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

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Showing 1191 - 1200 of 14117 results

Status:
Investigational
Source:
INN:cefaparole
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Cefaparole (cephaparole) is a cephem antibiotic of the cephalosporin subclass that was never marketed and used as phmarceutical intermediates for other drugs.
Status:
Investigational
Source:
INN:colestolone
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Colestolone (5 alpha-cholest-8(14)-en-3 beta-ol-15-one) is an inhibitor of sterol biosynthesis. The compound reduces the level of 3-hydroxy-3-methylglutaryl coenzyme A reductive activity in cultured mammalian cells. In nonhuman primates, the compound decreases the levels of total serum cholesterol and low-density lipoprotein and increases the percentage of total cholesterol associated with high-density lipoprotein.
Status:
Investigational
Source:
NCT04439188: Phase 2 Interventional Active, not recruiting Advanced Lymphoma
(2016)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



GSK-2636771 is a potent, orally bioavailable, PI3Kβ-selective inhibitor, sensitive to PTEN null cell lines. GSK-2636771 shows selectively inhibitory activity in PTEN null cell lines (human prostate adenocarcinoma PC-3 and breast cancer HCC70) with EC50 of 36 nM and 72 nM, respectively. GSK-2636771 significantly decreases cell viability in p110β-reliant PTEN-deficient PC3 prostate and BT549 and HCC70 breast cancer cell lines, and leads to a marked decrease of AKT phosphorylation only in the control prostate and breast cancer cell lines. On April 1 2016 GlaxoSmithKine completes a phase-I/II trial for Solid tumours (Late-stage disease) in USA, United Kingdom and South Korea (NCT01458067).
Status:
Investigational
Source:
Neurology. Jan 1969;19(1):101-4.: Not Applicable Human clinical trial Completed Multiple Sclerosis/blood
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Androsterone, a neurosteroid, acts as a positive allosteric modulator of GABA(A) receptors, that can cross into the brain and could have effects on brain function. It was discovered, that the association of beta subunits with alpha subunits GABA(A) receptor affects the sensitivity of glycine receptors to androsterone. In spite of that, androsteron is considered as an inactive metabolite of testosterone. In addition, was studied that androsterone possessed anticonvulsant properties. Although of low potency, the androsterone was present in high abundance and was able to represent endogenous modulator of seizure susceptibility.
Status:
Investigational
Source:
INN:quinaldine blue [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Pinacyanol iodide is a fluorescent cationic cyanine dye used to stain biological specimens. It is the obstetric diagnostic aid. The mechanism of tracing with pinacyanol iodide dyes is based on their lipid solubility. Pinacyanol iodide dyes are more efficacious than classical tracing methodologies especially during early stages of development and consequently have been used to reveal the spatiotemporal patterns of axonal development in different species. The unique properties of the pinacyanol iodide dye tracing method have opened up new avenues for tracing connections in human postmortem specimens. Pinacyanol iodide dye tracing is incompatible with alcohol fixation and paraffin embedding of tissue.
Status:
Investigational
Source:
INN:metogest
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Metogest, a hormone, is a progesterone receptor agonist. Metogest was used in acne treatment. However, this drug has never been marketed.
Fenretinide (4-HPR) is an orally-active synthetic phenylretinamide analogue of retinol (vitamin A) with potential antineoplastic and chemopreventive activities. Fenretinide binds to and activates retinoic acid receptors (RARs), thereby inducing cell differentiation and apoptosis in some tumor cell types. This agent also inhibits tumor growth by modulating angiogenesis-associated growth factors and their receptors and exhibits retinoid receptor-independent apoptotic properties. Phase III clinical trial data has suggested that fenretinide reduces breast cancer relapse in pre-menopausal women. Fenretinide is the most studied retinoid in breast cancer chemoprevention clinical trials due to its selective accumulation in breast tissue and its favorable toxicological profile. This agent showed a significative reduction of the incidence of second breast tumors in premenopausal women confirmed after 15-year followups. Fenretinide, a drug being developed by Sirion Therapeutics, slowed the progression of advanced dry age-related macular degeneration (AMD) by 45 percent for people receiving a higher dose of the treatment in a Phase II clinical trial. Sirion has been granted a Fast Track designation for the treatment by the FDA. Fenretinide is in phase II clinical trials for the treatment of B-cell lymphoma, chronic lymphocytic leukemia. It is also in phase I clinical trials for the treatment of cystic fibrosis.
Status:
Investigational
Source:
NCT03440632: Not Applicable Interventional Completed Cerebral Palsy
(2018)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Zearalenone (ZEN) is a toxic non-steroidal mycoestrogen produced by fungi that widely contaminate agricultural products, eliciting estrogenic responses by mimicking sex steroid hormones. Zearalenone is biosynthesised through a polyketide pathway by a variety of Fusarium fungi including Fusarium graminearum (Gibberella zeae), Fusarium culmorum, Fusarium equiseti, Fusarium crookwellense, Fusarium cerealis and Fusarium semitectum. Zearalenone and its derivatives share similar molecular mechanisms and activity with estrogens. They interact with the estrogen receptors (ERa and ERb) leading to functional and morphological changes in the reproductive system in both animals and humans. Zearalenone exposure is associated with the estrogenic syndrome and infertility in animals and premature thelarche and precocious puberty in girls. In animal models, it was found that prepubertal exposure to a low dose of Zearalenone, decreased breast cancer risk. When prepubertal rats were treated with 20 lg (1 mg ⁄ kg body weight) of Zearalenone, a significant reduction of both the incidence and multiplicity of DMBA-induced mammary tumours was noted. Zearalenone has been used to treat postmenopausal symptoms in women.
Status:
Investigational
Source:
NCT00409071: Phase 3 Interventional Completed Breast Cancer
(2005)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Cocculine is an alkaloid found in the leaves of Cocculus laurifolius, the laurel-leaved snail tree. Cocculine has hypotensive and ganglion blocking properties.
Status:
Investigational
Source:
INN:gloximonam
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Gloximonam (SQ-82531) is a beta-lactam antibiotic. This is a class of antibiotics that contains a beta-lactam ring in their molecular structure, such as penicillin derivatives. Gloximonam is orally absorbed and has shown anti-bacterial activity against different bacteria of the Enterobacteriaceae and Haemophilus influenzae families. Gloximonam is not effective against staphylococci and strict anaerobes (like aztreonam) and (unlike aztreonam) against Pseudomonas aeruginosa.

Showing 1191 - 1200 of 14117 results