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

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Showing 2371 - 2380 of 2546 results

Status:
Possibly Marketed Outside US
Source:
NCT02469337: Phase 4 Interventional Unknown status Insulin Resistance
(2012)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Dichloroacetic acid, often abbreviated DCA (dichloroacetate), is an acid analog of acetic acid in which two of the three hydrogen atoms of the methyl group have been replaced by chlorine atoms. The salts and esters of dichloroacetic acid are called dichloroacetates. Salts of DCA are used as drugs since they inhibit the enzyme pyruvate dehydrogenase kinase. Early reports of its activity against brain cancer cells led patients to treat themselves with DCA, which is commercially available in non-pharmaceutical grade. A phase 1 study in 5 patients concluded that DCA was safe, but wasn't designed to establish effectiveness. DCA was approved for use in Canada in 1989 (as a topical formulation for the treatment of warts and for cauterization and removal of a wide variety of skin and tissue lesions), but was cancelled post market. DCA is a noncompetitive inhibitor of the endoplasmic reticulum enzyme HMG CoA reductase, which catalyzes the rate limiting step in cholesterol biosynthesis. DCA has been researched in adults, children, animals, and cells as a monotherapy as well as in combination with other therapies for the treatment of severe metabolic disorders including diabetes and hypercholesterolemia, lactic acidosis, certain heart conditions, and cancer. DCA has been prescribed to reduce tumour size and tumour markers, prevent angiogenesis, reduce cancer related symptoms, manage pain, and aid in palliation.
Status:
Possibly Marketed Outside US
Source:
Unknown by Sotiropoulos, J.|El Batouti, N.
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Enzacamene, ( )-[Bicyclo[2.2.1]-heptan-2-one, 1,7,7-trimethyl-3-[(4-methylphenyl)methylene]-, (1R,3E,4S)-] is one of enantiomer of Enzacamene (4-MBC) -- organic sunscreen components, that protects against UV radiation and may therefore help in the prevention of skin cancer. Enzacamene can exist as a cis-(Z)- and trans-(E)-isomer due to the exocyclic carbon-carbon (styrene) double bond. A commercial Enzacamene from a major supplier of UV filters showed the presence of only the (E)-isomer However, it is known that, upon exposure to light, (E)-4-Enzacamene is photochemically isomerized reversably to (Z)-4-Enzacamene. Both (E)- and (Z)-Enzacamene are chiral and thus consist of enantiomers (optical isomers). In a technical material and in a major brand sun lotion, Enzacamene was shown to consist entirely (>99%) of (E)-isomers and to be racemic. Wastewater showed the presence of both (E)- and (Z)-Enzacamene with a clear excess of (E)-isomers (E >Z). Untreated wastewater showed a nearly racemic composition suggesting that most if not all commercial Enzacamene is racemic. Treated wastewater indicated some excess of (R)- or (S)-stereoisomers ikely as a result of some enantioselective (bio)degradation in wastewater treatment plants. Enantiomers may show different biological behavior with respect to uptake, metabolism, and excretion and often differ in toxicity and other biological effects.
Status:
Possibly Marketed Outside US
Source:
NCT02140073: Phase 4 Interventional Unknown status GERD
(2013)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Domperidone is a peripherally selective D2 receptor antagonist. It acts as an antiemetic and a prokinetic agent through its effects on the chemoreceptor trigger zone and motor function of the stomach and small intestine. Domperidone was not approved in USA due to risks of cardiac arrhythmias, cardiac arrest, and sudden death, but is available in other countries. However, FDA allows access to Domperidone through an expanded access investigational new drug application (IND) to patients with gastroesophageal reflux disease with upper GI symptoms, gastroparesis, and chronic constipation. As an “off-label” use, domperidone is prescribed to breastfeeding women to enhance their milk production.
Metomidate is a non-barbiturate imidazole which produces a sleepy condition of 20-60 minutes duration without substantial analgesia. Since the beginning of 1997 the use of the hypnotic drug metomidate (Hypnodil) in swine is nor longer allowed. This ban caused a substantial therapeutic deficit for anesthesia in swine. 11C-metomidate may be used with positron emission tomography which can differentiate adrenocortical from nonadrenocortical tumors and a suspected adrenocortical cancer may be characterized and staged before surgery. Metomidate hydrochloride is for the sedation and anesthesia of aquarium and non-food fish species. Aquacalm has been granted Indexed status by the FDA for this purpose.
Status:
Possibly Marketed Outside US
Source:
NCT02140073: Phase 4 Interventional Unknown status GERD
(2013)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Domperidone is a peripherally selective D2 receptor antagonist. It acts as an antiemetic and a prokinetic agent through its effects on the chemoreceptor trigger zone and motor function of the stomach and small intestine. Domperidone was not approved in USA due to risks of cardiac arrhythmias, cardiac arrest, and sudden death, but is available in other countries. However, FDA allows access to Domperidone through an expanded access investigational new drug application (IND) to patients with gastroesophageal reflux disease with upper GI symptoms, gastroparesis, and chronic constipation. As an “off-label” use, domperidone is prescribed to breastfeeding women to enhance their milk production.
Status:
Possibly Marketed Outside US
Source:
Robenz by Kantor, S.|Kennett, R.L.Jr.|Waletzky, E.|Tomcufcik, A.S.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Robenidine (l,3-6ts (p-chlorobenzylidenamino) guanidine hydrochloride) is an effective anticoccidial, first introduced by Kantor, Kennett, Waletzky & Tomcufcik (1970). It does not affect the earliest stages in the coccidial life-cycle and its main activity is against the almost mature first generation schizont. It is used as an aid in the prevention of coccidiosis caused by Eimeria mivati, E. brunetti, E. tenella, E. acervulina, E. maxima and E. necatrix in broiler chickens.
Status:
Possibly Marketed Outside US
Source:
ADVOCIN by Pfizer
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Danofloxacin is a quinolone antibacterial agent for veterinary medicine. The drug is approved by FDA for the treatment of bovine infectious respiratory disease under the name Advocin (mesylate salt). Danofloxacin exerts its action by inhibiting bacterial DNA gyrase.
Status:
Possibly Marketed Outside US
Source:
NCT04475276: Phase 4 Interventional Recruiting Non-Alcoholic Fatty Liver Disease
(2021)
Source URL:
First approved in 2001
Source:
Strovite OneCaplets by Exeltis USA, Inc.
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Thioctic acid also known as alpha-lipoic acid is a dietary supplement, which is a common ingredient in OTC (over-the-counter) multivitamin formulas and anti-aging supplements. Thioctic acid exists in both R- and S-enantiomeric forms, however, only R-form is essential as a cofactor in biological systems (the acid is coupled via an amide linkage to a lysine of several multienzyme complexes, such as the pyruvate dehydrogenase complex, the alpha-ketoglutarate dehydrogenase complex, the glycine cleavage system and the branched-chain oxo acid dehydrogenase complex). Most commercially available thioctic acid supplements are a mixture of both R and S enantiomers or R-form alone. Several studies have shown that the acid has beneficial effect on diabetes complications, cancer, glaucome, liver disease, etc. The mechanisms of thioctic acid is related to its antioxidant properties, metal chelator properties, however, those mechanisms need futher confirmation.
Status:
Possibly Marketed Outside US
Source:
NCT04475276: Phase 4 Interventional Recruiting Non-Alcoholic Fatty Liver Disease
(2021)
Source URL:
First approved in 2001
Source:
Strovite OneCaplets by Exeltis USA, Inc.
Source URL:

