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

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Status:
First approved in 1983

Class (Stereo):
CHEMICAL (ABSOLUTE)



Etoposide (trade name Etopophos) is a semisynthetic derivative of podophyllotoxin that exhibits antitumor activity. It has been in clinical use for more than two decades and remains one of the most highly prescribed anticancer drugs in the world. The primary cytotoxic target for etoposide is topoisomerase II. This ubiquitous enzyme regulates DNA under- and over winding, and removes knots and tangles from the genome by generating transient double-stranded breaks in the double helix. Etoposide kills cells by stabilizing a covalent enzyme-cleaved DNA complex (known as the cleavage complex) that is a transient intermediate in the catalytic cycle of topoisomerase II. The accumulation of cleavage complexes in treated cells leads to the generation of permanent DNA strand breaks, which trigger recombination/repair pathways, mutagenesis, and chromosomal translocations. If these breaks overwhelm the cell, they can initiate death pathways. Thus, etoposide converts topoisomerase II from an essential enzyme to a potent cellular toxin that fragments the genome. Although the topoisomerase II-DNA cleavage complex is an important target for cancer chemotherapy, there also is evidence that topoisomerase II-mediated DNA strand breaks induced by etoposide and other agents can trigger chromosomal translocations that lead to specific types of leukemia. Etopophos (etoposide phosphate) is indicated in the management of the following neoplasms: Refractory Testicular Tumors-and for Small Cell Lung Cancer. The in vitro cytotoxicity observed for etoposide phosphate is significantly less than that seen with etoposide, which is believed due to the necessity for conversion in vivo to the active moiety, etoposide, by dephosphorylation. The mechanism of action is believed to be the same as that of etoposide.
Flavin mononucleotide, or riboflavin-5′-phosphate, is a biomolecule produced from riboflavin by the enzyme riboflavin kinase and functions as prosthetic group of various oxidoreductases including NADH dehydrogenase as well as cofactor in biological blue-light photo receptors. Riboflavin (Vitamin B 2) (as riboflavin 5-phosphate sodium) is an ingredient of the FDA approved composition Infuvite Adult, indicated as a daily multivitamin maintenance supplement for adults and children aged 11 and older receiving parenteral nutrition. Infuvite Adult is also indicated in other situations where administration by the intravenous route is required. Such situations include surgery, extensive burns, fractures and other trauma, severe infectious diseases, and comatose states, which may provoke a “stress” situation with profound alterations in the body’s metabolic demands and consequent tissue depletion of nutrients. Flavin mononucleotide is also a component of Cytoflavin, used for the treatment of consequences of cerebral infarction, for the treatment of atherosclerosis, encephalopathy, neurasthenia. Cytoflavin is marketed in Russian Federation.
Phosphoric acid, also known as orthophosphoric acid, is used in dentistry and orthodontics to clean and roughen the surfaces of teeth where dental appliances or fillings will be placed. In addition, this acid is a part of product ProcalAmine, which is indicated for peripheral administration in adults to preserve body protein and improve nitrogen balance in well-nourished, mildly catabolic patients who require short-term parenteral nutrition. In combination with dextrose (glucose) and levulose (fructose), phosphoric acid relieves nausea due to upset stomach from intestinal flu, stomach flu, and food or drink indiscretions. In addition, homeopathic product, Brain power contains also phosphoric acid and this product is used to temporarily relieve symptoms of general physical weakness and listlessness, including: fatigue; sore muscles & joints; dry skin; absence of sexual desire; occasional sleeplessness.
Status:
First marketed in 1921
Source:
Sodium Glycerophosphate U.S.P.
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Synthetic glycerophosphates have been known for many years and have been prepared in several ways. The acid may exist in two isomeric forms, alpha and beta. The L-a-acid is the naturally occurring form; the b-acid, present in hydrolyzates of lecithins from natural sources, arises from migration of the phosphoryl group from the a-carbon atom. Dehydrogenation of L-glycerol 3-phosphate produces Dihydroxyacetone phosphate and is part of the entry of glycerol (sourced from triglycerides) into the glycolytic pathway.
Status:
US Approved OTC
Source:
21 CFR 333.110(f) first aid antibiotic:ointment tetracycline hydrochloride
Source URL:
First approved in 1953

Class (Stereo):
CHEMICAL (ABSOLUTE)



Discovered as natural products from actinomycetes soil bacteria, the tetracyclines were first reported in the scientific literature in 1948. They were noted for their broad spectrum antibacterial activity and were commercialized with clinical success beginning in the late 1940s to the early 1950s. By catalytic hydrogenation of Aureomycin, using palladium metal and hydrogen, the C7 deschloro derivative was synthesized, producing a compound of higher potency, a better solubility profile, and favorable pharmacological activity; it was subsequently named tetracycline. Tetracyclines are primarily bacteriostatic and exert their antimicrobial effect by the inhibition of protein synthesis by binding to the 30S ribosomal subunit. Tetracycline is active against a broad range of gram-negative and gram-positive organisms. Tetracycline is indicated in the treatment of infections caused by susceptible strains. To reduce the development of drug-resistant bacteria and maintain the effectiveness of tetracycline hydrochloride and other antibacterial drugs, tetracycline hydrochloride should be used only to treat or prevent infections that are proven or strongly suspected to be caused by bacteria.
Status:
US Approved OTC
Source:
21 CFR 331.11(i)(1) antacid:aluminum-containing aluminum phosphate
Source URL:
First approved in 1942
Source:
Phosphaljel by Wyeth
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Kasal (Sodium Aluminum Phosphate, basic, non-leavening) is a white odorless powder comprised of an autogenous mixture of alkaline sodium aluminum phosphate and dibasic sodium phosphate. Kasal is used primarily as an emulsifier in the production of processed cheese.
Status:
Investigational
Source:
INN:amiselimod [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Amiselimod (MT-1303) is a selective sphingosine 1-phosphate 1 (S1P1 ) receptor modulator which is currently being developed for the treatment of various autoimmune diseases. Unlike some other S1P receptor modulators, amiselimod seemed to show a favourable cardiac safety profile in preclinical, phase I and II studies. Amiselimod may be potentially useful for treatment of multiple sclerosis; inflammatory diseases; autoimmune diseases; psoriasis and inflammatory bowel diseases. Amiselimod is currently being developed by Mitsubishi Tanabe Pharma Corporation.
Status:
Investigational
Source:
JAN:TOLVAPTAN SODIUM PHOSPHATE [JAN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Status:
Investigational
Source:
NCT01060475: Phase 1 Interventional Completed Healthy
(2010)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
NCT01014208: Phase 3 Interventional Completed Lymphoma, Large-Cell, Diffuse
(2010)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)