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

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Showing 31 - 40 of 456 results

Status:
Investigational
Source:
NCT03731832: Phase 2 Interventional Active, not recruiting Refractory Multiple Myeloma
(2018)
Source URL:

Class (Stereo):
CHEMICAL (EPIMERIC)

Status:
Investigational
Source:
NCT03782376: Phase 3 Interventional Completed Crohn Disease
(2018)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Scandium is a soft, silvery transition element which occurs in rare minerals from Scandinavia. It develops a slightly yellowish or pinkish cast when exposed to air.Scandium is one of the rare chemicals, that can be found in houses in equipment such as colour televisions, fluorescent lamps, energy-saving lamps and glasses. The use of scandium is still growing, due to the fact that it is suited to produce catalysers and to polish glass. The main application by volume is in aluminium-scandium alloys for the aerospace industry and for sports equipment (bikes, baseball bats, etc.) which rely on high performance materials. It has been shown to reduce solidification cracking during the welding of high strength aluminium alloys. Certain isotopes of Scandium is used in cancer treatments. Scandium possesses two radionuclides emitting b+ radiations (44Sc or 43Sc) that become appropriate candidates in positron emission tomography/computed tomography (PET/ CT) diagnosis, due to the half-life of around 4 h and decay to the nontoxic Ca. For both radionuclides, the half-life is compatible with the pharmacokinetics of a fairly wide range of targeting vectors (such as peptides, antibodies, antibody fragments, and oligonucleotides). The validity, usefulness, and advantages of 44Sc have been demonstrated by examples featuring 44Sc-radiolabeled targeting vectors, including 44Sc-radiopharmaceuticals very recently used in patients. Finally, 47Sc is a low energy bemitter which is suitable for single photon emission computed tomography (SPECT) and planar imaging. 47Sc can be also used for targeted radionuclide therapy, opens the field of Sc-based vectors from diagnosis to therapy, and gives a great opportunity for dosimetric calculations and for the development of personalized medicine. 46Sc is used in isotope-carrying antibodies for bonding with tumor associated cell surface antigens (substances that causes the production of an antibody when introduced into the body, e.g., toxins, bacteria, and viruses). 46Sc is added to DTPA-derivatized (process by which a compound is chemically changed, producing a new compound that has properties more amenable to a particular analytical method) monoclonal antibodies and has been shown to target tumor cells, specifically in vivo,where it accumulates to high levels in the tumor.
Status:
Investigational
Source:
NCT03671694: Not Applicable Interventional Active, not recruiting Stress Urinary Incontinence
(2018)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

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

Class (Stereo):
CHEMICAL (RACEMIC)



Cizolirtine is a potent analgesic in mice and rats, with an efficacy superior to that of aspirin and other nonsteroid anti-inflammatory drugs. Recent studies have shown that the analgesic effect of cizolirtine could be related, at least partially, to an inhibition of spinal substance P and calcitonin gene-related peptide release. Cizolirtine has been in clinical trials for the treatment of pain and overactive bladder. Reported adverse events are: dry mouth, dizziness, nausea, vomiting, blurred vision.
Status:
Investigational
Source:
INN:tazomeline
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Tazomeline (also known as LY 287041), a neuropsychiatric agent, is a muscarinic M1 acetylcholine receptor agonist that was studied in patients with cognitive dysfunction. Tazomeline participated in clinical trials for the treatment of Alzheimer’s disease and dementia. However, all these studied were discontinued for unknown reasons.
Status:
Investigational
Source:
INN:gamfexine
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Gamfexine (WIN 1344) was introduced in the literature in 1966 as an anti-depressant. Although it was reported to be effective in the treatment of withdrawal in schizophrenia, it worsened psychotic symptoms.
Status:
Investigational
Source:
INN:nitromifene
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Nitromiphene (NIT; CI 628) is a triarylethylene antiestrogen shown to be effective in treatment of experimental breast cancer. Nitromiphene is one of the earliest nonsteroidal selective estrogen receptor modulators (SERMs). It is an anti-estrogen capable to translocate the estrogen receptor to the nucleus and to induce the replenishment of the cytosol receptor. Nitromiphene inhibited the uptake of [3H]-estradiol in rat whole homogenates and isolated cell nuclei tissues and the pituitary, and inhibited estradiol-induced female sexual behavior. Nitromiphene has thus been shown to suppress the growth of chemically induced and ransplantedmammary tumors in rodents. Also, Nitromiphene was shown to have potent, prolonged antiuterotropic effects in immature rats. Nitromiphene has been shown to undergo conversion to demethyl Nitromiphene (CI628M), a phenolic metabolite which had greater affinity for estrogen receptors and greater biological potency in vitro than did Nitromiphene. However, the in vivo antiestrogenic effects of Nitromiphene and demethyl Nitromiphene were similar, possibly due to facile O-demethylation of the former compound after administration.
Status:
Investigational
Source:
USAN:OCTICIZER [USAN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Octicizer is used as a plasticizer.
Status:
Investigational
Source:
INN:droloxifene
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Droloxifene, a derivative of the triphenylethylene drug tamoxifen, is a novel selective estrogen receptor modulator (SERM). Droloxifene also exhibits more rapid pharmacokinetics, reaching peak concentrations and being eliminated much more rapidly than tamoxifen. Its higher affinity to the estrogen receptor, higher anti-estrogenic to estrogenic ratio, more effective inhibition of cell growth and division in estrogen receptor-positive cell lines, and lower toxicity give it theoretical advantages over tamoxifen in the treatment of human breast cancer. Short-term toxicity was generally mild, and similar to that seen with other antiestrogens. Droloxifene appears active and tolerable. It may have a particular role in situations in which rapid pharmacokinetics, or an increased antiestrogenic to estrogenic ratio, are required. Droloxifene may also be a potentially useful agent for the treatment of postmenopausal osteoporosis because it can prevent estrogen deficiency-induced bone loss without causing uterine hypertrophy. Droloxifene may have an effect on bone and breast tissue because it induces apoptosis. Droloxifene has an anti-implantation effect in rats, and the effect appears to be not completely due to its anti-estrogenic activity.
Status:
Investigational
Source:
INN:noberastine
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)