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

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Showing 291 - 300 of 6009 results

Status:
Investigational
Source:
NCT03166085: Phase 1 Interventional Completed Metastatic Breast Cancer
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



PU-H71 is experimental inhibitor of Hsp90. It is being tested in clinical trials against lymphoma and solid tumors.
Status:
Investigational
Source:
NCT01269593: Early Phase 1 Interventional Active, not recruiting Non-Hodgkin's Lymphoma
(2010)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
NCT03388749: Phase 1/Phase 2 Interventional Completed Leukemia, Myeloid, Acute
(2018)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Annamycin is a highly lipophilic form of the anthracycline doxorubicin with the ability to bypass multidrug resistance mechanisms of cellular drug resistance. Annamycin belongs to the anthracycline class of drugs, and has a pleiotropic mechanism of action where it targets topoisomerase II, causing strand breaks in DNA. Annamycin forms complexes with DNA by intercalation between base pairs, and it inhibits topoisomerase II activity by stabilizing the DNA-topoisomerase II complex, preventing the religation portion of the ligation-religation reaction that topoisomerase II catalyzes. The agent is being evaluated in separate phase 1 and phase 2 trials in the United States and Europe. Studies in animal models showed the agent to be noncardiotoxic. Trials that included patients with leukemia showed the agent was associated with fewer dose-limiting toxicities than typically experienced with doxorubicin. The FDA granted fast track designation to Annamycin for treatment of patients with relapsed or refractory acute myeloid leukemia.
Status:
Investigational
Source:
NCT01193491: Phase 1 Interventional Terminated Hematologic Malignancies
(2010)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

IPI-493 (17-AG, 17-Aminogeldanamycin) is the major metabolite of tanespimycin (17-AAG) and retaspimycin (17-DMAG) with potent antineoplastic activity. Hsp90 controls the proper folding, function, and stability of various "client" proteins within cells. Many of the clients of Hsp90 (such as Akt, Bcr-Abl, EGFR, Flt-3, c-Kit and PDGFR α) are oncoproteins or important cell-signaling proteins, and therefore are critical for tumor cell growth and survival. Inhibition of Hsp90 results in degradation of these proteins, which abrogates growth and survival signaling and leads to tumor cell death. IPI-493 has been used in trials studying the treatment of Advanced Malignancies.
Status:
Investigational
Source:
INN:neutramycin
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT01550484: Phase 2/Phase 3 Interventional Completed Parkinson's Disease
(2012)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

FLORBENAZINE F-18 is a fluorinated vesicular monoamine transporter type 2 (VMAT-2) ligand for positron-emission tomography. It has completed Phase II/III as a commercial radiopharmaceutical for the early detection and monitoring of neurodegenerative diseases including Parkinson's disease, Alzheimer's disease, and dementia with Lewy bodies.
Omtriptolide (previously known as PG490-88 or F60008), an immunosuppressant that has been shown to be the safe and potent antitumor agent and it has been approved entry into Phase I clinical trial for the treatment of prostate cancer in the USA. In addition, the drug is participating in phase I clinical trial for the treatment of myeloid leukemia. Experiments on animals have shown omtriptolide was highly effective in the prevention of murine graft-versus-host disease (GVHD). The immunosuppressive effect of the drug was mediated by inhibition of alloreactive T cell expansion through interleukin-2 production. However, this study was discontinued. Recently published article has shown omtriptolide possesses the potential as a prophylactic agent to prevent ischemia/reperfusion (I/R)-induced lung injury.
Status:
Investigational
Source:
NCT02859857: Phase 1 Interventional Completed Neoplasms
(2016)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

1,​2-​Dioleoyl-​sn-​glycero-​3-​phospho-​L-​serine Sodium Salt is a lipid being studied in the assembly and long-term stability of solid supported lipid bilayers from artificial and natural lipid mixtures.
Status:
Investigational
Source:
INN:naxagolide
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Naxagolide (MK-458; L 647,339; (+)-PHNO) is a dopamine D2/D3-receptor agonist, which was studied for the treatment of patients with Parkinson's disease, but further study was discontinued. In addition, was discovered, that Naxagolide C-11 ([(11)C]-(+)-PHNO) was a potential radiotracer for imaging the high-affinity state of dopamine D2 receptors with positron emission tomography (PET) in human subjects. This radiotracer is a suitable for imaging the agonist binding sites (denoted D(2HIGH) and D(3)) of these receptors. PET studies in nonhuman primates documented that, in vivo, [(11)C]-(+)-PHNO displays a relative selectivity for D(3) compared with D(2HIGH) receptor sites and that the [(11)C]-(+)-PHNO signal is enriched in D(3) contribution compared with conventional ligands such as [(11)C] raclopride. Recently was published article reflects the relationship between social attachment and dopamine D2/3 receptor availability in the brains of healthy humans using [11C]-(+)-PHNO.
Status:
Investigational
Source:
NCT00942656: Not Applicable Interventional Completed Cardiovascular Disease
(2009)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Rumenic acid is the major conjugated linoleic acid (CLA), probably because of successive desaturation and chain elongation and can be considered as the principal dietary form. In experiments on rodents was shown that rumenic acid possessed the protective effect against colitis, which was associated with the activation of the Nrf2 pathway.