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

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Showing 1441 - 1450 of 4027 results

Status:
Possibly Marketed Outside US
Source:
THALOMID by Parker, H.G.|Low-Beer, A.de G.|Isaac, E.L.
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



(s)-Thalidomide is an enantiomer of immunomodulatory agent Thalidomide. Thalidomide enantiomers are converted to each other in vivo, and Thalidomide contains both left and right-handed isomers in equal amounts. (s)-Thalidomide has proven efficacy in multiple myeloma. s-thalidomide-induced apoptosis associated with increases in I-kB activity, downregulation of NF-kB activity and an increase in Bax: Bcl-2 ratio. In cells cultured with s-thalidomide, there was a four-fold downregulation of the NFkB gene that was associated with a significant decrease in its protein activity.
Status:
Possibly Marketed Outside US
Source:
NCT02744664: Phase 4 Interventional Completed Lung Neoplasms
(2016)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Icotinib is an orally available quinazoline-based inhibitor of epidermal growth factor receptor. It selectively inhibits the wild-type and several mutated forms of EGFR tyrosine kinase. The major organ of icotinib metabolism is the liver, with the primarily enzymes being CYP2C19 and CYP3A4 from the cytochrome P450 monooxygenase system. Icotinib Hydrochloride was approved for the treatment of patients with advanced stage Nonsmall cell lung cancer by the State Food and Drug Administration (SFDA) of China. The major drug related adverse reactions of the traditional cytotoxic agents include rash, diarrhea, severe bone marrow suppression, neuropathy, hair loss, and gastrointestinal reactions. Icotinib is under investigation as an active agent against other EGFR mutation-positive cancers, like lung adenocarcinoma, oesophageal cancer, nasopharyngeal cancer and others.
Status:
Possibly Marketed Outside US
Source:
NCT03231709: Phase 4 Interventional Completed Type 2 Diabetes Mellitus
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Trelagliptin (SYR-472), a novel dipeptidyl peptidase-4 inhibitor used for the treatment of type 2 diabetes mellitus. Trelagliptin (as the salt Trelagliptin succinate) was approved for use in Japan in March 2015. Takeda, the company that developed Trelagliptin, chose to not get approval for the drug in the USA and EU.
Status:
Possibly Marketed Outside US
Source:
Noopept by CJSC LEKKO Pharmaceuticals
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Noopept (DVD-111) is a peptide promoted and prescribed in Russia and neighbouring countries as a nootropic. Noopept was patented by Russian-based pharmaceutical company JSC LEKKO Pharmaceuticals in the 1996. Research shows Noopept has similar effects, but works differently than other nootropics in the racetam-family. The compound is patented in both the US and Russia with patent of Russian Federation number 2119496, U.S. Patent 5,439,930 issued 8/8/1995. Noopept exhibits a combined neuroprotector effect both in vitro and in vivo. Noopept decreases the extent of necrotic damage caused by photoinduced thrombosis of cortical blood vessels. It was established that the neuroprotector effect of noopept is related to its action upon the well-known "triad", whereby the drug reduces neurotoxic effects of excess extracellular calcium, glutamate, and free radicals. Two additional components of the neuroprotector action of noopept are related to the antiinflammatory and antithrombotic activity.
Status:
Possibly Marketed Outside US
Source:
Stillen by Kupchan, S. M.|Sigel, C.W.|Hemingway, R.J.|Knox, J.R.|Udayamurthy, M.S.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Eupatilin (5,7-dihydroxy-3',4',6-trimethoxyflavone) is the major lipophilic flavonoid from Artemísia umbellifórmis, mountain wormwood used for the production of the celebrated alpine liqueur genepy. Eupatilin is the active ingredient of Stillen, a herbal drug from the Asian wormwood Artemisia asiatica, developed in South Korea for the treatment of gastritis and peptic ulcer. Eupatilin has been shown to exert cytoprotective and antiapoptotic effects on gastric and esophageal epithelial primary cells and is endowed with antispasmodic and antimutagenic properties, while apoptotic and anti-proliferative activities have been demonstrated on cancer cells. Eupatilin has also been evaluated, with promising results, in several assays of relevance for inflammation and allergy. Thus, this flavonoid inhibits in vitro mast cell degranulation and histamine release, shows in vivo anti-allergic properties is an antioxidant, inhibits 5-lipoxygenase and the leukotrienes synthesis, decreases prostaglandin E2 production, and inhibits the activation of nuclear transcription factor NF-κB and the expression of cyclooxygenase-2 and different pro-inflammatory cytokines, such as interleukins (IL-4, IL-6, and IL-8) and tumor necrosis factor-R (TNF-R)
