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Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Isosakuranetin is a citrus fruit flavanone. It is a TRPM3 channel blocker and CYP1 enzyme isoforms inhibitor. It is a strong candidate, as chemopreventive food ingredient against CYP1B1-related carcinogenesis. Isosakuranetin may be useful in treating neuropathic pain without body temperature increase. Isosakuranetin attenuated ethanol-induced gastritis by inhibiting the infiltration of immune cells, including neutrophils, via the regulation of CXCL4 (or IL-8) secretion and the activation NF-κB.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Sesamolin from Sesamun indicum seeds plays important role in plant defense, such as antifeedant as well as potent antioxidants and insecticides. Sesaminol has potent inhibition of cytochrome P450 (CYPs). The neuroprotective effect of sesamolin was also observed in vivo using gerbils subjected to a focal cerebral ischemia induced by occlusion of the right common carotid artery and the right middle cerebral artery. Lipid peroxidation activity, measured as 2-thiobarbituric acid reactive substances, was significantly lower in the kidneys and liver of the sesamolin-fed rats than in the controls.
Status:
US Previously Marketed
Source:
NICLOCIDE by BAYER PHARMS
(1982)
Source URL:
First approved in 1982
Source:
NICLOCIDE by BAYER PHARMS
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Niclosamide is an antihelminth used against tapeworm infections. It may act by the uncoupling of the electron transport chain to ATP synthase. The disturbance of this crucial metabolic pathway prevents creation of adenosine tri-phosphate (ATP), an essential molecule that supplies energy for metabolism. Niclosamide works by killing tapeworms on contact. Adult worms (but not ova) are rapidly killed, presumably due to uncoupling of oxidative phosphorylation or stimulation of ATPase activity. The killed worms are then passed in the stool or sometimes destroyed in the intestine. Niclosamide may work as a molluscicide by binding to and damaging DNA. Niclosamide is used for the treatment of tapeworm and intestinal fluke infections: Taenia saginata (Beef Tapeworm), Taenia solium (Pork Tapeworm), Diphyllobothrium latum (Fish Tapeworm), Fasciolopsis buski (large intestinal fluke). Niclosamide is also used as a molluscicide in the control of schistosomiasis. Niclosamide was marketed under the trade name Niclocide, now discontinued.
Status:
US Previously Marketed
Source:
THEOMINAL RS THEOBROMINE by WINTHROP
(1961)
Source URL:
First marketed in 1921
Source:
Theobromine Sodio-Salicylate U.S.P.
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Theobromine is the primary alkaloid present in the cocoa and chocolate. Theobromine is found in the shells and beans of the cacao plant and it is extracted from the husks of the bean and used for the synthesis of caffeine. Theobromine is an adenosine A1 and A2a receptor antagonist. Thesodate is used as a vasodilator, a diuretic, and heart stimulant. And similar to caffeine, it may be useful in management of fatigue and orthostatic hypotension. The symptomatic adverse reactions produced by theobromine are more or less tolerable and if they become severe, they can be treated symptomatically, these include anxiety, restlessness, tremors, sleeplessness, nausea and vomiting, loss of appetite. Theobromine is currently not in use as a medicinal drug.
Status:
Possibly Marketed Outside US
Source:
21 CFR 333A
(2020)
Source URL:
First approved in 2020
Source:
21 CFR 333A
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Safrole is a natural product obtained from essential oil of the root bark of Sassafras tree. Safrole has been used as a flavoring agent in drugs and in the manufacture of heliotropin, perfumes, soaps, and piperonyl butoxide. Oil of sassafras, which contains safrole, was formerly used to flavor some soft drinks, such as root beer. However, this use or any other addition of safrole or oil of sassafras to food was banned in the United States in 1960 due to evidence of carcinogenicity. Numerous studies have shown that safrole from betel quid-containing safrole might be involved in the pathogenesis of hepatocellular carcinoma in human due to the formation of DNA adducts. Safrole has also been used in the illicit production of the drug 3,4-methylenedioxymethamphetamine (MDMA, or ecstasy), and the U.S. Drug Enforcement Administration has designated safrole a List I Chemical. Anticancer and anti-diabetic properties of safrole were investigated in vitro and in vivo.
