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

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Showing 311 - 320 of 1040 results

Status:
Possibly Marketed Outside US
Source:
LOWGAN by Yamanouchi Pharmaceutical
Source URL:
First approved in 2023
Source:
Slimming Patch by Guangzhou Hanhai Trading Co., Ltd
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Amosulalol is a beta- and alpha-1 adrenoceptor-blocking agent developed for the treatment of hypertension. Amosulalol does not cross blood brain barrier and does not have adverse affect on CNS system.The drug is marketed under the name Lowgan in Japan and Korea.
Sesamin is the most prominent lignan compound found in sesame seeds, one of the two highest sources of lignans in the human diet (the other being flax). Sesamin is catered to be a nutritional supplement that confers antioxidant and antiinflammatory effects (if touting its health properties) or possibly being an estrogen receptor modulator and fat burner (if targeting atheltes or persons wishing to lose weight). Sesamin has a few mechanisms, and when looking at it holistically it can be summed up as a fatty acid metabolism modifier. It appears to inhibit an enzyme known as delta-5-desaturase (Δ5-desaturase) which is a rate-limiting enzyme in fatty acid metabolism; inhibiting this enzyme results in lower levels of both eicosapentaenoic acid (EPA, one of the two fish oil fatty acids) as well as arachidonic acid, and this mechanism appears to be relevant following oral ingestion. The other main mechanism is inhibiting a process known as Tocopherol-ω-hydroxylation, which is the rate limiting step in the metabolism of Vitamin E; by inhibiting this enzyme, sesamin causes a relative increase of vitamin E in the body but particularly those of the gamma subset (γ-tocopherol and γ-tocotrienol) and this mechanism has also been confirmed to be active following oral ingestion. Sesamin is a potent and specific inhibitor of delta 5 desaturase in polyunsaturated fatty acid biosynthesis. Sesamin inhibits a particular CYP3A enzymes that is involved in vitamin E metabolism, where the enzyme initially ω-hydroxylates vitamin E (required step) and then the rest of vitamin E is subject to fat oxidation. By inhibiting this step, sesamin causes an increase in circulating and organ concentrations of vitamin E. Sesamin is thought to have PPARα activating potential in the liver, but it is uncertain how much practical relevance this has in humans due to this being a mechanism that differs between species.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)

MK-467 (also known as Vatinoxan) is a peripheral α2 -adrenoceptor antagonist patented by American multinational pharmaceutical company Merck & Co., Inc. for treatment of hypertension, diabetes, obesity, and as blood platelet aggregation. In preclinical models Vatinoxan administration alleviate the unwanted cardiopulmonary effects of various α2-agonists (such as bradycardia, vasoconstriction, and hypoxemia). Because of its low lipophilicity MK-467 poorly penetrates the mammalian central nervous system and preserve the centrally mediated desired effects of α2-agonists. Simultaneous intramuscular injection of MK-467 hastened the absorption of α2-agonist drugs, which was manifested by rapid onset of sedation.
Status:
Possibly Marketed Outside US
Source:
Hepad S5 by YOUNGJIN Korean Medicine Clinic
(2021)
Source URL:
First approved in 2021
Source:
Hepad S5 by YOUNGJIN Korean Medicine Clinic
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Isocorynoxeine is one of four bioactive tetracyclic oxinole alkaloids which can be isolated from Uncaria hooks used in traditional Chinese and Kampo medicines. The traditional remedies are claimed to have sedative and anti-spasmodic effects, however, isocorynoxeine does not appear to cross the blood-brain barrier. It is suspected that one or more metabolites of isocorynoxeine produce the effect of lower blood pressure, vasodilation and protection against ischemic neural damage. Furthermore, isocoynoxine has also shown reduce the viability of multi-drug resistant cancer cells when used in conjunction with doxycycline
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)


