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

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Showing 61 - 70 of 1197 results

Status:
Investigational
Source:
NCT03301454: Phase 2 Interventional Unknown status Esophageal Cancer, Squamous Cell
(2018)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Imazethapyr is an imidazole compound used as a selective herbicide. It is applied preplant incorporated, preemergence, at cracking, and postemergence. The compound controls weeds by reducing the levels of three branched-chain aliphatic amino acids, isoleucine, leucine and valine, through the inhibition of aceto-hydroxyacid synthase, an enzyme common to the biosynthetic pathway for these amino acids. This inhibition causes a disruption in protein synthesis which, in turn, leads to an interference in DNA synthesis and cell growth. The compound is used to control grasses and broadleaved weeds including barnyardgrass, crabgrass, cocklebur, panicums, pigweeds, nightshade, mustard, smartweed, velvetleaf, jimsonweed, foxtails, seedling johnsongrass, lambsquarters, morningglory and others. Tolerant crops include soybeans, peanuts, dry and edible beans, peas, alfalfa and imidazolinone resistant/tolerant corn. Additional research is being conducted on other leguminous crops. Acetolactate synthase inhibition is the primary mechanism of action of imazethapyr (IM).
Status:
Investigational
Source:
NCT04638387: Not Applicable Interventional Terminated Osteoarthritis, Knee
(2020)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Carnosol is an ortho-diphenolic diterpene with an abietane carbon skeleton with hydroxyl groups at positions C-11 and C-12 and a lactone moiety across the B ring. Carnosol is the product of oxidative degradation of carnosic acid. Carnosol is a naturally occurring phytopolyphenol found in rosemary that functions as an antioxidant, antimicrobial, and anticarcinogen. Carnosol has been shown to inhibit inductions of COX-2 by blocking PKC signaling. Carnosol is an inhibitor of AR and ER α. Several pre-clinical studies have suggested that carnosol selectively targets tumorigenic cell as opposed to non-tumorigenic cells and is safe and tolerable in animals. Carnosol has been shown to elicit chemopreventive effects by (1) blocking the bioactivation of carcinogens, (2) enhancing antioxidant and/or detoxification enzyme activities, (3) suppressing tumor-promoting inflammation, (4) inhibiting cell proliferation and inducing apoptosis selectively in cancer cells, and (5) blocking tumor angiogenesis and invasion.
Status:
Investigational
Source:
NCT01517256: Phase 3 Interventional Completed Chronic Pain
(2009)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

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

Class (Stereo):
CHEMICAL (ACHIRAL)

Senju Pharmaceutical is developing fonadelpar (also known as SJP-0035), a peroxisome proliferator activated receptor delta agonist as an ophthalmic solution. Fonadelpar was studied in phase III clinical trial in the USA for the treatment of patients with dry eye disease. This study was successfully completed. In addition, fonadelpar was involved in phase II clinical trial in the USA for the treatment of patients with moderate to severe corneal epithelial disorders. Besides, Senju Pharmaceutical also plans a phase II trial for corneal disorders in Japan.
Status:
Investigational
Source:
NCT01168479: Phase 3 Interventional Completed Prostate Cancer
(2009)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Imazapic is a selective herbicide for both the pre- and post-emergent control of some annual and perennial grasses and some broadleaf weeds. Imazapic kills plants by inhibiting the production of branched chain amino acids, which are necessary for protein synthesis and cell growth. It has been useful for weed control in natural areas, particularly in conjunction with the establishment of native warm-season prairie grasses and certain legumes. Imazapic is relatively non-toxic to terrestrial and aquatic mammals, birds, and amphibians. It has a low level of toxicity to birds but is more toxic to aquatic life and honey bees. It has a high potential for bioaccumulation. Imazapic has an average half-life of 120 days in soil. It is may be persistent in soil systems but usually degrades quickly in aquatic systems via photolysis. It has a high aqueous solubility, is volatile and, based on its chemical properties, is moderately mobile and may leach to groundwater.
Status:
Investigational
Source:
INN:nobiprostolan [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Mallinckrodt (previously Sucampo Pharmaceuticals) is developing nobiprostolan (RK 023), a topical therapy for male pattern baldness (androgenetic alopecia) and hypotrichosis. The drug is a physiologically active fatty acid derivative. Nobiprostolan is in Phase IIa clinical trials for the treatment of male pattern baldness.
Status:
Investigational
Source:
Hum Exp Toxicol. May 1996;15(5):369-75.: Not Applicable Human clinical trial Completed N/A
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Status:
Investigational
Source:
NCT00384423: Phase 2 Interventional Completed Alzheimer's Disease
(2006)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

PRX-03140 is a partial agonist of the 5-HT4 receptor that is being developed by EPIX Pharmaceuticals for Alzheimer's disease. In vitro shows potent binding to 5-HT4 receptor and increased cAMP production in human embryonic kidney-293 cells expressing recombinant rat 5-HT(4) receptors. In the clinical trial, PRX-03140 was associated with a statistically significant improvement in the Alzheimer’s Disease Assessment Scale.
Status:
Investigational
Source:
NCT01054118: Phase 1 Interventional Completed Diabetes Mellitus, Type 2
(2009)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Arena Pharmaceuticals was developing APD-597 (JNJ-38431055), a small molecule, an orally active agonist of the G-protein coupled receptor 119 (GPR119), for the treatment of Type 2 diabetes mellitus. JNJ-38431055 was selected for preclinical development based on a good balance between agonist potency, intrinsic activity and in particular on its good solubility and reduced drug-drug interaction potential. In addition, extensive in vivo studies showed a more favorable metabolic profile that may avoid the generation of long-lasting metabolites with the potential to accumulate in clinical studies. In humans, single-dose oral JNJ-38431055 increased postmeal plasma glucagon-like peptide 1 (GLP-1), glucose-dependent insulinotropic peptide (GIP), and peptide YY (PYY) concentrations but did not significantly decrease glucose excursion or increase insulin secretion. However, in a graded glucose infusion study, JNJ-38431055 was shown to induce a higher insulin secretion rate (ISR) relative to placebo at elevated plasma glucose levels. These studies provide evidence for the potential efficacy of JNJ-38431055 as an antidiabetes agent in humans.
Status:
Investigational
Source:
NCT02499497: Phase 2 Interventional Completed Prostate Cancer
(2016)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

LY2452473 is a selective androgen receptor modulator (SARM), with potential tissue-selective androgenic/anti-androgenic activity. Upon oral administration, LY2452473 acts as an agonist in select tissues and organs, including skeletal muscle, bone and the penis, thereby binding to and activating androgen receptor (AR) while acting as an antagonist in the prostate, thereby blocking AR activation and AR-mediated cellular proliferation. This may improve muscle mass and strength, bone formation, and erectile dysfunction while not stimulating growth of the prostate. Eli Lilly was developing LY 2452473/tadalafil combination for the treatment of erectile dysfunction. In addition, Eli Lilly is studying the use of a targeted LY 2452473 therapy, as a possible improvement in quality of life for prostate cancer patients who have undergone radical prostatectomy.