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

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Showing 161 - 170 of 1140 results

Status:
First marketed in 1921
Source:
Colchicine U.S.P.
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Targets:


Colchicine is an alkaloid obtained from the plant colchicum autumnale (also known as "meadow saffron"). Colchicine is an alternative medication for those unable to tolerate NSAIDs in gout. Mechanism of action of colchicine is inhibition of microtubule polymerization by binding to tubulin. Availability of tubulin is essential to mitosis, so colchicine effectively unctions as a "mitotic poison" or spindle poison.
Status:
US Approved OTC
Source:
21 CFR 333.210(a) antifungal clioquinol
Source URL:
First approved in 1961

Class (Stereo):
CHEMICAL (ACHIRAL)


Clioquinol is a broad-spectrum antibacterial with antifungal properties, bacteriostatic. It is used as an antifungal and antiprotozoal topical drug OTC product for treatment of human infections. Previousely was used for wide number of intestinal disorders including lambliasis, shigellosis, balantidiral dysentery and some forms of diarrheas. The physiologic effect of clioquinol is by increased histamine release and cell-mediated immunity. It is a member of a family hydroxyquinolines which inhibit certain enzymes related to DNA replication. It is a copper, iron and zink chelating agent. It is an organic molecule with a quinolinic acid as its apparent core which itself is a neurotransmitter. In large doses it possesses neurotoxicity and may induce neurological disease such as subacute myelo-optic neuropathy by creating copper deficiency that leads to zink excess. SMON (Sub-Acute-Myelo-Optical-Neuropathy) - a polio-like disease began as an epidemic in 1959 in Japan was believed to be a Clioquinol caused. Clioquinol is a standardized chemical allergen. It has been resurrected as a potential treatment for Alzheimer's disease since it perturbs metallo-chemistry of amyloid and clioquinol treatment has been shown to be beneficial in a mouse model of Alzheimer's disease.
Status:
Investigational
Source:
Cancer Chemother Rep. 1975;59(6):1117-21.: Phase 2 Human clinical trial Completed Neoplasms
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
NCT02649790: Phase 1/Phase 2 Interventional Completed Relapsed/Refractory Multiple Myeloma (RRMM)
(2016)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Targets:

Eltanexor (KPT-8602) is an investigational second-generation Selective Inhibitor of Nuclear Export (SINE) compound that is designed to selectively block the nuclear export protein XPO1. Most of the key tumor suppressor proteins (TSPs), are cargos of XPO1 and inhibition of XPO1 by eltanexor is believed to sequester TSPs in the nucleus where they can carry out their normal functions. Karyopharm Therapeutics is developing eltanexor for the treatment of relapsed/refractory cancers.
Status:
Investigational
Source:
NCT00028782: Not Applicable Interventional Terminated Advanced Malignant Mesothelioma
(2001)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Etanidazole (also known as Radinyl) is a 2-nitroimidazole with radiosensitizing properties. Etanidazole exerts its therapeutic action by depleting glutathione and inhibiting glutathione S-transferase, thus enhancing the anticancer effects of radiation therapy. Etanidazole was tested in Phase III clinical trials in patients with advanced head and neck cancer, however, its development was stopped. A fluorinated etanidazole (EF5) may also be useful as an imaging agent for identification of hypoxic, drug-resistant regions of primary tumors and metastases.
Status:
Investigational
Source:
NCT03939689: Phase 2 Interventional Active, not recruiting Metastatic Prostate Cancer
(2019)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT04238715: Phase 2 Interventional Active, not recruiting Cholangiocarcinoma
(2020)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



E-7090 is a novel selective inhibitor of fibroblast growth factor receptors, that displays potent anti-tumor activity. It is a promising candidate as a therapeutic agent for the treatment of tumors harboring FGFR genetic abnormalities. E-7090 is an orally available and selective inhibitor of the tyrosine kinase activities of FGFR1, -2, and -3. In kinetic analyses E-7090 associated more rapidly with FGFR1 than did the type II FGFR1 inhibitor ponatinib, and E-7090 dissociated more slowly from FGFR1, with a relatively longer residence time, than did the type I FGFR1 inhibitor AZD4547, suggesting that its kinetics are more similar to the type V inhibitors, such as lenvatinib. E-7090 showed selective antiproliferative activity against cancer cell lines harboring FGFR genetic abnormalities and decreased tumor size in a mouse xenograft model using cell lines with dysregulated FGFR. Furthermore, E-7090 administration significantly prolonged the survival of mice with metastasized tumors in the lung. It is being investigated in a Phase I clinical trial for treatment of patients with solid tumors.
Status:
Investigational
Source:
INN:meturedepa [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Meturedepa (also known as AB-132), an alkylating agent that was developed as an antineoplastic drug. Meturedepa was studied to treat lymphomas and leukemias. The drug also participated in the Eastern clinical drug evaluation program for 233 patients with advanced cancer. Information about the current use of this compound is not available.
Status:
Investigational
Source:
NCT00113893: Phase 2 Interventional Completed Bone Marrow Diseases
(2005)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Talmapimod is a p38 MAPK kinase inhibitor that inhibits p38 alpha with IC50 value of 9 nM which is 10-times lower then IC50 for p38 beta. Talmapimod was under clinical development for the treatment of Myelodysplastic Syndromes, Multiple Myeloma and Rheumatoid Arthritis (phase II), however, it seems to be discontinued as no longer presents in Janssen's pipeline.
Status:
Investigational
Source:
NCT01240590: Phase 1/Phase 2 Interventional Completed Solid Tumor
(2011)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Targets:

Crolibulin is a tubulin-disrupting agent, interacting at the colchicine-binding site, developed by EpiCept Corporation (which was later acquired by Immune Pharmaceuticals). The compound exhibits anti-cancer effect by vascular disruption and inhibition of apoptosis. In preclinical animal tumor models, combination therapy with crolibulin has demonstrated the synergistic activity with cytotoxic drugs as well as anti-angiogenic drugs, such as Avastin. The drug was investigated in clinical trials for the treatment of anaplastic thyroid cancer and has demonstrated a positive effect.