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Restrict the search for
obeticholic acid
to a specific field?
Status:
Investigational
Source:
JAN:TERALLETHRIN [JAN]
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Terallethrin is an insecticide that controls flying insects including houseflies, wasps and mosquitoes.
Status:
Investigational
Source:
NCT03747497: Phase 2 Interventional Completed Skin Diseases, Bacterial
(2018)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
MRX-I is a potent oxazolidinone antibiotic against Gram-positive pathogens, including methicillin-resistant Staphylococcus aureus, penicillin-resistant Streptococcus pneumoniae, penicillin-intermediate S. pneumoniae, and vancomycin-resistant enterococci. MRX-I demonstrated comparable or slightly higher activity than linezolid and was active against enterococci resistant to both vancomycin and teicoplanin. In addition, MRX-I exhibited bactericidal activities against staphylococci and streptococci but was bacteriostatic against enterococci. MRX-I inhibits formation of functional 70S initiation complex essential for bacterial protein synthesis, leading to the cessation of bacterial growth. Oral MRX-I was associated with a greater bioavailability and exposure when administered with food, and minimal accumulation of MRX-I occurred after multiple-dose administration. Oral MRX-I was well tolerated at single doses of up to 1,200 and 800 mg q12h for up to 28 days; all adverse events were mild to moderate in severity, and there was no drug discontinuation due to adverse events.
Status:
Investigational
Source:
NCT03084952: Phase 2 Interventional Unknown status Leishmaniasis; American, Cutaneous
(2021)
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
18-Methoxycoronaridine (18-MC) is a derivative of ibogaine invented in 1996 by the research team around the pharmacologist Stanley D. Glick from the Albany Medical College and the chemist Martin E. Kuehne from the University of Vermont. In animal studies it has proved to be effective at reducing self-administration of morphine, cocaine, methamphetamine, nicotine and sucrose. 18-MC is a α3β4 nicotinic antagonist and, in contrast to ibogaine, has no affinity at the α4β2 subtype nor at NMDA-channels nor at the serotonin transporter, and has significantly reduced affinity for sodium channels and for the σ receptor, but retains modest affinity for μ-opioid receptors where it acts as an antagonist, and κ-opioid receptors. The sites of action in the brain include the medial habenula, interpeduncular nucleus, dorsolateral tegmentum and basolateral amygdala. Unlike ibogaine and its principal metabolite noribogaine, 18-MC does not increase expression of glial cell line-derived neurotrophic factor (GDNF) in a dopaminergic–like cell line. 18-Methoxycoronaridine is a potent leishmanicide effect against Leishmania amazonensis, a causative agent of cutaneous and diffuse cutaneous leishmaniasis in the New World.
Status:
Investigational
Source:
NCT03216902: Phase 2 Interventional Completed Open-angle Glaucoma, Ocular Hypertension
(2017)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Sepetoprost (also known as ONO-9054), prostaglandin analog was developed as a dual agonist of prostaglandin E3 (EP3) and prostaglandin F (FP) receptors. It is known, that the use of a dual prostaglandin EP3 and prostaglandin F receptor agonists is a novel approach for the reduction of intraocular pressure (IOP) in open-angle glaucoma and ocular hypertension. Sepetoprost was successfully studied in clinical trials phase II for the treatment of open-angle glaucoma, ocular hypertension, and mild open angle-glaucoma.
Status:
Investigational
Source:
NCT04663308: Phase 2 Interventional Recruiting Primary Sclerosing Cholangitis
(2020)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
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:
NCT02171221: Phase 1 Interventional Completed Solid Tumors
(2014)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Source:
NCT04258462: Phase 2 Interventional Recruiting Benign Kidney Neoplasm
(2019)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Source:
NCT01597739: Phase 2 Interventional Completed Arthritis, Rheumatoid
(2012)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Source:
NCT00112554: Phase 3 Interventional Completed Leukemia
(2005)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
LAROMUSTINE is a sulfonylhydrazine alkylating agent. It is metabolized to yield a chloroethylating compound (VNP-4090-CE) and a carbamoylating compound (methyl isocyanate). The former is primarily responsible for the antineoplastic effect of LAROMUSTINE. It alkylates the O6 position of guanine, resulting in DNA crosslinking, strand breaks, chromosomal aberrations, and disruption of DNA synthesis. The carbamoylating species contribute to antitumor activity by inhibiting O6-alkylguanine transferase, an enzyme involved with DNA repair. It was studied in the treatment of several types of cancer, however, its development was discontinued.
Status:
Investigational
Source:
NCT03678610: Not Applicable Interventional Completed Infertility
(2018)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Ionomycin is an ionophore produced by the bacterium Streptomyces conglobatus. The molecules act as a motile Ca2+ carrier and enhances Ca2+ influx by direct stimulation of store-regulated cation entry across biological membranes. It is highly specific for divalent cations. Ion selectivity is as follows: Ca2+ > Mg2+ >> Sr2+ = Ba2+ Binding of Sr2+ and Ba2+ is insignificant and binding to monovalent cations or rubidium is negligible. La2+ is also bound to some extent. Complexation with a cation is always in a 1:1 stoichiometry and pH-dependent. Essentially no binding of Ca2+ occurs below pH 7.0 and maximum binding takes place at pH 9.5. At the micromolar level, ionomycin can activate Ca2+/Calmodulin dependent kinase and phosphatase to stimulate gene expression. Ionomycin has been shown to induce central demyelination, inhibit adrenal bovine TREK-1 channels, and to regulate cell division of mature human B cells [1]. It is used to study the effects of calcium flux on endoplasmic reticulum (ER) stress, mitochodrial stress and intrinsic apoptosis mechanisms. It is also used to stimulate the intracellular production of the cytokines, interferon, perforin, IL-2, and IL-4 usually in conjunction with PMA.
