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Restrict the search for
m nalidixic acid
to a specific field?
Status:
Investigational
Source:
NCT03592472: Phase 3 Interventional Recruiting Renal Cell Carcinoma
(2018)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Abexinostat (PCI-24781) is a novel, second-generation phenyl hydroxamic acid–based, orally bioavailable HDAC inhibitor that has previously been shown to have activity in vitro and in vivo against a broad array of cancers, including hematopoietic malignancies and bone and soft-tissue sarcomas. Abexinostat is a pan-HDAC inhibitor mostly targeting HDAC1 with Ki of 7 nM, modest potent to HDACs 2, 3, 6, and 10 and greater than 40-fold selectivity against HDAC8. Abexinostat exhibits potent antitumor activity against a variety of tumor cell lines with GI50 ranging from 0.15 uM to 3.09 uM. PCI-24781 also has an antiproliferative effect on HUVEC endothelial cells with GI50 of 0.43 uM. Abexinostat treatment causes dose-dependent accumulation of both acetylated histones and acetylated tubulin in HCT116 or DLD-1 cells, induces expression of p21, and leads to PARP cleavage and accumulation of the γH2AX. It has also shown good tolerability and activity in Phase I and II clinical trials against lymphoma, as well as against solid tumors in Phase-I trials. Additionally, it acts as a potent radiosensitizing agent and is synergistic with cytotoxic chemotherapy, such as doxorubicin in preclinical models.
Status:
Investigational
Source:
NCT02509546: Phase 1/Phase 2 Interventional Completed Acute Myeloid Leukemia Arising From Previous Myelodysplastic Syndrome
(2015)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
8-chloroadenosine (8-Cl-Ado) is a ribonucleoside analog. The mechanism of its action remains poorly understood, however, it is known that the drug inhibits RNA synthesis. It has significant cytotoxic activity against lymphoid and myeloid malignant cells. The nucleoside analog 8-Cl-Ado is phosphorylated into its cytotoxic triphosphate 8-Cl-ATP. The accumulation of the cytotoxic metabolite results in a parallel decrease of the ATP cellular pools. 8-Cl-Ado gets incorporated into RNA during transcription, hindering this process. In addition, this triphosphate inhibits ATP-dependent poly(A) tail synthesis, and, as a consequence, mRNA processing is inhibited, resulting in vitro cytotoxicity in several solid and hematological malignancies. This agent is currently in clinical trials for the treatment of chronic lymphocytic leukemia and acute myeloid leukemia.
Status:
Investigational
Source:
NCT01041677: Phase 2 Interventional Completed Obesity
(2008)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Johnson and Johnson was developing usistapide, a microsomal triglyceride transfer protein (MTTP) inhibitor, for the treatment of obesity and type 2 diabetes. Usistapide, also known as JNJ-16269110 and R256918, has been used in trials studying the treatment of obesity, overweight, metabolic diseases, nutrition disorders, and nutritional and metabolic diseases. Usistapide was removed from the company pipeline and appears to have been discontinued.
Status:
Investigational
Source:
NCT01452919: Phase 3 Interventional Completed Schizophrenia
(2011)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
LY404039 [(-)-(1R,4S,5S,6S)-4-amino-2-sulfonylbicyclo[3.1.0]-hexane-4,6-dicarboxylic acid] is an agonist of orthosteric metabotropic glutamate receptor (mGluR)2/3. In addition, it acts as an agonist at dopamine D2 receptors. LY404039 demonstrated broad antipsychotic and anxiolytic efficacy across multiple animal models. LY-2140023 is a methionine amide prodrug of LY-404039 being developed by Eli Lilly & Co for the potential oral treatment of schizophrenia.
Status:
Investigational
Source:
NCT03198663: Not Applicable Interventional Completed HIV/AIDS and Infections
(2016)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Source:
NCT00355914: Not Applicable Interventional Completed Low Back Pain
(2003)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Source:
NCT01308164: Not Applicable Interventional Completed Type 1 Diabetes
(2011)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Source:
NCT02533336: Phase 3 Interventional Terminated Malaria
(2015)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
FENPYROXIMATE is a pyrazole acaricide widely used in the prevention of acarids (mites) in fruit plant gardens. It is a potent inhibitor of the mitochondrial proton-translocating NADH-quinone oxidoreductase (complex I).
Status:
Investigational
Source:
NCT02680041: Phase 3 Interventional Completed Prostate Cancer
(2016)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
FLUCICLOVINE is a synthetic amino acid which is transported across mammalian cell membranes by amino acid transporters such as LAT-1 and ASCT2. Its 18F radiolabelled form is a positron emission tomography (PET) tracer targeting prostate cancer cells where aforementioned transporters are known to be upregulated, providing a mechanism for the enhanced accumulation of the tracer in these cells.
Status:
Investigational
Source:
NCT00655421: Phase 3 Interventional Unknown status Oral Cancer
(2008)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Toluidine Blue (also known as tolonium chloride or Toluidine blue O) is metachromatic dye used for a variety of histological staining, it selectively stains acidic tissue components (sulfates, carboxylates, and phosphate radicals. Toluidine blue has an affinity for nucleic acids, and therefore binds to nuclear material of tissues with a high DNA and RNA content. It was evaluated the toluidine blue staining in premalignancies, and superficial oral ulceration suggesting malignancy. The study showed 100% sensitivity in the detection of in situ and invasive carcinoma and no false-negative results occurred. The lesions that were diagnosed as dysplasia did not retain stain, and thus gave false-negative results. The reasons could be that the exact mechanisms by which the dye differentially stains malignant or dysplastic tissues remain unknown.
