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

Dexamethasone acetate (NEOFORDEX®) is the acetate salt form of dexamethasone, which is a synthetic glucocorticoid; it combines high anti-inflammatory effects with low mineralocorticoid activity. At high doses (e.g. 40 mg), it reduces the immune response. Dexamethasone acetate (NEOFORDEX®) is indicated in adults for the treatment of symptomatic multiple myeloma in combination with other medicinal products. Dexamethasone has been shown to induce multiple myeloma cell death (apoptosis) via a down-regulation of nuclear factor-κB activity and an activation of caspase-9 through second mitochondria-derived activator of caspase (Smac; an apoptosis promoting factor) release. Prolonged exposure was required to achieve maximum levels of apoptotic markers along with increased caspase-3 activation and DNA fragmentation. Dexamethasone also down-regulated anti apoptotic genes and increased IκB-alpha protein levels. Dexamethasone apoptotic activity is enhanced by the combination with thalidomide or its analogues and with proteasome inhibitor (e.g. bortezomib).
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