Ethamsylate (2,5-dihydroxy-benzene-sulfonate diethylammonium salt) is a synthetic hemostatic drug indicated in cases of capillary bleeding. Ethamsylate acts on the first step of hemostasis by improving platelet adhesiveness and restoring capillary resistance. In addition it inhibits prostaglandin biosynthesis. Well-controlled clinical trials clearly showed the therapeutic efficacy of ethamsylate in dysfunctional uterine bleeding, with the magnitude of blood-loss reduction being directly proportional to the severity of the menorrhagia. Other well-controlled clinical trials showed therapeutic efficacy of ethamsylate in periventricular hemorrhage in very low birth weight babies and surgical or postsurgical capillary bleeding.
Malvidin-3-O-glucoside is a polyphenolic anthocyanin. Anthocyanins are flavonoids widely distributed in fruits and vegetables that exhibit antioxidative and anti-inflammatory bioactivities. Among other polyphenolic components, malvidin-3-glucoside is present in ViNitrox™ a natural dietary supplement from apple and grape, it offers a number of exceptional sports nutrition properties including enhanced and lasting performance.
Vitexin, identified as apigenin-8-C-β-D-glucopyranoside, is a flavonoid compound found in Anthurium versicolor, Ficaria verna Huds. (Ranunculaceae), Cucumis sativus L. (Cucurbitaceae), and Acer palmatum (Aceraceae). Vitexin is an active component of many traditional Chinese medicines. Vitexin has recently received increased attention due to its wide range of pharmacological effects, including but not limited to anti-oxidant, anti-cancer, anti-inflammatory, anti-hyperalgesic, and neuroprotective effects.
Status:
Possibly Marketed Outside US
Source:
NCT02200978: Phase 4 Interventional Completed Childhood Acute Promyelocytic Leukemia
(2011)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Indirubin is derived from the Indigo Plant (Isatis Root, Isatis Leaf). It is used as part of a traditional Chinese herbal prescription called Dang Gui Long Hui Wan, to treat chronic myelogenous leukemia (CML). Indirubin inhibits DNA synthesis in several cell lines, in a cell-free assay and in vivo in rats with Walker-256 sarcoma. A weak binding of indirubin to DNA in vitro has been described. Indirubin inhibited all cyclin-dependent kinases (1,2,4,5) almost equally. Indirubin has been approved for clinical trials against chronic myelocytic and chronic granulocytic leukaemia. A few studies show that Indirubin is effective against psoriasis. Mild to severe nausea, vomiting, abdominal pain, diarrhea, headache, and edema are reported adverse events of Indirubin. Long-term oral ingestion has also occasionally been associated with hepatitis, pulmonary arterial hypertension and cardiac insufficiency.
Status:
Possibly Marketed Outside US
Source:
Unknown by Kromayer, A.
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Gentiopicrin is a naturally occurring iridoid glycoside. It is a bioactive component of gentian species of medical plants. It has proved to be the strongest inhibitor of myeloperoxidase. It could be absorbed rapidly in mice, but with a low bioavailability, and could distribute to tissues extensively. Gentiopicrin has been reported to be effective against inflammatory conditions such as rheumatoid arthritis, liver illness, fever, digestive and intestinal disorders. Gentiopicrin treatment can exert anti-inflammatory effects on experimental acute colitis through attenuating the expression levels of TNF-α, IL-1β, IL-6, iNOS and COX-2, and it may present the therapeutic potential in the treatment of colitis. The drug inhibits reserpine-induced pain/depression dyad by downregulating GluN2B receptors in the amygdala. Gentiopicrin injection was approved by SFDA for the treatment of acute jaundice and chronic active hepatitis.

Showing 1441 - 1450 of 4027 results