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

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Showing 1601 - 1610 of 42705 results

Status:
Investigational
Source:
NCT01677780: Phase 1 Interventional Completed Myelogenous Leukemia, Chronic, Neoplasms, Myelogenous Leukemia, Acute
(2012)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



RO-5045337 (RG7112) is a small molecule that binds to a MDM2, a negative regulator of tumor-supressor protein p53. It was discovered by Roche and investigated in clinical trials against solid tumors, leukemias and sarcomas.
Status:
Investigational
Source:
NCT02425241: Phase 1/Phase 2 Interventional Completed HIV
(2013)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


RO-638695 (also known as Miridesap, CPHPC and GSK-2315698) is an antineoplastic and a serum amyloid P component inhibitor. RO-638695 almost completely depletes circulating serum amyloid P component (SAP), but a small amount of SAP is left for recognition by subsequently administered therapeutic IgG anti-SAP antibodies. SAP is a blood protein that is the target of a novel immunotherapy approach. RO-638695 has therefore been evaluated in phase I and II clinical trials for its safety and potential in treatment of diseases like Alzheimer’s disease, HIV infection and other diseases with systemic amyloid deposition.
Status:
Investigational
Source:
NCT01472939: Phase 2 Interventional Completed Gastroesophageal Reflux Disease
(2012)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Revexepride is a selective 5-hydroxytryptamine receptor 4 agonist and member of a class of prokinetic agents that stimulate gastric emptying. Revexepride is thought to stimulate the release of acetylcholine at the myenteric plexus, leading to increased gastrointestinal contractions. This drug has been evaluated for potential use in treatment of gastroesophageal reflux disease. Phase I studies in healthy volunteers have shown no serious adverse events after administration of revexepride. However, a phase II study reported respiratory, thoracic and mediastinal disorders and pulmonary hypertension in 1 patient (0.85%). Furthermore, a European clinical trial showed that four weeks of treatment did not improve symptoms or gastric emptying in patients with symptoms suggestive of gastroparesis compared to placebo.
Status:
Investigational
Source:
NCT01054118: Phase 1 Interventional Completed Diabetes Mellitus, Type 2
(2009)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Arena Pharmaceuticals was developing APD-597 (JNJ-38431055), a small molecule, an orally active agonist of the G-protein coupled receptor 119 (GPR119), for the treatment of Type 2 diabetes mellitus. JNJ-38431055 was selected for preclinical development based on a good balance between agonist potency, intrinsic activity and in particular on its good solubility and reduced drug-drug interaction potential. In addition, extensive in vivo studies showed a more favorable metabolic profile that may avoid the generation of long-lasting metabolites with the potential to accumulate in clinical studies. In humans, single-dose oral JNJ-38431055 increased postmeal plasma glucagon-like peptide 1 (GLP-1), glucose-dependent insulinotropic peptide (GIP), and peptide YY (PYY) concentrations but did not significantly decrease glucose excursion or increase insulin secretion. However, in a graded glucose infusion study, JNJ-38431055 was shown to induce a higher insulin secretion rate (ISR) relative to placebo at elevated plasma glucose levels. These studies provide evidence for the potential efficacy of JNJ-38431055 as an antidiabetes agent in humans.
Status:
Investigational
Source:
USAN:IODOPYRACET I 131 [USAN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Iodopyracet (Diodone) is a radiocontrast agent used in urography before 1950. Renal clearance of iodopyracet is characterized by supply-limited elimination at low plasma concentrations and capacity-limited elimination at high plasma levels. Iodopyracet to be an effective agent for the estimation of renal plasma flow and tubular function has been used extensively in physiological studies. In 1945 was found, that p-aminohippuric acid was in some ways superior to diodone for these estimations in man because the urine and plasma blanks are small and because diodone penetrates human red blood cells whereas p-aminohippuric acid does not.
Status:
Investigational
Source:
USAN:IODOPYRACET I 125 [USAN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Iodopyracet I-125 is radiolabeled Iodopyracet
Cobalt protoporphyrin (CoPP) is a potent HO-1 inducer and generally known to be an antioxidant in various cell types. CoPP has been shown to downregulate various cytochrome P450 isoforms, and various mechanisms of action have been attributed to its ability to induced HO- 1. It has also been used to promote endogenous carbon dioxide (CO) generation and protect against myocardial infarction in vivo. CoPP also participated in regulating the inflammatory response in CNS which mainly suppressed inflammatory component. It has been demonstrated that CoPP reduced LPS/Interleukin 13 (IL-13)-induced microglial death.
Status:
Investigational
Source:
Dig Dis Sci. Sep 1979;24(9):680-3.: Not Applicable Human clinical trial Completed Stomach Ulcer/pathology
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT03042013: Phase 2 Interventional Withdrawn Subjects With NSCLC With an EGFR Activating Mutation
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Naquotinib (ASP8273) is an orally available, irreversible, mutant-selective, epidermal growth factor receptor (EGFR) inhibitor, with potential antineoplastic activity. Naquotinib was found by mass spectrometry to covalently bind to a mutant EGFR (L858R/ T790M) via cysteine residue 797 in the kinase domain of EGFR with long-lasting inhibition of EGFR phosphorylation for 24 h. In the NSCLC cell lines harboring the above EGFR mutations, Naquotinib had IC50 values of 8-33 nM toward EGFR mutants, more potently than that of WT EGFR (IC50 value of 230 nM). In mouse xenograft models, Naquotinib induced complete regression of the tumors after 14 days of treatment. ASP8273 even showed activity in mutant EGFR cell line which is resistant to other EGFR TKIs. Naquotinib is in phase III clinical trials for the oral treatment of EGFR mutated non-small cell lung cancer (NSCLC).
Status:
Investigational
Source:
NCT01626924: Phase 2 Interventional Terminated Perinatal Asphyxia
(2012)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



2-Iminobiotin (2-IB) is a cyclic guanidino analog of biotin (Vitamin B7) and combined neuronal and inducible (but not endothelial) nitric oxide synthase inhibitor that has been demonstrated to improve neuroprotection in animal models of hypoxic-ischemic Brain Injury. While the exact mechanism of action has yet to be defined, 2-Iminobiotin potentially protects against hypoxic-ischemic brain damage by preventing nitric oxide or peroxynitrite-induced mitochondrial damage. In preclinical models, 2-Iminobiotin provides gender-specific neuroprotection against hypoxia-ischemia in neonatal rats by a NO-independent mechanism.

Showing 1601 - 1610 of 42705 results