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Restrict the search for
phenyl aminosalicylate
to a specific field?
Class (Stereo):
CHEMICAL (ABSOLUTE)
Pobilukast is the Leukotriene D4 receptor antagonist. Pobilukast significantly attenuated the Salmonella enteritidis endotoxin-induced thrombocytopenia but had no effect on either the endotoxin-induced early leukopenia or late leukocytosis. Additionally, Pobilukast significantly reduced the endotoxin-induced hemoconcentration and improved survival to 30% at 48 hr. Pobilukast dose-dependently inhibited the immediate hemodynamic changes after leukotriene D4 (LTD4) injections. Pobilukast also attenuated the increase in vascular permeability and the prolonged decrease in CO, suggesting that the observed cardiac and vascular effects of LTs were mediated by stimulation of LT receptors. A shift toward the right of the dose-response curves to histamine with pobilukast compared to that with placebo in three subjects was demonstrated, whereas the active compound did not exhibit any protective effect against histamine in the remaining nine subjects. It was concluded that there is a leukotriene component to the bronchial responses to histamine in some, but not all, subjects. Pobilukast had been in phase II clinical trial for the treatment of asthma. However, this development was discontinued.
Status:
Investigational
Source:
INN:perafensine [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Perafensine is an isoquinoline derivative shown to be active in tests predictive of antidepressant activity. Perafensine is a potent antagonist of reserpine-induced effects and inhibits norepinephrine uptake into rat hypothalamic synaptosomes. Perafensine induced the biosynthesis of microsomal drug-metabolizing enzymes – in treated rats methylayapanine O-demethylase, ethoxycoumarin O-deethylase and cytochrome P-450 contents were increased and ketamine N-demethylase was decreased.
Status:
Investigational
Class (Stereo):
CHEMICAL (ABSOLUTE)
Enrasentan is an orally active mixed endothelin A/B receptor antagonist with a 100-fold greater affinity for the endothelin A receptor. In an animal model of hypertension and cardiac hypertrophy the drug has reduced blood pressure, prevented cardiac hypertrophy and preserved myocardial function. In rats with hyperinsulinemia and hypertension enrasentan normalized blood pressure and prevented cardiac and renal damage. In rats with stroke the drug reduced the ischemic area in the brain. Enrasentan had been in phase II clinical trial for the treatment of heart failure but the results suggested that enrasentan does not appear to have favorable effects on ventricular remodeling.
Status:
Investigational
Source:
NCT04484025: Phase 2 Interventional Enrolling by invitation Covid19
(2021)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Ebselen is a small molecule mimic and inducer of glutathione peroxidase activity and possesses antioxidant and anti-inflammatory properties. This drug has been investigated in phase II clinical trials for the treatment of Meniere's disease, bipolar disorder and in the prevention of hearing loss. Besides, experiments on mice have shown that ZIKV infection could be on the list for potential use of ebselen. It alleviates testicular pathology in mice with Zika virus infection and prevents its sexual transmission. Ebselen has various mechanisms of action. It binds to the N-terminal domain of soluble epoxide hydrolase and chemically reacts with the enzyme to quickly and irreversibly inhibit one of the enzymes' activity: phosphatase (Nterm-phos). Besides, ebselen inhibits inositol monophosphatase and thus exhibits lithium-like on human central nervous system (CNS) function. In addition, ebselen inhibits the G4 isoform of acetylcholinesterase. It is a well-known relationship between the cholinergic system and learning, memory and other common cognitive processes, thus ebselen can be studied for the treatment of memory impairment diseases.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Metesind (AG-331) is a lipophilic thymidylate synthase inhibitor. It inhibits the cofactor binding site of the enzyme. It exerts cytotoxic properties. Metesind was being developed as an anticancer and antimetabolite agent.
Status:
Investigational
Source:
INN:levofacetoperane [INN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Levophacetoperane is a piperidine derivative. Levofacetoperane is a sympathomimetic central nervous system stimulant and is commonly used to treat depression. Levophacetoperane is also a known analeptic and is strongly linked to apnea reversal in dogs after a single intravenous injection.
Status:
Investigational
Source:
NCT03759392: Phase 3 Interventional Completed Heart Failure With Reduced Ejection Fraction
(2019)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Omecamtiv mecarbil (CK-1827452) is a specific cardiac myosin activator and a clinical drug for left ventricular systolic heart failure (in Phase 2 of development). Omecamtiv mecarbil is an inotropic agent that prolongs systolic ejection time and increases ejection fraction through myosin ATPase activation.
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
Source:
INN:icanbelimod [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Source:
NCT02063295: Phase 2 Interventional Completed Obesity
(2014)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Beloranib (also known as ZGN-433 or CKD-732), a fumagillin anticancer drug that initially was developed by CKD Pharmaceuticals for the treatment of solid tumors. Beloranib is a potent inhibitor of methionine aminopeptidase 2 (MetAP2), an enzyme that modulates the activity of key cellular processes that control metabolism. This drug was studied for the treatment of Prader-Willi syndrome and obesity caused by hypothalamic injury, including craniopharyngioma-associated obesity and severe obesity in the general population. European Commission has granted orphan drug designation for beloranib for the treatment of craniopharyngioma, a rare form of benign brain tumor and for the treatment of Prader-Willi syndrome. Beloran participated in phase III clinical trials to evaluate efficacy and safety in obese adolescent and adult subjects with Prader-Willi Syndrome, but these studies were terminated. In 2016, Zafgen, the company developed the drug, based on discussions with the regulatory authority and review of obstacles, costs and development timelines to gain marketing approval for beloranib, has decided to discontinue further development of the drug.
