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

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Showing 261 - 270 of 19755 results

Status:
Investigational
Source:
NCT01954238: Phase 1 Interventional Completed Healthy Volunteers
(2013)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT04418895: Phase 2 Interventional Withdrawn Rectal Adenocarcinoma
(2021)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
NCT01588548: Phase 1 Interventional Completed Advanced Solid Malignancies
(2012)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



AZD-1208 is an orally available, potent and highly selective Pim inhibitor that effectively inhibits all three isoforms. AZD-1208 inhibits the growth of several AML cell lines and sensitivity correlates with the level of Pim-1 expression, STAT5 activation and presence of protein tyrosine kinase mutation. AZD-1208 causes cell cycle arrest and apoptosis in MOLM-16 cells in culture. This is accompanied by a dose-dependent reduction in phosphorylation of BAD, 4EBP1 and p70S6K. In addition, AZD-1208 leads to potent inhibition of colony growth of primary AML cells from bone marrow aspirates and downregulates phosphorylation of Pim targets. AZD-1208 was in Phase 1 trials to evaluate the safety and tolerability profile and to determine the maximum tolerated dose (MTD). There were two trials where AZD-1208 had been administered orally in AML and solid tumour (of all types) patients. The studies had being discontinued due to safety reasons.
Status:
Investigational
Source:
INN:bioresmethrin [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Bioresmethrin is a synthetic pyrethroid insecticide. It is the (+)-trans isomer of resmethrin which itself contains a minimum of 30% bioresmethrin. Bioresmethrin is the [1R, trans] isomer of resmethrin and has greater insecticidal activity than the racemic mixture. Bioresmethrin is a potent contact insecticide effective against a wide range of household insects, plant pests, grain pests and insects found in animal housing. It exhibits a high order of insecticidal activity, which when coupled with its excellent toxicological properties, makes it potentially one of the safest and most useful insecticides now being produced.
Status:
Investigational
Source:
INN:libvatrep [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
NCT00988949: Phase 1 Interventional Completed Bipolar Depression
(2009)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Pfizer was developing PF-4455242, a selective, short-acting (non-"inactivating") antagonist of the κ-opioid receptor. PF-4455242 was pursued in phase I clinical trial for the treatment of the bipolar disorder and was also investigated as a treatment for depression and substance abuse. In September 2010 Pfizer discontinued the development of the compound.
Status:
Investigational
Source:
NCT01340183: Phase 1 Interventional Suspended Healthy
(2011)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT01106599: Phase 1 Interventional Completed Solid Cancers
(2010)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



DC-0623 is an orally active, selective and ATP-uncompetitive MEK inhibitor with potential antineoplastic activity. GDC-0623 specifically inhibits mitogen-activated protein kinase kinase (MEK or MAP/ERK kinase), resulting in inhibition of growth factor-mediated cell signaling and tumor cell proliferation. In a panel of mutant cancer cell lines, GDC-0623 inhibits cellular proliferation with EC50 values in the low nanomolar range. In vivo, GDC-0623 (40 mg/kg, p.o.) causes potent tumor growth inhibition (TGI) in mouse MiaPaCa-2 (120%), A375 (102%) and HCT116 (115%) xenografts. GDC-0623 had been in phase I clinical trials by Genentech, Inc. for the treatment of Advanced or Metastatic Solid Tumors. However, the clinical development of GDC-0623 was discontinued.
Valopicitabine is a nucleoside analog and the orally bioavailable prodrug of NM107 that competitively inhibits HCV NS5B polymerase, causing chain termination. Valopicitabine had been in phase II clinical trial for once-daily oral treatment of Hepatitis C virus infection. However, because of the overall risk/benefit profile of subjects undergoing clinical trials, further development of the drug has been temporarily placed on hold by the Swiss drug major Novartis and USA-based Idenix Pharmaceuticals company and the FDA.
Status:
Investigational
Source:
INN:emilium tosilate
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Emilium is an antiarrhythmic agent and cardiac depressant.