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

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Showing 11751 - 11760 of 13501 results

Status:
Investigational
Source:
USAN:INDIUM CHLORIDES IN 113M [USAN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Indium Chloride In-113 is a salt of the only stable Indium isotope with applications in organic synthesis as a Lewis acid. Indium Chloride is the most available soluble derivative of indium with high reproductive toxicity. In in vitro models, Indium Chloride inhibits cell viability by elevating intracellular ROS and inducing apoptosis. In animal models Indium chloride exposure cause the accumulation of indium in blood and lung, bone marrow micronucleus rate increased, the occurrence of oxidative damage and pathological changes. Besides that, the indium chloride exposed showed significant toxicity to sperm function, as well as an increased percentage of sperm morphological abnormality and chromatin DNA damage.
Status:
Investigational
Source:
INN:furofenac
Source URL:

Class (Stereo):
CHEMICAL (UNKNOWN)


Furofenac (also known as SAS 650), a drug that has antiplatelet-aggregation activity and anti-inflammatory activity combined with low ulcerogenic power. It was shown that the furofenac mechanism of action involved the modulation of the platelet cyclooxygenase pathway.
Status:
Investigational
Source:
INN:furofenac
Source URL:

Class (Stereo):
CHEMICAL (UNKNOWN)


Furofenac (also known as SAS 650), a drug that has antiplatelet-aggregation activity and anti-inflammatory activity combined with low ulcerogenic power. It was shown that the furofenac mechanism of action involved the modulation of the platelet cyclooxygenase pathway.
Status:
Investigational
Source:
INN:sulfasuccinamide
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Sulfasuccinamide is a sulfonamide antibacterial with properties similar to those of sulfamethoxazole. It has been applied topically in the treatment of local infections of the ear, nose, and throat. It has also been given as the sodium salt. Sulfasuccinamide is a carbonic anhydrase inhibitor.
Status:
Investigational
Source:
NCT01033396: Phase 2 Interventional Completed Allergic Rhinitis
(2010)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

PF-03654764 binds with high affinity to the human H3 receptor and with lower affinity to the rat H3 receptor, in addition to having >1000-fold selectivity versus other human histamine receptor subtypes (H1, H2, and H4). PF-03654764 displayed potent antagonist properties in functional assays measuring cAMP utilizing a reporter gene assay (β-lactamase) in HEK293 cells stably expressing full length human or rat H3 receptors. In human hepatic microsomes, PF-03654764 was metabolically stable and were predicted to have low clearance. It has low potential to inhibit activities of CYP 1A2, 2B6, 2C8, 2C9, 2C19, 2D6, and 3A4. PF-03654764 + fexofenadine failed to provide superior relief of allergic rhinitis-associated nasal symptoms upon exposure to ragweed pollen compared to fexofenadine + pseudoephedrine. Side effects in the PF-03654764-treated groups were clinically significant compared to the controls. PF-03654764 had been in phase II clinical trial for the treatment of allergic rhinitis and in phase I clinical trial for the treatment of Alzheimer's disease. However, these investigations were discontinued.
Status:
Investigational
Source:
INN:pibrozelesin [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Pibrozelesin (KW-2189) is a semisynthetic water-soluble derivative of the antineoplastic antibiotic duocarmycin B2. Activated by carboxyl esterase, pibrozelesin alkylates DNA by binding to adenine-thymine (A-T)-rich sequences in the minor groove of DNA, thereby inhibiting DNA replication and inducing apoptosis. KW-2189 induced DNA strand breaks in H69 cells in a concentration-dependent manner. DNA cleavage is one of the major mechanisms of KW-2189-mediated cytotoxicity. KW-2189 showed evidence of anti-tumor activity in hepatocellular carcinoma (HCC). However, because of significant and prolonged hematologic toxicity, when given as a single dose every 6 weeks, further development of this drug in HCC is not possible. Pibrozelesin had been in phase II clinical trial for the treatment of advanced malignant melanoma and advanced renal cell carcinoma. No activity in metastatic renal cell carcinoma was demonstrated and the lack of significant antitumor activity in advanced malignant melanoma treatment was shown.
Status:
Investigational
Source:
INN:pirralkonium bromide
Source URL:

Class (Stereo):
CHEMICAL (MIXED)

Pirralkonium is the antiseptic agent.
Status:
Investigational
Source:
INN:oxmetidine
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Oxmetidine is an H2-receptor antagonist that was studied as a gastrointestinal agent. Oxmetidine possesses efficacy in the treatment of peptic ulcers. However, information about the further development of this drug is not available.
Status:
Investigational
Source:
INN:haletazole [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Halethazole has been studied as an active antifungal compound.
Status:
Investigational
Source:
NCT03417739: Phase 2 Interventional Active, not recruiting Uveal Melanoma
(2018)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



BVD-523 potently and selectively inhibits ERK1 and ERK2 kinases in a reversible, ATP-competitive fashion. Consistent with its mechanism of action, BVD-523 inhibits signal transduction, cell proliferation, and cell survival, most potently in cell lines bearing mutations that activate MAPK pathway signaling. Similarly, single-agent BVD-523 inhibits tumor growth in vivo in BRAF-mutant melanoma and colorectal xenografts as well as in KRAS-mutant colorectal and pancreatic models. BioMed Valley Discoveries is developing ulixertinib, a potent and selective small molecule inhibitor of ERK 1 and 2 kinases, as an oral treatment for cancers harbouring mutations in the MAPK signaling pathway. Phase I/II development of the drug for advanced cancers including, acute myeloid leukaemia and myelodysplastic syndromes is underway in the US. A phase I trial is underway in the US for pancreatic cancer.

Showing 11751 - 11760 of 13501 results