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

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Showing 49101 - 49110 of 55039 results

Dasotraline, also known as SEP-225,289, is a serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI). It has an extended half-life (47-77 hours) that supports the potential for plasma concentrations yielding a continuous therapeutic effect over the 24-hour dosing interval at steady state. Dasotraline has shown a lower potential for abuse than methylphenidate in clinical testing. Dasotraline was discovered by Sunovion Pharmaceuticals Inc. and is currently in development to evaluate its use in treating ADHD in adults and children, and BED in adults in the United States. It has not been approved by the U.S. Food and Drug Administration (FDA) for the treatment of ADHD, BED or any other disorder.
Status:
Investigational
Source:
INN:bioresmethrin [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


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:
NCT02711553: Phase 2 Interventional Active, not recruiting Biliary Tract Cancer
(2016)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Merestinib (LY2801653) is a small molecule that has been shown in vitro to be a reversible type II ATP-competitive slowoff inhibitor of MET tyrosine kinase with a dissociation constant (Ki) of 2 nM, a pharmacodynamic residence time (Koff) of 0.00132 min−1 and a half-life (t1/2) of 525 min. Preclinical testing also has shown merestinib to inhibit several other receptor tyrosine oncokinases including MST1R, FLT3, AXL, MERTK, TEK, ROS1, NTRK1/2/3, and DDR1/2 and the serine/threonine kinases MKNK1/2. Merestinib is being investigated in a phase II clinical trials in patients with biliary tract cancer, non-small cell lung cancer and solid tumours.
Status:
Investigational
Source:
INN:namoxyrate [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Xenbucin is an antihyperlipidemic agent. Information about the current use of this agent is not available.
Status:
Investigational
Source:
NCT04434482: Phase 1/Phase 2 Interventional Completed Advanced Solid Tumours
(2020)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
INN:domitroban
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Domitroban is a phenylsulfony;aminobicycloheptenoic acid derivative. It is a thromboxane A2 receptor antagonist. It is a potential antiasthmatic and an experimental cerebroprotective drug. It inhibits proteinuria in animal models of renal injury. Calcium salt of R-domitroban had been in phase II clinical trial for the treatment of allergic rhinitis. Also, it was in preregistration stage for the treatment of asthma in Japan. However, these studies were discontinued.
Status:
Investigational
Source:
NCT04350736: Phase 1 Interventional Completed Acute Lung Injury (ALI) Associated With COVID-19
(2020)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT00598806: Phase 3 Interventional Completed Bladder Cancer
(2007)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Targets:


Apaziquone (EOquin, EO9) is an indolequinone that is a bioreductive prodrug and a chemical analog of the older chemotherapeutic agent mitomycin C. In hypoxic cells, such as those on the inner surface of the urinary bladder, apaziquone is converted to active metabolites by intracellular reductases (such as NQO1). The active metabolites alkylate DNA and lead to apoptosis. In animal tumour models, EO9 was inactive against the P388 murine leukaemia but exhibited anti-tumour activity against human tumour xenografts and the generally chemo-resistant murine adenocarcinomas of the colon (MAC) tumours. Initial evidence that in vivo response correlated with NQO1 activity. Apaziquone was selected for clinical evaluation based upon its novel mechanism of action (which was distinct from MMC), its preferential activity against cells derived from solid tumours in vitro and in vivo, its ability to target both aerobic and hypoxic cells and the lack of myelosuppression in mice and rats. Apaziquone has been applied in clinical studies sponsored by Spectrum Pharmaceuticals and Allergan, Inc. for the treatment of superficial (non-muscle invasive) bladder cancer. However, the US-FDA determined that it was not statistically effective.
Status:
Investigational
Source:
INN:carfloglitazar [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Status:
Investigational
Source:
NCT02173457: Phase 3 Interventional Completed Type 2 Diabetes
(2014)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Showing 49101 - 49110 of 55039 results