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

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Showing 31 - 40 of 8923 results

Status:
Investigational
Source:
USAN:Actodigin
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Actodigin is a semisynthetic cardiac glycoside compounded from digitoxigenin and one molecule of glucose. In addition, unlike the naturally occurring glycosides, the C-2 instead of the C-3 atom of the lactone ring is attached to the steroid nucleus. Actodigin is a cardiovascular agent. When injected at 30 min invervals into dogs with barbiturate-induced heart failure, actodigin caused a marked positive inotropic action of short duration. It converted arrhythmia to normal sinus rhythm. Actodigin effectively and quickly reduced the ventricular rate in patients with atrial fibrillation. Actodigin, because of its rapid onset and brief duration of action, may be useful in controlling the ventricular rate in patients with atrial fibrillation.
Status:
Investigational
Source:
NCT01588756: Phase 1/Phase 2 Interventional Completed Healthy
(2010)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
INN:ruvazone
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
NCT04655599: Phase 1 Interventional Recruiting Irritable Bowel Syndrome
(2021)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT02345382: Phase 1 Interventional Completed Leukemia
(2015)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Atuveciclib (previously known as BAY 1143572) was developed as a highly selective inhibitor of positive transcription elongation factor b (PTEFb) /CDK9 for the treatment of cancer. PTEFb is a heterodimer of CDK9 and one of four cyclin partners, cyclin T1, cyclin K, cyclin T2a or cyclin T2b. Atuveciclib also inhibits RNA polymerase II (Ser2) phosphorylation and downregulate MYC protein expression in hematologic malignancies. The drug participated in phase I clinical trials in subjects with advanced acute leukemia and for patients with advanced malignancies. Information about further studies for these types of cancer is not available. Recently published article has shown that atuveciclib enhanced the antineoplastic effects of cisplatin and promoted inhibitory effects on breast cancer stem-like cells grown as mammospheres. In addition, was suggested that CDK9 could be a potential therapeutic target in aggressive forms of CDK9-high triple-negative breast cancer (TNBC).
Status:
Investigational
Source:
INN:CLOMOXIR [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Clomoxir (POCA, B 807-27) is a potent inhibitor of mitochondrial fatty acid oxidation at the stage of carnitine palmitoyltransferase I (CPT-I). It acts by the tight binding of POCA-CoA to this enzyme. The compound demonstrated hypoketonaemic and hypoglycaemic activities in fasted normal and diabetic rats.
Status:
Investigational
Source:
NCT03101085: Phase 1/Phase 2 Interventional Recruiting Alzheimer Disease
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



EQUOL, (-)- is the (S)-enantiomer of the naturally-occurring isoflavandiol estrogen, equol. EQUOL, (-)- (US-131), is a first-in-class, nonsteroidal, nonhormonal, small molecule (S-equol) that has higher selectivity toward estrogen receptor β (ERβ) than to estrogen receptor α (ERα). S-equol is the exclusive product of human intestinal bacterial synthesis from soy isoflavones. Two-Phase 1 studies have seen completed and published; AUS-131 was safe and well-tolerated in humans. A Phase 2a trial in menopausal women with vasomotor symptoms (VMS) has recently been completed (169 patients). A second Phase 2a trial in men with benign prostatic hyperplasia (BPH) is on track.
Status:
Investigational
Source:
NCT03740100: Phase 2 Interventional Completed HNSCC
(2019)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


PQR-309 is an orally bioavailable pan inhibitor of phosphoinositide-3-kinases (PI3K) and inhibitor of the mammalian target of rapamycin (mTOR), with potential antineoplastic activity. PI3K/mTOR kinase inhibitor PQR-309 inhibits the PI3K kinase isoforms alpha, beta, gamma and delta and, to a lesser extent, mTOR kinase, which may result in tumor cell apoptosis and growth inhibition in cells overexpressing PI3K/mTOR. By inhibiting mTOR to a lesser extent than PI3K, PQR-309 does not interfere with the mTOR-mediated negative feedback loop on PI3K signaling. Blocking the negative feedback loop would potentially increase PI3K signaling and decrease therapeutic efficacy. PQR-309 is in phase II clinical trial for the treatment of glioblastoma, head and neck cancer, lymphoma and breast cancer. Common adverse events included fatigue, hyperglycemia, nausea, diarrhea, constipation, rash, anorexia and vomiting.
Status:
Investigational
Source:
INN:azaspirium chloride
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Azaspirium was studied as a spasmolytic and antihypertensive agent.
Status:
Investigational
Source:
NCT01147029: Phase 1 Interventional Terminated Unspecified Adult Solid Tumor, Protocol Specific
(2008)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Glutathione arsenoxide (GSAO) is a peptide trivalent arsenical that has potential anti-angiogenic capability, suggesting that it could be used for treatment in cancers where tumor metastasis relies on new blood vessel formation (angiogenesis). Endothelial cell proliferation drives new blood vessel formation. GSAO treatment causes a concentration-dependent increase in superoxide levels, ATP depletion, mitochondrial depolarization, and apoptosis in proliferating, but not endothelial cells. GSAO is able to block blood flow to solid tumors in mice, thereby inhibiting tumor growth in mice with no apparent toxicity at efficacious doses. Initial experiments have implicated GSAO in perturbing mitochondrial function. Other molecular effects of GSAO in human cells, for example on the phosphorylation of proteins, are still largely unknown. A phase I clinical trial has been terminated.