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

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Showing 1 - 10 of 12 results

Sulindac is a nonsteroidal anti-inflammatory agent (NSAIA) of the arylalkanoic acid class that is marketed in the U.S. by Merck as Clinoril. Like other NSAIAs, it may be used in the treatment of acute or chronic inflammatory conditions. Sulindac is a prodrug, derived from sulfinylindene, that is converted in vivo to an active sulfide compound by liver enzymes. The sulfide metabolite then undergoes enterohepatic circulation; it is excreted in the bile and then reabsorbed from the intestine. This is thought to help maintain constant blood levels with reduced gastrointestinal side effects. Some studies have shown sulindac to be relatively less irritating to the stomach than other NSAIA's except for drugs of the cyclooxygenase-2 (COX-2) inhibitor class. The exact mechanism of its NSAIA properties is unknown, but it is thought to act on enzymes COX-1 and COX-2, inhibiting prostaglandin synthesis.
Methotrexate is an antineoplastic anti-metabolite. Anti-metabolites masquerade as purine or pyrimidine - which become the building blocks of DNA. They prevent these substances becoming incorporated in to DNA during the "S" phase (of the cell cycle), stopping normal development and division. Methotrexate inhibits folic acid reductase which is responsible for the conversion of folic acid to tetrahydrofolic acid. At two stages in the biosynthesis of purines and at one stage in the synthesis of pyrimidines, one-carbon transfer reactions occur which require specific coenzymes synthesized in the cell from tetrahydrofolic acid. Tetrahydrofolic acid itself is synthesized in the cell from folic acid with the help of an enzyme, folic acid reductase. Methotrexate looks a lot like folic acid to the enzyme, so it binds to it quite strongly and inhibits the enzyme. Thus, DNA synthesis cannot proceed because the coenzymes needed for one-carbon transfer reactions are not produced from tetrahydrofolic acid because there is no tetrahydrofolic acid. Methotrexate selectively affects the most rapidly dividing cells (neoplastic and psoriatic cells). Methotrexate is indicated in the treatment of gestational choriocarcinoma, chorioadenoma destruens and hydatidiform mole. In acute lymphocytic leukemia, methotrexate is indicated in the prophylaxis of meningeal leukemia and is used in maintenance therapy in combination with other chemotherapeutic agents. Methotrexate is also indicated in the treatment of meningeal leukemia. Methotrexate is used alone or in combination with other anticancer agents in the treatment of breast cancer, epidermoid cancers of the head and neck, advanced mycosis fungoides (cutaneous T cell lymphoma), and lung cancer, particularly squamous cell and small cell types. Methotrexate is also used in combination with other chemotherapeutic agents in the treatment of advanced stage non-Hodgkin’s lymphomas. Methotrexate is indicated in the symptomatic control of severe, recalcitrant, disabling psoriasis. Methotrexate is indicated in the management of selected adults with severe, active rheumatoid arthritis (ACR criteria), or children with active polyarticular-course juvenile rheumatoid arthritis.
Status:
Designated
Source:
FDA ORPHAN DRUG:868421
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Designated
Source:
FDA ORPHAN DRUG:806520
Source URL:

Class (Stereo):
CHEMICAL (UNKNOWN)

Status:
US Previously Marketed
First marketed in 1921

Class (Stereo):
CHEMICAL (ACHIRAL)



Pastaron (Urea) is a waste product of many living organisms, and is the major organic component of human urine. It is a very important starting material in a number of chemical syntheses, and is used on an industrial scale for the manufacture of fertilizers, pharmaceuticals, and resins. Urea is an osmotic diuretic similar to mannitol but more irritant. Applied topically, urea promotes hydration of keratin and mild keratolysis in dry skin. It increases water uptake by the stratum corneum and has an antipruritic effect. Pastaron is used to soften rough or dry skin caused by skin conditions such as eczema, psoriasis, keratosis, and others.
Status:
US Previously Marketed
Source:
melatonin
(1921)
Source URL:
First marketed in 1921
Source:
melatonin
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Melatonin (5-methoxy N-acetyltryptamine) is a hormone synthesized and released from the pineal gland at night, which acts on specific high affinity G-protein coupled receptors to regulate various aspects of physiology and behaviour, including circadian and seasonal responses, and some retinal, cardiovascular and immunological functions. Melatonin is also made synthetically and available without a prescription as an over-the-counter (OTC) dietary supplement in the U.S. Melatonin supplementation has many uses, however, it has been widely studied for treatment of jet lag and sleep disorders. Parents may consider using melatonin to help their child who has a trouble falling asleep. A medical professional should always evaluate insomnia or other sleeping disorders in children. Additionally, melatonin has been shown to protect against oxidative stress in various, highly divergent experimental systems. There are many reasons for its remarkable protective potential. In mammals, melatonin binds to a number of receptor subtypes including high-affinity (MT1 and MT2) and low-affinity (MT3, nuclear orphan receptors) binding sites, which are distributed throughout the central nervous system and periphery.
Status:
Possibly Marketed Outside US
Source:
NCT03915535: Phase 4 Interventional Terminated Healthy Athletes
(2019)
Source URL:
First approved in 2007

Class (Stereo):
CHEMICAL (ACHIRAL)



Doconexent (Docosahexaenoic acid, DHA) is an omega-3 fatty acid that is a primary structural component of the human brain, cerebral cortex, skin, and retina. DHA is widely used as a food supplement, and is beleived to support healthy brain development in young childred, prevent cardiovascular disease and cognitive decline during Alzheimer's disease. Most of these claims, however, were not supported by clinical trials. DHA spray is used as a tanner.
Status:
Discontinued
Source:
Puralor by Centurion Labs
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Acetylcysteine amide (NACA) is a novel thiol-containing antioxidant. NACA is a modified form of its parent compound N-acetylcysteine (NAC) that is a precursor of the most abundant endogenous antioxidant, glutathione (GSH). NACA demonstrated the multiple therapeutic abilities, including antioxidant, anti-apoptotic, and anti-inflammatory properties with greater efficacy compared to its parent compound. NACA treatment significantly maintained acute mitochondrial bioenergetics and normalized GSH levels following spinal cord injury. It is a new neuroprotective drug, that might be effective at slowing down nigral neuronal degeneration and illness progression in patients with Parkinson's disease.

Showing 1 - 10 of 12 results