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

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Showing 831 - 840 of 2546 results

Bruceantin is a compound isolated from Brucea antidysenteriea, a plant used in Ethiopia as an anticancer treatment. The primary action of Bruceantin appears to be an inhibition of protein synthesis which takes place at the ribosomal level. Bruceantin induced marked decreases of c-myc mRNA and protein expression in all cell lines. Bruceantin-induced c-myc downregulation might trigger cell death mechanisms preferentially in those cell lines with wild-type p53 protein expression. Bruceantin was evaluated in three separate phase I clinical trials in patients with various types of solid tumors. Hypotension, nausea, and vomiting were common side effects at higher doses, but hematologic toxicity was moderate to insignificant and manifested mainly as thrombocytopenia. Bruceantin was then tested in two separate phase II trials including adult patients with metastatic breast cancer and malignant melanoma. No objective tumor regressions were observed, and clinical trials were terminated.
Ginkgolide B belongs to the class of organic compounds known as ginkgolides and bilobalides. These are diterpene lactones with a structure based either on the gingkolide or the bilobalide skeleton. The ginkgolide skeleton is a very rigid structure consisting of hexacyclic C20 trilactone. The cis-fused F/A/D/C ring junction forms an empty semi-ball hole, the D ring contains a cage form tetrahydrofuran ring which occupies the center of the empty hole, and the oxygen atoms of the D,C and F ring and 10-hydroxyl group consist of an analogous crown ether structure. Ginkgolide B is one of the ginkgolides isolated from the leaves of the Ginkgo biloba tree. The Ginkgolide B is the most potent antagonist of platelet activating factor (PAF) and exhibits therapeutic action in a variety of diseases mainly by the PAF receptor. The ginkgolide B possesses a number of beneficial effects such as anti-inflammatory, anti-allergic, antioxidant, and neuroprotective effects. It promotes the proliferation, migration and adhesion of endothelial progenitor cells, and the induction of angiogenesis through vascular endothelial factor (VEGF). Ginkgolide B is considered a valid non-pharmacological (or nutraceutical) approach to the prophylaxis of both migraine with and without aura. Effects of ginkgolide B include reduction of Ca2+-stimulated intracellular events, scavenging of free radicals, modulation of central nervous system glutamatergic transmission and reduction of antiplatelet activating factor (PAF) levels in brain. Ginkgolide B is an active component of EGb, a standardised extract of Ginkgo biloba leaves. Ginkgolide B is one of the major components of EGb-761.
Ligustrazine (tetramethylpyrazine) is a bioactive ingredient extracted from the widely-used Chinese herb, Chuanxiong. It inhibits of platelet aggregation, enhances of vessel dilation, increases cerebral blood flow and possesses neuroprotective properties. The injection solution of ligustrazine has been used especially in China to treat ischemic stroke, coronary heart disease, diabetic nephropathy, and knee osteoarthritis. Ligustrazine was also evaluated in clinical as a remedy for pressure sores, as a salvage agent for patients with non-Hodgkin's lymphoma, as a treatment for bronchial asthma and vertebrobasilar insufficiency.
Epichatechin is one of the 4 catechin diastereoisomers. It can be isolated from a number of species of Palmae, as well as Dryas octopetala and guarana seeds. Epicatechin has been widely studied as a potential therapeutic compound in a wide variety of conditions including cancers, diabetes, heart conditions, and neurological conditions. Epicatechin is available as a natural health supplement and marketed for bodybuilding and the treatment of high blood pressure, high cholesterol, immune support, low testosterone, high blood sugar, and improved memory.
Status:
Possibly Marketed Outside US
Source:
NCT03198572: Phase 4 Interventional Recruiting Non-alcoholic Steatohepatitis
(2017)
Source URL:
First approved in 2023
Source:
sugar management gummies by XIAN CHIANG COMPANY LIMITED
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Berberine, an alkaloid isolated from Rhizoma Coptidis, is known to have a wide array of therapeutic effects including antimicrobial, antineoplastic, and hepatoprotective effects. It is found in several plants including European barberry, goldenseal, goldthread, Oregon grape, phellodendron, and tree tumeric. Berberine seems to slightly reduce blood sugar levels in people with diabetes. Berberine might lower blood pressure. Berberine is possibly safe for most adults for short-term use when taken by mouth or applied to the skin.
Status:
Possibly Marketed Outside US
Source:
Imepitoin
Source URL:
First approved in 2022

Class (Stereo):
CHEMICAL (ACHIRAL)



