mechanism of action, BVD-523 inhibits signal transduction, cell proliferation, and cell survival, most potently in cell lines bearing mutations that activate MAPK pathway signaling. Similarly, single-agent BVD-523 inhibits tumor growth in vivo in BRAF-mutant melanoma and colorectal xenografts as well as in KRAS-mutant colorectal and pancreatic models. BioMed Valley Discoveries is developing ulixertinib, a potent and selective small molecule inhibitor of ERK 1 and 2 kinases, as an oral treatment for cancers harbouring mutations in the MAPK signaling pathway. Phase I/II development of the drug for advanced cancers including, acute myeloid leukaemia and myelodysplastic syndromes is underway in the US. A phase I trial is underway in the US for pancreatic cancer.
Status:
Investigational
Source:
NCT00294346: Phase 2 Interventional Completed Social Phobia
(2006)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
AV608, a 4-aminopiperidine derivative, is a selective, specific, long-acting, orally active and potent nonpeptidic antagonist of the NK-1 receptor. AV-608 had been in phase II clinical trials for the treatment of social phobia and overactive bladder (OAB). This compound was originally discovered by Novartis, and then licensed to Areva Pharmaceuticals in October 2003. Addition this drug was in phase I clinical trial for the treatment of Irritable Bowel Syndrome (IBS), this disease is characterized by chronic abdominal pain and frequent comorbid anxiety. The substance P ⁄ neurokinin-1 receptor system is implicated in the regulation of both pain and anxiety, suggesting a potential therapeutic target in IBS. However, the researches on this drug candidate were discontinued in 2010.
Status:
Investigational
Source:
NCT00436852: Phase 2 Interventional Completed Disseminated Neuroblastoma
(2007)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
ABT-751 is an orally bioavailable antimitotic sulfonamide, which binds to the colchicine-binding site on beta-tubulin and inhibits the polymerization of microtubules, leads to a block in the cell cycle at the G2M phase, resulting in cellular apoptosis. ABT-751 had been in phase Ⅱ clinical studies for the treatment of breast cancer; colorectal cancer; non-small cell lung cancer; renal cancer, prostate cancer, but these researches have been discontinued.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Luminespib (NVP-AUY922) is a highly potent isoxazole-based, nongeldanamycin HSP90 inhibitor that inhibits the adenosine triphosphatase activity of
HSP90. Luminespib is a highly potent HSP90 inhibitor for HSP90α/β with IC50 of 13 nM /21 nM in cell-free assays, weaker potency against the HSP90 family members GRP94 and TRAP-1, exhibits the tightest binding of any small-molecule HSP90 ligand. Luminespib potently inhibited in vitro growth in all 41 NSCLC cell lines evaluated with IC50 less than 100 nM. IC100 value less than 40 nM was seen in 36 of 41 lines. Luminespib (NVP-AUY922) has greater potency, reduced hepatotoxicity, and lower dependence on DT-diaphorase than the first-generation HSP90 inhibitors. Luminespib was discovered in a multiparameter lead optimization program based on a high-throughput screening hit methodology developed jointly by The Institute of Cancer Research, UK and the pharmaceutical company Vernalis. It has been licensed to Novartis. Luminespib activity is independent of NQO1/DT-diaphorase, maintained in drug-resistant cells and under hypoxic conditions. The molecular signature of HSP90 inhibition, comprising induced HSP72 and depleted client proteins, was readily demonstrable. Pre-clinical studies proved that Luminespib acts via several processes (cytostasis, apoptosis, invasion, and angiogenesis) to inhibit tumor growth and metastasis. These results helped Luminespib to enter clinical trials for various cancers including breast cancers. From 2011 to 2014 it was in Phase II clinical trials.
