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

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Showing 1961 - 1970 of 42705 results

Status:
Investigational
Source:
INN:idrapril
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Idrapril is an inhibitor of the angiotensin-converting enzyme the last is responsible for recurrent myocardial infarction in patients with left ventricular dysfunction. Idrapril participated in phase II clinical trials in essential hypertensive patients, where was shown that the drug was well tolerated. In addition, it was involved in preclinical studies as a potential drug to treat heart failure and postmyocardial infarction. However, the development of the drug was discontinued.
Status:
Investigational
Source:
J Zoo Wildl Med. Sep 2016;47(3):834-843.: Not Applicable Veterinary clinical trial Completed N/A
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Etorphine was the first potent opiate agonist employed primarily for use in non-domestic and wild species. Etorphine was 500 times as potent as morphine, with a very rapid onset and short duration of action. In morphine-dependent subjects, etorphine suppressed abstinence but for a shorter period than morphine. Etorphine is a full opiate agonist and binds to multiple opiate sites in the central nervous system. It is believed to produce its clinical effects through binding the µ-, δ-, and κ- opiate sites. It has a potent effect on depressing the respiratory centers of the CNS thus resulting in apnea being commonly seen in immobilized animals. Etorphine revolutionized the ability of biologists and veterinarians to safely capture and restrain many species that previously could not be handled. Etorphine is not currently commercially available due to lack of production by the manufacturer.
Status:
Investigational
Source:
INN:merafloxacin
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Merafloxacin (CI 934) is a quinolone antibacterial. It is an inhibitor of Type II DNA topoisomerase. It demonstrated excellent activity against gram-positive organisms, including Corynebacterium sp. In addition, although the activity of merafloxacin against gram-negative bacilli was less than that reported for similar agents, it was comparable to that of aminoglycosidic aminocyclitol antibiotics. Merafloxacin development has been discontinued.
Status:
Investigational
Source:
INN:adarotene [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Adarotene (ST1926) is a new pro-apoptotic and cytodifferentiating antitumour drug, belongs to the so-called class of atypical retinoids. Adarotene is active on its own or in combination with other chemotherapeutics for the treatment of a vast number of experimental tumors. It was found in preclinical investigations the potential therapeutic use it in chronic myeloid leukemia (CML), against Rhabdomyosarcoma and for treatment of Adult T-cell leukemia/lymphoma (ATL). ST1926 induced an early DNA damage response, which led to increase in apoptosis, in addition to S-phase cell cycle arrest and a reduction in protein levels of the cell cycle kinase CDK1. The presence of the phenolic hydroxyl group on adarotene structure allows a rapid O-glucuronidation as a major mechanism of elimination of the drug, favoring a fast excretion of its glucuronide metabolite in the urines.
Status:
Investigational
Source:
INN:solimastat [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

British Biotech was developing solimastat [BB 3644], an inhibitor of tumour necrosis factor and matrix metalloproteinase, as a potential treatment for colorectal cancer, inflammatory bowel diseases and rheumatoid arthritis. BB-3644 is an oral, broad-spectrum matrix metalloproteinase inhibitor (MMPI) structurally related to marimastat and BB-94. It is also >10-fold more active than marimastat in inhibiting the processing of cell-bound TNF-alpha. Solimastat development has been discontinued due to significant musculoskeletal toxicity.
Status:
Investigational
Source:
INN:niraxostat [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Y-700 (Niraxostat or 1-[3-Cyano-4-(2,2-dimethylpropoxy)phenyl]-1H-pyrazole-4-carboxylic acid) is an inhibitor of xanthine oxidoreductase. Y-700 demonstrated high oral bioavailability being predominantly eliminated via the liver. It potently reduces serum uric acid levels. Y-700 was in clinical trials for the treatment of gout.
Status:
Investigational
Source:
Photodiagnosis Photodyn Ther. Sep 2018;23:165-170.: Not Applicable Human clinical trial Completed Soft Tissue Neoplasms
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Acridine Orange is a cell-permeant nucleic acid binding dye that emits green fluorescence when bound to double-stranded DNA and red fluorescence when bound to single-stranded DNA or RNA. This unique characteristic makes acridine orange useful for cell-cycle studies. Acridine orange has been widely accepted and used in many different areas, such as epifluorescence microscopy, the assessment of sperm chromatin quality. Acridine orange stain is particularly useful in the rapid screening of normally sterile specimens, and its recommended for the use of fluorescent microscopic detection of microorganisms in direct smears prepared from clinical and nonclinical materials. The staining has to be performed at an acid pH in order to obtain this differential staining effect with bacteria showing orange stain and tissue components yellow to green. Acridine orange can be used in conjunction with ethidium bromide to differentiate between viable, apoptotic and necrotic cells. Additionally, acridine orange may be used on blood samples to cause bacterial DNA to fluoresce, aiding in the clinical diagnosis of bacterial infection once serum and debris have been filtered. Acridine orange can be used in photodynamic Cancer Therapy.
Status:
Investigational
Source:
INN:alamifovir
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Alamifovir is a novel antiviral agent which was under development with Mitsubishi Pharma Corporation in Japan as a potential treatment for hepatitis B (HBV). Alamifovir and its hydrolyzed derivatives have shown preclinical efficacy activity against wild-type and lamivudine-resistant hepatitis B virus. The effective concentration of alamifovir required to reduce replication by 50% (EC50) for the wild-type was 0.027 uM, which is approximately 20 times less than lamivudine, and the EC50 for the lamivudine-resistant mutants was 2.6 to 3.3 uM. The mechanism of action of alamifovir appears to be via the inhibition of the protein priming reaction and the packaging reaction, thereby decreasing HBV replication. Alamifovir`s development has been discontinued.
Status:
Investigational
Source:
USAN:Actinoquinol Sodium
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Actinoquinol is sunscreen agent that absorbs Ultraviolet B light. Actinoquinol in combination with hyaluronic acid drops might be helpful for the human eye in the defense against photooxidative and other oxidative processes.
Status:
Investigational
Source:
NCT00671580: Phase 2 Interventional Completed Skin Infections
(2008)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Razupenem (also known as PZ-601 or PTZ601) is an anti-MRSA carbapenem antibiotic. It is active against Enterobacteriaceae and Gram-positive bacteria including methicillin-resistant staphylococci and enterococci, and was investigated as potential alternative drug (replacing common antibiotics) against resistant bacteria. In healthy male volunteers, razupenem did not cause serious adverse events. The potential effect and safety of razupenem has been evaluated in a phase II clinical trial studying skin infection.

Showing 1961 - 1970 of 42705 results