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Restrict the search for
alpha-tocopherol acetate
to a specific field?
Status:
Investigational
Source:
NCT02258555: Phase 1 Interventional Terminated Follicular Lymphoma
(2015)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Status:
Investigational
Source:
NCT03155620: Phase 2 Interventional Active, not recruiting Advanced Malignant Solid Neoplasm
(2017)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
LY3023414, an investigational drug, is a small molecule that that demonstrates activity against PI3K, mTOR, and DNA-PK in tumor cells, thereby inducing cell-cycle effects and inhibiting cancer cell viability. As shown in vitro LY3023414 inhibits the ability of PI3K and mTOR to phosphorylate substrates in the PI3K/mTOR pathway, one of the most frequently mutated pathways in cancer, leading to cancer progression and resistance to existing treatments. Downstream target inhibition by LY3023414 occurs rapidly via an intermittent “on/off” mechanism that may enhance the drug's clinical tolerability, which may in turn allow LY3023414 to overcome some of the toxicities associated with PI3K/mTOR inhibitors and potentially reduce the emergence of feedback mechanisms leading to resistance. The physicochemical and absorption properties of LY3023414 are favorable, as evidenced by the molecule's high solubility across a wide pH range and high oral bioavailability. On the basis of these findings, LY3023414 is currently being evaluated in clinical trials in patients with advanced cancer such as metastatic prostate cancer and non-small cell lung cancer in combination with other chemotherapeutic agents and in endometrial cancer as a monotherapy.
Status:
Investigational
Source:
NCT01589432: Phase 2 Interventional Completed Diabetic Neuropathic Pain
(2012)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
ABT-639 is a T-type calcium (Cav3.2) channel antagonist that was in development with AbbVie for the treatment for pain. ABT-639 is a potent and selective T-type calcium channel blocker. ABT-639 effectively reduces nociceptive and neuropathic pain in rats. ABT-639 produces robust antinociceptive activity in experimental pain models at doses that do not significantly alter psychomotor or hemodynamic function in the rat. ABT-639 blocks recombinant human T-type (Cav3.2) Ca2+ channels in a voltage-dependent fashion (IC50=2 uM) and attenuates low voltage-activated (LVA) currents in rat DRG neurons (IC50=8 uM). ABT-639 was significantly less active at other Ca²⁺ channels (e.g. Ca(v)1.2 and Ca(v)2.2) (IC₅₀ > 30 uM). ABT-639 has high oral bioavailability (%F = 73), low protein binding (88.9%) and a low brain:plasma ratio (0.05:1) in rodents.
Status:
Investigational
Source:
NCT03448016: Early Phase 1 Interventional Completed Alcohol Use Disorder
(2016)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
11C-NOP-1A is a new radioligand for thenociceptin/orphanin FQ peptide (NOP) receptor, with high affinity (Ki, 0.15 nM) and appropriate lipophilicity (measured logD, 3.4) for PET brain imaging. 11C-NOP-1A is the the first successful radioligand to image NOP receptors in rat and monkey brain. 11C-NOP-1A is a selective antagonist at the NOP receptor and has high affinity and appropriate lipophilicity for blood–brain barrier permeability. 11C-NOP-1A imaging in rhesus monkeys showed high brain uptake and a large receptor-specific signal and could be quantified with the gold standard method of compartmental modeling. In humans 1C-NOP-1A reliably quantified NOP receptors in human brain both in large brain regions and at a voxelwise level using parametric imaging. The radiation absorbed dose in humans was similar to that observed with other 11C-labeled ligands and would allow multiple scans of a single subject. Thus, 11C-NOP-1A is a promising radioligand for reliably quantifying NOP receptors in human brain.
Status:
Investigational
Source:
NCT02802969: Phase 2 Interventional Completed Skull Base Chordoma
(2016)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Fluoroazomycin Arabinoside F-18 (18F-FAZA) is a radiofluorinated 2-nitroimidazole derivative with hypoxia (low oxygen)-specific tracer activity. 18F-FAZA is reduced under hypoxic conditions, forming highly reactive intermediates. In its reduced form, 18F-FAZA covalently binds to macromolecules, thereby accumulating in hypoxic cells (e.g. malignant tumors) and allowing radioisotopic imaging of these particular cells with positron emission tomography (PET). (18)F-FAZA shows superior biokinetics and is, thus, a promising PET tracer for the visualization of tumor hypoxia. Clinical evaluation of 18F-FAZA is currently ongoing, and early results have been reported for head and neck, lung, prostate, and rectal cancers.
Status:
Investigational
Source:
NCT04625595: Phase 1 Interventional Completed Type1 Diabetes
(2020)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
D-Methyldopa is an inactive isomer of methyldopa. It is known, that only L-isomer has the ability to inhibit dopa decarboxylase and possesses the antihypertensive activity in man. Moreover, about twice the dose of the racemate (DL-form of methyldopa) is required for the equal antihypertensive effect.
Status:
Investigational
Source:
NCT01951222: Phase 2 Interventional Completed Asthma
(2013)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
(R)-Mequitazine or V0162 (10-[(3R)-1-azabicyclo[2.2.2]oct-3-ylmethyl]-10H-phenothiazine) is an anticholinergic enantiomer of mequitazine, an existing oral racemic antihistamine commercialized for over 30 years. (R)-Mequitazine was found to be an antagonist at muscarinic acetylcholine receptors behaving as an inverse agonist. (R)-Mequitazine was investigated in clinical trials for the treatment of chronic obstructive pulmonary disease, asthma and urinary incontinence.
Status:
Investigational
Source:
NCT03189992: Phase 1 Interventional Unknown status Malignant Tumor of Small Intestine Metastatic to Liver
(2014)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Cinobufotalin, the bufadienolide isolated from toad venom,
has displayed antitumor activities in many in vitro systems. It has been shown that cinobufotalin induced significant apoptosis in cultured human lymphoma U-937 cells. It induced DNA fragmentation, mitochondrial membrane
potential decrease, and reactive oxygen species (ROS)
production in U-937 cells. Cinobufotalin induces cytotoxic effect in cultured lung cancer cells. Cinobufotalin (1/5 mg/kg, i.p. twice
daily, for 7 days) significantly inhibited A549 xenograft growth in
mice. Further, same cinobufotalin administration improved mice
survival at week five. Cinobufotalin administration didn’t
significantly affect mice body weight, indicating the relative safety
of this regimen. Thus, cinobufotalin inhibits A549 xenograft
growth in vivo and improves mice survival.
Status:
Investigational
Source:
NCT00302731: Phase 2 Interventional Terminated Menopause
(2006)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Status:
Investigational
Source:
NCT03078322: Phase 2 Interventional Completed Major Depressive Disorder
(2018)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
4‐Chlorokynurenine (AV-101) is a neuropharmaceutical drug candidate in development for the treatment of major depressive disorder. Pharmacology studies conducted in rodent models have demonstrated AV-101’s antihyperalgesic activity in models of facilitated
pain processing was seen at serum concentrations ranging from
150–300 M. In addition, AV-101 has been shown to be
neuroprotective activity against an intrahippocampal injection of
quinolinic acid, reductions in seizures, and antidepressive activity. An oral prodrug, AV-101, which, in the brain, is converted into one of the most potent and selective GlyB site antagonists of the NMDAR, has been demonstrated to be active in animal models of neuropathic pain. The two Phase 1 studies were designed to assess the safety and pharmacokinetics of AV-101, over a wide dose range, after daily dosing for 14-days. AV-101 has excellent safety and PK characteristics providing support for advancing AV-101 into Phase 2 studies in neuropathic pain.
