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

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Showing 821 - 830 of 13408 results

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

Class (Stereo):
CHEMICAL (ABSOLUTE)


Gosogliptin (PF-734200) is a compound developed for treatment of type II diabetes and has been approved for use in Russia. It is a selective dipeptidyl peptidase 4 (DPP-4) inhibitor, with hypoglycemic activity. The drug is safe and well tolerated at all doses tested when added to metformin (a diabetes drug), and safely and effectively lowered HbA (1c) in subjects receiving metformin. A phase 3 study to study the safety and efficacy of gosogliptin has been completed. Gosogliptin has also been studied as potential drug for the treatment of renal insufficiency.
Status:
Investigational
Source:
INN:roxolonium metilsulfate
Source URL:

Class (Stereo):
CHEMICAL (EPIMERIC)

Roxolonium, a derivative of glycyrrhetic acid, was studied as an antiulcer agent. Information about the further development of this compound is not available.
Status:
Investigational
Source:
INN:cefoselis
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
INN:tacapenem
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

CS-834 is a beta-lactam antibiotic of a carbapenem class, developed by the Japanese company Sankyo Co. Ltd. CS-834 is an ester-type prodrug of the active metabolite R-95867. The drug showed potent and well balanced antibacterial activity as well as stability against dehydropeptidase-I. The in vivo efficacy of CS-834 was evaluated in murine systemic infections caused by 16 strains of gram-positive and -negative pathogens. The efficacy of CS-834 was in many cases superior to those of cefteram pivoxil, cefpodoxime proxetil, cefdinir, and cefditoren pivoxil, especially against infections caused by S. aureus, penicillin-resistant S. pneumoniae, E. coli, Citrobacter freundii, and Proteus vulgaris. Pharmacokinetics of CS-834 was evaluated in healthy male volunteers, but no further clinical development of the drug was reported.
Status:
Investigational
Source:
NCT01139151: Phase 1 Interventional Completed Leukemia
(2010)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Thiarabine (also known as OSI-7836) is a new-generation deoxycytidine nucleoside analog with potent anticancer activity. As with other nucleoside analogs, Thiarabine is a prodrug and requires intracellular phosphorylation by deoxycytidine kinase to the active form (Thiarabine-triphosphate), which then competes with deoxycytidine for incorporation into DNA resulting in cell death. In xenograft studies using lung, colon, pancreatic, breast, and melanoma models, Thiarabine shows superior antitumor activity in most of these tumors, particularly in lung and pancreatic models, compared with gemcitabine, cisplatin, and paclitaxel. Thiarabine seems to be less schedule dependent than gemcitabine, showing antitumor activity with a variety of schedules in preclinical studies. In clinical trials, Thiarabine administration was associated with excessive fatigue, and despite changes in its schedule and duration of administration.
Status:
Investigational
Source:
INN:norboletone
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Norbolethone is a 19-nor anabolic steroid first synthesized in 1966. During the 1960s it was administered to humans in efficacy studies concerned with short stature and underweight conditions. It has never been reported by doping control laboratories prior to 2001. Norbolethone matches the description for what is described as a "designer steroid. " In fact, Norbolethone was given in clinical trials over 30 years ago and never given the green light. No supply was ever manufactured, and no test was ever developed to detect this substance, yet ironically, it was suspected of being used in the 2000 Olympics based on blood and urine assays done by the IOC. Norbolethone was used in the treatment of idiopathic underweight, prevention of indomethacin-induced intestinal ulcers.
Status:
Investigational
Source:
NCT00842335: Phase 1/Phase 2 Interventional Completed Advanced Solid Tumors
(2009)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


CGI-1842 (also known as JI-101) is an oral multi-kinase inhibitor that targets vascular endothelial growth factor receptor type 2 (VEGFR-2), platelet derived growth factor receptor β (PDGFR-β), and ephrin type-B receptor 4 that has been used in trials studying the treatment of Cancer, Colon Cancer, Neuroendocrine, Ovarian Cancer, and Advanced Solid Tumors. By targeting multiple angiogenesis signaling pathways in tumor vessel beds, CGI-1842 has the potential to inhibit multiple stages of tumor angiogenesis and thus enhance anti-tumor efficacy. In preclinical models, CGI-1842 induced concentration-dependent blocking of both EphB4- and VEGF-stimulated signaling pathways and has shown excellent antitumor activity. CGI-1842 is well tolerated in cancer patients and has shown impressive activity in Phase I clinical trials.
Status:
Investigational
Source:
INN:relomycin
Source URL:

Class (Stereo):
CHEMICAL (UNKNOWN)

Relomycin is a macrolide antibiotic that was first reported in the literature in 1963. It is a fermentation product of Streptomyces hygroscopicus and has also been observed in cultures of Streptomyces fradiae (a species of Actinobacteria).
Status:
Investigational
Source:
INN:alphamethadol
Source URL:

Class (Stereo):
CHEMICAL (MIXED)

Dimepheptanol is one of the phenylpiperidine series, an opioid receptor agonist, which is active as an opioid analgesic. It is also elaborated in a number of close analogues, derivatives or diastereoisomers with similar properties. Dimepheptanol is a synthetic narcotic analgesic that has no accepted medical use in the United States.
Status:
Investigational
Source:
INN:cloracetadol
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Cloracetodol is a para-aminophenol NSAID analgesic with anti-inflammatory and antipyretic activity.