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

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Showing 1001 - 1010 of 13240 results

Status:
Investigational
Source:
NCT01291108: Phase 2 Interventional Completed Glaucoma, Open-Angle
(2011)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Simenepag (AGN-210676) is a a small molecule selective prostaglandin EP2 agonist with EC50 of 5 nM. Allergan was developing simenepag for the treatment of glaucoma and ocular hypertension.
Status:
Investigational
Source:
NCT00874302: Phase 3 Interventional Withdrawn Uterine Fibroids
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Telapristone is an orally available 21-substituted-19-nor-progestin and selective progesterone receptor modulator (SPRM), with potential anti-progesterone and antineoplastic activities. Its acetate form, the telapristone Acetate is a clinically used and a studied drug.
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:
NCT00274716: Phase 2 Interventional Completed Hypertension
(2005)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

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.
Status:
Investigational
Source:
NCT03034967: Phase 2 Interventional Completed Pulmonary Disease, Chronic Obstructive
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Danixirin is a potent, competitive, selective and reversible antagonist of the chemokine receptor (CXCR2) (also known as interleukin 8B receptor). In preclinical models, danixirin blocked neutrophils chemotaxis in response to inflammation. The drug is being developed by GlaxoSmithKline for the treatment of chronic obstructive pulmonary disease, influenza, respiratory syncytial virus. In phase 2 clinical trials in patients with acute, uncomplicated influenza, danixirin was well tolerated and did not impede viral clearance.
Status:
Investigational
Source:
NCT00934089: Phase 2 Interventional Completed Glaucoma, Open-Angle
(2010)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Taprenepag isopropyl (also known as PF-04217329) a prodrug of CP-544326 (active acid metabolite), a potent and selective EP(2) receptor agonist. Taprenepag isopropyl was studied in a clinical trials phase II involving patients with primary open angle glaucoma. According to Pfizer’s pipelines in May 2011, the study was discontinued.
Status:
Investigational
Source:
NCT03677492: Not Applicable Interventional Completed Infertility
(2018)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Cytochalasin D, a tropical fungal metabolite, is a disruptor of actin filament function, resulting in multinucleated cell formation, reversible inhibition of cell movement, and the induction of cellular extrusion. It was shown that cytochalasin D inhibits murine CT26 colorectal carcinoma cells growth and angiogenesis.
Status:
Investigational
Source:
NCT01471665: Phase 2 Interventional Completed Asthma
(2011)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Fiboflapon sodium (GSK2190915) is a high affinity 5-lipoxygenase-activating protein inhibitor being developed for the treatment of asthma. The compound was originally developed by Amira Pharmaceuticals. Fiboflapon sodium (GSK2190915) exhibits excellent preclinical toxicology and pharmacokinetics in rat and dog. GSK2190915 also demonstrated an extended pharmacodynamic effect in a rodent bronchoalveolar lavage (BAL) model. Oral administration of Fiboflapon sodium (GSK2190915) (1 mg/kg) resulted in sustained inhibition of ex vivo ionophore-challenged whole blood LTB4 biosynthesis with >90% inhibition for up to 12 h and an EC50 of approximately 7 nM. When rat lungs were challenged in vivo with calcium-ionophore, Fiboflapon sodium inhibited LTB4 and cysteinyl leukotriene (CysLT) production with ED50s of 0.12 mg/kg and 0.37 mg/kg, respectively. Fiboflapon sodium is in Phase-II for Asthma (Adjunctive treatment) in Poland, Ukraine, Bulgaria, USA, United Kingdom and Canada (PO).
Status:
Investigational
Source:
NCT00929539: Phase 2 Interventional Completed Type II Diabetes Mellitus
(2009)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Granotapide (JTT-130) has been studied for use in treatment of diabetes mellitus type II. This intestine-specific microsomal transfer protein inhibitor has hypoglycemic effects. Granotapide is thought to block fat absorption, which results in enhanced glucose-stimulated insulin secretion and enhanced insulin sensitivity. In an animal study, granotapide improved hyperglycemia and dyslipidemia via a mechanism independent of suppression of food intake. Granotapide enhances glucagon-like peptide-1 secretion and reduces lipotoxicity. A phase 2 study has been conducted to evaluate the effect of JTT-130 on diabetes as well as the safety and tolerability of JTT-130 in obese Type 2 diabetic patients.

Showing 1001 - 1010 of 13240 results