U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 351 - 360 of 4351 results

Status:
Investigational
Source:
INN:timapiprant [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

OC-459 is a highly potent and selective CRTH2 antagonist which is active on both the recombinant and native human receptor. The Atopix lead compound OC-459 is effective in improving lung function and symptoms in patients with atopic eosinophilic asthma. This group represents 40-50% of all asthmatics and the magnitude of improvement in the responder population is equivalent to high dose inhaled corticosteroids. OC-459 has also been shown to reduce both nasal and eye symptoms in allergic subjects exposed to grass pollen. Of particular interest is the ability of OC-459 to reduce the rate of respiratory infections, an effect related to reduction in Th2 immunity which has a damaging effect on host defence. OC-459 has also demonstrated an excellent safety profile in around 800 subjects exposed drug and no safety issues have been highlighted in long term toxicology. OC-459 is in Phase 2 clinical trial in patients with moderate to severe atopic dermatitis.
Status:
Investigational
Source:
NCT03292822: Early Phase 1 Interventional Unknown status Squamous Cell Carcinoma
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Licochalcone A (LicA) is a flavonoid isolated from the famous Chinese medicinal herb Glycyrrhiza uralensis Fisch and has a wide spectrum of pharmacological activities such as anti-oxidant, anti-bacterial, anti-viral, and anti-cancer. However, its pharmacological mechanism is not well defined. The anti-Inflammatory effects of LicA on IL-1β-Stimulated human osteoarthritis chondrocytes was reached by activating Nrf2 signaling pathway. LicA showed anti-proliferative and apoptotic effects in breast cancer cells through regulating Sp1 and apoptosis-related proteins in a dose- and a time-dependent manner. In addition, the chemotherapeutic potential of LicA for treatment of human cervical cancer was achieved by inhibition of PI3K/Akt/mTOR signaling.
Status:
Investigational
Source:
JAN:PEFCALCITOL [JAN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Pefcalcitol (previously known as M518101), an analog of vitamin D3 (VD3), is an antipsoriatic drug candidate that is designed to achieve much higher pharmacological effects, such as keratinocyte differentiation. This drug is a phosphodiesterase inhibitor and is being developed as a topical ointment formulation. Pefcalcitol was involved in phase III clinical trials in the USA and in Japan in subjects with plaque psoriasis and with palmoplantar keratoderma. In addition, it participated in phase II clinical trial for the warts treatment.
Status:
Investigational
Source:
NCT02863952: Not Applicable Interventional Unknown status Coronary Artery Disease
(2016)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Zinc telluride is a binary chemical compound with the formula ZnTe. Zinc telluride (ZnTe) is a wide-band-gap II–VI semiconductor (E g=2.25 eV at 300 K) crystallizing in the cubic, zinc-blende structure. This material is promising for application as a purely green light-emitting diode. As Zinc telluride can be easily doped, and for this reason it is one of the more common semiconducting materials used in optoelectronics. Zinc telluride finds applications in the following: LEDs and laser diodes Solar cells Tetrahertz imaging Electro-optic detector Holographic interferometry Laser optical phase conjugation devices. Gold–zinc telluride (Au–ZnTe) core–shell nanoparticles were synthesized to support surface modifications for enhanced drug delivery in cancer therapeutics.
Status:
Investigational
Source:
Clin Pharmacol Ther. May 1990;47(5):647-54.: Phase 1 Human clinical trial Completed N/A
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Dideoxyadenosine (2′,3′-dideoxyadenosine) is a prodrug form of didanosine (2',3'-dideoxyinosine), a nucleoside reverse transcriptase inhibitor analog of adenosine. 2',3'-Dideoxyadenosine and 2',3'-dideoxyinosine were shown to be equally effective in the inhibition of HIV proliferation in human T cells. Dideoxyadenosine competitively inhibits adenylyl cyclase, thereby reducing levels of cyclic adenosine monophosphate (cAMP). By inhibiting cAMP-mediated gene activation in tumor cells, this agent may retard tumor cell proliferation. 2',3'-dideoxyadenosine inhibits retroviral DNA synthesis and mRNA expression in T cells exposed to the virus that causes acquired immunodeficiency syndrome, and affords such cells long-term protection in vitro under conditions of substantial viral excess. 2',3'-dideoxyadenosine appears to completely block reverse transcription from viral RNA to viral DNA. 2',3'-dideoxyadenosine was also shown not only to possess antibacterial activity in vitro against a variety of Enterobacteriaceae, but also to be effective in vivo, dideoxyadenosine was active in experimental mouse infections by the oral route against 5 Salmonella strains, 2 of 3 Arizona strains, 5 of 7 Citrobacter strains, 3 of 8 Klebsiella strains, 3 of 5 Escherichia strains, 1 of 3 Shigella strains, and 3 of 15 Serratia strains at concentrations generally well below the toxic level.
Status:
Investigational
Source:
NCT00264433: Phase 2 Interventional Completed Neoplasms
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Targets:


Exherin is a small, cyclic pentapeptide vascular-targeting agent with potential antineoplastic and antiangiogenic activities. ADH-1 selectively and competitively binds to and blocks N-cadherin, which may result in disruption of tumor vasculature, inhibition of tumor cell growth, and the induction of tumor cell and endothelial cell apoptosis. In murine melanoma xenografts, ADH-1 in combination with melphalan significantly reduced tumor growth up to 30-fold over melphalan alone. ADH-1 enhancement of response to melphalan was associated with increased formation of DNA adducts, increased apoptosis, and intracellular signaling changes. In a pilot study (phase I trial), ADH-1 intravenous pretreatment before chemotherapy in metastatic melanoma completely destroyed tumors in half of patients
Status:
Investigational
Source:
INN:desmetramadol [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

O-Desmethyl tramadol (O-Desmethyltramadol, O-DSMT) is a metabolite of tramadol. O-Desmethyltramadol is an opioid analgesic and the main active metabolite of tramadol. (+)-O-Desmethyltramadol is the most important metabolite of tramadol produced in the liver after tramadol is consumed. This metabolite is considerably more potent as a μ-opioid agonist than the parent compound. O-desmethyl tramadol, inhibits 5-hydroxytryptamine type 2C receptors expressed in xenopus oocytes. O-desmethyl tramadol inhibits functions of M(1) receptors but has little effect on those of M(3) receptors. O-desmethyl tramadol has been widely used clinically and has analgesic activity.
Vorasidenib (also known as AG 881) was developed as an isocitrate dehydrogenase (IDH) type 1 in the cytoplasm and type 2 in the mitochondria, with potential antineoplastic activity. It is known that IDH is an essential enzyme for cellular respiration in the tricarboxylic acid (TCA) cycle. Isocitrate dehydrogenases 1 and 2 (IDH1/2) are homodimeric enzymes that catalyze the conversion of isocitrate to α-ketoglutarate (α-KG) in the tricarboxylic acid cycle. Vorasidenib participated in phase I clinical trials in patients with advanced hematologic malignancies and in gliomas.
Status:
Investigational
Source:
INN:decoglurant [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Decoglurant is a negative allosteric modulator of the mGlu2 and mGlu receptors developed by Roche. Decoglurant was investigated in a phase 2 clinical trials in patients with major depressive disorder. Negative results were reported and the development was discontinued in 2015.