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

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Showing 781 - 790 of 13408 results

Status:
Investigational
Source:
INN:neutramycin
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
INN:iodophthalein sodium
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Iodophthalein was used as an iodine-containing X-ray contrast agent in icteric subjects. There is also existed mention, that iodophthalein has also been used as a wound treatment, and for the treatment of intestinal catarrhs. But nowadays more modern drugs are being used.
Status:
Investigational
Source:
NCT04523870: Not Applicable Interventional Completed Healthy
(2020)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Dequalinium salicylate is a bisquanternary quinolinium antiseptic which kills many gram-positive and gram-negative bacteria. Dequalinium Salicylate have antibacterial (mediated by Dequalinium action) and anti-inflammatory activities (mediated by Salicylic acid action). Dequalinium has an antiseptic effect against a wide range of bacteria, yeasts, and some fungi and viruses. It kills the micro-organisms associated with various mild infections of the mouth and throat. Salicylic acid have direct anti-inflammatory activity mediated by inhibition of both types of cyclo-oxygenases (COX-1 and COX-2) to decrease the formation of precursors of prostaglandins and thromboxanes from arachidonic acid.
Triptolide, the active component of Tripterygium wilfordii Hook F has been used to treat autoimmune and inflammatory conditions for over two hundred years in traditional Chinese medicine. Triptolide possesses immunosuppressive, anti-inflammatory, and anti-cancer effects. Triptolide is a woody vine which is widely distributed in Eastern and Southern China. In China, triptolide is frequently used to treat autoimmune and/or inflammatory diseases due to its favorable cost–benefit ratio. Commercial preparations of triptolide have been commonly used for the treatment of inflammatory and autoimmune diseases such as rheumatoid arthritis, systemic lupus erythematosus, nephritis and psoriasis.Triptolide has been demonstrated to exert novel chondroprotective and anti-inflammatory effects on rheumatoid arthritis. Triptolide has been used to treat ADPKD patients in clinical trials in China. Triptolide significantly protected glomerular filtration rate (eGFR) of ADPKD patients compared with placebo. Two recent small clinical studies have demonstrated tiptolide’s effectiveness against rheumatoid arthritis. A larger study confirmed the therapeutic effects of triptolide in the aforementioned studies. Triptolide is among the most powerful and broadly active antiinflammatory/immunomodulating natural products ever discovered. Triptolide acts at nanomolar concentrations and inhibits the production of various cellular targets including inflammatory cytokines, cyclooxygenase, inducible nitric oxide synthase and metalloproteinases and transcription factors. The anti-tumor activity of Triptolide in vitro and in various tumor-bearing animal models has been investigated for years, and many findings showed that Triptolide is a promising agent in anti-tumor therapy. Triptolide has been approved for Phase I clinical trials for the treatment of prostate cancer, but the anti-tumor effect and mechanism of TPL need to be further elucidated.
Status:
Investigational
Source:
NCT03735420: Phase 1 Interventional Active, not recruiting Healthy
(2019)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Xanthohumol is a prenylated flavonoid most abundant in hops. It is found in beers and refreshment drinks. It can attenuate several factors of the metabolic syndrome. It has been reported to inhibit adipogenesis or increase cell apoptosis and therefore can be used in preventing obesity. Xanthohumol inhibited angiogenesis by suppressing NF-κB activity in pancreatic cancer. Xanthohumol may represent a novel therapeutic agent for the management of pancreatic cancer. Moreover, it is in phase I clinical trials for preventing many types of cancer. It has a range of other biological properties: antiviral, antimalarial, antibacterial and as an osteoporosis preventing agent.
Status:
Investigational
Source:
NCT00129194: Phase 1 Interventional Completed HIV Infections
(2005)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

KP-1461 is a prodrug of KP-1212, an antiviral agent developed for the treatment of human immunodeficiency virus (HIV) infection. KP-1212 induces an increase in the HIV mutation rate thus leading to viral ablation.
Status:
Investigational
Source:
INN:orpanoxin [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Orpanoxin (previously known as F-776), a nonsteroidal anti-inflammatory drug that was developed as an analgesic agent. Orpanoxin is a prostaglandin synthetase inhibitor and may have a potential for the treatment of rheumatic. However, information about the current development of this drug is not available.
Status:
Investigational
Source:
INN:solabegron
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Solabegron (GW427353), a beta-3 adrenoceptor agonist, is in development with AltheRx (now Velicept Therapeutics) for the treatment of irritable bowel syndrome (IBS) and overactive bladder (OAB). Solabegron was discovered and first developed by GlaxoSmithKline. It was acquired by AltheRx, which merged with Velicept in 2015 to continue development of the program. Solabegron has been tested in over 800 study subjects in a twice-a-day formulation and demonstrated efficacy in the treatment of OAB as well as IBS. A once daily formulation designed to optimize patient convenience as well as efficacy has been developed and is currently being evaluated in a phase 2b dose ranging clinical trial. A Phase 2b dose ranging study with the twice daily formulation also began enrollment in Q1 2018.
Status:
Investigational
Source:
INN:sergolexole
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Sergolexole [LY 281067] is an ergoline ester similar in structure to amesergide [LY 237733], with potent and highly selective antagonist activity at serotonin 2. The preclinical pharmacologic activity of LY 281067 shows it to be a potent and highly selective serotonergic (5-HT2) receptor antagonist. Based upon binding studies with 5-HT2 receptors in brain cortical membranes and block of 5-HT-induced contractions in the rat jugular vein, LY 281067 showed high affinity at 5-HT2 receptors with a dissociation constant of approximately 1 nM. LY 281067 was a highly selective 5-HT2 receptor antagonist without appreciably binding to 5-HT1, D1 or D2 receptors or interacting with histamine (H1), cholinergic, beta adrenergic or alpha-1 adrenergic receptors in smooth muscle. LY 281067 had modest affinity at alpha-2 receptors with a dissociation constant of approximately 100 nM. Oral bioavailability of LY 281067 in spontaneously hypertensive rats was excellent with an oral to i.v. dose ratio approximating 4. Sergolexole was undergoing phase II clinical trials with Eli Lilly in the USA as a potential treatment for migraine and anxiety, but development of this compound, but development of this compound has been discontinued.