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

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Showing 21 - 30 of 1990 results

Status:
Investigational
Source:
INN:dazucorilant [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
INN:zavacorilant [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
INN:zurletrectinib [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
INN:timefurone [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Timefurone is a benzopyranone derivative patented by pharmaceutical company Upjohn Co. for the treatment of atherosclerosis. Timefurone mediates the hypolipidemic effect via the reduction of the intracellular synthesis of cholesterol. In preclinical studies, Timefurone significantly lowered low-density lipoprotein cholesterol, high-density lipoprotein cholesterol, and total cholesterol in cholesterol-fed male rats and monkeys. Timefurone caused small but significant changes in several clinical chemistry parameters including creatinine, total bilirubin, albumin, glucose, serum glutamic-oxalacetic transaminase, and serum glutamic-pyruvic transaminase in cynomolgus monkeys
Status:
Investigational
Source:
INN:lurtotecan
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Lurtotecan is a semisynthetic analog of camptothecin with antineoplastic activity. It is an inhibitor of DNA topoisomerase I. Liposomal formulation of lurtotecan was being studied in the treatment of cancer. Lurtotecan development has been discontinued.
Status:
Investigational
Source:
INN:nafazatrom [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Nafazatrom [BAY G 6575] is a leukotriene synthesis inhibitor that was being developed by Bayer in Germany. It is a pyrazolinone derivative with potential antimetastatic activities. Nafazatrom, originally developed as an antithrombotic agent, inhibits the key prostaglandin catabolic enzyme, 15-hydroxyprostaglandin dehydrogenase, which prolongs the biological half-life of prostacyclin (prostaglandin I2; PGI2) and prevents intravascular coagulation. Nafazatrom, in the micromolar range, inhibits the metabolism of PGs (prostaglandins) by 15-OH PGDH in a dose-dependent manner. The IC50 for inhibition of 15-OH PGDH was estimated to be 18.5 uM when [3H]PGF2 alpha was used as substrate. This agent also serves as a reducing cofactor with the hydroperoxidase moiety of cyclooxygenase and accelerates the conversion of arachidonic acid into precursors of PGI2. An elevated level of PGI2 prevents aggregation of platelets; subsequently it decreases the formation of tumor cell-platelet aggregates as well as their sequestration in blood vessels, which is an important initiating step in the development of metastasis. Nafazatrom may have had potential as an antithrombotic, anti-ischaemic and antiasthmatic agent. However, the development of nafazatrom was discontinued.
Status:
Investigational
Source:
INN:droxacin
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Droxacin is quinolone antibiotic. It is topoisomerase inhibitor.
SITOGLUSIDE (Daucosterol) inhibits cancer cell proliferation by inducing autophagy through reactive oxygen species-dependent manner. It also perturbs cell cycle and induces apoptotic cell death in A549 cells. Daucosterol has being shown to promote the proliferation of neural stem cells. Daucosterol also protects neurons against oxygen-glucose deprivation/reperfusion-mediated injury by activating IGF1 signaling pathway. Daucosterol could be potentially developed as a medicine for ischemic stroke treatment.
Status:
Investigational
Source:
INN:adicillin
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Adicillin (Penicillin N) is a penicillin derivative produced by Cephalosporium acremonium. Adicillin is dextrorotatory. Inactivated by penicillinase as is penicillin G, but differs from the common penicillin by its antibacterial activity and hydrophilic character. Active against Sarcina lutea, Proteus vulgaris, Salmonella typhimurium, Diplococcus pneumoniae. Shows practically no activity against B. subtilis and Staph. aureus. The toxicity is somewhat less than that of penicillin G, although penicillin N is excreted more slowly.
Status:
Investigational
Source:
NCT03911388: Phase 1 Interventional Recruiting Neoplasms, Brain
(2019)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)