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

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Showing 41 - 50 of 234 results

Status:
US Previously Marketed
Source:
Syntetrin by Bristol
(1959)
Source URL:
First approved in 1959
Source:
Syntetrin by Bristol
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Rolitetracycline, launched in the late 1950s, was the first of the semi -synthetic tetracyclines. Rolitetracycline is formed by a Mannich condensation of formaldehyde and pyrrolidine with tetracycline. Rolitetracycline is a pro -drug of tetracycline, in which the pyrrolidine moiety improves bioavailability compared with tetracycline. Rolitetracycline has broad spectrum Gram positive activity in vivo, but pH instability limits use to parenteral administration. Rolitetracycline passively diffuses through porin channels in the bacterial membrane and reversibly binds to the 30S ribosomal subunit, preventing binding of tRNA to the mRNA-ribosome complex, and thus interfering with protein synthesis.
Status:
US Previously Marketed
Source:
TRIPLE SULFA by ALPHARMA US PHARMS
(1976)
Source URL:
First approved in 1943
Source:
Sulfamerazine by Lederle
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Sulfamerazine is a sulfonamide antibiotic, which acts by inhibiting folic acid synthesis in bacterias. The primary target of sulfamerazine is believed to be dihydropteroate synthetase. Sulfamerazine (in comination with Sulfadiazine and Sulfamethazine) was used in the US under different names, including the earliest brand of Neotrizine. Nowdays, the drugs containing sulfamerazine are no longer available for use in humans in the US, however, they may be prescribed for veterinary purposes.
Status:
US Previously Marketed
First marketed in 1921
Source:
gentian violet
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Gentian violet ((GV) hexamethyl pararosaniline, also known as crystal violet, methyl violet) is a triphenylmethane dye with anti-bacterial, anti-fungal, anti-helminithic, anti-trypanosomal, anti-angiogenic and anti-tumor properties. GV has a lengthy history and has been used successfully as monotherapy and an adjunct to treatment in a variety of diseases. Gentian violet interacts with negatively charged components of bacterial cells including the lipopolysaccharide (on the cell wall), the peptidoglycan and DNA. A similar cell penetration and DNA binding process is thought to take place for fungal cells as well. Because Gentian violet is a mutagen and mitotic poison, cell growth is consequently inhibited. A photodynamic action of gentian violet, apparently mediated by a free-radical mechanism, has recently been described in bacteria and in the protozoan T. cruzi. Evidence also suggests that gentian violet dissipates the bacterial (and mitochondrial) membrane potential by inducing permeability. This is followed by respiratory inhibition. This anti-mitochondrial activity might explain gentian violet's efficacy towards both bacteria and yeast with relatively mild effects on mammalian cells.
Status:
US Previously Marketed
Source:
21 CFR 310.545(a)(27)(iii) antimicrobial:antiseptic hand wash tribromsalan
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Tribromsalan (trade name Temasept IV) is a member of brominated salicylanilides chemical family. Was initially registered in 1964 manufactured by Hexcel Corporation, Sherwin Williams Chemicals. It is a pesticide type with antimicrobial and preservative features found its application in hard surfaces, laundry, textiles, and manufactured products. Types of tribromsalan formulations include solid, solutions, and sprays and its usual carrier is soap. Limited exposure is possible based on the registered uses of these products as disinfectants, laundry additives, textile preservatives, and manufactured products and do not include direct application to a food or feed crop. In 1974 FDA directed the removal of tribromsalan drug products from the market because it was found to make skin extrasensitive to light. For the same reason it was forbidden in Europe since the 1970s. Since 1982 the OTC topical antimicrobial drug products rulemaking was reopened and included tribromsalan in a list of antimicrobial OTC Drug Products. At present tribromsalan is considered an antiseptic active ingredient eligible for the OTC use as a consumer antiseptic hand and body wash drug product. It was reported that tribromsalan, inhibits NF-kappaB signaling via inhibition of IkappaBalpha phosphorylation with IC50 of 7.9 uM. This finding provides new information on activities and mechanisms of action that may suggest mechanisms of potential novel applications in cancer treatment of such drugs as tribromsalan.
Status:
Possibly Marketed Outside US
Source:
Canada:BORNYL ACETATE
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Isobronyl acetate (an isomer of bornyl acetate) is a component of many essential oils, which was observed to be inhibitory to microorganisms. It was also shown to have sedative effect on mice after inhalation. Isobronyl acetate is mainly used in cosmetics as a flavor and fragrance agent.
Status:
Possibly Marketed Outside US
Source:
Japan:Acrinol
Source URL:
First approved in 2015