Status:
Possibly Marketed Outside US
First approved in 2018
Source:
AZULENE FINISHING OIL INGREDIENTS by Coty US LLC
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Guaiazulene is a blue compound. It is a derivative of azulene, guaiazulene is a bicyclic sesquiterpene that is a constituent of some essential oils, mainly oil of guaiac and chamomile oil. Guaiazulene is an U.S. FDA-approved cosmetic color additive. Guaiazulene is used in the formulation of bath products, cleansing products, depilatories, hair bleaches, hair conditioners, hair dyes and colors, hair straighteners, permanent waves, skin care products and skin fresheners. Guaiazulene has antioxidant, antifungal, antimicrobial, anti-inflammatory, anti-spasmodic, anti-ulcer, antitumoral activities and relaxant properties. Common side effects are: diarrhea, constipation, etc.
Status:
Possibly Marketed Outside US
Source:
NCT04677712: Phase 4 Interventional Completed Edematous Fibrosclerotic Panniculopathy (EFP)
(2020)
Source URL:
First approved in 2017
Source:
M006
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
1-(4-hydroxy-3-methoxyphenyl)decan-3-one (Paradol, 6-paradol ), a major constituent of A. melegueta seeds, exhibited potent proliferative and ossification characteristics in bone cells. It enhanced alkaline phosphatase activity and vitamin D content and decreased the osteoporotic marker acid phosphatase. Paradol enhanced the expression of osteocyte and osteoblast-related genes and inhibited osteoclast and RUNX suppressor genes. Paradols are unsaturated ketones produced by biotransformation of shogaols in gingers. Among them, 6-paradol has been investigated as a new drug candidate due to its anti-inflammatory, apoptotic, and neuroprotective activities. 6-paradol exhibited a significant
glucose-lowering effect and decreased body weight. 6-paradol possesses good anti-hyperglycemic activity, therefore it may serve as a novel
target for the development of anti-obesity and anti-hyperglycemic functional food. 6-paradol effectively protects brain after cerebral ischemia, likely by attenuating neuroinflammation in microglia, suggesting it as a potential therapeutic agent to treat cerebral ischemia.
Status:
Possibly Marketed Outside US
Source:
M021
(2012)
Source URL:
First approved in 2012
Source:
M021
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Hesperetin is a cholesterol-lowering flavanoid found in a number of citrus juices. It appears to reduce cholesteryl ester mass and inhibit apoB secretion by up to 80%. Hesperetin may have antioxidant, anti-inflammatory, anti-allergic, hypolipidemic, vasoprotective and anticarcinogenic actions. In vitro research also suggests the possibility that hesperetin might have some anticancer effects and that it might have some anti-aromatase activity, as well as activity again. Hesperetin reduces or inhibits the activity of acyl-coenzyme A: cholesterol acyltransferase genes (ACAT1 and ACAT2) and it reduces microsomal triglyceride transfer protein (MTP) activity. Hesperetin also seems to upregulate the LDL receptor. This leads to the reduced assembly and secretion of apoB-containing lipoproteins and enhanced reuptake of those lipoproteins, thereby lowering cholesterol levels. Hesperetin's 7-O-glycoside, hesperidin, is a naturally occurring flavanon-glycoside, the main flavonoid in lemons and sweet oranges.
Status:
Possibly Marketed Outside US
Source:
Kaydia Patch by Strong Current Enterprises Limited
Source URL:
First approved in 2011
Source:
EnBrace HR by Jaymac Pharma
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Piperine is a simple and pungent alkaloid found in the seeds of black pepper (Piper nigrum). Following its isolation and full characterization, the biological properties of piperine have been extensively studied, and piperine-like derivatives have shown an interesting range of pharmacological activities. Piperine is currently paving its way to become a privileged scaffold for the development of bioactive compounds with therapeutic application in multiple human diseases. In particular, piperine derivatives were shown to modulate the activity of several targets related to neurological disorders, including epilepsy, Parkinson's disease, depression and pain related disorders. Moreover, the efflux pump inhibitory ability of piperine and its analogues tackles important drug resistance mechanisms and may improve the clinical efficacy of antibiotic and anticancer drugs. Piperine has been found to have immunomodulatory, anti-oxidant, anti-asthmatic, anti-carcinogenic, anti-inflammatory, anti-ulcer, and anti-amoebic properties.
Status:
Possibly Marketed Outside US
Source:
21 CFR 350
(2010)
Source URL:
First approved in 2010
Source:
21 CFR 350
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Palmatine is a protoberberine alkaloid. Palmatine is major component of herbal preparations mainly used in traditional medicine Chinese, Korean and Indian. Palmatine can be found in various medicinal plants such as Coptis chinensis, Rhizoma coptidis, Corydalis yanhusuo, Radix tinosporae, among others. It exerts diverse pharmacological and biological properties. Palmatine has been proposed as a promising DNA phototherapy drug, notably due to its ability to produce in situ singlet oxygen only when interacting with DNA.