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Status:
Class (Stereo):
CHEMICAL (ACHIRAL)
Hedaquinium was studied as an antibacterial agent.
Status:
Investigational
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Otenzepad is the first competitive muscarinic M2 antagonist that is cardioselective and had been in phase III clinical trials for the treatment of arrhythmias and bradycardia. Otenzepad was originally developed by Boehringer Ingelheim Pharma KG (Boehringer Ingelheim) in Germany. The parent company is developing oral and IV formulations of the drug for use in symptomatic bradycardia, sinus bradycardia, sick sinus syndrome and symptomatic arrhythmias after intoxication. However, all these research has been discontinued. Otenzepad binds to muscarinic cholinergic receptors in a simple competitive manner. Its affinity for cardiac (M2) muscarinic receptors is about 7 times greater than for ganglionic (M1) receptors and about 36 times greater than for glandular (M3) receptors. The (+)-enantiomer of otenzepad is about 8 times more potent at M2-receptors than the (−)-enantiomer. In a double-blind study, 48 healthy male volunteers were randomised to single oral doses of placebo or otenzepad (120, 240 or 480mg). Heart-rate (HR) was significantly increased by the 250 and 480mg doses (by 15 and 21 beats/minute, respectively). The 480mg dose also increased Diastolic Blood Pressure (DBP) significantly compared with placebo. The oral pharmacokinetics of otenzepad were investigated in a double-blind study in which 48 healthy male volunteers were randomised to single oral doses of placebo or otenzepad (120, 240 or 480mg). Otenzepad bioavailability was 45%, mean residence time (MRT) was 12.5 hours and tmax occurred 2.5 hours postdose.
Status:
Investigational
Source:
NCT03585296: Phase 2 Interventional Completed Atopic Dermatitis
(2018)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Source:
NCT03086226: Phase 2 Interventional Completed Mycetoma
(2017)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Ravuconazole is a triazole with antifungal properties that inhibits cytochrome P450 sterol 14a-demethylase, an enzyme involved in sterol synthesis, resulting in lysis of the fungal cell wall and fungal cell death. It was investigated for the treatment of aspergillosis, candidiasis, and onychomycosis, but these studies were discontinued. Ravuconazole is now in phase II clinical trials to investigate efficacy in preventing fungal infections in patients undergoing chemotherapy and stem cell transplantation.
Status:
Investigational
Source:
NCT04503629: Phase 2 Interventional Completed Duodenal Ulcer,DU
(2018)
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Status:
Class (Stereo):
CHEMICAL (ACHIRAL)
Otimerate, an antifungal and antibacterial agent was used as a preservative for serum and bone. Information about the current use of this compound is not available.
Status:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Dacuronium is an aminosteroid, acting as a competitive antagonist of nicotinic acetylcholine receptors. In animals, dacuronium worked as a short-acting muscle relaxant with a rapid onset of action. In a clinical trial, dacuronium was markedly less potent than tubocurarine and did not show a rapid recovery from its action.
Status:
Class (Stereo):
CHEMICAL (ACHIRAL)
Disiquonium is a quaternary ammonium derivative. It was developed as antiseptic agent.
Status:
Class (Stereo):
CHEMICAL (ACHIRAL)
Pentacynium bis-methylsulphate (presidal) is a salt of pentacynium, which was studied as a ganglion-blocking agent to treat hypertension. Glaxo Wellcome developed this drug; however, information about the further use of pentacynium is not available.
Status:
Investigational
Source:
NCT01226407: Phase 1 Interventional Unknown status Solid Tumour
(2010)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
CG-200745 is a novel inhibitor of histone deacetylases (HDACs), initially developed by CrystalGenomics, Inc for treatment of various hematological and solid cancers. Combinations of CG-200745 with SN38 (the active form of irinotecan), or oxaliplatin were more effective than the agents alone when used to inhibit the growth of HCT116 cells. The protein expressions of acetyl-H3, p21, caspase-3, -8, and -9, PARP, and XIAP were affected in a time- and dose-dependent manner in HCT116 cells treated with the CG-200745 alone or combined CG-200745 and SN-38. In HCT116 xenografts, the HDACI CG-200745 in combination with irinotecan dramatically inhibited tumor growth without showing additive toxicity.