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

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Showing 511 - 520 of 10251 results

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

Class (Stereo):
CHEMICAL (ABSOLUTE)

Namitecan (ST1968) is a camptothecin analogue being developed by sigma-tau (a subsidiary of Alfasigma) in Switzerland for the treatment of cancer. Namitecan, a novel hydrophilic camptothecin analog of the 7-oxyiminomethyl series, was selected for clinical development on the basis of its promising preclinical efficacy. Namitecan is a topoisomerase I inhibitor. Namitecan exhibited an acceptable toxicity profile, with neutropenia being the dose-limiting toxic effect, and clinical benefit was appreciable in patients with different tumor types, particularly bladder and endometrium carcinomas.
Status:
Investigational
Source:
USAN:Azanator Maleate
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Azanator (previously known as Sch 15280), a bronchodilator and an antihistamine drug that acts via a non-adrenergic mechanism to block both histaminergically and cholinergically mediated responses in the tracheobronchial tree. Besides, the drug inhibits cyclic CMP phosphodiesterase. Azanator can have a therapeutic application in cases of chronic cough and cystic fibrosis in man.
Status:
Investigational
Source:
INN:lagociclovir [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

LAGOCICLOVIR is a nucleoside reverse transcriptase inhibitor with activity against human immunodeficiency virus and hepatitis B virus.
Status:
Investigational
Source:
INN:sarafloxacin
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Sarafloxacin [A 55620] is a quinolone antibiotic that was under development with Abbott Laboratories in the USA. It was removed from clinical use by its manufacturer Abbott Laboratories from April 30, 2001. It was never approved for use in the US or Canada.
Cidoxepin is the cis-isomer of the widely prescribed tricyclic compound doxepin. Commercial preparations of the tricyclic anti-depressant doxepin contain 15% of the more active cis-doxepin and 85% of the trans-isomer. Elorac, Inc., a rapidly growing specialty pharmaceutical company focused on the treatment of dermatological disorders, is pleased to announce that it has acquired worldwide rights to the active agent Cidoxepin from Gideon Pharmaceuticals. Cidoxepin appears to be much more potent than doxepin while having less sedative and cholinergic side effects. Elorac plans to develop oral formulations of the drug to treat urticaria and topical formulations for treatment of atopic and contact dermatitis.
Status:
Investigational
Source:
NCT02303262: Phase 2 Interventional Completed Metastatic Leiomyosarcoma
(2015)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Mocetinostat is an rationally designed, orally available, Class 1-selective, small molecule, 2-aminobenzamide HDAC inhibitor with potential antineoplastic activity. Mocetinostat binds to and inhibits Class 1 isoforms of HDAC, specifically HDAC 1, 2 and 3, which may result in epigenetic changes in tumor cells and so tumor cell death; although the exact mechanism has yet to be defined, tumor cell death may occur through the induction of apoptosis, differentiation, cell cycle arrest, inhibition of DNA repair, upregulation of tumor suppressors, down regulation of growth factors, oxidative stress, and autophagy, among others. It is undergoing clinical trials for treatment of various cancers including bladder cancer, diffuse large B cell lymphoma, follicular lymphoma, myelodysplastic syndromes, non-small cell lung cancer. Fatigue, weight loss or anorexia were most common treatment-related adverse events.
Status:
Investigational
Source:
INN:pinadoline
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Pinadoline is a competitive PGE2 antagonist. It is an analgesic agent. Pinadoline demonstrated the antinociceptive activity in the rat using the writhing and the formalin tests. In the writhing test, pinadoline was significantly more potent than inhibitors of PG synthesis, but less potent than opiate analgesics. In the formalin test, pinadoline appeared less active than aspirin and ibuprofen and more active than acetaminophen. Pinadoline does not possess the antiinflammatory activity of aspirin and ibuprofen and may be more like acetaminophen, which had diminished antiinflammatory activity. At high concentrations, pinadoline is a non-competitive antagonist of serotonin in guinea-pig ileum.
Status:
Investigational
Source:
INN:flutizenol [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Tozasertib, originally developed as VX-680 by Vertex (Cambridge, MA) and later renamed MK-0457 by Merck (Whitehouse Station, NY), was the first aurora kinase inhibitor to be tested in clinical trials. The drug, a pyrimidine derivative, has affinity for all aurora family members at nanomolar concentrations with inhibitory constant values (Ki(app)) of 0.6, 18, and 4.6 nM for aurora A, aurora B, and aurora C, respectively. Preclinical studies confirmed that tozasertib inhibited both aurora A and aurora B kinase activity, and activity has been reported against prostate, thyroid, ovarian, and oral squamous cancer cell lines. Upon treatment with tozasertib, cells accumulate with a 4N DNA content due to a failure of cytokinesis. This ultimately leads to apoptosis, preferentially in cells with a compromised p53 function. Tozasertib is an anticancer chemotherapeutic pan-aurora kinase (AurK) inhibitor that also inhibits FMS-like tyrosine kinase 3 (FLT3) and Abl. Tozasertib is currently in clinical trials as a potential treatment for acute lymphoblastic leukemia (ALL). In cellular models of cancer, tozasertib activates caspase-3 and PARP and decreases expression of HDAC, increasing apoptosis and inhibiting cell growth. In other cellular models, tozasertib inhibits cell proliferation and metastasis by blocking downstream ERK signaling and downregulating cdc25c and cyclin B. This compound also decreases tumor growth in an in vivo model of prostate cancer.
Metitepine, a psychotropic agent was developed as a non-selective antagonist of serotonin, dopamine, and adrenergic receptors. Metitepine has never been marketed.