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

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Showing 931 - 940 of 39585 results

Status:
Investigational
Source:
INN:eclazolast
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Eclazolast (REV 2871 or CHBZ) is a non-disodium cromoglycate (DSCG)-like, antiallergic drug. Eclazolast is taken up by rat mast cells and human leukocytes in a specific and saturable manner. The compound can be hydrolyzed by a granule-associated enzyme in the mast cell to an ionic metabolite (REV 3579) whose in vitro profile is identical to that of DSCG. Eclazolast is a potent inhibitor of both immunologic and non-immunologic histamine release. It inhibits exocytosis by intracellularly affecting only direct Fc(epsilon)RI linked processes and not through inhibition of Ca2+ influx channels.
Status:
Investigational
Source:
INN:omonasteine
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Omonasteine was used in sequential peptide ligation for the synthesis of the BRD7 bromodomain.
Status:
Investigational
Source:
INN:cefedrolor
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Cefedrolor is a broad-spectrum cephalexin antibiotic patented by pharmaceutical company Bristol-Myers Co.
Status:
Investigational
Source:
NCT01018550: Phase 2 Interventional Completed Asthma
(2009)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Vidupiprant, also known as AMG 853, is an orally bioavailable and potent dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors. Vidupiprant inhibits PGD2-induced down modulation of CRTH2 on CD16- granulocytes in human whole blood as well as PGD2-induced cAMP response in platelets. It inhibits PGD2-induced airway constriction in vivo. Also inhibits BRD4 (Kd = 170 nM). AMG 853 as an add-on to inhaled corticosteroid therapy demonstrated no associated risks but was not effective at improving asthma symptoms or lung function in patients with inadequately controlled moderate-to-severe asthma. AMG 853 has been discontinued due to poor efficacy.
Status:
Investigational
Source:
INN:benurestat
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Benurestat is a urease inhibitor, which as was shown in experiments on rats, could decrease in the urinary excretion of ammonia with experimental P. mirabilis genitourinary tract infection.
Status:
Investigational
Source:
USAN:Actodigin
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Actodigin is a semisynthetic cardiac glycoside compounded from digitoxigenin and one molecule of glucose. In addition, unlike the naturally occurring glycosides, the C-2 instead of the C-3 atom of the lactone ring is attached to the steroid nucleus. Actodigin is a cardiovascular agent. When injected at 30 min invervals into dogs with barbiturate-induced heart failure, actodigin caused a marked positive inotropic action of short duration. It converted arrhythmia to normal sinus rhythm. Actodigin effectively and quickly reduced the ventricular rate in patients with atrial fibrillation. Actodigin, because of its rapid onset and brief duration of action, may be useful in controlling the ventricular rate in patients with atrial fibrillation.
Status:
Investigational
Source:
INN:flucrilate [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

FLUCRYLATE, fluoroalkyl cyanoacrylate, is a surgical tissue adhesive.
Status:
Investigational
Source:
INN:carperone
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Carperone is a fluorobutyrophenone compound which in animal studies has showed calming or tranquilizing effects resembling those of haloperidol, trifluperidol, and other antipsychotic drugs
Status:
Investigational
Source:
NCT00012259: Phase 2 Interventional Completed Leukemia
(2000)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Troxacitabine is a synthetic nucleoside analogue. It is a poor substrate for nucleoside transporters and gains entry into cells by passive diffusion. Intracellular conversion to its active triphosphate form is via deoxycytidine kinase. Incorporation of this metabolite into DNA results in immediate chain termination and apoptosis induction. It is the first nucleoside analog with anticancer activity that has an unnatural stereochemical configuration. The dose-limiting adverse reactions were stomatitis and hand–foot syndrome.
Status:
Investigational
Source:
NCT04671303: Phase 2 Interventional Completed Lung Cancer
(2021)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



AST-1306, also known as Allitinib, is an orally active potent, selective, irreversible inhibitor of the HER family of receptor tyrosine kinases. AST-1306 inhibits the enzymatic activities of wild-type epidermal growth factor receptor (EGFR) and ErbB2 as well as EGFR resistant mutant in both cell-free and cell-based systems. AST1306 potently suppressed tumor growth in ErbB2-overexpressing adenocarcinoma xenograft and FVB-2/N(neu) transgenic breast cancer mouse models. Allitinib is in Phase I clinical trial for the treatment of advanced solid tumors. Serious adverse effects detected were: diarrhea, dehydration and hyperbilirubinemia.