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

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Showing 611 - 620 of 4712 results

Status:
Investigational
Source:
NCT00174837: Phase 3 Interventional Completed Head and Neck Squamous Cell Carcinoma
(2005)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Tumor hypoxia remains one of the greatest challenges in the treatment of solid tumors, as cancer cells in these regions are resistant to killing by radiation therapy and most anticancer drugs. Tirapazamine (3-Amino-1,2,4-benzotriazine-1,4-dioxide or SR 4233) is a cytotoxic drug with selective toxicity towards hypoxic mammalian cells. Under both aerobic and hypoxic conditions, tirapazamine is reduced by an intracellular reductase to form a highly reactive radical, which can cause DNA single- and double-strand breaks. In addition, tirapazamine under hypoxic conditions reduces the activity of topoisomerase II and stabilizes DNA topoisomerase II cleavable complexes, and these complexes remain bound to DNA. Despite the very promising results obtained in various preclinical studies and early-Phase clinical trials, several Phase III trials have failed to demonstrate any survival benefit of adding tirapazamine to chemotherapy or radiation therapy of cancers.
Status:
Investigational
Source:
NCT00195325: Phase 1 Interventional Terminated Tumors
(2005)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Targets:


Cevipabulin is a synthetic, water-soluble tubulin-binding agent with potential antineoplastic activity. Cevipabulin appears to bind at the vinca-binding site on tubulin but seems to act more similar to taxane-site binding agents in that it enhances tubulin polymerization and does not induce tubulin depolymerization. The disruption in microtubule dynamics may eventually inhibit cell division and reduce cellular growth.
Status:
Investigational
Source:
INN:morazone
Source URL:

Class (Stereo):
CHEMICAL (MIXED)

Morazone is is a nonsteroidal anti-inflammatory drug (NSAID), originally developed by the German pharmaceutical company Ravensberg in the 1950s. Morazone was used as a moderately strong analgesic but was discontinued due to high abuse potential
Status:
Investigational
Source:
NCT01692197: Phase 2 Interventional Completed Leukemia
(2013)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Indisulam (also known as E7070) is a sulfonamide derivative patented by Japanese pharmaceutical company Eisai Co. as antitumor agent. Indisulam inhibits cyclin-dependent kinases (CDK), which regulate cell cycle progression and are usually over-expressed in cancerous cells. Inhibition of CDK results in G1/S phase arrest of the cell cycle, and may lead to induction of apoptosis and inhibition of tumor cell proliferation. Preclinical and clinical studies have established the synergy of indisulam with nucleoside analogs as well as topoisomerase inhibitors. These combinations were tolerated with acceptable toxicities, including diarrhea, vomiting, and myelosuppression. In Phase II clinical trials Combination of indisulam with DNA‐damaging agent (idarubicin) and nucleoside analog (cytarabine) in patients with relapsed and refractory AML is effective and largely well tolerated.
Status:
Investigational
Source:
NCT00005093: Phase 3 Interventional Completed Lung Cancer
(1999)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



A second generation of HDACs, synthetic benzamide-containing HDACs such as Tacedinaline (CI-994), have reached phase I and II clinical trials. It has been investigated for its applications to the treatment of cancers such as Breast cancer and Colorectal cancer. Tacedinaline has been in phase III clinical trials by Pfizer for the treatment of advanced non-small cell lung cancer and pancreatic cancer combined with gemcitabine. However, this research has been discontinued. Mechanism of Action: Angiogenesis inhibitors; Histone deacetylase inhibitors. Pharmacokinetics showed that CI-994 absorption and disposition were unaffected by carboplatin and paclitaxel coadministration.
Status:
Investigational
Source:
USAN:Aclantate
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Aclantate is a nonsteroidal anti-inflammatory drug.
Status:
Investigational
Source:
INN:peradoxime [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Peradoxime is an antihypertensive agent. In normal animals, 37-48% of the radioactivity from an oral dose of labeled peradoxime or parenteral dose was excreted in the urine, and 48-50% in the feces. Biliary and urinary metabolites of peradoxime were principally found as conjugates with glucuronic acid.
Status:
Investigational
Source:
INN:niguldipine
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

S-(+)-niguldipine is a more active enantiomer and is a selective antagonist for the and α1A-adrenoceptor. In addition, it can be used for discriminating of alpha 1A- from alpha 1B-adrenoceptors. There were made attempts to investigate the antidepressant action of S-(+)-niguldipine on rats, but that studies were unsuccessful.
Status:
Investigational
Source:
NCT00277810: Phase 2/Phase 3 Interventional Completed Alzheimer Disease
(2006)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

LECOZOTAN, a benzodioxanylpiperazine derivative, is a selective serotonin 1A receptor antagonist. It was in development for the symptomatic treatment of cognitive deficits in Alzheimer's disease.
Status:
Investigational
Source:
NCT02384083: Phase 1/Phase 2 Interventional Completed Multiple Myeloma
(2015)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Filanesib is a highly selective, targeted KSP inhibitor with a mechanism of action distinct from currently available myeloma therapies such as immunomodulatory drugs (IMiDs®) and proteasome inhibitors. Across multiple studies, filanesib has demonstrated activity in heavily pretreated multiple myeloma patients, with a consistent safety profile including no drug-induced peripheral neuropathy and limited non-hematologic toxicity. Adverse events are generally limited to transient, non-cumulative and predominantly asymptomatic myelosuppression (decreases in blood counts) when supportive measures are used. Alpha 1-acid glycoprotein (AAG), a plasma protein, is a potential patient selection marker for filanesib. AAG is undergoing further investigation in clinical trials and could represent the first patient selection marker for a myeloma therapy. Filanesib is in Phase II for Multiple myeloma treatment.