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

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Showing 881 - 890 of 34955 results

Acifran (AY-25,712), an uncommercialized Ayerst compound exerting lipid-lowering activity in vivo, has been shown to also elicit similar effects as niacin in preliminary clinical testing and has been shown to bind to both high affinity (HM74A; GPR109A) and low affinity (HM74; GPR109B) niacin receptors. The EC50 values of the separated acifran enantiomers for the GPR109a and 109b receptors showed that, as with acifran itself, the (+)-enantiomers were essentially twice as active as the racemic mixtures, whereas the activity of the (-)-enantiomers was more variable and highly dependent on purity. S-enantiomer of acifran is the active principle. All of the activity of racemic acifran could be attributed to the (S)-enantiomer, and hence, from this precedent, (+)-enantiomers would be assigned to the S-configuration. However, the absolute configuration was not confirmed experimentally.
Status:
Investigational
Source:
NCT02117258: Phase 2 Interventional Completed Metastatic Pancreatic Adenocarcinoma
(2014)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Nastorazepide (Z-360) is a selective, orally available, gastrin/cholecystokinin 2 (CCK-2) receptor antagonist with potential antineoplastic activity. Z-360 binds to the gastrin/CCK-2 receptor, thereby preventing receptor activation by gastrin, a peptide hormone frequently associated with the proliferation of gastrointestinal and pancreatic tumor cells. It is currently under development as a therapeutic drug for pancreatic cancer, gastroesophageal reflux disease and peptic ulcers. The most commonly reported adverse events were nausea, abdominal pain, vomiting and fatigue.
Status:
Investigational
Source:
NCT00095797: Phase 1 Interventional Completed Adult Acute Basophilic Leukemia
(2004)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



XK-469 (2-[4-(7-chloro-2-quinoxalinyloxy)phenoxy]-propionic acid) is a novel synthetic quinoxaline phenoxypropionic acid derivative. The R-isomer of XK-469 was approximately twice as effective as the S-isomer of XK-469R. R( )-isomers induce reversible protein DNA crosslinks in mammalian cells. It acts as a selective topoisomerase IIβ inhibitor. A phase I study was performed to determine the safety and pharmacokinetics of XK-469, (R)- in patients with various neoplasms.
Status:
Investigational
Source:
NCT01930903: Not Applicable Interventional Unknown status Coronary Artery Disease
(2013)
Source URL:

Class (Stereo):
CHEMICAL (EPIMERIC)

Status:
Investigational
Source:
NCT01871298: Not Applicable Interventional Completed Drug Abuse Illicit
(2014)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Status:
Investigational
Source:
NCT04538066: Phase 2 Interventional Completed Alzheimer Disease
(2020)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Bryostatin 1 is a macrocyclic lactone which can be isolated from the marine bryozoan, Bugula neritina. The effects of bryostatin 1 are attributed to its ability to selectively modulate the activity of two of the three subgroups of protein kinase C (PKC) isozymes. PKC isozymes are divided into three subgroups which differ in their molecular structures and co-factor requirements: classical PKC (cPKC), novel PKC (nPKC), and atypical PKC (aPKC). Bryostatin-1 modulates nPKC activity independent of a Ca2+ signaling. It activates cPKC only when associated with Ca2+ signaling. And, aPKC activity is not sensitive to bryostatin-1 administration. Ca2+ signals play an important role in synaptic transmission and information processing which creates a biological environment where Bryostatin-1 possesses a unique action profile. Bryostatin-1 will not affect cPKC activity in neurons which are not functioning as an active part of the signaling processing circuit with significant Ca2+influx and intracellular Ca2+ release. Bryostatin 1 is in phase II clinical trials for investigation as an anticancer agent; specifically for treatment of metastatic or recurrent head and neck cancer, ovarian epithelial cancer that has not responded to previous chemotherapy, and myelodysplastic syndrome. Bryostatin 1 has also generated interest as an investigational compound for the treatment of Alzheimer's disease.
Status:
Investigational
Source:
NCT02355613: Not Applicable Interventional Completed Metastases to Brain
(2014)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Haloxyfop-p-methyl ester, a selective herbicide, is used to control a wide range of annual and perennial grass weeds in broad-leaved crops, such as legume, cotton, peanut, rape, and vegetables
Status:
Investigational
Source:
INN:propyl docetrizoate
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Docetrizoate (trade name: Pulmidol) is the bronchographic agent (radiopaque medium). The most important characteristic of a bronchographic medium, that it should flow readily into small bronchial branches, but not pass into bronchioles, is well fulfilled by Pulmidol. Propyl docetrizoate in 60 or 75 per cent suspension in arachis oil produced satisfactory bronchograms in the cat and in man. The radio-opaque material was cleared from the lung within two to four days, and produced no significant histological changes in the lungs of cats receiving a high concentration into one lobe. Early in 1962 a change to Pulmidol was made because of the increased contrast due to its higher iodine content, but its use had to be discontinued following reports of deaths in children due to its absorption under anaesthesia.
Status:
Investigational
Source:
NCT03042702: Phase 2 Interventional Completed Ovarian Cancer
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


4-Isothioureidobutyronitrile (Kevetrin) is a small molecule that has demonstrated the potential of becoming a breakthrough cancer treatment by inducing activation of p53. It is a water-soluble, small molecule and activator of the tumor suppressor protein p53, with potential antineoplastic activity. Upon intravenous administration, 4-thioureidobutyronitrile activates p53 which in turn induces the expressions of p21 and PUMA (p53 up-regulated modulator of apoptosis), thereby inhibiting cancer cell growth and causing tumor cell apoptosis. 4-Thioureidobutyronitrile may be effective in drug-resistant cancers with mutated p53. p53 tumor suppressor, a transcription factor regulating the expression of many stress response genes and mediating various anti-proliferative processes, is often mutated in cancer cells. Cellceutix continues to build upon the successful Phase 1 trial evaluating Kevetrin in treating advanced solid tumors conducted at Dana-Farber Cancer Institute and Beth Israel Deaconess Medical Center. Kevetrin, in IV form, was shown to safely modulate, in a non-genotoxic manner, the key tumor suppressor protein p53 as measured through increased expression of p21, a key downstream biomarker of p53. Cellceutix is advancing Kevetrin under an Orphan Drug designation from the Food and Drug Administration (FDA) for the treatment of ovarian cancer, pancreatic cancer and childhood retinoblastoma.
Status:
Investigational
Source:
NCT01052012: Phase 3 Interventional Completed Postoperative Pain
(2009)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Lambda-cyhalothrin (λ-cyhalothrin), a mixture of isomers of cyhalothrin belongs to a class of insecticides known as synthetic pyrethroids. Synthetic pyrethroids are often preferred to the real thing as an active ingredient because they offer the added bonus of remaining effective for longer period. λ-cyhalothrin was the most commonly used pyrethroid insecticide for vegetable farming in Benin. Experiments have shown that λ-cyhalothrin residues in lettuce and cabbage from farms and markets in Parakou and Cotonou were relatively safe for consumption.