Class (Stereo):
CHEMICAL (ACHIRAL)


Ethacridine (Rivanol) is an acridine derivative indicated for the treatment of bacterial infections. In many countries the drug was in clinical practice for the second trimester termination of pregnancy.
Status:
Possibly Marketed Outside US
Source:
Canada:SALINOMYCIN SODIUM
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Salinomycin Sodium is active against certain Gram-positive bacteria, while Gram-negative species are resistant. The use of Salinomycin Sodium as a feed additive at the proposed concentration is unlikely to increase shedding of Salmonella, Escherichia coli, and Campylobacter or to induce resistance and cross-resistance to antimicrobials important in human and animal therapy. Salinomycin Sodium is safe for chickens for fattening at a concentration of 70 mg/kg complete feed with a margin of safety of 1.7. For chickens reared for laying, 50 mg Salinomycin Sodium /kg complete feed is considered safe for a feeding period of the first 12 weeks of life; a margin of safety cannot be given. The simultaneous use of Salinomycin Sodium and certain antibiotic drugs (e.g. tiamulin) is contraindicated. Salinomycin Sodium is absorbed to a certain extent in the chicken and extensively metabolized. Unchanged Salinomycin Sodium represents a very small fraction of the metabolites in tissue and excreta. Many metabolites, predominantly mono- and multi-hydroxylated, have been identified in tissues and excreta. The metabolites in excreta showed a higher degree of hydroxylation than in the liver. Salinomycin -related metabolites have a reduced ionophoric activity when compared with Salinomycin. Salinomycin is considered the MR; ratios of MR to total residue are available for all relevant tissues for 1 and 6 h withdrawal. No residues eggs are expected provided that the proposed maximum dose and duration of administration are respected.
Ubiquinone Q2 (CoQ(2)) is a member of the chemical class known as Polyprenylbenzoquinones. These are compounds containing a polyisoprene chain attached to a quinone at the second ring position. Ubiquione-2 has just 2 isoprene units. Normally in humans it has 10. Ubiquinone-2 is an intermediate in the synthesis of Ubiquionone 10. Ubiquionone is involved in cellular respiration. It is fat-soluble and is therefore mobile in cellular membranes; it plays a unique role in the electron transport chain (ETC). In the inner bacterial membrane, electrons from NADH and succinate pass through the ETC to the oxygen, which is then reduced to water. The transfer of electrons through ETC results in the pumping of H+ across the membrane creating a proton gradient across the membrane, which is used by ATP synthase (located on the membrane) to generate ATP. The first ubiquinone was isolated in 1957. Since that time, ubiquinones have been extensively studied in Japan, Russia, and Europe with research in the US beginning more recently. Popular press accounts claim that roughly 12 million Japanese use ubiquinones as the medication of choice for management of cardiovascular diseases, with more than 250 commercially available preparations. Ubiquinone is touted as an effective treatment of congestive heart failure (CHF), heart rhythm irregularities, high blood pressure, and in reducing injury to the heart muscle caused by lack of oxygen. Other claims include increasing exercise tolerance, stimulating the immune system, and counteracting the aging process. Ubiquinone has not been approved for therapeutic use in the US, but it is available as a food supplement. Ubiquinone may have applications in heart disease, especially CHF, although there is a lack of consensus. Studies in neurological disorders are less promising. Limited clinical trials have been conducted to support its widespread use for other conditions.
1,2-Dipalmitoyl-sn-glycero-3-phosphorylglycerol sodium salt (DPPG) is phosphorylglycerol acylated with palmitic acid, that can be used for the preparation of liposomes with negatively charged hydrophilic head groups.
Glabridin is an isoflavane found in the root extract of licorice (Glycyrrhiza glabra). Glabridin is considered to be a phytoestrogen and has been associated with numerous biological properties ranging from antioxidant, anti-inflammatory, neuroprotective, anti-atherogenic effects, to the regulation of energy metabolism, but also including anti-tumorigenic, anti-nephritic, antibacterial and skin-whitening activities. A glabridin-enriched extract is widely used in a cosmetic formulation as anti-inflammatory, antioxidant and skin whitening agent. Anti-inflammatory action of glabridin is linked to downregulation of NF-κB, AP-1 and MAPKS signaling. Glabridin-induced attenuation of atherosclerosis is related to a reduction in macrophages-associated oxidation of low-density lipoprotein.