Class (Stereo):
CHEMICAL (EPIMERIC)


Thioctic acid also known as alpha-lipoic acid is a dietary supplement, which is a common ingredient in OTC (over-the-counter) multivitamin formulas and anti-aging supplements. Thioctic acid exists in both R- and S-enantiomeric forms, however, only R-form is essential as a cofactor in biological systems (the acid is coupled via an amide linkage to a lysine of several multienzyme complexes, such as the pyruvate dehydrogenase complex, the alpha-ketoglutarate dehydrogenase complex, the glycine cleavage system and the branched-chain oxo acid dehydrogenase complex). Most commercially available thioctic acid supplements are a mixture of both R and S enantiomers or R-form alone. Several studies have shown that the acid has beneficial effect on diabetes complications, cancer, glaucome, liver disease, etc. The mechanisms of thioctic acid is related to its antioxidant properties, metal chelator properties, however, those mechanisms need futher confirmation.
Borneol, a monoterpenoid alcohol, is a component of many essential oils. Barneol occurs in nature as a single enantiomer (d- or l-, depending on the oil type) or, less frequently, as the racemate. Several studies have proved the effectiveness of borneol. In Chinese medicines borneol has been used in relieving symptoms of anxiety, fatigue and insomnia; inducing anesthesia and analgesia to alleviate abdominal pain, wounds and burns; relieving rheumatic pain, hemorrhoids, skin diseases and ulcerations of the mouth, ears, eyes or nose; to treat sore throats and skin infections, and is mainly used to treat cardiovascular and cerebrovascular diseases. Borneol has a significant therapeutic effect on neuralgia. This compound is considered a GRAS approved by the FDA as food flavor. Additionally, borneol is a fragrance ingredient. GABAA, TRPV3, TRPM8 and TRPA1 have been identified as the molecular targets of borneol.

Showing 2371 - 2380 of 2546 results