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Restrict the search for
m nalidixic acid
to a specific field?
Status:
Investigational
Source:
JAN:SEPANTRONIUM BROMIDE [JAN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Sepantronium bromide (YM155) is a selective survivin suppressant that exhibits potent antitumor activities by inducing apoptosis and autophagy in various types of cancer. Sepantronium bromide inhibited the growth of various human cancer cell lines in vitro with GI50 values in the low nM range. Sepantronium bromide blocked the growth of 119 human cancer cell lines, with the greatest inhibition in lines derived from non-Hodgkin's lymphoma, hormone-refractory prostate cancer, ovarian cancer, sarcoma, non-small-cell lung cancer, breast cancer, leukemia, and melanoma, with an average GI50 of 15 nM. Sepantronium bromide inhibited the growth of tumor cell lines regardless of their p53 status and demonstrated significant antitumor activity in 5 mice xenograft models. It also caused tumor regressions in vivo, possibly by its effects in reducing intratumoral survivin expression levels and increasing apoptosis. Sepantronium Bromide had been in phase II clinical trials by Astellas for the treatment of prostate cancer, melanoma, non-Hodgkin's lymphoma, breast cancer, diffuse large B cell lymphoma, non-small cell lung cancer (NSCLC) and other solid tumors. This compound had also been in clinical trials by National Cancer Institute (NCI) for the treatment of solid tumors (phase I) and advanced non-small cell lung cancer (NSCLC) (phase II). However, all these researches about this compound for all indications were discontinued.
Status:
Investigational
Source:
NCT00784875: Phase 2 Interventional Completed Primary Insomnia
(2008)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
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
Source:
NCT01002963: Phase 1 Interventional Completed Healthy
(2009)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
PF-04418948 is an orally active, potent, and selective EP2 receptor antagonist. It is used as a tool compound to study involvement of EP2 receptor in various pathologies. In combination with EP4 antagonist, PF-04418948 attenuates PGE2-induced airway microvascular leak in model of asthma, and PGE2-induced gut dismotility.
Status:
Investigational
Source:
NCT00046696: Phase 1 Interventional Completed Neoplasms
(2001)
Source URL:
Class (Stereo):
CHEMICAL (EPIMERIC)
1H-2-BENZOPYRAN-3-ACETIC ACID, 8-HYDROXY-6-METHOXY-Α-METHYL-1-OXO- (NM-3) is an orally bioavailable antiangiogenic isocoumarin with potential antineoplastic activity. NM-3 inhibits vascular endothelial growth factor (VEGF), a pro-angiogenic growth factor, thereby inhibiting endothelial cell proliferation. NM-3 induces apoptosis by a mechanism involving reactive oxygen species. In human MCF-7 and ZR-75-1 breast cancer cells, NM-3 induces the p21 cyclin-dependent kinase inhibitor, cell cycle arrest at G1-S-phase, and necrotic cell death. NM-3 has been used in trials studying the treatment of solid tumours.
Status:
Investigational
Source:
NCT02467023: Not Applicable Interventional Completed Sepsis
(2015)
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Etocrylene is an organic ester that appears as an off-white crystalline powder and functions as a UV absorber. When applied to the skin, this product absorbs UV rays. It can also be used to protect cosmetics and personal care products from deterioration. This product can be used in the formulation of sun protection products, as well as bath, skin, cleansing, hair, nail and fragrance products.
Status:
Investigational
Source:
JAN:S-HYDROPRENE [JAN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
S-Hydroprene is an insecticide used against cockroaches, beetles, and moths. S- Hydroprene belongs to the class of insecticides known as insect growth regulators. S-Hydroprene disrupts normal development and molting of insects by mimicking hormones produced by immature insects. S-Hydroprene causes different effects on different insects. It may cause adult sterility, physical body changes, water loss, and premature death. S-hydroprene is currently used indoors, and therefore are not expected to pose a risk to the environment.
Class (Stereo):
CHEMICAL (RACEMIC)
Temiverine was developed as an antimuscarinic and calcium-antagonist agent for the treatment of overactive bladder. Temiverine participated in clinical trials; however, the development of the drug was discontinued on the pre-registration stage.
