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Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Tosulur is a coccidiostat.
Status:
Investigational
Class (Stereo):
CHEMICAL (ABSOLUTE)
Tosagestin (Org 30659) is a synthetic 19-nortestosterone derived progestogen. It was under clinical development by NV Organon for use in oral contraceptive and hormone replacement therapy. After oral administration of [14C]-Org 30659 to postmenopausal women, the compound was extensively metabolized. The dosed radioactivity was predominantly excreted via urine. Org 30659 was to a large extent metabolized at the C3- and the C17-positions. Species comparison of the metabolic routes of Org 30659 after oral administration indicated that the monkey seems to be a better representative species than the rat for the metabolism of Org 30659 in humans. Daily oral administration of Org 30659 suppresses ovarian function to a level sufficient to inhibit ovulation. This effect is dose-dependent, and the suppressive effect is readily reversible at all doses tested. Tosagestin had been in phase II clinical trial for the treatment of the menopausal syndrome. However, this development was discontinued.
Class (Stereo):
CHEMICAL (ACHIRAL)
Traxanox is a diuretic agent possessing an uricosuric effect in animals. The diuretic and uricosuric effects of the drug have also been demonstrated in normotensive healthy subjects. The chronic administration of traxanox reduces serum uric acid level as well as blood pressure in patients with mild to moderate hypertension. This reduction in serum uric acid is due in part to a traxanox-induced elevation of urinary uric acid excretion. Traxanox sodium stimulates the phagocytic activity of leukocytes or macrophages and prevents the drug-induced suppression of the phagocytic activity of these cells. Traxanox may be clinically effective in treating patients with nasal allergies. The mode of action of traxanox on inflammatory responses resembles that of D-penicillamine or levamisole, so that it may prove to be clinically effective in treating rheumatoid arthritis. Also, traxanox may be effective for the treatment of allergic bronchial asthma.
Status:
Investigational
Source:
Sci Rep. Sep 2019;9(1):12760.: Phase 3 Human clinical trial Completed Breast Neoplasms/metabolism/mortality
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Maytansine is an ansamycin antibiotic originally isolated from the Ethiopian shrub Maytenus serrata. Maytansine inhibits the assembly of microtubules by binding to tubulin at or near the vinblastine-binding site, decreases microtubule dynamic instability and cause mitotic arrest in cells. It exerts cytotoxicity against a number of tumor cell lines and inhibits tumor growth in vivo. However, in human clinical trials, maytansine showed a small therapeutic window due to its neurotoxicity and harmful effects on the gastrointestinal tract. The potent cell killing ability of maytansine can be used in a targeted delivery approach, such as an antibody-drug conjugate, for the selective delivery of the drug and destruction of cancer cells.
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Source:
Rev Med Interna Neurol Psihiatr Neurochir Dermatovenerol Med Interna. 1978;30(4):299-304.: Not Applicable Human clinical trial Completed Gastrointestinal Diseases
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Metiamide is an antagonist of histamine H2-receptors synthesized at Smith Kline & French Laboratories. It potently inhibited gastric acid secretion. Metiamide demonstrated promising clinical effects in patients with duodenal ulcers but questionable safety.
Status:
Investigational
Source:
NCT02503657: Phase 2 Interventional Completed Idiopathic Pulmonary Fibrosis
(2016)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Tioxaprofen is a sulfidopeptide leukotriene receptor antagonist. It is an orally bioavailable anti-inflammatory agent, originated by Kyorin Pharmaceutical, which is being developed in clinical trials by the US company MediciNova for the treatment of interstitial cystitis and asthma. The actions of the drug are described by MediciNova as consisting of eosinophil migration inhibition, leukotriene antagonism, and phosphodiesterase IV inhibition. Other mechanisms described for Tioxaprofen include the inhibition of phosphodiesterases III, 5-lipoxygenase, phospholipase C as well as thromboxane A2. Tioxaprofen in doses of 1 and 5 mg/kg inhibits bronchoconstriction induced by inhalation of antigen and propranolol in a dose-dependent manner. Tioxaprofen was in phase III clinical trial for the treatment of asthma. However, this development was discontinued. It is under investigation for the treatment of idiopathic pulmonary fibrosis and Non-alcoholic steatohepatitis.
Status:
Investigational
Source:
NCT03231800: Phase 3 Interventional Completed Attention-Deficit Hyperactivity Disorder (ADHD)
(2017)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Dasotraline, also known as SEP-225,289, is a serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI). It has an extended half-life (47-77 hours) that supports the potential for plasma concentrations yielding a continuous therapeutic effect over the 24-hour dosing interval at steady state. Dasotraline has shown a lower potential for abuse than methylphenidate in clinical testing. Dasotraline was discovered by Sunovion Pharmaceuticals Inc. and is currently in development to evaluate its use in treating ADHD in adults and children, and BED in adults in the United States. It has not been approved by the U.S. Food and Drug Administration (FDA) for the treatment of ADHD, BED or any other disorder.
Class (Stereo):
CHEMICAL (ACHIRAL)
Tienopramine is a benzazepine derivative patented by Roussel-UCLAF as antidepressive agent. Tienopramine is a tricyclic antidepressant and an imipramine analogue where one of the benzene rings has been replaced with a thiophene ring.
Status:
Investigational
Source:
NCT01757873: Phase 2 Interventional Completed Postherpetic Neuralgia
(2012)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
NMED-160 (also known as MK-6721, NP-118809, Z-160) is a potent N-type calcium channel blockers, which has good selectivity over L-type calcium channels. Neuromed Pharmaceuticals developed this compound for the treatment of the chronic pain. However, that study was discontinued in 2007 in spite of absence of adverse events, but because drug did not demonstrate the ideal, pharmaceutical characteristics considered necessary to advance the compound further in development. Then Zalicus, Inc. was developing that drug for the treatment of chronic neuropathic pain associated with lumbosacral radiculopathy and post-herpetic neuralgia and drug was in the phase II clinical trial. Nevertheless, based on the result from trials, where Z160 did not meet the primary endpoint, Zalicus was also discontinuing the Z160 program.