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

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Showing 1381 - 1390 of 24164 results

Status:
Investigational
Source:
NCT04027517: Phase 3 Interventional Completed Anemia of Chronic Kidney Disease
(2019)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
NCT03452488: Phase 2 Interventional Completed Sarcopenia
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Conditions:

20-Hydroxyecdysone is a naturally occurring ecdysteroid hormone, which is marketed as dietary supplements that can increase strength and muscle mass during resistance training, particularly bodybuilding. It was found, that 20-hydroxyecdysone did not affect body composition or training adaptations nor did they influence the anabolic/catabolic hormone status or general markers of catabolism in resistance-trained males. Because is known, that ecdysteroids have been shown to prevent various changes in mammalian tissues after female sex hormone deprivation. 20-Hydroxyecdysone also was investigated on these properties. It was found in rats, that 20-Hydroxyecdysone had a beneficial effect on reducing blood pressure and consequently preventing dilated cardiac hypertrophy. Some in vitro experiments showed, that 20-hydroxyecdysone had effects on lymphocytes and neutrophils, and may act as an immunomodulator.
Status:
Investigational
Source:
NCT04072861: Phase 1 Interventional Completed Healthy Volunteers
(2019)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
NCT02103959: Phase 2 Interventional Completed Non STEMI
(2014)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

CMX-2043 is a is an α-lipoic acid analog developed by Ischemix LLC for reduction of cellular injury and organ damage due to ischemia-reperfusion injury (IRI). CMX-2043 was more effective than lipoic acid in antioxidant effect, activation of insulin receptor kinase, soluble tyrosine kinase, and Akt phosphorylation, and activated insulin-like growth factor 1 as effectively as lipoic acid. In a rat model of cardiac ischemia-reperfusion injury, treatment with CMX-2043 reduced myocardial IRI as measured by the myocardial infarction/area at risk ratio, and reduced the incidence of arrhythmia. In a 360-patient Phase 2 trial, CMX-2043 demonstrated safety but did not meet pre-specified endpoints regarding prevention of contrast-induced acute kidney injury or cardiac injury in cardiac catheterization lab subjects, and no further development of the drug was reported.
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:
NCT00606424: Early Phase 1 Interventional Completed Head and Neck Cancer
(2008)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Caffeine N-Acetyl-L-Tryptophan is Caffeine salt which can be used as a stimulant for the nervous system and as a vasodilator.
Status:
Investigational
Source:
NCT00631007: Phase 2 Interventional Completed Type 2 Diabetes Mellitus
(2008)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



INT-131, a novel, non-thiazolidinedione (TZD), selective peroxisome proliferator-activated receptor (PPAR) gamma modulator and partial agonist, which was investigated in phase II of clinical trial for the treatment of type 2 diabetes mellitus (non-insulin dependent diabetes) and Multiple Sclerosis, Relapsing Remitting. The concept of selective modulation involves targeting and activating specific genes to minimize side effects while maintaining therapeutic benefits. In vitro, INT-131 attenuated adipogenic properties, indicating moderate PPAR gamma activation/cofactor recruitment compared with the full agonistic properties of TZD compounds.
Status:
Investigational
Source:
NCT04053582: Not Applicable Interventional Completed Adolescents With Early Life Stress
(2019)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Alpha methyltryptamine (AMT) is a tryptamine (indole ethylamine) derivative, which was developed in the 1960's by Upjohn with the intention for use as an antidepressant. It was used in Russia under the trade name Indopan for the treatment of Bipolar disorder and some form of depression, but currently not being produced because of serious side effects. In the 1990's, alpha-methyltryptamine became regulated as a Schedule I controlled substance in the United States. Pharmacologically, AMT has high affinity for the serotonin (5-HT) transporter, a number of 5-HT receptors, and potently inhibits reuptake of monoamines dopamine, 5-HT, and norepinephrine reuptake. AMT is also a monoamine oxidase A inhibitor that conceivably could contribute to its pharmacological effect and this drug also the most potent inhibitor of semicarbazide-sensitive amine oxidase (SSAO).
Status:
Investigational
Source:
NCT01222546: Phase 1 Interventional Completed Solid Tumors
(2010)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Chugai Pharma Europe is developing CH-5132799, a phosphatidylinositol-3-kinase (PI3K) inhibitor, for the treatment of solid tumours. CH-5132799 is a selective class I PI3K inhibitor with potent antitumor activity against tumors harboring the PIK3CA mutations. CH-5132799 selectively inhibits class I PI3Ks, PI3Kα (IC50 = 0.014 uM ), PI3Kβ (IC50 = 0.12 uM ), PI3Kδ (IC50 = 0.50 uM ), PI3Kγ (IC50 = 0.036 uM ), but shows less inhibition of class II PI3Ks, class III PI3k and mTOR and also no inhibitory activity (IC50 > 10 uM) against 26 protein kinases. CH-5132799 exhibits more inhibitory activities against PI3Kα with oncogenic mutations E542K (IC50 = 6.7 nM), E545K (IC50 = 6.7 nM) and H1047R (IC50 = 5.6 nM) than wild-type PI3Kα. CH-5132799 treated breast cnacer KPL-4 cells, which harbor the PIK3CA mutation, phosphorylation of Akt and its direct substrates, PRAS40 and FoxO1/3a and phosphorylation of downstream factors, including S6K, S6 and 4E-BP1, are effectively suppressed. Cancer cell lines harboring PIK3CA mutations are significantly sensitive to CH-5132799. CH-5132799 is orally available and showed significant antitumor activity in PI3K pathway-activated human cancer xenograft models in mice. CH-5132799 is in phase I study to evaluate safety, pharmacokinetics and activity of CH-5132799 administered orally as a single agent in patients with advanced solid tumors.

Showing 1381 - 1390 of 24164 results