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

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Showing 1981 - 1990 of 24423 results

Lomeguatrib is a O6-methylguanine-DNA-methyl-transferase inhibitor which was developed by AstraZeneca for the treatment of cancer. It was tested in phase I and II of clinical trials for the treatment of colorectal cancer, melanoma and other solid tumors.
Vanoxerine, also known as GBR-12909, is a piperazine derivative exhibiting potent selective inhibition of sodium-dependent dopamine reuptake transporters. Vanoxerine has been in clinical trials for Parkinsonism, depression and cocaine addiction but lacked efficacy. Vanoxerine has also been observed as a potent blocker of the following channels: cardiac hERG/IKr potassium channel, Calcium channel, voltage-dependent, L type, alpha 1C subunit (also known as Cav1.2) and voltage-gated sodium channel Nav 1.5. Vanoxerine was studied as a potential treatment for atrial fibrillation. However, phase III clinical trials for this condition were terminated because of cardiac safety concerns. Research also indicates that vanoxerine may have additional mechanisms of action including antagonist action at nicotinic acetylcholine receptors (nAChRs).
Status:
Investigational
Source:
INN:mimbane [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Mimbane was developed by Parke-Davis as an analgesic. Information about the current use of the drug is not available.
Status:
Investigational
Source:
NCT01943162: Not Applicable Interventional Completed PTSD With a History of Mild to Moderate TBI
(2012)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Mureletecan is a water-soluble prodrug, consisting of camptothecin covalently linked to polymeric backbone methacryloylglycynamide, with potential antineoplastic activity. After entering tumor cells, the active moiety camptothecin is slowly released from mureletecan via hydrolysis of the ester linkage. Camptothecin, the active moiety, is an alkaloid isolatable from the Chinese tree Camptotheca acuminata. Camptothecin itself suffers from poor solubility, which is why it is often investigated with a solubilizing conjugate; such as in Mureletecan. Camptothecin binds to and stabilizes the topoisomerase I-DNA covalent complex producing potentially lethal double-stranded DNA breaks when encountered by DNA replication machinery. Camptothecin has also been shown to inhibit HIF1a. Camptothecin has been investigated with a number of solubilizing conjugates as a potential treatment in various forms of cancer.
Status:
Investigational
Source:
NCT00143091: Phase 2 Interventional Terminated Depressive Disorder, Major
(2005)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
NCT00987753: Phase 1/Phase 2 Interventional Completed Hormone Refractory Prostate Cancer
(1999)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT00090025: Phase 3 Interventional Terminated Biliary Tract Cancer
(2004)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Targets:


Rebeccamycin analog (RA, Becatecarin/ BMS 181176, rebeccamycin derivative, NSC 655649) is an antitumor antibiotic with inhibitory activity against both topoisomerase I and II, and DNA-intercalating properties. The mechanism of action of becatecarin is not exactly known, but it is thought that by inhibiting (blocking) the function of topoisomerase enzymes, it will destroy cancer cells and slow down the growth of the tumour. On 25 July 2006, orphan designation (EU/3/06/388) was granted by the European Commission to Helsinn Birex Pharmaceuticals Ltd, Ireland, for becatecarin for the treatment of cancers of the biliary tree.
Status:
Investigational
Source:
INN:lintitript [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Lintitript (SR 27897) is a selective cholecystokinin type A (CCK-A) receptor antagonist, which was initially developed by Sanofi for appetite disorders. It is known, that CCK modulates feeding and dopamine-induced behavior in the central and peripheral nervous system. Lintitript presumably alters feeding habits, however, the exact mechanism of action is not known. Lintitript was investigated in animals with anorexia nervosa, in addition, drug was in clinical trial for the patients with advanced pancreatic cancer, but these studies were discontinued.
Status:
Investigational
Source:
INN:sulfaclorazole
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Sulfaclorazole is a benzenesulfonamide derivative patented by Farbwerke Hoechst A.-G. as an antibacterial agent that active against Streptococcus pyogenes.
Status:
Investigational
Source:
INN:sulfiram [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Sulfiram (also known as monosulfiram) is a sulfide derivative patented by L. Givaudan & Cie. S. A. as effective anti-parasitic medicine used for the treatment and prevention of scabies and other skin related problems like itching, skin irritation, and inflammation. Sulfiram is a very weak inhibitor of aldehyde dehydrogenase. Sulfiram is usually sold as a solution or medicated soap, sometimes in combination with benzyl benzoate. Sulfiram is now rarely used, but, as of 2015, is still available in Brazil, India, and South Africa.

Showing 1981 - 1990 of 24423 results