Imepitoin (AWD 131–138 or ELB 138; 1-(4-chlorophenyl)-4-morpholino-imidazolin-2-one) is a new anti-epileptic drug recently approved in the European Union for the treatment of canine idiopathic epilepsy. It was developed from a series of imidazolinones due to its pronounced ant seizure activity in a large variety of rodent models of epileptic seizures, combined with a high tolerability in these models. Imepitoin is a centrally acting antiepileptic substance, which crosses the blood brain barrier without involvement of active transport or active clearance, resulting in immediate equilibrium between plasma and brain. Imepitoin acts as low-affinity partial agonists at the benzodiazepine (BZD) site of the GABAA receptor. Hopefully, that the favorable profile of imepitoin for the treatment of epilepsy in dogs will reactivate the interest in partial BZD site agonists as new treatments for human epilepsy.
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 (ACHIRAL)



Honokiol is a biphenolic natural product isolated from the bark and leaves of Magnolia plant spp. Honokiol possesses anti-carcinogenic, anti-inflammatory, anti-oxidative, anti-angiogenic as well as the inhibitory effect on malignant transformation of papillomas to carcinomas in vitro and in vivo animal models without any appreciable toxicity. Honokiol affects multiple signaling pathways, molecular and cellular targets including nuclear factor-κB (NF-κB), STAT3, epidermal growth factor receptor (EGFR), cell survival signaling, cell cycle, cyclooxygenase and other inflammatory mediators, etc. Honokiol can permeate the blood-brain barrier and the blood-cerebrospinal fluid to increase its bioavailability in neurological tissues. Diverse studies have provided evidence on the neuroprotective effect of honokiol in the central nervous system, due to its potent antioxidant activity, and amelioration of the excitotoxicity mainly related to the blockade of glutamate receptors and reduction in neuroinflammation. Honokiol can attenuate neurotoxicity exerted by abnormally aggregated Abeta in Alzheimer's disease. Honokiol is being developed by Huons as HL tablet for the treatment of alcoholic and non-alcoholic fatty liver.
Status:
Possibly Marketed Outside US
Source:
NCT04126135: Phase 4 Interventional Completed Nicotine Addiction
(2022)
Source URL:
First approved in 2018
Source:
Bei Ling Tong Bao Er Zheng Yuan Antibacterial Creams by Jilin Mancaotang Health Management Group Co Ltd
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Cytisine ( aka baptitoxine and sophorine) is a naturally occurring alkaloid that can be found in several plant genera, such as Laburnum and Cytisus of the family Fabaceae. It has been found to be clinically superior to nicotine replacement therapy for the cessation of smoking. It is available in Eastern Europe under the brand names Tabex and Desmoxan and in Canada under the brand name Cravv. However certain undesirable side effects exist, Cytisine can interfere with breathing and cause death (LD50 i.v., in mice, is about 2 mg/kg) and Cytisine is also teratogenic. Cytosine is an α4β2 nicotinic Acetylcholine receptor agonist. In addition to clinical use as a smoking cessation aid, It has demonstrated anti-depressant effects in mice.
Status:
Possibly Marketed Outside US
Source:
NCT02556814: Phase 4 Interventional Completed Immune Thrombocytopenia
(2015)
Source URL:
First approved in 2018
Source:
SUPER FIRST C SERUM PURE VITAMIN C 13 PERCENT by LIZK Co., Ltd.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Caffeic acid is an organic compound that is classified as a hydroxycinnamic acid. Caffeic acid is naturally found in many agricultural products, such as fruit, vegetables, wine, olive oil, and coffee, and therefore, significantly present in human diet. Caffeic acid has been reported to have a wide variety of biological activities, including antioxidants, antithrombosis, antihypertensive, antifibrosis, antiviral and anti-tumor properties. Caffeic acid can be effectively employed as a natural antioxidant in various food products such as oils. Caffeic acid exhibits potent anticancer effect in HT-1080 cell line and that it may be used as an anticancer agent. Caffeic acid showed neuroprotective action against oxidative and DNA damage produced in the kindling epilepsy model, although they did not produce antiepileptogenic effect in vivo. Caffeic acid was effective in patients with primary immune thrombocytopenia. Detected in clinical trial caffeic acid-related adverse events were: mild nausea and elevation of liver enzymes.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)


Melarsomine (melarsomine dihydrochloride) is an organic arsenical chemotherapeutic agent and is a trypanocidal antiparasitic drug. As of 2016 DIROBAN, a generic melarsomine dihydrochloride product, is the only FDA-approved treatment for adult heartworm (Dirofilaria immitis) infection in dogs. It is not approved for treatment in cats, or dogs in late-stage infection. It is marketed by Merial under the trade name Immiticide and is not currently available in the U.S. due to a manufacturing shortage. Sponsored by Anzac Animal Health, LLC and distributed by Zoetis, Inc., DIROBAN is a prescription animal drug supplied as a sterile powder that must be reconstituted with an accompanying sterile water diluent. The exact mode of action on D. immitis is unknown. Post-treatment mortality due to thromboembolism and/or progression of the underlying disease may occur in 10 to 20% of the Class 3 patients treated with DIROBAN.