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

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

Showing 1 - 10 of 22 results

Status:
Investigational
Source:
NCT02104050: Phase 2 Interventional Completed Osteoarthritis
(2014)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Dapansutrile is an inhibitor of the NLRP3 inflammasome, developed by Olatec Therapeutics LLC. NLRP3 inflammasome is a driver of sterile inflammation in response to myocardial ischemia-reperfusion and other inflammatory conditions. Dapansutrile limits infarct size and prevents left ventricular systolic dysfunction in the mouse model of ischemia-reperfusion injury and suppresses joint inflammation in the mouse model of acute arthritis. Dapansutrile demonstrated a clinical and inflammatory cytokine response in a clinical trial for the treatment of acute gout and is being investigated for the treatment of Systolic Heart Failure and Schnitzler Syndrome.
Status:
Investigational
Source:
NCT01048255: Phase 2 Interventional Completed Partial Epilepsy
(2010)
Source URL:

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:
NCT00659802: Phase 2 Interventional Completed Ulcerative Colitis
(2008)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Andrographolide, a diterpenoid, is known for its anti-inflammatory effects. It can be isolated from various plants of the genus Andrographis, commonly known as 'creat'. Andrographolide has been tested for its anti-inflammatory effects in various stressful conditions, such as ischemia, pyrogenesis, arthritis, hepatic or neural toxicity, carcinoma, and oxidative stress. Apart from its anti-inflammatory effects, andrographolide also exhibits immunomodulatory effects by effectively enhancing cytotoxic T cells, natural killer (NK) cells, phagocytosis, and antibody-dependent cell-mediated cytotoxicity (ADCC). The properties of andrographolide, such as its ability to induce apoptosis of cancer cells and inhibition of DTH, its anti-oxidative and cytoprotective effect, and its ability to enhance CTLs and NK cell activation makes it a potent antiviral agent. Andrographolide inhibited the growth of human breast, prostate, and hepatoma tumors. Andrographolide could be a potent anticancer agent when used in combination with other chemotherapeutic agents.
Potassium tetrachloroplatinate is used in the preparation of platinum (Pt) nanoparticles. Ligands like ammonia or triphenyl phosphine can able to replace the chloride ligands to afford various derivatives. The replacement by ammonia results in the preparation of cisplatin, which is used in the cancer treatment. Further, it is used as catalyst in the hydroarylation reaction. Cisplatin and potassium tetrachloroplatinate are shown to bind to DNA that encapsulates SWNTs in aqueous solution. The bound platinum salt can then be reduced to decorate the DNA-encapsulated SWNTs with platinum nanoparticles. The unique combination of catalytic activity of nanoscale platinum, biological functionality of DNA, and optoelectronic properties of SWNTs suggests a myriad of applications including fuel cells, catalysts, biosensors, and electrochemical devices.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)



