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Restrict the search for
telotristat ethyl
to a specific field?
Status:
Investigational
Source:
INN:tracazolate [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Tracazolate (ICI 136,753), a pyrazolopyridine, is a non-benzodiazepine with anxiolytic-like activity in animal models. It is known to interact with gamma-aminobutyric acid (GABA)(A) receptors, adenosine receptors, and phosphodiesterases. Its intrinsic efficacy, potentiation, or inhibition is determined by the nature of the third subunit (gamma1-3, delta, or epsilon) within the GABA(A) receptor complex.
Status:
Investigational
Source:
NCT02260661: Phase 1 Interventional Completed Advanced Solid Malignancies
(2014)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
AZD-8835 is a potent inhibitor of PI3Kα and PI3Kδ with selectivity versus PI3Kβ, PI3Kγ, and other kinases that preferentially inhibited growth in cells with mutant PIK3CA status, such as in estrogen receptor-positive (ER(+)) breast cancer cell lines BT474, MCF7, and T47D (sub-umol/L GI50s). Consistent with this, AZD-8835 demonstrated antitumor efficacy in corresponding breast
cancer xenograft models when dosed continuously. AZD-8835 is a selective, oral inhibitor of PI3K isoforms α and δ with the following activity in enzymatic assays: PI3K α – IC50 = 6nM (equipotent vs wt and E545K / H1047R mutants); PI3K δ – IC50 = 6nM; PI3K γ – IC50 = 90nM; PI3K β – IC50 = 431nM. Inhibition of signalling in cells (pAKT endpoint): PI3K α – IC50 = 57nM; PI3K δ – IC50 = 49nM; PI3K β – IC50 = 3.6uM; PI3K γ - IC50 = 532nM. AZD-8835 is in phase I clinical studies by AstraZeneca for the treatment of advanced solid tumors and ER+ and HER-2 negative breast cancer.
Status:
Investigational
Source:
INN:fenpipalone [INN]
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
FENPIPALONE is an oxazolidinone derivative with central nervous system depressant and antiinflammatory activity in animal models. However, FENPIPALONE did not demonstrate any usefulness for severely ill chronic schizophrenic patients.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Etocrylene is an organic ester that appears as an off-white crystalline powder and functions as a UV absorber. When applied to the skin, this product absorbs UV rays. It can also be used to protect cosmetics and personal care products from deterioration. This product can be used in the formulation of sun protection products, as well as bath, skin, cleansing, hair, nail and fragrance products.
Status:
Investigational
Source:
JAN:S-HYDROPRENE [JAN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
S-Hydroprene is an insecticide used against cockroaches, beetles, and moths. S- Hydroprene belongs to the class of insecticides known as insect growth regulators. S-Hydroprene disrupts normal development and molting of insects by mimicking hormones produced by immature insects. S-Hydroprene causes different effects on different insects. It may cause adult sterility, physical body changes, water loss, and premature death. S-hydroprene is currently used indoors, and therefore are not expected to pose a risk to the environment.
Status:
Class (Stereo):
CHEMICAL (RACEMIC)
Hexasonium, an anticholinergic agent, was studied as a spasmolytic. Information about the current use of this drug is not available.
Status:
Investigational
Source:
NCT04432090: Phase 2 Interventional Completed Diabetes Mellitus, Type 1
(2021)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
MBX-2982 is a potential first-in-class treatment for type 2 diabetes that targets G protein-coupled receptor 119 (GPR119), a receptor that interacts with bioactive lipids known to stimulate glucose-dependent insulin secretion. Preclinical data indicate that MBX-2982 is a potent selective orally-active GPR119 agonist that functions through a unique dual mechanism of action. First, it acts directly on the beta cell to increase insulin secretion. In addition, MBX-2982 stimulates release of the incretin GLP-1 from the gut. This dual action is unique and may offer improved glucose homeostasis over existing diabetes therapies, with potential for weight loss and improved islet health. MBX-2982 has completed four Phase 1 studies and one Phase 2 study. In the 4-week Phase 2 study in diabetics, MBX-2982 lowered mean weighted glucose and postprandial glucose during an extended mixed-meal tolerance test (MMTT). Treatment with MBX-2982 increased insulin, active GLP-1, and total GLP-1 during an extended MMTT. Treatment with MBX-2982 also tended to increase fasting insulin and c-peptide, and decrease fasting triglycerides. In all studies to date, MBX-2982 demonstrated dose-dependent increases in drug exposure with a profile supporting once daily oral dosing that was safe and well tolerated with no serious adverse events, adverse event trends or dose-limiting toxicities. These results provide clinical validation for the potential therapeutic benefits of MBX-2982 as a type 2 diabetes treatment.
Status:
Investigational
Source:
NCT01573819: Phase 1 Interventional Completed Huntington Disease
(2011)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
GlaxoSmithKline is developing GSK-356278 as a selective, brain-penetrant phosphodiesterase 4 (PDE4) inhibitor that demonstrates anxiolytic and cognition-enhancing effects. Small molecule phosphodiesterase (PDE) 4 inhibitors have long been known to show therapeutic benefit in various preclinical models of psychiatric and neurologic diseases because of their ability to elevate cAMP in various cell types of the central nervous system. The drug was studied for the treatment of Huntington's disease, depressive and anxiety disorders. GSK-356278 has completed phase I clinical trials for evaluation of the safety, tolerability, and pharmacokinetics in male volunteers with the therapeutic dose for future clinical development.
Status:
Investigational
Source:
NCT02573870: Phase 2 Interventional Completed Pulmonary Disease, Chronic Obstructive
(2015)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Batefenterol, previously known as GSK961081, a bifunctional muscarinic (M2 and M3 receptors) antagonist β2-agonist that is developed for chronic obstructive pulmonary disease (COPD). The drug has successfully completed phase II clinical trials with clinically significant improvements in lung function. No new or unexpected safety signals were observed in this COPD population. The conclusion from the trial was following that batefenterol 300 µg might represent the optimal dose for Phase III studies.
Status:
Investigational
Source:
NCT00719394: Phase 1 Interventional Completed Alzheimer Disease
(2008)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
GSI-136 is an amyloid protein secretase inhibitor that has been tested for treatment of Alzheimer Disease. This γ-Secretase inhibitor was evaluated in a phase I clinical trial to determine its safety and tolerability in healthy subjects after administration of single oral doses.
