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

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Showing 49161 - 49170 of 55039 results

Status:
Investigational
Source:
NCT00920205: Phase 1 Interventional Completed Cancer
(2009)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

MPC-3100 is a fully synthetic, orally bioavailable, Hsp90 inhibitor developed by Myriad Pharmaceuticals, Inc for cancer treatment. MPC-3100 targets the N-terminal ATP-binding site of Hsp90 and blocks the activity of ATPase. MPC-3100 shows a broad spectrum anti-proliferative activity against various cancer cell lines, such as HCT-116, NCI-N87 and DU-145. MPC-3100 also inhibits tumor growth in the NCI-N87 gastric cancer xenograft mode. Moreover, pharmacokinetics studies show that MPC-3100 displays a superior oral pharmacokinetics profile, good overall exposure and a reasonable hepatic clearance rate. Phase I clinical studies demonstrate MPC-3100 is safe and tolerated when administered at doses below 600 mg per day
Status:
Investigational
Source:
NCT04021368: Phase 1 Interventional Active, not recruiting Acute Myeloid Leukemia
(2019)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Indoximod is an orally available Indoleamine 2,3-dioxigenase inhibitor. It shows higher potency in reversing IDO-mediated T cell suppression. Indoximod improves the efficacy of multiple chemotherapeutics agents and some immunological checkpoints mediators in Phase I/II clinical studies for metastatic breast cancer, metastatic melanoma, non-small cell lung cancer, primary malignant brain tumors, metastatic pancreatic cancer, as well as metastatic prostate cancer.
Status:
Investigational
Source:
NCT02654899: Phase 1 Interventional Terminated Hypercholesterolemia
(2015)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT04524351: Phase 1/Phase 2 Interventional Completed Alzheimer Disease
(2020)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Phenserine, a derivative of physostigmine, was first described as an inhibitor of acetylcholinesterase (AChE) and was shown to improve cognition in various experimental paradigms in rodents and dogs. It was clinically tested for Alzheimer's disease, with moderate success in initial Phase II studies. Phenserine is also unique because of differing actions of its enantiomers: (-)-phenserine is the active enantiomer for inhibition of AChE, whereas ( )-phenserine (Posiphen®) has weak activity as an AChE inhibitor and can be dosed much higher. Posiphen® is a small, hydrophobic, orally available molecule that enters the brain readily. It is the only drug ever described that inhibits more than one neurotoxic aggregating protein. Posiphen® inhibits synthesis of amyloid precursor protein (APP), tau and α-Synuclein. mRNA translation of neurotoxic aggregating proteins is up-regulated by iron (Fe) and down-regulated by iron regulatory protein-1 (IRP1). Posiphen® interferes with this second step of the common cascade of the aggregating proteins. It enhances the binding and/or activity of IRP1 to the iron response element (IRE) stem loop in the 5’UTR of the mRNAs of neurotoxic aggregating proteins, therefore specifically lowering their synthesis. By potentiating the IRE/IRP1 complex, Posiphen® lowers the level of free mRNA to be translated by the ribosome. Posiphen® is in development for the treatment neurodegenerative diseases.
Status:
Investigational
Source:
INN:imlunestrant [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

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

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
NCT03189914: Phase 1/Phase 2 Interventional Completed Metastatic Pancreatic Cancer
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Fluorocyclopentenylcytosine (RX-3117) is a novel small molecule nucleoside compound that is incorporated into DNA or RNA of cancer cells and inhibits both DNA and RNA synthesis which induces apoptotic cell death of tumor cells. Fluorocyclopentenylcytosine also mediates the down-regulation of DNA methyltransferase 1 (DNMT1), an enzyme responsible for the methylation of cytosine residues on newly synthesized DNA and also a target for anticancer therapies. Preclinical studies have shown Fluorocyclopentenylcytosine to be effective in both inhibiting the growth of various human cancer xenograft models, including colon, lung, renal and pancreas, as well as overcoming chemotherapeutic drug resistance. Fluorocyclopentenylcytosine has demonstrated a broad spectrum anti-tumor activity against 50 different human cancer cell lines and efficacy in 12 different mouse xenograft models. The efficacy in the mouse xenograft models was superior to that of gemcitabine. In addition, in human cancer cell lines made resistant to the anti-tumor effects of gemcitabine, Fluorocyclopentenylcytosine still retains its full anti-tumor activity. In August 2012, Rexahn reported the completion of an exploratory Phase I clinical trial of Fluorocyclopentenylcytosine in cancer patients conducted in Europe, to investigate the oral bioavailability, safety and tolerability of the compound. In this study, oral administration of Fluorocyclopentenylcytosine demonstrated an oral bioavailability of 34-58% and a plasma half-life (T1/2) of 14 hours. In addition, Fluorocyclopentenylcytosine was safe and well tolerated in all subjects throughout the dose range tested. Fluorocyclopentenylcytosine is in phase I/II clinical trials by Rexahn for the treatment of bladder cancer and pancreatic cancer. This compound was granted Orphan Drug Designation by the U.S. Food and Drug Administration (FDA) for the treatment of patients with pancreatic cancer in September 2014.
Status:
Investigational
Source:
NCT01241422: Phase 2 Interventional Completed Asthma
(2010)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Cerdulatinib is an oral, dual spleen tyrosine kinase (Syk) and janus kinase (JAK) inhibitor that uniquely inhibits two key cell signaling pathways that promote cancer cell growth in certain hematologic malignancies – the B-cell receptor pathway via Syk and key cytokine receptors via JAK Being developed to treat patients with hematologic cancers, specifically those who have relapsed or who have not responded to prior therapies. Cerdulatinib is in Phase 2 study evaluating the safety and efficacy of cerdulatinib in patients with relapsed/refractory B-cell malignancies who have failed multiple therapies.

Showing 49161 - 49170 of 55039 results