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

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Showing 521 - 530 of 4343 results

MKC-1 is an orally available cell cycle inhibitor with downstream targets that include tubulin and the importin-β family. MKC-1 has shown broad antitumor activity in preclinical models. MKC-1 and its metabolites inhibit tubulin polymerization, blocking the formation of the mitotic spindle, which may result in cell cycle arrest at the G2/M phase and apoptosis. In addition, this agent has been shown to inhibit the activities of the oncogenic kinase Akt, the mTOR pathway, and importin-beta, a protein essential to the transport of other proteins from the cytosol into the nucleus. MKC-1 had been in phase II clinical trials for the treatment of ovarian cancer, endometrial cancer, pancreatic cancer and breast cancer. This compound was originally discovered by Roche, then licensed to EntreMed (now CASI Pharmaceuticals) the exclusive worldwide rights to develop and commercialize. However, no recent development has been reported.
Status:
Investigational
Source:
INN:terciprazine [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Terciprazine was developed as an antihypertensive agent that has never been marketed. Information about the current use of this drug is not available.
Status:
Investigational
Source:
INN:dezinamide [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Dezinamide is a potential antiepileptic drug that binds to the voltage-sensitive sodium channel. It is a metabolite of fluzinamide. It was active in preventing maximal seizures induced in mice or rats by electroshock and threshold seizures induced in mice by metrazol, bicuculline, and picrotoxin. It was predominantly active against tonic-clonic seizures. Adverse experiences included headache, ataxia, blurred vision, diplopia, dizziness, lightheadedness, and mild confusion. Dezinamide development was discontinued because of toxicity problems not observed with the metabolite.
Status:
Investigational
Source:
INN:fluprostenol
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Status:
Investigational
Source:
INN:flosatidil
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

FLOSATIDIL is an antihypertensive drug discontinued in Phase II for angina pectoris.
Status:
Investigational
Source:
INN:fluperamide [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Fluperamide was developed as an antiperistaltic agent for the treatment of diarrhea. However, information about the current use of the drug is not available.
Status:
Investigational
Source:
NCT00033384: Phase 2 Interventional Completed Breast Cancer
(2002)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



CI 1040 is an inhibitor of the mitogen-activated protein (MAP) kinase signal transduction pathway and has been shown to specifically inhibit MAP kinase kinase (MEK). CI 1040 was being developed by Parke-Davis (formerly a division of WarnerLambert, Now Pfizer) as an anticancer agent. It was the initial MEK inhibitor to undergo clinical evaluation based on promising preclinical activity. However, its development has been discontinued.
Status:
Investigational
Source:
INN:texacromil
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Texacromil is a benzopyran derivative patented by C. M. Industries S. A. as passive cutaneous anaphylaxis inhibitor
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.
Status:
Investigational
Source:
INN:mureletecan
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.