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Status:
Investigational
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Terutroban (S18886), a specific thromboxane A2 receptor antagonist, which improves endothelial function and has an antiatherosclerotic effect. The compound is under development by Servier for the potential treatment of cardiovascular diseases and coronary artery disease. In addition, it participated in phase III clinical trials PERFORM (Prevention of cerebrovascular and cardiovascular Events of ischemic origin with teRutroban in patients with a history oF ischemic strOke or tRansient ischeMic attack), but this study was stopped, and the result was not achieved.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Icrocaptide, also known as ITF 1697, a chemically modified LYS-Pro tetrapeptide that was studied to reduce reperfusion injury. The ability of icrocaptide to inhibit the early functions of activated endothelial cells could be used as pharmacological tool in model of pathologies of a variety of microvascular disorders. In addition, tetrapeptide was involved in phase II clinical trials for patients undergoing percutaneous transluminal coronary angioplasty with or without coronary stenting. As a result, a trend toward reperfusion improvement was seen.
Status:
Investigational
Source:
NCT00367887: Phase 2 Interventional Completed Hepatitis C
(2006)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Nesbuvir (previously known as VB-19796 and HCV-796) is an inhibitor of hepatitis C NS5B RNA-dependent RNA polymerase. The drug was tested in phase II in patients with hepatitis C in combination with rebetol and peg-intron, however, its development was terminated due to safety issues.
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Decloxizine (UCB-1402; NSC289116) is a histamine 1 receptor antagonist. Decloxizine is a broncholyticum.
Class (Stereo):
CHEMICAL (ACHIRAL)
Decitropine is an anticholinergic and antiulcer agent, developed by Koninklije Pharma FAB NV in the 1960s.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Deboxamet is a synthetic drug with anti-ulcer and anti-secretory activity, discovered by the Italian Istituto Biologico Chemioterapico ABC, S.p.A. The compound is claimed to have high anti-inflammatory action, as evidenced by the results of the tests of acute and chronic experimental phlogosis. Deboxamet demonstrated cytoprotective activity in a model of rat gastric mucosa necrosis. The cytoprotective effect of deboxamet is mediated by the rise of the availability of prostacyclins in the rat gastric mucosa.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Homprenorphine is an opioid receptor agonist with opioid analgesic activity. This compound has never been marketed.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Guaiapate was studied as a sedative agent for a cough. This drug has never been marketed.
Status:
Investigational
Source:
NCT01314014: Phase 2 Interventional Completed Follicular Lymphoma
(2011)
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Imexon (INN, trade name Amplimexon) is a substance that is being studied in the treatment of some types of cancer, including pancreatic, lung, breast, prostate, melanoma, and multiple myeloma. Imexon is a thiol-binding small molecule which induces mitochondrial oxidation, a loss of membrane potential and cytochrome C, leading to apoptosis.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Almoxatone (compound MD 780236) is a selective inhibitor of the B-form of monoamine oxidase. Inhibition involves an initial non-covalent interaction between enzyme and inhibitor followed by a time-dependent process resulting in irreversible inhibition. The initial, reversible, phase of inhibition was found to be competitive with respect to phenethylamine and 5-hydroxytryptamine, and a comparison of the Ki values indicated the affinity of the inhibitor for the B-form of the enzyme to be some 7-fold greater than its affinity for the A-form. In vitro studies of the effect of MD 780236, a selective monoamine oxidase (MAO)-B inhibitor, on a semicarbazide-sensitive amine oxidase (SSAO) in rat testis and lung showed that this compound dose-dependently inhibited SSAO activity. The inhibition of SSAO by MD 780236 was non-competitive with or without preincubation, with a Ki value of 110 muM. Although MD 780236 is a selective and "suicide substrate" inhibitor of MAO-B, these present results indicate that this compound may also inhibit SSAO activity, but by a mechanism different from that for MAO-B. Almoxatone is stereoselective. The enantiomer with the R absolute configuration (MD 240928) is fully reversible in ex-vivo conditions, whereas the S-enantiomer (MD 240931) has kept the irreversible component of the inhibition seen with MD 780236. The corresponding racemic alcohol derivative (MD 760548) is also a short-acting inhibitor of the B form of MAO; its S-enantiomer, which has an absolute configuration corresponding to that of MD 240928, has a selectivity towards the B form superior to that of the other enantiomer. Almoxatone was patented as an antidepressant and antiparkinsonian agent.