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

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Showing 49641 - 49650 of 55039 results

Status:
Investigational
Source:
NCT01049113: Phase 1 Interventional Terminated Lymphoma
(2009)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Briciclib (also known as ON-013105 and ON-014185) has the potential of targeting and inhibition of eukaryotic translation initiation factor 4E (eIF4E) for solid cancers. eIF4E is a proto-oncogene that promotes translation of several genes essential for cellular proliferation (cyclin D1, c-Myc, mTOR), survival (Akt), angiogenesis (VEGF), and metastasis (MMP9). Overexpression of eIF4E has been observed in almost all major groups of cancers and has been shown to induce increased expression of cyclin D1 and c-Myc). An intravenous formulation of briciclib was being investigated in the Phase 1 clinical trial. The purpose of the study was to determine the highest dose of briciclib that could be given safely in patients with relapsed/refractory Lymphoma or B-cell Acute Lymphocytic Leukemia (Philadelphia chromosome negative). However, this study was terminated because of the lack of available clinical drug supply. In addition, briciclib was also involved in phase I clinical trials with advanced cancer and solid tumors, to determine the highest dose that can be safely given.
Status:
Investigational
Source:
NCT04505267: Phase 1 Interventional Recruiting Recurrent Lung Non-Small Cell Carcinoma
(2021)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Hafnium oxide is a radio enhancer; its nanoparticles (NBTXR3) were designed for high dose energy deposition within cancer cells when exposed to ionizing radiation. When activated by radiotherapy (RT), NBTXR3 allows for a higher energy deposit than RT alone, yielding an increased tumoral cell death. Nanocrystals of hafnium oxide are under investigation in phase II/III in patients with locally advanced soft tissue sarcoma (STS) of the extremity and trunk wall. In addition, NBTXR3, nanoparticles are being studied in phase I/II in patients with head and neck cancer; liver cancer; prostate cancer and rectal cancer.
Status:
Investigational
Source:
INN:traxanox
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Traxanox is a diuretic agent possessing an uricosuric effect in animals. The diuretic and uricosuric effects of the drug have also been demonstrated in normotensive healthy subjects. The chronic administration of traxanox reduces serum uric acid level as well as blood pressure in patients with mild to moderate hypertension. This reduction in serum uric acid is due in part to a traxanox-induced elevation of urinary uric acid excretion. Traxanox sodium stimulates the phagocytic activity of leukocytes or macrophages and prevents the drug-induced suppression of the phagocytic activity of these cells. Traxanox may be clinically effective in treating patients with nasal allergies. The mode of action of traxanox on inflammatory responses resembles that of D-penicillamine or levamisole, so that it may prove to be clinically effective in treating rheumatoid arthritis. Also, traxanox may be effective for the treatment of allergic bronchial asthma.
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:
NCT04467840: Phase 2/Phase 3 Interventional Completed COVID-19
(2020)
Source URL:

Class (Stereo):
CHEMICAL (MIXED)



ABC-294640 is an orally bioavailable and selective sphingosine kinase-2 (SphK2) inhibitor with IC50 of approximately 60 uM. ABC-294640 inhibits SK2, a lipid kinase that catalyzes formation of the lipid signaling molecule sphingosine 1-phosphate (S1P). S1P promotes cancer growth, and proliferation and pathological inflammation, including TNFα signaling and other inflammatory cytokine production. Specifically, by inhibiting the SK2 enzyme, ABC-294640 blocks the synthesis of S1P which regulates fundamental biological processes such as cell proliferation, migration, immune cell trafficking and angiogenesis, and are also involved in immune-modulation and suppression of innate immune responses from T cells. Preliminary evidence suggests that because of its specificity for targeting SK2, rather than SK1, ABC-294640 may have a better therapeutic ratio than nonspecific sphingosine kinase inhibitors or those targeting only SK1. Oral administration of ABC-294640 to mice bearing mammary adenocarcinoma xenografts results in dose-dependent antitumor activity associated with depletion of S1P levels in the tumors and progressive tumor cell apoptosis. Therefore, this newly developed SK2 inhibitor provides an orally available drug candidate for the treatment of cancer and other diseases. ABC-294640 has completed multiple successful pre-clinical studies in inflammatory, GI, radioprotection and oncology models, as well as a Phase I clinical study in cancer patients with advanced solid tumors.
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:
NCT01281189: Phase 3 Interventional Completed Amyotrophic Lateral Sclerosis
(2011)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Dexpramipexole (also known as KNS-760704/R-pramipexole) was originally developed by University of Virginia researchers to treat Amyotrophic Lateral Sclerosis and then was licensed to global biotechnology company Biogen Idec for further development. However, on phase III clinical trial the study of this drug was discontinued. Biogen said the drug neither slowed the loss of muscle function nor prolonged the lives of patients with ALS, often called Lou Gehrig’s disease. Nor did it show any efficacy in secondary endpoints of the clinical trial, or work in any sub-group of patients—about a big a failure as a company could have a Phase III trial. In addition, was discovered, that dexpramipexole was able to bind to beta-subunit of the mitochondrial F1/FO ATP synthase complex and increased its activity, thus reduced ischemic brain injury. These findings, together with the excellent brain penetration and favorable safety profile in humans, make dexpramipexole a drug with realistic translational potential for the treatment of stroke.
Status:
Investigational
Source:
NCT02311933: Phase 2 Interventional Active, not recruiting Recurrent Breast Carcinoma
(2015)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Endoxifen, also known as N-desmethyl-4-hydroxytamoxifen, is active metabolites of tamoxifen. This metabolite exhibits a 100-fold higher binding affinity to the estrogen receptor (ER) and are more effective in suppressing cell proliferation than tamoxifen. In humans, the conversion from tamoxifen to endoxifen is predominant. Endoxifenis is an orally active, selective estrogen receptor modulator (SERM) that was developed for the treatment of estrogen receptor-positive breast cancer. In addition, this drug possesses antimanic properties, what can be used in the treatment of patients with bipolar I disorder (BPD I).
Status:
Investigational
Source:
NCT01281189: Phase 3 Interventional Completed Amyotrophic Lateral Sclerosis
(2011)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Dexpramipexole (also known as KNS-760704/R-pramipexole) was originally developed by University of Virginia researchers to treat Amyotrophic Lateral Sclerosis and then was licensed to global biotechnology company Biogen Idec for further development. However, on phase III clinical trial the study of this drug was discontinued. Biogen said the drug neither slowed the loss of muscle function nor prolonged the lives of patients with ALS, often called Lou Gehrig’s disease. Nor did it show any efficacy in secondary endpoints of the clinical trial, or work in any sub-group of patients—about a big a failure as a company could have a Phase III trial. In addition, was discovered, that dexpramipexole was able to bind to beta-subunit of the mitochondrial F1/FO ATP synthase complex and increased its activity, thus reduced ischemic brain injury. These findings, together with the excellent brain penetration and favorable safety profile in humans, make dexpramipexole a drug with realistic translational potential for the treatment of stroke.
Status:
Investigational
Source:
Int J Oral Maxillofac Surg. Feb 2016;45(2):186-93.: Not Applicable Human clinical trial Completed Sensation Disorders/etiology
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Showing 49641 - 49650 of 55039 results