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

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Showing 1941 - 1950 of 24423 results

Status:
Investigational
Source:
INN:fasiplon
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Fasiplon (RU 33203), an imidazo[1,2-a]pyrimidine derivative, is agonist of GABA(A) receptors at benzodiazepine binding site. It was in preclinical studies for the treatment of anxiety.
Status:
Investigational
Source:
Zhonghua Nan Ke Xue. Apr 2015;21(4):338-41.: Not Applicable Human clinical trial Completed Infertility, Male
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Calcimycin is an ionophore, polyether antibiotic from Streptomyces chartreusensis. It binds and transports calcium and other divalent cations across membranes and uncouples oxidative phosphorylation while inhibiting ATPase of rat liver mitochondria. The substance is used mostly as a biochemical tool to study the role of divalent cations in various biological systems. Calcimycin has antibiotic properties against gram-positive bacteria and fungi. Inex Pharmaceuticals Corporation (Canada) reported an innovative application of Calcimycin. "Inex" used Calcimycin as a molecular tool in order to make artificial liposomes loaded with anti-cancer drugs such as Topotecan. In in vitro fertilization (IVF) field, Ca Ionophore can be used in case of low fertilization rate after ICSI procedure, particularly with Globozoospermia (Round Head sperm syndrome), Ca Ionophore plays role in oocyte activation after ICSI. Recommended use is 0.5 microgram/ml twice for 10 min interrupted with fresh media with 30 min incubation, followed with regular injected eggs culture for IVF
Pralnacasan is a potent, non-peptide inhibitor of interleukin-1beta converting enzyme (ICE, aka Caspase-1). It was originally discovered by Vertex Pharmaceuticals and licensed for development to Aventis Pharma. In 2003 Aventis and Vertex Pharmaceuticals agreed to voluntarily discontinue development based on results from a 9-month animal toxicity trial that showed liver abnormalities due to chronic high doses of pralnacasan. Pralnacasan has also been investigated for the treatment of Partial Epilepsy; advancing to Phase II clinical trials.
Status:
Investigational
Source:
NCT03292406: Phase 2 Interventional Completed Cutaneous T Cell Lymphoma
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Resiquimod is an imidazoquinolinamine and Toll-like receptor (TLR) agonist with potential immune response modifying activity. Resiquimod exerts its effect through the TLR signaling pathway by binding to and activating TLR7 and 8 mainly on dendritic cells, macrophages, and B-lymphocytes. This induces the nuclear translocation of the transcription activator NF-kB as well as activation of other transcription factors. This may lead to an increase in mRNA levels and subsequent production of cytokines, especially interferon-alpha (INF-a) and other cytokines, thereby enhancing T-helper 1 (Th1) immune responses. In addition, topical application of resiquimod appears to activate Langerhans' cells, leading to an enhanced activation of T-lymphocytes. Resiquimod is used as a topical gel[1] in the treatment of skin lesions[2] such as those caused by the herpes simplex virus[3][4] and cutaneous T cell lymphoma. Due to its immunostimulatory activity, this agent may potentially be used as a vaccine adjuvant.
Status:
Investigational
Source:
INN:losigamone [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Losigamone possesses an unique anticonvulsant activity profile and has an excellent tolerability. Losigamone causes dose-dependent inhibition of the tonic hind leg extension produced by electric shock, pentylenetetrazole, bicuculline, nicotine and 4-aminopyridine. Losigamone also inhibits clonic seizures induced by pentylenetetrazole, bicuculline and picrotoxin, whereas it has no effect on the hind leg extension caused by strychnine and picrotoxin or the clonic seizures induced by NMDA. Losigamone had been in phase III clinical trial for the treatment of partial epilepsies. However, this development was discontinued.
Status:
Investigational
Source:
NCT00090532: Phase 1/Phase 2 Interventional Terminated Age-Related Macular Degeneration
(2004)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Pfizer developed AG-013958, also known as AG-13958 for treatment of age-related macular degeneration (AMD). As a VEGFR tyrosine kinase inhibitor, AG13958 was targeted to FLT/TYK receptor inhibition.
Status:
Investigational
Source:
INN:morpheridine
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Morpheridine is a pethidine analog with strong analgesic activity. Morpheridine does not cause convulsions, although it produces the standard opioid side effects such as sedation and respiratory depression. Morpheridine is not currently used in medicine and is a Schedule I drug which is controlled under United Nations drug conventions.
Status:
Investigational
Source:
INN:fananserin
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Fananserin is a potential antipsychotic compound with a high affinity for both D4 and 5-HT2A receptors, and negligible affinity for D2 receptors. Fananserin has been researched for the treatment of schizophrenia. Fananserin was the first selective D4/5-HT2A antagonist to undergo clinical trials for schizophrenia. It has a high affinity for D4 (Ki 2.9 nM) and 5-HT2A (Ki 0.37 nM) receptors and is over 100-fold selective versus H1, a1 adrenergic, 5-HT1A and D2 dopamine receptors. Development of this compound was halted following phase II clinical trials due to lack of efficacy.
Status:
Investigational
Source:
NCT03748758: Phase 1 Interventional Completed Healthy Adult Volunteers
(2018)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT00281736: Phase 2 Interventional Completed Esophageal Cancer
(2004)
Source URL:

Class (Stereo):
CHEMICAL (EPIMERIC)

2-(1-Hexyloxyethyl)-2-devinyl pyropheophorbide-a (HPPH), a chlorin-based photosensitize, is used in photodynamic therapy. It has been shown the therapeutic potential of HPPH in phase II clinical trials for the treatment of esophageal cancer. Besides, HPPH participated in clinical trials in treating patients with advanced non-small cell lung cancer that blocks the air passages. However, these studies were terminated.

Showing 1941 - 1950 of 24423 results