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Showing 131 - 140 of 2667 results

Status:
Investigational
Source:
Clin Pharmacol Ther. May 2021;109(5):1274-1281.: Not Applicable Human clinical trial Completed Multiple System Atrophy/blood
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

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

Class (Stereo):
CHEMICAL (ACHIRAL)

Safotibant (previously known as LF22-0542) was developed as an antagonist at bradykinin B1 receptor for the topical treatment of diabetic macular edema. This drug participated in phase II clinical trials in Australia, in Belgium and in the Czech Republic. However, further, development was discontinued.
Status:
Investigational
Source:
NCT00960557: Phase 1 Interventional Completed Neoplasm Metastasis
(2009)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Oxi0-4503 (now known as combretastatin A1 phosphate), a diphosphate prodrug of combretastatin A1, was developed by Mateon therapeutics as a second-generation, dual-mechanism vascular disrupting agent from the combretastatin family. On November 21, 2012, Oxi-4503 has been granted orphan designation by the US Food and Drug Administration for the treatment of acute myelogenous leukemia. It is known that the orphan drug designation qualifies a company for several benefits, including the potential for market exclusivity, development grants, and tax credits. Oxi0-4503 is currently participating in phase I/II clinical trial the treatment of patients with acute myelogenous leukemia or myelodysplastic syndrome. In addition, phase I clinical trial was successfully completed where was studied the safety of Oxi0-4503 in patients with advanced solid tumors.
Status:
Investigational
Source:
INN:defoslimod [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Defoslimod is an analog of lipopolysaccharide endotoxin-derived lipid A obtained from E. coli, developed as an immunomodulatory adjuvant and an immunotherapeutic agent for the treatment of cancer. Defoslimod acts as an agonist of Toll-like receptor (TLR) 2/4. In a phase 1 clinical study in patients with solid tumors, conducted in 2007, defoslimod was administered as an intravenous infusion. The therapy was well tolerated at biologically active concentrations, with 3 patients of 17 exhibited disease stabilization with a mean duration of 4 months. No further development of the drug was reported.
Status:
Investigational
Source:
NCT02950103: Phase 2 Interventional Terminated Solid Tumor
(2016)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
NCT04404569: Phase 1 Interventional Enrolling by invitation Neoplasms
(2020)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

1,​2-​Dioleoyl-​sn-​glycero-​3-​phospho-​L-​serine Sodium Salt is a lipid being studied in the assembly and long-term stability of solid supported lipid bilayers from artificial and natural lipid mixtures.
Status:
Investigational
Source:
USAN:STIROFOS [USAN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

(E)-Tetrachlorovinphos is an (E)- isomer of Tetrachlorovinphos. Tetrachlorovinphos is an organophosphate cholinesterase inhibitor that is used as an insecticide. Tetrachlorvinphos was introduced and first used commercially in 1966 in the USA. Tetrachlorvinphos was originally registered for use on various food crops, livestock, pet animals. Tetrachlorvinphos is applied dermally to livestock to control flies and mites. It is used as an oral larvicide in cattle, hog, goats and horses; in cattle ear tags to control flies; in cattle feedlots; in poultry dust boxes to control poultry mites; and in poultry houses. Tetrachlorvinphos also is used in pet sleeping areas and pet flea collars and to control flies around refuse sites, recreational areas, and for general outdoor treatment. Tetrachlorvinphos can cause cholinesterase inhibition in humans; that is, it can overstimulate the nervous system causing nausea, dizziness, confusion, and at very high exposures (e.g., accidents or major spills), respiratory paralysis and death. In 2014, the Natural Resources Defense Council (NRDC) filed a lawsuit against the United States Environmental Protection Agency (EPA) seeking EPA to respond to NRDC’s 2009 petition to ban tetrachlorvinphos in common pet flea treatment products. Tetrachlorvinphos is reportedly registered for use in Canada, South Africa, and Australia.
Status:
Investigational
Source:
INN:ilmofosine
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Ilmofosine (1-hexadecylthio; 2-methoxyethyl-racglycero-3-phosphocholine) is a synthetic 1-S-thioether alkyl lysophospholipid derivative with potential antineoplastic activity. In extensive preclinical evaluation against tumor cell lines and in the human tumor colony-forming assay, Ilmofosine was cytotoxic against both leukemias and solid tumors. Ilmofosine was effective against many tumor types, including ovary, non-small cell lung, kidney, and melanoma. Ilmofosine exhibited competitive inhibition of protein kinase C activity with respect to phosphatidyl-serine and inhibited the enzyme activated by diolein.
Triciribine is a purine analogue which inhibits DNA and protein synthesis, it is a synthetic tricyclic nucleoside which acts as a specific inhibitor of the Akt signaling pathway. It selectively inhibits the phosphorylation and activation of Akt1, -2 and -3 but does not inhibit Akt kinase activity nor known upstream Akt activators such as PI 3-Kinase and PDK1. It inhibits cell growth and induces apoptosis preferentially in cells that express aberrant Akt1. In whole cells triciribine is phosphorylated by adenosine kinase which may be necessary for its activity. Triciribine is a cancer drug which was first synthesised in the 1970s and trialled clinically in the 1980s and 1990s without success. Following the discovery in the early 2000s that the drug would be effective against tumours with hyperactivated Akt, it is now again under consideration in a variety of cancers. As PTX-200, the drug is currently in two early stage clinical trials in breast cancer and ovarian cancer being conducted by the small molecule drug development company Prescient Therapeutics.
Status:
Investigational
Source:
J Antimicrob Chemother. Nov 2023;78(11):2702-2714.: Not Applicable Human clinical trial Completed Leishmaniasis, Visceral
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Phosphorylcholine (ChoP) is a small zwitterionic amino alcohol, which is composed of a negatively charged phosphate bonded to a small, positively charged choline group. Phosphorylcholine is the precursor metabolite of choline in the glycine, serine, and threonine metabolism pathways and in intermediate between choline and cytidine-diphosphate choline in the glycerophospholipid metabolism pathway. Phosphorylcholine is an interesting compound from an immunologic point of view, being an immunodominant determinant of pneumococcal teichoic acids and also a major prerequisite for proinflammatory effects of PAF and PAF-like lipids where PC is a common denominator. PC is also a component of some bacteria, apoptotic cells, and OxLDL, which, if exposed, is immunogenic. PC has several properties that could in principle both promote and protect against disease, depending on the pathogen and type of inflammatory reaction. In the field of interventional cardiology, phosphorylcholine is used as a synthetic polymer-based coating, applied to drug-eluting stents, to prevent the occurrence of coronary artery restenosis. To date, more than 120,000 Phosphorylcholine-coated stents have been implanted in patients with no apparent deleterious effect in the long term compared to bare metal stent technologies