There is no information related to the biological or pharmacological application of Sodium ferrocyanide decahydrate. It is known, that this substance is used for bleaching, toning, and fixing in photography, and in the petroleum industry, as a removal of mercaptans.
Aloe emodin is a hydroxyanthraquinone found in Aloe vera leaves. It plays an important role in the regulation of cell growth and death. It has been reported to promote the anti-cancer effects in various cancer cells by inducing apoptosis. Aloe emodin selectively inhibits human neuroectodermal tumor cell growth in tissue cultures and in animal models. It has significant antileukemic activity against the P-388 lymphocytic leukemia in mice. Anti-glioma action of Aloe emodin involves ERK-independent induction of both apoptosis and autophagy, as well as ERK inhibition-mediated differentiation of glioma cells. Aloe-emodin can not pass through the blood-brain barrier.
Status:
Possibly Marketed Outside US
Source:
NCT00680121: Phase 4 Interventional Completed Alcoholism
(2008)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Benfotiamine is a derivative of vitamin B1. It was developed in Japan specifically to treat Korsakoff's syndrome and patented in the United States in 1962, but never became popular. It has been in use as a widely used prescription drug in Europe since 1978 to treat diabetes and is available at many vitamin shops in the United States. It has been licensed for use in Germany since 1993 under the trade name Milgamma. (Combinations with pyridoxine or cyanocobalamin are also sold under this name). It is prescribed there for treating sciatica and other painful nerve conditions. It is marketed as a medicine and/or dietary supplement, depending on the respective Regulatory Authority. Unfortunately apparent evidences from human studies are scarce and especially endpoint studies are missing. Benfotiamine has proven to affect glucose metabolic process through various mode of actions, and plays a part in obstructing age-associated glycation end products (AGEs). Benfotiamine reduces the extra biosynthesis and accumulation of a number of glucose metabolites, including glyceraldeyde-3-phosphate and dihydroxyacetone phosphate. Elevated levels of those glucose intermediates function as a trigger to most of the mechanisms accountable for hyperglycemia-caused cell damage. Benfotiamine increases tissue amounts of thiamine diphosphate, consequently growing transketolase activity and producing a significant decrease in glucose metabolites and precursors to AGEs. Up to now, two of the most effective AGE inhibitors in living microorganisms would be the Vitamin B1 derivative, benfotiamine and also the Vitamin B6 derivative, pyridoxamine. Additionally, benfotiamine has long been proven to lessen NF-kB activity, therefore restricting the over-production from the harmful superoxide toxin. Excess superoxide production may partly hinder a vital enzyme in glucose metabolic process, glyceraldehyde-3-phosphate dehydrogenase, directing glucose metabolites from glycolysis in to the major glucose-driven signaling paths that cause hyperglycemic damage. Theoretically, overdose with benfotiamine should cause menopausal flashes, bluish skin (because of rapid utilization of oxygen), tingling, and difficulty breathing, but used, this merely has not happened.
Status:
Possibly Marketed Outside US
Source:
AQUA DE FOLLI HAIR BOOSTER PRO by ROKIT HEALTHCARE Inc.
(2020)
Source URL:
First approved in 2020
Source:
AQUA DE FOLLI HAIR BOOSTER PRO by ROKIT HEALTHCARE Inc.
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Thymidine is a water-soluble pyrimidine deoxynucleoside and potent thymidine kinase substrate. Thymidine is known to be converted to dTTP and utilized for DNA synthesis. It is also known that thymidine is converted by catabolic enzymes to several end products. Excess thymidine results in high levels of dTTP, which exerts a regulatory feedback inhibition in the nucleotide biosynthesis pathways leading to DNA synthesis. This property of thymidine is used when it is given in high doses to patients with solid tumors. Thymidine is being tested in Phase II of clinical trials for the treatment of cancer and 5'-Nucleotidase Syndrome.
Status:
Possibly Marketed Outside US
Source:
Japan:Cloperastine Hydrochloride
Source URL:
First approved in 2018

Class (Stereo):
CHEMICAL (RACEMIC)

Conditions:

Cloperastine (INN) or cloperastin is an antitussive and antihistamine that is marketed as a cough suppressant in Japan, Hong Kong, and in some European countries. It was first introduced in 1972 in Japan, and then in Italy in 1981. The precise mechanism of action of cloperastine is not fully clear, but several different biological activities have been identified for the drug, of which include: ligand of the gamma1 receptor (Ki = 20 nM) (likely an agonist), GIRK channel blocker (described as "potent"), antihistamine (Ki = 3.8 nM for the H1 receptor), and anticholinergic. Cloperastine possesses dual activity. It also acts as a mild bronchorelaxant and has antihistaminic activity, without acting on the central nervous system or the respiratory center.
Status:
Possibly Marketed Outside US
Source:
ENTYCE by Pfizer
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Capromorelin is a potent ghrelin receptor agonist. Capromorelin is indicated for appetite stimulation in dogs. Plasma insulin-like growth factor-I (IGF-I) was elevated progressively over a 5-d course of daily oral dosing in dogs. In healthy older adults at risk for functional decline, administration of the capromorelin may improve body composition and physical function. Adverse events included fatigue, insomnia, and small increases in fasting glucose, glycosylated hemoglobin, and indices of insulin resistance.