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

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Showing 71 - 80 of 2257 results

VX-970 (VE-822) is an ATR kinase inhibitor. VE-822 decreased maintenance of cell-cycle checkpoints, increased persistent DNA damage and decreased homologous recombination in irradiated cancer cells. Vertex Pharmaceuticals is developing VX 970 for the treatment of advanced solid tumours. Phase I/II development is underway in the US for small-cell lung cancer and in the UK for solid tumours. Phase II development of VX 970 as a combination therapy in urogenital cancer, ovarian, primary peritoneal and fallopian tube cancer indications is underway in the US.
Status:
Investigational
Source:
INN:gartisertib [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
JAN:TERALLETHRIN [JAN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Terallethrin is an insecticide that controls flying insects including houseflies, wasps and mosquitoes.
Status:
Investigational
Source:
INN:trempamotide [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Trempamotide immunological agent used for active immunization. It is an antineoplastic drug.
Status:
Investigational
Source:
NCT03189992: Phase 1 Interventional Unknown status Malignant Tumor of Small Intestine Metastatic to Liver
(2014)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Cinobufotalin, the bufadienolide isolated from toad venom, has displayed antitumor activities in many in vitro systems. It has been shown that cinobufotalin induced significant apoptosis in cultured human lymphoma U-937 cells. It induced DNA fragmentation, mitochondrial membrane potential decrease, and reactive oxygen species (ROS) production in U-937 cells. Cinobufotalin induces cytotoxic effect in cultured lung cancer cells. Cinobufotalin (1/5 mg/kg, i.p. twice daily, for 7 days) significantly inhibited A549 xenograft growth in mice. Further, same cinobufotalin administration improved mice survival at week five. Cinobufotalin administration didn’t significantly affect mice body weight, indicating the relative safety of this regimen. Thus, cinobufotalin inhibits A549 xenograft growth in vivo and improves mice survival.
Status:
Investigational
Source:
JAN:PEFCALCITOL [JAN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Pefcalcitol (previously known as M518101), an analog of vitamin D3 (VD3), is an antipsoriatic drug candidate that is designed to achieve much higher pharmacological effects, such as keratinocyte differentiation. This drug is a phosphodiesterase inhibitor and is being developed as a topical ointment formulation. Pefcalcitol was involved in phase III clinical trials in the USA and in Japan in subjects with plaque psoriasis and with palmoplantar keratoderma. In addition, it participated in phase II clinical trial for the warts treatment.
Status:
Investigational
Source:
NCT02043899: Phase 1/Phase 2 Interventional Completed Metastatic Neuroblastoma
(2014)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
NCT02294266: Phase 1 Interventional Completed Amphetamine-Related Disorders
(2014)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Mephedrone (4-methylmethcathinone) is a β-ketoamphetamine belonging to the family of synthetic cathinones, an emerging class of designer drugs known for their hallucinogenic and psychostimulant properties as well as for their abuse potential. Mephedrone is a stimulant of dopamine (DA) release and blocks its reuptake through its interaction with the dopamine transporter. Furthermore, it has some affinity for various 5-hydroxytryptamine (5-HT) receptor subtypes. Neurotoxic effect of mephedrone on 5-HT and DA systems remains controversial. Although some studies in animal models reported no damage to DA nerve endings in the striatum and no significant changes in brain monoamine levels, some others suggested a rapid reduction in 5-HT and DA transporter function. Persistent serotonergic deficits were observed after binge like treatment in a warm environment and in both serotonergic and dopaminergic nerve endings at high ambient temperature. Oxidative stress cytotoxicity and an increase in frontal cortex lipid peroxidation were also reported. Despite the re-classification of mephedrone as a Class B restricted substance by the United Kingdom and restrictive legislation by the United States, international policy regarding mephedrone control is still developing and interest in synthetic amphetamine-like drugs could drive the development of future mephedrone analogues.
Status:
Investigational
Source:
INN:florbenguane (<SUP>18</SUP>F) [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
NCT03417817: Not Applicable Interventional Completed Gastroesophageal Reflux
(2018)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Chlorothalonil (2,4,5,6-tetrachloroisophthalonitrile) is an organic compound mainly used as a broad spectrum, nonsystemic fungicide, with other uses as a wood protectant, pesticide, acaricide, and to control mold, mildew, bacteria, algae. Chlorothalonil reduces fungal intracellular glutathione molecules to alternate forms which cannot participate in essential enzymatic reactions, ultimately leading to cell death. Chlorothalonil is slightly toxic to mammals, but it can cause severe eye and skin irritation in certain formulations. Very high doses may cause a loss of muscle coordination, rapid breathing, nose bleeding, vomiting, and hyperactivity. Dermatitis, vaginal bleeding, bright yellow and/or bloody urine, and kidney tumors may also occur, followed by death. In a number of tests of varying lengths of time, rats which were fed a range of doses of chlorothalonil generally showed no effects on physical appearance, behavior, or survival. Kidney changes such as kidney enlargement were common. In the US, chlorothalonil is used predominantly on peanuts (about 34% of usage), potatoes (about 12%), and tomatoes (about 7%), though the EPA recognizes its use on many other crops. It is also used on golf courses and lawns (about 10%) and as a preservative additive in some paints (about 13%), resins, emulsions, and coatings. Chlorothalonil is commercially available in many different formulations and delivery methods. It is applied as a dust, dry or water-soluble grains, a wettable powder, a liquid spray, a fog, and a dip. It may be applied by hand, by ground sprayer, or by aircraft