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

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Showing 11581 - 11590 of 13240 results

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

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT01970215: Phase 2 Interventional Completed Dyslipidemia
(2013)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT00858377: Phase 1 Interventional Completed Advanced Malignancy
(2009)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Amgen is developing AMG-900, an orally active, small molecule aurora kinase A, B and C inhibitor for the treatment of solid tumours and haematological malignancies. In tumor cells, AMG-900 inhibited autophosphorylation of aurora-A and -B as well as phosphorylation of histone H3 on Ser(10), a proximal substrate of aurora-B. The predominant cellular response of tumor cells to AMG-900 treatment was aborted cell division without a prolonged mitotic arrest, which ultimately resulted in cell death. AMG-900 inhibited the proliferation of 26 tumor cell lines, including cell lines resistant to the antimitotic drug paclitaxel and to other aurora kinase inhibitors (AZD1152, MK-0457, and PHA-739358), at low nanomolar concentrations. Furthermore, AMG-900 was active in an AZD1152-resistant HCT116 variant cell line that harbors an aurora-B mutation (W221L). Oral administration of AMG-900 blocked the phosphorylation of histone H3 in a dose-dependent manner and significantly inhibited the growth of HCT116 tumor xenografts. Importantly, AMG-900 was broadly active in multiple xenograft models, including 3 multidrug-resistant xenograft models, representing 5 tumor types. AMG-900 has entered clinical evaluation in adult patients with advanced cancers and has the potential to treat tumors refractory to anticancer drugs such as the taxanes.
Status:
Investigational
Source:
NCT00620568: Phase 1 Interventional Terminated Healthy
(2008)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Adoprazine (SVL-313) is a full 5-HT1A receptor agonist and full D2/3 receptor antagonist possessing characteristics of an atypical antipsychotic, representing a potential novel treatment for schizophrenia and bipolar disorder. This drug together with some others, e.g. Mazapertine succinate, PF-217830 was discontinued from clinical trials due to either non-optimal pharmacokinetic properties or insufficient therapeutical efficacy.
Status:
Investigational
Source:
INN:octacaine
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Octacaine was developed as a local anesthetic agent. Information about the current use of this drug is not available.
Status:
Investigational
Source:
NCT03025308: Phase 3 Interventional Active, not recruiting Rheumatoid Arthritis
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Filgotinib (GLPG0634) is a highly selective JAK1 inhibitor. GLPG0634 is a promising drug candidate for the future treatment of autoimmune and inflammatory disorders. It is in phase III clinical trials (initiated mid-2016) for the treatment of rheumatoid arthritis, Crohn's disease and ulcerative colitis. Most common adverse events observed were infections, gastrointestinal disorders and nervous system disorders.
Status:
Investigational
Source:
NCT03025308: Phase 3 Interventional Active, not recruiting Rheumatoid Arthritis
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Filgotinib (GLPG0634) is a highly selective JAK1 inhibitor. GLPG0634 is a promising drug candidate for the future treatment of autoimmune and inflammatory disorders. It is in phase III clinical trials (initiated mid-2016) for the treatment of rheumatoid arthritis, Crohn's disease and ulcerative colitis. Most common adverse events observed were infections, gastrointestinal disorders and nervous system disorders.
Status:
Investigational
Source:
NCT03863574: Phase 2 Interventional Completed Non Alcoholic Steatohepatitis
(2019)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Saroglitazar, a dual peroxisome proliferator-activated receptor PPAR-α/γ agonist, was an emerging therapeutic option on glycemic and lipid parameters. The Zydus Group has launched LipaglynTM ((Saroglitazar) in India for diabetic dyslipidemia and hypertriglyceridemia with type 2 diabetes mellitus not controlled by statin therapy. In addition, saroglitazar participated in phase II clinical trials that completed enrolment in patients with primary biliary cholangitis and in patients with non-alcoholic steatohepatitis.
Status:
Investigational
Source:
NCT04663308: Phase 2 Interventional Recruiting Primary Sclerosing Cholangitis
(2020)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Volixibat (SHP626; formerly LUM002) is a potent inhibitor of the apical sodium-dependent bile acid transporter (ASBT) that was developed for the treatment of nonalcoholic steatohepatitis. Volixibat participated in phase II clinical trial to investigate its safety, effectiveness in adults with nonalcoholic steatohepatitis. However, this study was discontinued, without any further explanation for the possible causes. In addition, volixibat was studied in a clinical trial in healthy adults and in patients with type 2 diabetes mellitus, where was shown that the drug was generally well tolerated.
Status:
Investigational
Source:
NCT00414999: Phase 1 Interventional Completed Macular Degeneration
(2006)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



AGE-RELATED MACULAR DEGENERATION (AMD), PROLIFERATIVE DIABETIC RETINOPATHY (PDR) AND DIABETIC MACULAR EDEMA (DME) are collectively characterized by VEGF mediated retinal leakage, angiogenesis, and an underlying inflammatory process. TargeGen's TG100801 is designed to inhibit a select group of kinases involved in those three processes. Currently approved drug based therapy for macular degeneration requires repeated injection into the eye. TG100801 is the first topically applied, VEGFR)/Src kinase inhibitor to advance into the clinic for the treatment of Age-related macular degeneration, diabetic retinopathy. The formation of new blood vessels (angiogenesis), blood vessel leakage, and inflammation contribute to the progression of the eye disease, which is the leading cause of irreversible, severe loss of vision in people 55 years of age and older in the developed world. In cell based assays, following topical instillation, TG100572, the active drug produced by conversion of TG100801 as it penetrates the eye, was shown to induce apoptosis in proliferating endothelial cells responsible for neovasculariztion and to inhibit inflammatory-mediated processes as measured by endotoxin-induced nitric oxide release in vitro.

Showing 11581 - 11590 of 13240 results