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Status:
Investigational
Source:
INN:rafigrelide [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Rafigrelide is an imidazoquinazoline derivative patented by pharmaceutical company Shire LLC as platelet-lowering agent for the treatment of myeloproliferative diseases. Rafigrelide is a chemical analog of anagrelide, which is used to reduce platelet counts in myeloproliferative disorders. Compared with anagrelide, Rafigrelide has reduced potency against phosphodiesterase III, which may help to reduce potential side effects. The concentration of Rafigrelide that produces 50% of the maximum inhibition (IC50) of PDE III is 164 nM, making it an approximately 200-fold less potent inhibitor of phosphodiesterase III than 3-hydroxy anagrelide. In the clinical trial, Rafigrelide showed antithrombotic properties during a two-week treatment period in healthy male volunteers. The reductions in thrombus formation were seen in surrogate models of both high and low shear rates suggesting drug efficacy in different arterial conditions.
Status:
Investigational
Source:
NCT00315250: Phase 2 Interventional Completed Parkinson's Disease
(2006)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Iometopane I-123 is a tropane derivative labeled with iodine-123 that was being developed by MGI GP (MGI Pharma) as an injectable Single-photon emission computed tomography (SPECT) imaging agent. The ability of iometopane to bind to the dopamine transporter on presynaptic dopaminergic nerve terminal in the striatum has been used to differentiate the uptake of the agent by the neurons in the striatum in patients with a Parkinsonian disorder from patients without a Parkinsonian disorder with high sensitivity and specificity. The diminished uptake of iometopane in the striatum on the SPECT images of patients with a Parkinsonian disorder can be applied to assess both disease trait and disease state (severity) reflected by the severity of the brain dopamine neuron loss. Unfortunately Phase III clinical trials and further development of iometopane was discontinued due to the inability to contract a suitable manufacturer for the clinical and commercial supply of iometopane on acceptable conditions in the US. Currently, Iometopane is mainly used in scientific research into the dopamine reuptake transporter.
Status:
Investigational
Source:
INN:zosurabalpin [INN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Tianafac (also known as L8109) is a thienylacetic acid derivative patented by Labaz group as antipyretics and anti-inflammatory agent useful for the treatment of arthritis. In preclinical models, Tianafac inhibits prostaglandin formation by seminal vesicle microsomes and exerts antipyretic, analgetic, and moderate gastric ulcerogenic activity and had a wide safety margin between toxic and pharmacologically active doses.
Class (Stereo):
CHEMICAL (ACHIRAL)
Pheneridine is a synthetic opioid. It was developed as a narcotic agent.
Class (Stereo):
CHEMICAL (ACHIRAL)
Carbubarb is hydroxyalkylmalonylurea derivatives patented by pharmaceutical company Consortium Mondial des Grandes Marques as sedatives and hypnotic agent.
Class (Stereo):
CHEMICAL (RACEMIC)
Talmetacin is a cyclo-oxygenase inhibitor that was studied as an analgesic and antipyretic agent. This drug was studied in Argentina in patients with rheumatic disorders. However, further development of talmetacin is not available.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Idremcinal (previously known as EM574), a motilin receptor agonist, has been studied for the treatment of gastritis. The drug was involved in phase II in Japan for the treatment of chronic gastritis and Gastro-esophageal reflux in the USA. However, the development of the drug was discontinued.
Status:
Investigational
Source:
NCT04638803: Early Phase 1 Interventional Completed Healthy Volunteers
(2021)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Status:
Investigational
Source:
NCT03756103: Phase 2 Interventional Completed Hypertension,Essential
(2019)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)