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

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Showing 49071 - 49080 of 55039 results

Status:
Investigational
Source:
INN:lorundrostat [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
INN:pirandamine [INN]
Source URL:

Class (Stereo):
CHEMICAL (UNKNOWN)

Pirandamine is the potential antidepressant drug. It is a relatively selective inhibitor of the serotonin uptake mechanism and does not exhibit appreciable norepinephrine uptake blocking activity in contrast to the tricyclic antidepressant drugs imipramine and amitriptyline. Pirandamine is equivalent to amitriptyline and greater than imipramine in potency as a serotonin uptake blocker and a potentiator of central serotonin pharmacological actions, and in contrast, does not exhibit appreciable central anticholinergic effects. Pirandamine potentiated the behavioral effects of 5-hydroxytryptophan in mice. Pirandamine, in contrast to desimipramine and imipramine, did not prevent reserpine-induced hypothermia. The (-)-enantiomer of pirandamine retained the activity of the racemate; the (+I-enantiomer was much less effective.
Status:
Investigational
Source:
INN:tanuxiciclib [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
INN:clonitazene [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Clonitazene is a synthetic opioid analgesic, structurally related to etonitazene. In the USA clonitazene is a schedule I narcotic controlled substance.
Status:
Investigational
Source:
NCT04238715: Phase 2 Interventional Active, not recruiting Cholangiocarcinoma
(2020)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



E-7090 is a novel selective inhibitor of fibroblast growth factor receptors, that displays potent anti-tumor activity. It is a promising candidate as a therapeutic agent for the treatment of tumors harboring FGFR genetic abnormalities. E-7090 is an orally available and selective inhibitor of the tyrosine kinase activities of FGFR1, -2, and -3. In kinetic analyses E-7090 associated more rapidly with FGFR1 than did the type II FGFR1 inhibitor ponatinib, and E-7090 dissociated more slowly from FGFR1, with a relatively longer residence time, than did the type I FGFR1 inhibitor AZD4547, suggesting that its kinetics are more similar to the type V inhibitors, such as lenvatinib. E-7090 showed selective antiproliferative activity against cancer cell lines harboring FGFR genetic abnormalities and decreased tumor size in a mouse xenograft model using cell lines with dysregulated FGFR. Furthermore, E-7090 administration significantly prolonged the survival of mice with metastasized tumors in the lung. It is being investigated in a Phase I clinical trial for treatment of patients with solid tumors.
Status:
Investigational
Source:
NCT03013998: Phase 1/Phase 2 Interventional Recruiting Previously Untreated Relapsed Refractory Acute Myeloid Leukemia
(2016)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


HCI-2084 (wider known as TP-0903) is developing by Tolero Pharmaceuticals for the treatment of different cancers. HCI-2084 is a small molecule AXL receptor tyrosine kinase (RTK) inhibitor. AXL is involved in maintaining a mesenchymal phenotype in cancer cells that enhanced cell survival in stressed environments, and increased resistance to targeted therapies compared to epithelial cells. AXL overexpression has been observed in multiple tumor types that have acquired resistance to various agents. TP-0903 is participating in phase I/II clinical trial in patients with previously treated chronic lymphocytic leukemia (CLL). This study will investigate the safety, pharmacokinetics, pharmacodynamics, and clinical activity of TP-0903. Besides, phase I is currently being conducted in patients with advanced solid tumors in the presence of TP-0903. In addition, TP-0903 was investigated in neuroblastoma (NB) cells, where this drug makes NB cells more vulnerable to the conventional chemotherapeutics.
Status:
Investigational
Source:
INN:desomorphine
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Desomorphine is the common name for 4,5--epoxy-17- methylmorphinan-3-ol or dihydrodesoxymorphine-D. It is an opioid analogue and morphine derivative in which the 6-hydroxyl group and the double bond at carbons 7 and 8 of morphine are reduced. Desomorphine can cross the blood–brain barrier, binding to opioid receptors, similar to the pharmacokinetic distribution of all phenanthrene-structured alkaloids. Taking Desomorphine causes euphoria as well as sedative and analgesic relief. In addition to its faster onset than other powerful painkillers drugs such as morphine, desomorphine also initiates less sedative effects and seems to have favorable postoperative results, such as reduced need for catheterization, less dizziness, and decreased vomiting incidence. In comparison with Morphine, Desomorphine is faster reduced. It follows that it has to be taken it more frequently to get the same effects. Furthermore, it causes side effects such as respiratory and gastrointestinal problems and increased blood pressure. In addition, Desomorphine’s withdrawal symptoms are up to three times longer than Morphine’s. This leads to the conclusion that Desomorphine is more addictive. At present, desomorphine is classified as a narcotic drug (DEA code number 9055) in Schedule I of the U.S. Controlled Substances Act and is listed as a controlled substance under the international Single Convention on Narcotic Drugs of 1961.
Status:
Investigational
Source:
NCT02253342: Phase 1 Interventional Completed Intrapulmonary Pharmacokinetics of WCK 2349
(2014)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Levonadifloxacin is the S-(-) isomer of the benzoquinolizine fluoroquinolone nadifloxacin and is two- to four-fold more active than the racemic mixture. Levonadifloxacin is a potent antibacterial agent against Gram-positive bacteria especially against methicillin resistance Staphylococcus aureus. It also possesses potent bactericidal activity against other resistant variants like quinolone-resistant Staphylococcus aureus, vancomycin and glycopeptide intermediate Staphylococcus aureus and vancomycin resistant Staphylococcus aureus. Intravenous dosage form developed to treat complicated skin and skin structure infections and has recently completed Phase III studies in India and Phase I studies in USA.
Status:
Investigational
Source:
INN:selnoflast [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Showing 49071 - 49080 of 55039 results