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Restrict the search for
omidenepag isopropyl
to a specific field?
Status:
Investigational
Source:
NCT03117920: Phase 2 Interventional Completed Pancreatic Cancer
(2017)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Omtriptolide (previously known as PG490-88 or F60008), an immunosuppressant that has been shown to be the safe and potent antitumor agent and it has been approved entry into Phase I clinical trial for the treatment of prostate cancer in the USA. In addition, the drug is participating in phase I clinical trial for the treatment of myeloid leukemia. Experiments on animals have shown omtriptolide was highly effective in the prevention of murine graft-versus-host disease (GVHD). The immunosuppressive effect of the drug was mediated by inhibition of alloreactive T cell expansion through interleukin-2 production. However, this study was discontinued. Recently published article has shown omtriptolide possesses the potential as a prophylactic agent to prevent ischemia/reperfusion (I/R)-induced lung injury.
Class (Stereo):
CHEMICAL (ACHIRAL)
Risotilide is a Class III antiarrhythmic agent that inhibits the voltage-dependent potassium channel. Risotilide prolongs cardiac action potentials and refractory periods. It was shown to reduce ventricular vulnerability in a study on arrhythmogenic effects of left ventricular hypertrophy (LVH) in the intact heart in cats. Phase I and II trials have been conducted, but development of this drug has been discontinued.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Sergolexole [LY 281067] is an ergoline ester similar in structure to amesergide [LY 237733], with potent and highly selective antagonist activity at serotonin 2. The preclinical pharmacologic activity of LY 281067 shows it to be a potent and highly selective serotonergic (5-HT2) receptor antagonist. Based upon binding studies with 5-HT2 receptors in brain cortical membranes and block of 5-HT-induced contractions in the rat jugular vein, LY 281067 showed high affinity at 5-HT2 receptors with a dissociation constant of approximately 1 nM. LY 281067 was a highly selective 5-HT2 receptor antagonist without appreciably binding to 5-HT1, D1 or D2 receptors or interacting with histamine (H1), cholinergic, beta adrenergic or alpha-1 adrenergic receptors in smooth muscle. LY 281067 had modest affinity at alpha-2 receptors with a dissociation constant of approximately 100 nM. Oral bioavailability of LY 281067 in spontaneously hypertensive rats was excellent with an oral to i.v. dose ratio approximating 4. Sergolexole was undergoing phase II clinical trials with Eli Lilly in the USA as a potential treatment for migraine and anxiety, but development of this compound, but development of this compound has been discontinued.
Class (Stereo):
CHEMICAL (ACHIRAL)
Suricainide (also known as AHR 10718) is an aminoalkylurea derivative patented by A. H. Robins Co., Inc. as an antiarrhythmic agent. Suricainide induces a use-dependent decrease in Vmax and significantly decreased Purkinje fiber conduction velocity and action potential duration. Suricainide had no effect on slow response action potentials induced by isoproterenol but ventricular muscle action potentials were significantly prolonged by Suricainide. Suricainide significantly decreased normal automaticity, catecholamine-enhanced automaticity, and abnormal automaticity induced by barium or myocardial infarction. In preclinical modes, Suricainide suppresses the aconitine-induced canine atrial arrhythmia.
Status:
Investigational
Source:
NCT00233441: Phase 2/Phase 3 Interventional Completed Atrial Fibrillation
(2004)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Celivarone is a benzofuran derivative with a multifactorial mode of action including class IV Vaughan Williams’ electrophysiological as well as anti-adrenergic properties. It has no iodine and has a limited tissue accumulation compared with amiodarone. Celivarone exhibits effective anti-arrhythmic properties in several ventricular ischemia- or reperfusioninduced arrhythmia models as well as in in vitro and in vivo atrial fibrillation (AF) models. Its electrophysiological properties are similar to amiodarone (multifactorial mode of action) but with different relative effects on the ion channels. At the ventricular level, celivarone shows anti-arrhythmic activities by suppressing reperfusion-induced arrhythmias (i.v. and oral routes) and reducing the early mortality due to myocardial infarction (oral route) in rats models. At the atrial level, celivarone is effective in atrial fibrillation models with restoration of sinus rhythm or prevention of AF induction and AF recurrence.
Class (Stereo):
CHEMICAL (ACHIRAL)
Recainam is an investigational Class I anti-arrhythmic agent that has been studied for its potential in treatment of heart rhythm disorders. No severe adverse events of intravenous recainam adminstration were reported in a study in patients with frequent ventricular premature complexes (extra heart beats) and nonsustained ventricular tachycardia (abnormally fast heartbeat).
Class (Stereo):
CHEMICAL (ACHIRAL)
Brinazarone (SR33557) is a calcium channel blocker, that inhibits acid sphingomyelinase activity and enhances ricin-A chain immunotoxin activity. Brinazarone may act, much like perhexiline, by disturbing membrane lipid composition through their inhibitory action on lysosomal phospholipid hydrolases, such as acid sphingomyelinase, leading to modifications in intracellular routing and to subsequent degradation of ricin-A chain immunotoxins.
Class (Stereo):
CHEMICAL (ACHIRAL)
Bisfentidine (DA-5047), a histamine-2 receptor antagonist was studied for the treatment of colds and gingivitis.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Opaviraline (also known as GW 420867), a nonnucleoside reverse transcriptase inhibitor that was studied for the treatment of HIV infections. The drug participated in clinical trials phase II in Germany, in South Africa, and in the United Kingdom, however, these studies were discontinued.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Mipimazole was developed as a thyroid inhibitor. However, information about the further development of the drug is not available.
