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

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Showing 501 - 510 of 13311 results

Status:
Investigational
Source:
INN:ciprokiren
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Ciprokinen is a renin inhibitor discovered by Roche. Ciprokinen inhibited human renin in a buffer and human plasma with an IC50 of 0.07 and 0.65 nmol/L, respectively. In animal models, acute and chronic administration of ciprokinen lead to a reduction in arterial blood pressure. Development of ciprokinen was discontinued at a preclinical stage.
Status:
Investigational
Source:
NCT00244751: Phase 2 Interventional Completed Cirrhosis, Liver
(2005)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Farglitazar is a non-thiazolidinedione insulin sensitizer and agonist of peroxisome proliferator-activated receptor-gamma. GlaxoSmithKline was developing farglitazar for the treatment of liver fibrosis and Type 2 diabetes mellitus.
Status:
Investigational
Source:
NCT04671303: Phase 2 Interventional Completed Lung Cancer
(2021)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



AST-1306, also known as Allitinib, is an orally active potent, selective, irreversible inhibitor of the HER family of receptor tyrosine kinases. AST-1306 inhibits the enzymatic activities of wild-type epidermal growth factor receptor (EGFR) and ErbB2 as well as EGFR resistant mutant in both cell-free and cell-based systems. AST1306 potently suppressed tumor growth in ErbB2-overexpressing adenocarcinoma xenograft and FVB-2/N(neu) transgenic breast cancer mouse models. Allitinib is in Phase I clinical trial for the treatment of advanced solid tumors. Serious adverse effects detected were: diarrhea, dehydration and hyperbilirubinemia.
Status:
Investigational
Source:
INN:nictindole
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Nictindole is a non-steroidal anti-inflammatory agent. It is a thromboxane synthetase inhibitor. Nictindole inhibits generation of TXA2 in human platelet rich plasma.
Status:
Investigational
Source:
INN:coumamycin [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Coumermycin is from the aminocoumarin class of antibiotic compounds which acts by inhibiting DNA gyrase. Coumermycin is effective against gram-positive bacteria, but not gram-negative bacteria. Coumermycin its derivatives have been studied since the 1950's as potential antibiotic. However, it has seen little to no clinical development because of its low water solubility, toxicity profile, and ineffectiveness against gram-negative bacteria.
Status:
Investigational
Source:
NCT00006363: Phase 3 Interventional Completed Adult Acute Basophilic Leukemia
(2000)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Valspodar (PSC-833) is a derivative of cyclosporin but devoid of the immunosuppressive and nephrotoxic properties seen in cyclosporin A. It exhibited high-affinity binding to Mdr1 P-glycoprotein (P-gp) and demonstrated multidrug resistance-reversing activity superior to cyclosporin A and verapamil both in vitro and in vivo. Preclinical and phase I/II clinical data have indicated that plasma levels of PSC-833 with multidrug resistance-reversing activities are achievable. Potent inhibition of intestinal, hepatobiliary and blood-brain barrier P-gp function has been demonstrated. The toxicity profiles of valspodar are acceptable and dose-limited by transient and reversible cerebellar ataxia. It has shown multidrug resistance-modulating activities towards acute myeloid leukemia, multiple myeloma and ovarian cancer in phase I/II clinical trials. However, the company discontinued development of valspodar in April 2001 following disappointing results reported from several multicentre phase III studies.
Status:
Investigational
Source:
NCT03201419: Phase 2 Interventional Completed Nocturia
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT03019653: Phase 1 Interventional Completed Heart Failure
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT04205227: Phase 1/Phase 2 Interventional Active, not recruiting Cancer
(2020)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

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

Class (Stereo):
CHEMICAL (ABSOLUTE)