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

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Showing 191 - 200 of 655 results

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

Class (Stereo):
CHEMICAL (ABSOLUTE)

Conditions:

Dexbudesonide (22R- Budesonide) is an epimer R of Budesonide, last is used as a mixture of 22R and 22S epimers for the topical treatment of asthma, rhinitis, and inflammatory bowel disease
Status:
Investigational
Source:
INN:pentafluranol [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

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

Class (Stereo):
CHEMICAL (ABSOLUTE)

Tosagestin (Org 30659) is a synthetic 19-nortestosterone derived progestogen. It was under clinical development by NV Organon for use in oral contraceptive and hormone replacement therapy. After oral administration of [14C]-Org 30659 to postmenopausal women, the compound was extensively metabolized. The dosed radioactivity was predominantly excreted via urine. Org 30659 was to a large extent metabolized at the C3- and the C17-positions. Species comparison of the metabolic routes of Org 30659 after oral administration indicated that the monkey seems to be a better representative species than the rat for the metabolism of Org 30659 in humans. Daily oral administration of Org 30659 suppresses ovarian function to a level sufficient to inhibit ovulation. This effect is dose-dependent, and the suppressive effect is readily reversible at all doses tested. Tosagestin had been in phase II clinical trial for the treatment of the menopausal syndrome. However, this development was discontinued.
Status:
Investigational
Source:
INN:topilutamide [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Topilutamide is a non-steroidal anti-androgen. Topilutamide downregulated androgen receptor expression by 40% at 3 uM and up to 95% at 10 uM in LNCaP Cells After 48-h drug incubation. While highly hydrophobic and hydrolytically degradable, it is systemically nonresorbable. In animals, fluridil demonstrated high local and general tolerance. After 3 months of topical application of topilutamide, the average anagen percentage did not change in placebo subjects but increased in topilutamide subjects (male with androgenetic alopecia) from 76% to 85%, and at 9 months to 87%. In former placebo subjects, topilutamide increased the anagen percentage after 6 months from 76% to 85%. Sexual functions, libido, hematology, and blood chemistry values were normal.
Status:
Investigational
Source:
INN:posatirelin
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Posatirelin is a synthetic peptide that, in animal models, has been shown to improve cognitive and motor disturbances associated with aging or induced by central neurotransmission disruption. Modulation of various neurotransmission systems and activation of excitatory amino acid receptors have been suggested as possible mechanisms of action, since posatirelin increases the turnover and release of catecholamines in several brain areas as well as choline acetyltransferase activity in the cerebral cortex. In neuronal cultures, posatirelin has been shown to have trophic effects, accelerating the maturation of cerebellar granule cells and stimulating neurite growth. The benefits of posatirelin therapy in patients with late-onset Alzheimer's disease have potential clinical relevance. Significant improvements in motor, intellectual and emotional impairments were seen in posatirelin recipients. The difference in these parameters with respect to the reference and inactive drugs was significant. Posatirelin can improve cognitive and functional abilities of patients suffering from degenerative or vascular dementia. Posatirelin had been in phase III clinical trial for the treatment of cognition disorders. However, this development was discontinued.
Status:
Investigational
Source:
INN:turosteride
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Turosteride [FCE 26073] is a selective 5α-reductase inhibitor being developed by Pharmacia Corporation. Turosteride inhibits human and rat prostatic 5 alpha-reductases with IC50 values of 55 and 53 nM, respectively. It was in phase II clinical trials in Italy for the treatment of benign prostatic hyperplasia.
Status:
Investigational
Source:
NCT00156156: Phase 3 Interventional Completed Fibroid Uterus
(2004)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Asoprisnil (J867) is a novel selective steroid receptor modulator that shows unique pharmacodynamic effects in animal models and humans. Asoprisnil, its major metabolite J912, and other structurally related compounds represent a new class of progesterone receptor (PR) ligands that exhibit partial agonist and antagonist activities in vivo. Asoprisnil demonstrates a high degree of receptor and tissue selectivity, with a high-binding affinity for PR, moderate affinity for glucocorticoid receptor (GR), low affinity for androgen receptor (AR), and no binding affinity for estrogen or mineralocorticoid receptors. This compound was recently in clinical trials for the treatment of uterine fibroids and endometriosis, but those studies were discontinued.
Status:
Investigational
Source:
INN:formebolone
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Formebolone is an orally active anabolic-androgenic steroid that is included in the list of prohibited substances by the World Anti-Doping Agency. Formebolone was used in Italy and Spain for infants with malnutrition.
Status:
Investigational
Source:
USAN:DEXAMETHASONE BELOXIL [USAN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Dexamethasone beloxil is anti-inflammatory used in the treatment of uveitis, iritis, keratitis, postsurgical inflammation, vernal keratoconjunctivitis, and giant papillary conjunctivitis.
Status:
Investigational
Source:
INN:lintitript [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Lintitript (SR 27897) is a selective cholecystokinin type A (CCK-A) receptor antagonist, which was initially developed by Sanofi for appetite disorders. It is known, that CCK modulates feeding and dopamine-induced behavior in the central and peripheral nervous system. Lintitript presumably alters feeding habits, however, the exact mechanism of action is not known. Lintitript was investigated in animals with anorexia nervosa, in addition, drug was in clinical trial for the patients with advanced pancreatic cancer, but these studies were discontinued.

Showing 191 - 200 of 655 results