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

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Showing 1 - 10 of 11 results

Betamethasone and its derivatives, betamethasone sodium phosphate and betamethasone acetate, are synthetic glucocorticoids. Used for its antiinflammatory or immunosuppressive properties, betamethasone is combined with a mineralocorticoid to manage adrenal insufficiency and is used in the form of betamethasone benzoate, betamethasone dipropionate, or betamethasone valerate for the treatment of inflammation due to corticosteroid-responsive dermatoses. Betamethasone and clotrimazole are used together to treat cutaneous tinea infections. Betamethasone is a glucocorticoid receptor agonist. This leads to changes in genetic expression once this complex binds to the GRE. The antiinflammatory actions of corticosteroids are thought to involve lipocortins, phospholipase A2 inhibitory proteins which, through inhibition arachidonic acid, control the biosynthesis of prostaglandins and leukotrienes. The immune system is suppressed by corticosteroids due to a decrease in the function of the lymphatic system, a reduction in immunoglobulin and complement concentrations, the precipitation of lymphocytopenia, and interference with antigen-antibody binding. Betamethasone binds to plasma transcortin, and it becomes active when it is not bound to transcortin.Betamethasone is used for: treating certain conditions associated with decreased adrenal gland function. It is used to treat severe inflammation caused by certain conditions, including severe asthma, severe allergies, rheumatoid arthritis, ulcerative colitis, certain blood disorders, lupus, multiple sclerosis, and certain eye and skin conditions.
Status:
Investigational
Source:
NCT01009931: Phase 2 Interventional Terminated Leukemia
(2011)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Phorbol 12-myristate 13-acetate (PMA) also commonly known as 12-O-Tetradecanoylphorbol-13-acetate (TPA) is a phorbol ester that is commonly used to activate phospholipid-dependent protein kinase (protein kinase C). PMA/ TPA possesses potential antineoplastic effects and was studied in phase II clinical trials together with dexamethasone in patients with relapsed or refractory acute myeloid leukemia. In addition, PMA/ TPA participated in phase I trial for treating patients with hematologic cancer or bone marrow disorder that has not responded to previous treatment. Nevertheless, both clinical trials were terminated. Besides, PMA/ TPA was studied in patients with solid tumors, which had depressed white blood cell and neutrophil counts because of prior treatment with cytotoxic cancer chemotherapeutic drugs. It was shown, that the drug increased the low white blood cell and neutrophil counts toward the normal range.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)

Conditions:

β-Estradiol 17-acetate is a natural metabolite of estradiol. Hydrolytic enzymes in human cadaver, hairless dog, rat and hairless mouse skin can metabolize β-Estradiol 17-acetate to β-Estradiol. β-Estradiol 17-acetate transported across the human and hairless dog skin can be effectively metabolized before entering the capillary.
Retonol, also known as Vitamin A1, is a vitamin found in food and used as a dietary supplement. It is used to treat and prevent vitamin A deficiency. It is also used to prevent further issues in those who have measles. Retinol is used as a metabolic precursor of retinoic acid to treat skin-related conditions, such as cellulite, skin aging, photodamage.
Status:
First marketed in 1921
Source:
Sodium Chloride U.S.P.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Hydroxocobalamin (also hydroxycobalamin, OHCbl) is a natural form, or vitamer, of vitamin B12. It is a member of the cobalamin family of compounds. Hydroxocobalamin, the active ingredient in Cyanokit, is cobinamide dihydroxide dihydrogen phosphate (ester), mono (inner salt), 3’-ester with 5,6-dimethyl-1-α-D-ribofuranosyl-1H-benzimidazole. The drug substance is the hydroxylated active form of vitamin B12 and is a large molecule in which a trivalent cobalt ion is coordinated in four positions by a tetrapyrol (or corrin) ring. It is a hygroscopic, odorless, dark red, crystalline powder that is freely soluble in water and ethanol, and practically insoluble in acetone and diethyl ether. Cyanokit contains hydroxocobalamin, an antidote indicated for the treatment of known or suspected cyanide poisoning. Cyanide is an extremely toxic poison. In the absence of rapid and adequate treatment, exposure to a high dose of cyanide can result in death within minutes due to the inhibition of cytochrome oxidase resulting in arrest of cellular respiration. Specifically, cyanide binds rapidly with cytochrome a3, a component of the cytochrome c oxidase complex in mitochondria. Inhibition of cytochrome a3 prevents the cell from using oxygen and forces anaerobic metabolism, resulting in lactate production, cellular hypoxia and metabolic acidosis. In massive acute cyanide poisoning, the mechanism of toxicity may involve other enzyme systems as well. Signs and symptoms of acute systemic cyanide poisoning may develop rapidly within minutes, depending on the route and extent of cyanide exposure. The action of Cyanokit is based on its ability to bind cyanide ions. Each hydroxocobalamin molecule can bind one cyanide ion by substituting it for the hydroxo ligand linked to the trivalent cobalt ion, to form cyanocobalamin, which is then excreted in the urine.
Status:
Investigational
Source:
NCT02637284: Phase 1 Interventional Unknown status Healthy Volunteers
(2015)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Body protective compound – 15 also known as bepecin, BPC 157 or PL 14736, a small, chemically synthesized pentadecapeptide which has been shown to be safe in clinical trials for inflammatory bowel disease and may be able to cure intestinal anastomosis dehiscence. BPC 157 also was involved in phase I development in Ulcerative colitis, however, no reports of development identified. Recently published article has described that BPC 157 had huge potential as a therapy to conservatively treat or aid recovery in hypovascular and hypocellular soft tissues such as tendon and ligaments. Although is still a need to understand the precise healing mechanisms for this therapy to achieve clinical realization.
Status:
US Previously Marketed
Source:
VI SYNERAL DL-ALPHA TOCOPHERYL ACETATE by FISONS
(1961)
Source URL:
First marketed in 1921
Source:
DL-alpha tocopheryl acetate
Source URL:

Class (Stereo):
CHEMICAL (MIXED)



dl-α-tocopheryl phosphate has a growth acceleration effect on domestic fowl. Also was confirmed, that in all investigated animals dl-α-tocopheryl phosphate has an ability to being converted into vitamin E.

Showing 1 - 10 of 11 results