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Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Ofornine is a vasodilator with antihypertensive activity. Experiments on rats have shown that ofornine reduced spontaneously hypertensive (SH) blood pressure through vasodilating and presynaptic adrenolytic activities, and that a dopaminergic mechanism may be involved. Information about the current use of this drug is not available.
Status:
Investigational
Source:
INN:cericlamine [INN]
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Cericlamine (INN) is a potent and moderately selective serotonin reuptake inhibitor (SSRI) of the amphetamine family that was investigated as an antidepressant for the treatment of depression, anxiety disorders, and anorexia nervosa by Jouveinal
Status:
Investigational
Source:
NCT04593940: Phase 3 Interventional Completed Covid19
(2020)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Cenicriviroc (also referred to as TBR-652 and TAK-652) is an orally active, potent inhibitor of ligand binding to C-C chemokine receptor type 2 (CCR2) and C-C chemokine receptor type 5 (CCR5). Cenicriviroc does not inhibit ligand binding to CCR1 (an alternative target of CCR5 ligands). The mean half-life in healthy volunteers is 35 to 40 hours, which allows daily dosing of the drug. Due to its CCR5 blocking activity, Cenicriviroc has initially been tested as a drug against CCR5-tropic HIV infection. In a double-blind placebo-controlled trial involving 54 HIV infected participants, Cenicriviroc monotherapy at different doses (25, 50, 75, 100, or 150 mg) led to a dose-dependent reduction in HIV-1 RNA levels and concomitant increases in circulating levels of the CCR2 ligand monocyte chemoattractant protein 1 (MCP-1, or CCL2), suggesting potent CCR2 and CCR5 inhibition in vivo. According to clinical trials, Cenicriviroc is a very safe drug with a wide therapeutic range and fairly low pharmacokinetic variability. In animal models of liver diseases, Cenicriviroc potently inhibits macrophage accumulation in the liver and ameliorates fibrosis. In a phase 2b clinical trial on 289 patients with NASH and fibrosis, Cenicriviroc consistently demonstrated liver fibrosis improvement after 1 year of therapy and had an excellent safety profile.
Status:
Investigational
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Cemadotin (LU103793) is a cytotoxic water-soluble pentapeptide analogue of dolastatin 15. The dolastatin peptides were originally isolated from the shell-less mollusc Dolabella auricularia. Cemadotin blocks cells at mitosis. It exerts its antitumor activity by suppressing spindle microtubule dynamics through a distinct molecular mechanism by binding at a novel site in tubulin. Cemadotin was in phase II clinical trials as a promising cancer chemotherapeutic agent. However, this agent appears to be inactive in the treatment of advanced non-small-cell lung cancer and other tumors and this research has been discontinued.
Status:
Investigational
Source:
INN:diethylthiambutene [INN]
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Diethylthiambutene is an analgesic agent with an effect like that of morphine. Diethylthiambutene mainly used in veterinary. It is highly toxic to cats. Can cause convulsions if injected intravenously. Diethylthiambutene is a synthetic opioid drug. It is under international control according to the UN Single Convention 1961 and its amendments, schedule I.
Status:
Investigational
Class (Stereo):
CHEMICAL (ABSOLUTE)
Fasobegron is an agonist of β3-adrenoreceptor.
Status:
Investigational
Source:
NCT01521585: Phase 2 Interventional Completed Huntington's Disease
(2011)
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Selisistat (EX 527) was discovered by Elixir scientists as a selective human SIRT1 inhibitor and exhibits >200-fold selectivity against SIRT2 and SIRT3. Human SIRT1 is an enzyme that deacetylates the p53 tumor suppressor protein and has been suggested to modulate p53-dependent functions including DNA damage-induced cell death. It was shown that drug was highly safe in toxicology studies. Selisistat passed Phase II clinical trials to treat Huntington’s disease, but that study was discontinued.
Status:
Investigational
Source:
NCT00265551: Phase 2 Interventional Completed Schizophrenia
(2006)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Vabicaserin is a 5-hydroxytryptamine 2C (5-HT2C) receptor-selective agonist with an EC50 of 8 nM. Pfizer was developing vabicaserin, an oral serotonin (5-HT)2C receptor agonist, for the treatment of schizophrenia and bipolar disorder. Vabicaserin decreases nucleus accumbens extracellular dopamine levels in rats, without affecting striatal dopamine, indicating mesolimbic selectivity. Vabicaserin had been in phase II clinical trials for the treatment of schizophrenia. However, research of Vabicaserin for the treatment schizophrenia and obesity was discontinued.
Status:
Investigational
Class (Stereo):
CHEMICAL (ABSOLUTE)
Inakalant is diazabicyclo[3.3.1]nonane derivative patented by pharmaceutical company AstraZeneca AB as antiarrhythmic agent.
Class (Stereo):
CHEMICAL (ACHIRAL)
Barucainide, an IB anti-arrhythmic agent, was evaluated in patients with coronary artery disease. Its antiarrhythmic effect was studied in patients with markedly depressed left-ventricular function. Barucainide was in phase II clinical trials to treat the patients with arrhythmias but the development of the drug was discontinued.