Menthone is a naturally occurring organic compound. It is found in oils of peppermint, Japanese mint, pennyroyal, Micromeria abyssinica benth, geranium and other oils. It is widely used as fragrances and flavors in the cosmetic, perfume, drug, and food industries. Menthone is a naturally occurring pesticide. Menthone and isomenthone were mild skin irritants and of low acute dermal toxicity in rabbits. Neither showed any sensitizing potential in volunteer studies with dilute solutions. In rats, menthone demonstrated a moderate to low acute oral toxicity. On repeated oral administration, menthone produced increases in liver, kidney and spleen weights of rats. Mutagenic activity was reported for menthone in the bacterium Salmonella typhimurium (Ames test) and in fruitflies.
Gallium nitrate (brand name Ganite) is a drug that is used to treat hyper-calcemia, or too much calcium in the blood. Ganite exerts a hypocalcemic effect by inhibiting calcium resorption from bone, possibly by reducing increased bone turnover. It was shown, that gallium favorably altered the mineral properties to enhance hydroxyapatite crystallization and reduced mineral solubility. The drug also acted on the cellular components of bone to reduce bone resorption by decreasing acid secretion by osteoclasts. Nevertheless, ganite was withdrawn from sale, although the reasons was not the safety or effectiveness. Gallium nitrate inhibits the growth of various lymphoma cell lines in vitro and exhibits antitumor activity in patients with lymphoma. Gallium binds avidly to the iron transport protein transferrin. Transferrin-gallium complexes preferentially target cells that express transferrin receptors on their surface. Expression of transferrin receptors is particularly high on lymphoma cells. Cellular uptake of the gallium-transferrin complex leads to inhibition of cellular proliferation primarily via disruption of iron transport and homeostasis and blockade of ribonucleotide reductase. In phase II of clinical trials in patients with relapsed or refractory lymphoma, the antitumor activity of gallium nitrate is similar to, or better than, that of other commonly used chemotherapeutic agents.
Monolaurin, derived naturally from coconut, is a source of the medium chain fatty acid lauric acid. Monolaurin has been widely researched for its antiviral, antibacterial, and antimicrobial properties, as it can break down and destroy the lipid layer of enveloped viruses where many pharmaceuticals fail. Fatty acids and monoglycerides produce their killing/inactivating effects by several mechanisms. An early postulated mechanism was the perturbing of the plasma membrane lipid bilayer. The antiviral action attributed to monolaurin is that of fluidizing the structure in the envelope of the virus, causing the disintegration of the microbial membrane. More recent studies, indicate that one antimicrobial effect in bacteria is related to monolaurin's interference with signal transduction/toxin formation. Another antimicrobial effect in viruses is due to lauric acid's interference with virus assembly and viral maturation. The third mode of action may be on the immune system itself. Monolaurin does not appear to have an adverse effect on desirable gut bacteria, but rather on only potentially pathogenic microorganisms. It is classified by the FDA as "generally regarded as safe" (GRAS).
Stearic monoethanolamide (widely known as N-stearoylethanolamine, NSE) is a biologically active cell membrane component with anti-inflammatory and membrane-protective properties. Preliminary data from a model of experimental burn in rats have shown that N-stearoylethanolamine externally applied has an anti-inflammatory effect. A significant decrease of cytokines (IL-1beta, IL-6, and TNF-alpha) levels under the NSE action, it could be one of the mechanisms of its anti-inflammatory action. The large increase in the level of N-stearoylethanolamine in myalgic muscles may reflect an attempt by the body to counteract noxious processes and activation of nociceptors because of the myalgia. If this is the case, then compound preventing their breakdown N-stearoylethanolamine may be useful analgesics for this indication. In addition, recently was studied the therapeutic potential of NSE for prevention of cognitive disfunction caused by neuroinflammation or autoimmune reaction that allowed suggesting this drug as a candidate for the treatment or prophylaxis of Alzheimer's pathology.
Romurtide (Muroctasin) is a non-specific immune stimulant derived from muramyl dipeptide, which is obtained from gram-positive bacterial cell walls. Muroctasin stimulates macrophages, which release interleukin-l, which in turn increases production of colony-stimulating factors; muroctasin also evokes an increased production of neutrophils. It is used in Japan for chemotherapy-induced leukopenia.
Status:
Possibly Marketed Outside US
Source:
NCT03855007: Phase 4 Interventional Completed Arthritis, Rheumatoid
(2016)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Iguratimod, a methanesulfonanilide, is an anti-inflammatory drug for the treatment of rheumatoid arthritis that has been developed exclusively in Japan and China. It inhibits the production of immunoglobulins and various inflammatory cytokines (interleukin-1, -6 and -8 and TNF), and exerts anabolic effects on bone metabolism by stimulating osteoblastic differentiation and inhibiting osteoclastogenesis. On the molecular level, it inhibits the nuclear transcription factor NF-κB but not its inhibitor, IκBα. In addition to these immunomodulatory and other long-lasting effects, iguratimod inhibits cyclooxygenase-2, which provides a synergistic short-term action against pain and inflammation. Efficacy and tolerability are comparable to salazosulfapyridine, and probably also to methotrexate. Combination with methotrexate is synergistic in patients with insufficient response to methotrexate and does not significantly increase adverse events.