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Showing 1341 - 1350 of 24164 results

Status:
Investigational
Source:
NCT04148287: Phase 2 Interventional Completed Candidemia
(2019)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
NCT02138812: Phase 1 Interventional Terminated Medical Oncology
(2014)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Empesertib (previously known as BAY-1161909) was developed as a selective inhibitor of the serine/threonine monopolar spindle 1 (Mps1) kinase for the treatment of cancer. Empesertib participated in phase I clinical trials in combination with paclitaxel in subjects with advanced malignancies. The studies were terminated because another more successful Mps1 inhibitor was being developed in parallel.
Status:
Investigational
Source:
NCT02414516: Phase 1 Interventional Unknown status Solid Tumor
(2015)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

OBP-801 (spiruchostatin A) is an inhibitor of histone deacetylase (HDAC) enzymes, with potential antineoplastic activity. OBP-801 was originally identified as an enhancer of PAI-1 gene expression and was established as a new HDAC inhibitor by a p21 promoter reporter screen. Upon administration, OBP-801 inhibits the activity of HDACs; this results in an accumulation of highly acetylated chromatin histones, the induction of chromatin remodeling and an altered pattern of gene expression. This leads to selective transcription of tumor suppressor genes, tumor suppressor protein-mediated inhibition of tumor cell division and induction of tumor cell apoptosis. This may inhibit proliferation of susceptible tumor cells. HDAC, which is upregulated in many tumor cell types, deacetylates chromatin histone proteins. OBP‑801 induces M‑phase arrest and apoptosis in rhabdomyosarcoma cells. OBP‑801 is expected to show anticancer effect by promoting an expression of tumor suppressor genes in cancer cell and inducing apoptotic and autophagic cell death. The results of pre-clinical studies on OBP-801 indicated the most potent HDAC inhibitory activity as compared to other HDAC inhibitors including and Zolinza® and Istodax®, and its efficacy on a wide range of cancers is expected. Furthermore, Oncolys has been exploring the potential ophthalmic use of OBP-801 in collaboration with Kyoto Prefectural University of Medicine. OBP-801 has been used in trials studying the treatment of solid tumor.
Status:
Investigational
Source:
NCT03320941: Phase 2 Interventional Completed Obesity
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

LIK-066 (licogliflozin) is an inhibitor of the sodium-dependent glucose co-transporter (sodium-glucose transporter; sodium-glucose transport protein; sodium-glucose linked transporter; SGLT) family members 1 and 2 (SGLT1/2) with antihyperglycemic activity. By binding to and blocking SGLT1/2, licogliflozin suppresses the reabsorption of glucose in the proximal tubule within the kidneys and enhances urinary excretion of glucose. This normalizes blood glucose levels. LIK-066 is in phase II clinical trials by Novartis for the treatment of type 2 diabetes. Licogliflozin treatment (1-84 days) leads to significant weight loss and favorable changes in a variety of metabolic parameters and incretin hormones. Dual inhibition of SGLT1/2 with licogliflozin in the gut and kidneys is an attractive strategy for treating obesity and diabetes.
Status:
Investigational
Source:
NCT04092452: Phase 2 Interventional Completed Acne Inversa
(2019)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



PF-06700841 is an inhibitor of JAK1 and TYK2 kinases. PF-06700841 tosylate salt is potentially a treatment of systemic lupus erythematosus and plaque psoriasis.
Status:
Investigational
Source:
NCT04052516: Phase 2 Interventional Completed Non Alcoholic Steatohepatitis (NASH)
(2019)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Icosabutate (also known as PRC-4016 or NST-4016), a cholesterol ester transfer protein inhibitor was developed by NorthSea Therapeutics for the treatment of combined dyslipidemias and hypertriglyceridemia. Icosabutate successfully completed phase II clinical trial for hypertriglyceridemic subjects, where was studied the drug efficacy and safety. In April 2018 NorthSea Therapeutics announced that its lead product, icosabutate would be further developed as an effective and safe therapeutic approach to treating both non-alcoholic steatohepatitis and its associated comorbidities.
Status:
Investigational
Source:
NCT02243917: Phase 1 Interventional Terminated Advanced Solid Tumors
(2014)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



CB-5083 is a novel first in class, potent orally bio-available p97 inhibitor that disrupts cellular protein homeostasis and demonstrates anti-tumor activity in solid and hematological models. CB-5083 causes rapid and sustained accumulation of poly-ubiquitin in tumor xenografts after a single administration. CB-5083 showed activity to inhibit tumor growth in multiple rodent models of human cancer. Furthermore, CB-5083 appears to exhibit greater potency over current proteasome inhibitors that further validate targeting p97 and protein homeostasis in the treatment of cancer. CB-5083 is a potent inhibitor of endoplasmic reticulum associated degradation and induces a lethal unfodled protein response. CB-5083 recently began Phase 1 testing in relapsed/refractory or refractory multiple myeloma, and advanced solid tumors.
Status:
Investigational
Source:
INN:monophosphothiamine
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Monophosphothiamine is thiamine derivative used for the treatment of neuritis, polyneuritis, asthenic conditions (weakness), as an additional remedy for chronic blood circulation insufficiency, chronic gastritis accompanied by motor and secretory disorders functions of the stomach. Monophosphothiamine underwent metabolic phosphorylation to active metabolite thiamine pyrophosphate, that acts as a coenzyme in the different metabolic process.
Status:
Investigational
Source:
NCT02334982: Phase 1 Interventional Completed Dose Finding Study
(2013)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
NCT03881059: Phase 2 Interventional Completed Active Psoriatic Arthritis
(2019)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

BMS-191011, an opener of the cloned large-conductance, Ca2+-activated potassium (maxi-K) channel, demonstrated efficacy in in vivo stroke models, which led to its nomination as a candidate for clinical evaluation. Its maxi-K channel opening properties were consistent with its structural topology, being derived by combining elements from other known maxi-K openers. BMS-191011 demonstrated efficacy as an opener of the cloned large-conductance Ca2+-activated potassium (maxi-K) channel in in vivo stroke models

Showing 1341 - 1350 of 24164 results