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Status:
Investigational
Source:
INN:icofungipen [INN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Icofungipen is a generic name of the compound, previously known as BAY 10-8888 or PLD-118. Icofungipen, a cyclic beta-amino acid was developed by PLIVA, under license from Bayer, for the potential oral treatment of fungal infection. The drug exerts its antifungal activity by inhibition of isoleucyl-tRNA synthetase activity and consequently disrupting protein biosynthesis. Phase II trials with an oral formulation of icofungipen were underway in Europe for Candida infection and for the treatment of vulvovaginal candidiasis in the USA, but these studies have been discontinued. In human toxicity studies, suppression of spermatogenesis in male volunteers was observed as a possible off-target adverse event.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Prenisteine is an enylhomocysteine derivative used as reagent in organic synthesis
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Elsibucol (AGI-1096) is a phenolic intracellular antioxidant with anti-inflammatory and antiproliferative properties. In vitro, elsibucol inhibited the inducible expression of vascular cell adhesion molecule (VCAM)-1, E-selectin, and monocyte chemoattractant protein (MCP)-1 in endothelial cells and tumor necrosis factor (TNF)-alpha and interleukin (IL)-1beta secretion from lipopolysaccharide (LPS)-stimulated peripheral blood mononuclear cells. It also inhibited serum-stimulated proliferation of aortic smooth-muscle cells. In vivo, elsibucol demonstrated anti-inflammatory properties in a murine delayed-type hypersensitivity model. In hypercholesterolemic animals, elsibucol inhibits atherosclerosis and preserves endothelial healing following arterial injury. Elsibucol development for the prevention of transplant rejection has been discontinued.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Elarofiban is a novel nonpeptide glycoprotein IIb/IIIa (GPIIb/IIIa) antagonist. It inhibits thrombin-induced platelet aggregation in human gel-filtered platelets and platelet aggregation in human platelet-rich plasma (PRP) in response to collagen, arachidonic acid, ADP, and SFLLRN-NH(2). Elarofiban had adequate oral pharmacokinetics in dogs and excellent oral pharmacodynamics. Elarofiban has been in phase II clinical trials for the treatment of myocardial infarction and thrombosis. However, this research has been discontinued.
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Etomoxir is an irreversible inhibitor of carnitine O-palmitoyltransferase (CPT) I. It inhibits fatty acid oxidation and fatty acid and cholesterol synthesis in an enantiomer-selective manner: only the R-enantiomer of etomoxir inhibits fatty acid oxidation, S-enantiomer inhibits fatty acid and cholesterol synthesis but not fatty acid oxidation. Etomoxir was studied for the treatment of congestive heart failure and type II diabetes, however, its development was discontinued.
Class (Stereo):
CHEMICAL (RACEMIC)
Triclazate is an anticholinergic agent.
Class (Stereo):
CHEMICAL (ACHIRAL)
Pimetacin is the thio-ester of indometacin. It is antithrombotic and anti-inflammatory agent. Pimetacin produced dose-related enhancement of the OpZ-induced chemiluminescence from resident peritoneal macrophages.
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Difloxacin is an aryl fluoroquinolone derivative. The primary bacterial target of fluoroquinolones is the enzyme deoxyribonucleic acid gyrase. Difloxacin is very potent against a broad spectrum of bacteria including aerobic ana anaerobic gram-positive and gram-negative oragnisms. DICURAL® (difloxacin hydrochloride) TABLETS are indicated for the management of diseases in dogs associated with bacteria susceptible to difloxacin.
Status:
Investigational
Class (Stereo):
CHEMICAL (RACEMIC)
Erbulozole (R 55104) is a water soluble congener of the microtubule inhibitor tubulozole, which has proven to possess anti-invasive, antitumoral and radiosensitizing capacities. Erbulozole development for the treatment of cancer has been discontinued.