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

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Showing 71 - 80 of 81 results

Status:
US Approved OTC
Source:
21 CFR 341.14(a)(3) cough/cold:antitussive dextromethorphan
Source URL:
First approved in 1954
Source:
Romilar by Hoffmann-La Roche
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Dextromethorphan is a non-narcotic morphine derivative widely used as an antitussive for almost 40 years. It has attracted attention due to its anticonvulsant and neuroprotective properties. It is a cough suppressant in many over-the-counter cold and cough medicines. In 2010, the FDA approved the combination product dextromethorphan/quinidine for the treatment of pseudobulbar affect. Dextromethorphan suppresses the cough reflex by a direct action on the cough center in the medulla of the brain. Dextromethorphan shows high-affinity binding to several regions of the brain, including the medullary cough center. This compound is an NMDA receptor antagonist and acts as a non-competitive channel blocker. It is one of the widely used antitussives and is used to study the involvement of glutamate receptors in neurotoxicity. Dextromethorphan (DM) is a sigma-1 receptor agonist and an uncompetitive NMDA receptor antagonist. The mechanism by which dextromethorphan exerts therapeutic effects in patients with pseudobulbar affect is unknown. Dextromethorphan should not be taken with monoamine oxidase inhibitors due to the potential for serotonin syndrome. Dextromethorphan is extensively metabolized by CYP2D6 to dextrorphan, which is rapidly glucuronidated and unable to cross the blood-brain barrier.
Status:
Investigational
Source:
INN:bevemipretide [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT04688164: Phase 3 Interventional Completed Major Depressive Disorder
(2021)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT03671811: Phase 2 Interventional Active, not recruiting Atypical Endometrial Hyperplasia
(2019)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Pterostilbene is a naturally derived compound found primarily in blueberries and Pterocarpus marsupium heartwood. The multiple benefits of pterostilbene in the treatment and prevention of human disease have been attributed to its antioxidant, anti-inflammatory, and anti-carcinogenic properties leading to improved function of normal cells and inhibition of malignant cells. The antioxidant activity of pterostilbene has been implicated in anti-carcinogenesis, modulation of neurological disease, anti-inflammation, attenuation of vascular disease, and amelioration of diabetes. Pterostilbene increases LDL and reduces blood pressure in adults. Low doses of pterostilbene seem to hold some benefit for cognition.
Status:
Designated
Source:
FDA ORPHAN DRUG:1019324
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Designated
Source:
EU-Orphan Drug:EU/3/15/1527
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Designated
Source:
FDA ORPHAN DRUG:354611
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

AEOL-10150 is a small-molecule antioxidant developed by Aeolus (formerly Incara) for potential subcutaneous treatment for amyotrophic lateral sclerosis (ALS), stroke, spinal cord injury, lung inflammation, and mucositis. Structurally, AEOL-10150 functions as a superoxide-dismutase mimic and contains metalloporphyrin moiety. AEOL-10150 possess high superoxide-dismutase activity as well as catalase-like activity and has the capacity to scavenge peroxynitrite and lipid peroxides. In 2017 Aeolus Pharmaceuticals has announced that the FDA has granted Fast Track designation to AEOL 10150 for the prevention of fatal respiratory failure among patients at risk for radiation pneumonitis following a radiological/nuclear incident sufficient to cause the Acute Radiation Syndrome.
Leucine is an α-amino acid used in the biosynthesis of proteins. Leucine is an essential hydrophobic amino acid. It is used in the Leucine may be used some people as a supplement to build muscle. Leucine is also found in fish, meat, and poultry. In the pharmaceutical industry, L-leucine is used for parenteral and enteral nutrition and feeding, and is also used as a flavoring product and tablet lubricant in manufacturing. Leucine is an mTOR activator. It is a dietary amino acid with the capacity to directly stimulate muscle protein synthesis. As a dietary supplement, leucine has been found to slow the degradation of muscle tissue by increasing the synthesis of muscle proteins in aged rats. Long-term leucine supplementation does not increase muscle mass or strength in healthy elderly men. Leucine potently activates the mammalian target of rapamycin kinase that regulates cell growth. Infusion of leucine into the rat brain has been shown to decrease food intake and body weight via activation of the mTOR pathway.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)



Fasudil is a potent Rho kinase inhibitor, which was developed by Asahi Kasei. The drug is used in Asia for the prevention of cerebral vasospasm in patients with subarachnoid hemorrhage.
Masitinib is a new orally administered tyrosine kinase inhibitor that targets mast cells and macrophages, important cells for immunity, through inhibiting a limited number of kinases. Based on its unique mechanism of action, masitinib can be developed in a large number of conditions in oncology, in inflammatory diseases, and in certain diseases of the central nervous system. In oncology due to its immunotherapy effect, masitinib can have an effect on survival, alone or in combination with chemotherapy. Through its activity on mast cells and consequently the inhibition of the activation of the inflammatory process, masitinib can have an effect on the symptoms associated with some inflammatory and central nervous system diseases and the degeneration of these diseases. AB Science is developing masitinib in multiple sclerosis and alzheimer's disease. Masitinib targets kinases, including c-Kit, PDGFR, and Lyn. It is used in the treatment of mast cell tumors in animals, specifically dogs. Since its introduction in November 2008 it has been distributed under the commercial name Masivet. It has been available in Europe since the second part of 2009. In the USA it is distributed under the name Kinavet.

Showing 71 - 80 of 81 results