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Restrict the search for
beta carotene
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Status:
Investigational
Class (Stereo):
CHEMICAL (ABSOLUTE)
Status:
Investigational
Source:
NCT03313297: Phase 2 Interventional Completed Diabetes Mellitus, Type 2
(2018)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
AZD4017, a 11β-hydroxysteroid dehydrogenase type 1 inhibitor, has been developed by AstraZeneca for the treatment of obesity, raised intraocular pressure (IOP) and type 2 diabetes. Inhibition of 11β-HSD1 is an attractive mechanism for the treatment of obesity and other elements of the metabolic syndrome. However, studies were discontinued due to safety and efficacy reasons. Besides, specific inhibition of 11β-HSD1 can decrease intracranial pressure and consequently treat patients with Idiopathic Intracranial Hypertension (IIH), thus AZD4017 participated in phase II clinical trials to treat this disease. IIH, also known as benign intracranial hypertension or pseudotumor cerebri, is a condition of unknown etiology characterized by elevated intracranial pressure (ICP) and papilledema. In addition, AZD4017 in combination with prednisolone participated in phase II clinical trials for patients with Iatrogenic Cushing's Disease. It was postulated that the adverse metabolic effects of prednisolone could be reduced by co-administration of AZD4017.
Status:
Investigational
Source:
INN:serabelisib [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Serabelisib (INK1117 and TAK-117) is an orally bioavailable, PI3K p110α- isoform-specific inhibitor with an in vitro IC50 of 15 nM, highly selective against other isoforms (p110β, p110γ, and p110δ) and mTOR (no significant inhibitions at 1 μM concentration). It displayed significant efficacy in several PI3Kα mutant-specific preclinical mouse xenograft tumor models, and blocked signaling to Akt and inhibited the growth of cancer cells harboring wild-type or mutated p110α. Preclinical studies showed TAK-117 to have the low potential for disrupting glucose metabolism or for causing cardiac adverse events; in rats and monkeys, doses up to 50 mg/kg/day were well tolerated. Serabelisib is currently under clinical evaluation.
Status:
Investigational
Source:
NCT00588185: Not Applicable Interventional Recruiting Prostate Cancer
(2003)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Status:
Investigational
Class (Stereo):
CHEMICAL (ABSOLUTE)
Endrysone is a glucocorticoid with anti-inflammatory and antiallergic properties. It is used topically for skin conditions as an ophthalmic anti-inflammatory agent.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Tipredane is one of the compounds of a new series of sulfur-containing steroids synthesized at The Squibb Institute for Medical Research and is being developed for topical treatment of human dermatoses. Tipredane is structurally unique in that the classical l7-beta two-carbon side chain and the 17-alpha hydrogen of the steroid have been replaced by two alkylthio substituents. Tipredane has been shown to possess moderate to potent anti-inflammatory activity in various animal models, and to exhibit favorable separation of local anti-inflammatory activity from adverse systemic effects in both animals and humans. After oral administration, [3H]tipredane was rapidly absorbed, metabolized, and excreted into urine and feces. Metabolism of tipredane was rapid and complex, with significant species differences, although the disposition in rhesus and cynomolgus monkeys seemed to be similar to humans. Tipredane had been investigated as the therapeutic agent for the treatment of allergic rhinitis, asthma and skin disorders. However, this development was discontinued.
Status:
Investigational
Source:
NCT00666081: Phase 1 Interventional Withdrawn Cancer
(2008)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
GSK690693 is an aminofurazan derivative, a novel ATP-competitive, low-nanomolar pan-Akt kinase inhibitor. It is selective for the Akt isoforms versus the majority of kinases in other families; however, it does inhibit additional members of the AGC kinase family. GlaxoSmithKline was developing this compound for the treatment of lymphoma solid tumours but the clinical development of this compound was terminated due to the associated side-effect of transient hyperglycemia.
Status:
Investigational
Source:
INN:itanapraced [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
CHF-5074 is a small molecule with a unique microglial modulating mechanism of action capable of selectively reducing pro-inflammatory activities of microglial cells while increasing their ability to remove neurotoxic amyloid beta (“Aβ”) aggregates in the brain by phagocytosis. CHF-5074 reduces Aβ42 and Aβ40 secretion, with an IC50 of 3.6 and 18.4 μM, respectively. Microglia are small cells that migrate through the brain to remove waste products, such as amyloid aggregates that cause inflammation and irreversible damage to nerve cells. Chronic dysfunction of microglia is increasingly believed to play an important role at the very beginnings of Alzheimer’s disease. The results from Chiesi’s human clinical studies corroborate the large body of data from published preclinical studies. In Alzheimer’s disease transgenic mouse models, CHF-5074 was shown to reduce neuroinflammation, inhibit brain amyloid β plaque deposits, reduce tau pathology, and reverse associated memory deficits. These findings indicate CHF-5074 acts simultaneously on several important therapeutic targets, and this neuroprotective multi-target approach may translate into preventing the memory loss that is the hallmark of Alzheimer’s disease.
Status:
Investigational
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Belnacasan (VX-765), and its active metabolite VRT- 043198, is a novel and irreversible IL-converting enzyme/ caspase-1 inhibitor. VRT-043198 exhibits 100- to 10,000-fold selectivity against other caspase-3, -6 and -9. It exhibited potent inhibition against ICE/caspase-1 and caspase-4 with Ki of 0.8 nM and less than 0.6 nM, respectively. And VRT-043198 also inhibits IL-1β release from both PBMCs and whole blood with IC50 of 0.67 uM and 1.9 uM, respectively. Belnacasan inhibits the release of IL-1, IL-18 and IL-33. Belnacasan has shown to inhibit acute partial seizures in preclinical models and has shown activity in preclinical models of chronic partial epilepsy that do not respond to currently available compounds for epilepsy. In addition, it seems to reduce disease severity and the expression of inflammatory mediators in models of rheumatoid arthritis and skin inflammation. Belnacasan had been in phase II clinical trials by Vertex for the treatment of epilepsy. However, this study has been terminated later.
Status:
Investigational
Class (Stereo):
CHEMICAL (ABSOLUTE)
Dimesone is a synthetic glucocorticoid with anti-inflammatory and anti-allergic activity.
