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Restrict the search for
methyl salicylate
to a specific field?
Status:
Investigational
Source:
NCT01951222: Phase 2 Interventional Completed Asthma
(2013)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
(R)-Mequitazine or V0162 (10-[(3R)-1-azabicyclo[2.2.2]oct-3-ylmethyl]-10H-phenothiazine) is an anticholinergic enantiomer of mequitazine, an existing oral racemic antihistamine commercialized for over 30 years. (R)-Mequitazine was found to be an antagonist at muscarinic acetylcholine receptors behaving as an inverse agonist. (R)-Mequitazine was investigated in clinical trials for the treatment of chronic obstructive pulmonary disease, asthma and urinary incontinence.
Status:
Investigational
Source:
NCT01408667: Phase 1/Phase 2 Interventional Completed Metabolic Cardiovascular Syndrome
(2011)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
TRC-150094 is a synthetic compound that displays the capacity to stimulate energy expenditure. TRC-150094 increases whole body energy expenditure, increases mitochondrial fatty acid oxidation (FAO), and reduces abdominal adiposity in rats fed a high-fat diet. TRC-150094 attenuates the progression of hypertension, insulin resistance, dysglycemia, and atherogenic dyslipidemia, factors reported to signify significant cardiovascular (CV) risk amongst viscerally obese dysglycemic subjects. Moreover, at organ level, TRC150094 reduced steatohepatitis, reduced progression of nephropathy, and preserved cardiac contractile function. Pharmacological profile of TRC-150094 may constitute a promising new class of molecules that may have a potential beneficial therapeutic approach for the treatment of nontraditional CV risk factors and may reduce residual risk in viscerally obese dysglycemic patients. Moreover, the observed metabolic and functional effects on skeletal muscle suggest that TRC-150094 as a therapy may help to facilitate adherence to prescribed exercise, which would remain the mainstay along with diet control in such patients. Simultaneous systemic administration of TRC-150094 to rats receiving an high-fat diet results in a reduction in fat accumulation within the liver and a marked reduction in adipose tissue mass. TRC-150094 is in phase-III clinical trials for the treatment of diabetes mellitus, hypertension and dyslipidaemias (adjunctive treatment) in India.
Status:
Investigational
Source:
NCT03418623: Phase 2 Interventional Completed Alcohol Use Disorder
(2018)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
GET-73 (N-[(4-trifluoromethyl)benzyl]4-methoxybutyramide) is a compound with a structure related to that of gamma-hydroxybutyric acid (GHB), which is used in the treatment of alcohol withdrawal. Like GHB, GET-73 has the capacity to reduce alcohol intake in rats. GET-73 also exerts anxiolytic effects in rats and seemed to improve memory in a water maze test. Although the exact mechanism of GET-73 action is still unknown, it was suggested that an allosteric modulation of metabotropic glutamate receptor 5 (mGlu5 receptor) by GET-73 may represent the mechanism underlying the effects of the compound. GET73 was suggested to have a multifaceted pharmacological profile, importantly including the capacity to reduce alcohol drinking and anxiety-related behaviors. A phase II study was completed in November 2018, in which physical effects and changes in cognitive performance as a result of GET-73 administration were studied in alcohol-dependent individuals.
Status:
Investigational
Source:
NCT03730961: Phase 2 Interventional Completed Cardiac Failure
(2019)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Source:
NCT02232646: Phase 2 Interventional Withdrawn Urologic Malignancies
(2017)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Amcasertib is an orally administered investigational agent designed to inhibit cancer stemness pathways, including Nanog, by targeting stemness kinases. Amcasertib is undergoing multiple Phase I and Phase II studies as monotherapy and combination therapy for treating a range of tumor types.
Status:
Investigational
Source:
NCT00387140: Phase 2 Interventional Completed Pain, Postoperative
(2006)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Status:
Investigational
Source:
NCT04669067: Phase 1/Phase 2 Interventional Active, not recruiting Acute Myeloid Leukemia
(2021)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
p53 is a critical tumor suppressor and is the most frequently inactivated gene in human cancer. Inhibition of the interaction of p53 with its negative regulator MDM2 represents a promising clinical strategy to treat p53 wild-type tumors. AMG 232 is a potential best-in-class inhibitor of the MDM2-p53 interaction and is currently in clinical trials. Based on X-ray cocrystal structures a model of AMG 232 bound to MDM2 was developed. The model shows that the m-chlorophenyl, the p-chlorophenyl, and C-linked isopropyl fragments of AMG 232 bind to the Leu 26(p53), Trp 23(p53), and Phe 19(p53) pockets of MDM2, respectively. The carboxylic acid forms a salt bridge with His 96 and the isopropyl sulfone forms a novel interaction with the glycine shelf region of MDM2. AMG 232 in phase II in combination with trametinib and dabrafenib in subjects with metastatic melanoma; in phase I for the treatment of solid tumors, multiple myeloma and Acute Myeloid Leukemia.
Status:
Investigational
Source:
NCT03045861: Phase 2 Interventional Completed Infection, Human Immunodeficiency Virus
(2017)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Status:
Investigational
Source:
NCT03547115: Phase 1 Interventional Recruiting Follicular Lymphoma (FL)
(2018)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Voruciclib (also known as P1446A-05) is a flavone-based, potent and selective CDK 4/6 inhibitor with activity in multiple BRAF-mutant and wild type cell lines. It is currently in clinical trials in combination with BRAF inhibitor (PLX4032) to treat advanced BRAF-mutant melanoma. Voruciclib has significant inhibitory activity against cutaneous and uveal melanoma. Mechanistic studies revealed that P1446A-05 inhibits phosphorylation targets of CDK members, and induces cell cycle arrest and apoptosis irrespective of melanoma genotype or phenotype. Voruciclib Hydrochloride is in phase I clinical trials by Piramal Life Sciences for the treatment of chronic lymphocytic leukaemia and malignant melanoma.
Status:
Investigational
Source:
NCT02222363: Phase 1 Interventional Terminated Refractory Cancer
(2015)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
VLX600 - is a lipophilic cation-based triazinoindolyl-hydrazone compound and mitochondrial oxidative phosphorylation (OxPhos) inhibitor, with potential antineoplastic activity. VLX600 is designed to increase the efficacy of radiotherapy and to kill cancer cells that survive traditional chemotherapy. VLX 600 is a small molecule that inhibits deubiquitinating enzymes USP14 (a ubiquitin thiolesterase) and UCHL5 (a carboxypeptidase). Upon infusion, in normal cells and proliferating tumor cells where glucose is readily available, inhibition of OxPhos by VLX600 induces a hypoxia-inducible factor 1-alpha (HIF-1alpha)-dependent shift to, and an increase in glycolysis. Glycolysis alone does not produce enough energy to support the growth of tumor cells in this environment, and the induction of autophagy occurs. In the metabolically compromised tumor microenvironment, the availability of oxygen and glucose is limited due to poor vascularization and perfusion of tumor micro-areas. Tumor cells growing in this environment are thus unable to compensate for decreased mitochondrial function by increasing glycolysis. This leads to nutrient depletion, decreased energy production, induction of autophagy, tumor cell death and an inhibition of cell proliferation in quiescent tumor cells. Mitochondrial OxPhos, which is hyperactivated in cancer cells, plays a key role in the promotion of cancer cell proliferation. VLX-600 is in phase I clinical trials for the treatment of solid tumours. This compound was originally jointly discovered and developed by Vivolux and Karolinska Institute.
