U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 371 - 380 of 4343 results

Status:
Investigational
Source:
INN:zelavespib [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



PU-H71 is experimental inhibitor of Hsp90. It is being tested in clinical trials against lymphoma and solid tumors.
Status:
Investigational
Source:
INN:sodium timerfonate
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Thimerfonate is a alkyl mercuric derivative with germicidal activity.
Status:
Investigational
Source:
NCT02267863: Phase 1 Interventional Terminated Acute Myelogenous Leukemia in Relapse
(2014)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



APTO-253 is a novel small molecule that can induce expression of the genes that code for the Krüppel-like factor 4 (KLF4) master transcription factor and for the p21 cell cycle inhibitor protein, and can inhibit expression of the c-Myc oncogene, leading to cell cycle arrest and programmed cell death (apoptosis) in human-derived solid tumor and hematologic cancer cells. A Phase 1 study with APTO-253 was completed and demonstrated modest clinical activity in patients with colon cancer, acute leukemia, myelodysplastic syndrome, hematological malignancies and non-small cell lung cancers.
Status:
Investigational
Source:
NCT03388749: Phase 1/Phase 2 Interventional Completed Leukemia, Myeloid, Acute
(2018)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Annamycin is a highly lipophilic form of the anthracycline doxorubicin with the ability to bypass multidrug resistance mechanisms of cellular drug resistance. Annamycin belongs to the anthracycline class of drugs, and has a pleiotropic mechanism of action where it targets topoisomerase II, causing strand breaks in DNA. Annamycin forms complexes with DNA by intercalation between base pairs, and it inhibits topoisomerase II activity by stabilizing the DNA-topoisomerase II complex, preventing the religation portion of the ligation-religation reaction that topoisomerase II catalyzes. The agent is being evaluated in separate phase 1 and phase 2 trials in the United States and Europe. Studies in animal models showed the agent to be noncardiotoxic. Trials that included patients with leukemia showed the agent was associated with fewer dose-limiting toxicities than typically experienced with doxorubicin. The FDA granted fast track designation to Annamycin for treatment of patients with relapsed or refractory acute myeloid leukemia.
Status:
Investigational
Source:
NCT01740609: Phase 1 Interventional Completed Healthy
(2012)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Parafluorofentanyl is a selective mu-opioid agonist, an analog of fentanyl, developed by Janssen. The drug was not developed for human use but is produced and abused illegally.
Status:
Investigational
Source:
NCT03506945: Not Applicable Interventional Recruiting Depressive Symptoms
(2018)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



MPEP (2-methyl-6-(phenylethynyl)pyridine) was one of the first compounds found to act a selective antagonist for the metabotropic glutamate receptor subtype mGluR5. It was under development by Novartis in the late 1990's. MPEP was found to produce neuroprotective effects following acute brain injury in animals. MPEP was also found to have positive effects on animal models of depression, anxiety and morphine withdrawl.
Status:
Investigational
Source:
NCT00446342: Phase 1 Interventional Completed B-lymphoid Malignancies
(2007)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



SNS-032 (formerly BMS-387032) is a potent, selective inhibitor of cyclin-dependent kinases (CDK). SNS-032 blocks the cell cycle via inhibition of CDKs 2 and 7, and transcription via inhibition of CDKs 7 and 9. SNS-032 was investigated for the treatment of solid tumors and hematologic malignancies (Phase I studies), however, its development was discontinued.
Avelestat, also known as AZD9668, is a novel, oral inhibitor of neutrophil elastase (NE), an enzyme implicated in the signs, symptoms, and disease progression in NE-driven respiratory diseases such as bronchiectasis, Cystic Fibrosis and chronic obstructive pulmonary disease via its role in the inflammatory process, mucus overproduction, and lung tissue damage. Its development was discontinued due to unknown reasons. Nevertheless, this drug in the phase II of clinical trial as adjunctive therapy in improving insulin sensitivity of insulin-resistant type 2 diabetic subjects. The drug's clinical profile suggests that it will be well tolerated with few, if any, side effects, and the existence of simple methods that can indirectly measure its activity in vivo.
Mavoglurant (AFQ056) was developed as a new metabotropic glutamate receptor 5 (mGluR5) antagonist. The efficacy of mavoglurant in humans has been assessed in L-dopa induced dyskinesia in Parkinson's disease and Fragile X syndrome in proof of principle clinical studies. However, Novartis had announced that the company would be discontinuing its development program in Fragile X following negative results in a large international clinical trial in adults, and more recently in a trial in adolescents. In both placebo-controlled trials, patients taking mavoglurant did not show improvement over placebo in any outcome measures. In patients with L-Dopa-induced dyskinesias studies failed to meet the primary objective of demonstrating improvement of dyskinesia. Mavoglurant was also investigated in phase II clinical trials to reduce chorea in Huntington's disease, but the target result was not achieved. Currently Novartis is conducting a phase II clinical trial to demonstrate whether or not this drug can benificially reduce cocaine use in Cocaine Use Disorder.
Status:
Investigational
Source:
INN:aganepag [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Aganepag is a potent Prostanoid EP2 receptor agonist, with an EC50 of 0.19 nM, and shows no activity at EP4 receptor. Aganepag can be used in the research of wound healing, scar reduction, scar prevention and wrinkle treatment and prevention. Aganepag is an antiglaucoma agent.