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

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Showing 1561 - 1570 of 24164 results

Status:
Investigational
Source:
NCT01039701: Phase 2 Interventional Completed Mild to Moderate Alzheimer's Disease
(2009)
Source URL:

Class (Stereo):
CHEMICAL (UNKNOWN)

Status:
Investigational
Source:
NCT04251182: Phase 2 Interventional Completed Alzheimer Disease
(2021)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT00740610: Phase 2 Interventional Completed Nonalcoholic Steatohepatitis
(2008)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Nivocasan (aka GS-9450) was discovered by LG Life Sciences and developed by Gilead Sciences. Nivocasan is an irreversible inhibitor of caspase 1, 8, and 9, and therefore able to prevent apoptosis. Nivocasan has been investigated as a treatment option for Hepatic fibrosis and Non-alcoholic steatohepatitis related to Hepatitis C infection. It had advanced to Phase II clinical trials before the development program was suspended.
Status:
Investigational
Source:
NCT03808714: Not Applicable Interventional Terminated Smoking Cessation
(2016)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
NCT03166085: Phase 1 Interventional Completed Metastatic Breast Cancer
(2017)
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:
NCT01269593: Early Phase 1 Interventional Active, not recruiting Non-Hodgkin's Lymphoma
(2010)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
NCT03838926: Phase 1 Interventional Unknown status Relapsed or Refractory Hematologic Malignancies
(2018)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Trichostatin A (TSA) was originally isolated as an antifungal antibiotic along with its fermentation congeners trichostatin B ((TSA)3-Fe) and the D-glucopyranosides trichostatin C and D. TSA inhibits HDAC in the low nanomolar range and is an inducer of histone hyperacetylation, both in vitro and in vivo. It inhibits all class I and II deacetylases to a similar extent in both tumor and non-tumor cells, although HDAC4 is slightly resistant when compared with HDAC1 and HDAC6. Class III HDAC is not affected by TSA. It has been shown that TSA dosedependently inhibits growth and induces apoptosis in a plethora of carcinoma cell lines in vitro. Recently, it was also found that TSA inhibits angiogenesis, which is important for the growth and metastasis of solid tumors, both in vivo and in vitro. In HT-29 colon carcinoma cells, a single dose of TSA induced transient hyperacetylation of histone H4 resulting in the induction of p21WAF1/Cip1 and inhibition of cellular proliferation at both the G1 and G2 phases of the cell cycle. Growth inhibition was associated with decreased cyclin D1 mRNA and cdk6 protein levels and increased cyclin D3 protein and p21WAF1/Cip1 mRNA levels. Cyclin D1 protein, cyclin D3 mRNA, cdk2 and cdk4 remained unaffected. In addition, TSA induced apoptosis by upregulating the expression of the pro-apoptotic genes ID1, ID2 and ID3, whereas the expression of the anti-apoptotic genes BclxL and Hsp27 was decreased In vivo, TSA induces differentiation and shows chemotherapeutic activity against N-methylnitrosureainduced rat mammary cancer without toxic side effects. TSA may also have therapeutic potential for the treatment of a variety of genetic and infectious diseases since silenced, transduced genes are reactivated probably due to structural changes of the chromatin on integrated viral sequences.
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:
NCT00960557: Phase 1 Interventional Completed Neoplasm Metastasis
(2009)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Oxi0-4503 (now known as combretastatin A1 phosphate), a diphosphate prodrug of combretastatin A1, was developed by Mateon therapeutics as a second-generation, dual-mechanism vascular disrupting agent from the combretastatin family. On November 21, 2012, Oxi-4503 has been granted orphan designation by the US Food and Drug Administration for the treatment of acute myelogenous leukemia. It is known that the orphan drug designation qualifies a company for several benefits, including the potential for market exclusivity, development grants, and tax credits. Oxi0-4503 is currently participating in phase I/II clinical trial the treatment of patients with acute myelogenous leukemia or myelodysplastic syndrome. In addition, phase I clinical trial was successfully completed where was studied the safety of Oxi0-4503 in patients with advanced solid tumors.
Status:
Investigational
Source:
NCT01211470: Phase 2 Interventional Completed Acute Bacterial Skin and Skin-structure Infection(ABSSSI) Due to Staphylococcus Aureus (MSSA)
(2010)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Brilacidin (formerly PMX-30063) is a polymer-based antibiotic and an investigational new drug, that was studied in human clinical trials, and represents a new class of antibiotics called host defense protein mimetics. Brilacidin is an antibiotic that works by disrupting bacterial cell membranes, mimicking defensins that play a role in innate immunity. Brilacidin has shown great efficacy in phase II clinical trials against acute Staphylococcus aureus skin and skin structure infections, comparable to that of the lipopeptidic drug daptomycin, which is currently used clinically to treat drug-resistant staph infections. Brilacidin also has potent broad-spectrum activity in vitro against several other Gram-positive and Gram-negative pathogenic bacteria, including several multidrug-resistant strains.

Showing 1561 - 1570 of 24164 results