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

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Showing 31 - 40 of 2117 results

Status:
Investigational
Source:
INN:moxnidazole
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Moxnidazole is an antiparasitic drug suitable for oral use against parasites in farm animals. administration of Moxnidazole in the drinking water gave good prophylaxis of dysentery in swine, histomoniasis in hens and turkeys, and trichomoniasis in pigeons. Isolated relapses were due to renfections and were successfully treated by another dose of the drug.
Status:
Investigational
Source:
INN:nifursol
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Nifursol is an antibiotic of the nitrofuran class which inhibits the growth of the protozoa Histomonas meleagridis but is non-lethal. Although previously approved as a prophylactic feed additive for turkeys, the European Union has since banned Nifursol use in agricultural operations.
Status:
Investigational
Source:
INN:bicozamycin
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Bicyclomycin has been used to treat diarrhea in humans and bacterial diarrhea in calves and pigs and is marketed by Fujisawa (Osaka, Japan) under the trade name Bicozamycin. This drug is the selective inhibitor of rho, a member of the RecA-type ATPase class of enzymes that use nucleotide contacts to couple oligonucleotide translocation to ATP hydrolysis.
Plinabulin (formerly known as NPI-2358) is a potent microtubule-destabilizing agent that exerts its effect by binding to the colchicine-binding site of tubulin. Plinabulin projects its potent antitumor activity against a broad spectrum of tumor cell lines. This drug in combination with docetaxel is under development by BeyondSpring Pharmaceuticals in a worldwide Phase 3 clinical trial for non-small cell lung cancer. Pegfilgrastim is also in phase II clinical trial for the prevention of chemotherapy-induced neutropenia, where docetaxel, doxorubicin, and cyclophosphamide (TAC) were used as the chemotherapy. Plinabulin also possessed antitumor activity in animal models with multiple myeloma cancer cells, where the JNK protein appeared to be a primary target of plinabulin.
Sonolisib (PX-866) is a small-molecule inhibitor of the alpha, gamma, and delta isoforms of phosphoinositide 3-kinase (PI3K) with potential antineoplastic activity. Sonolisib inhibits the production of the secondary messenger phosphatidylinositol-3,4,5-trisphosphate (PIP3) and activation of the PI3K/Akt signaling pathway, which may result in inhibition of tumor cell growth and survival in susceptible tumor cell populations. Inhibition of the PI3K pathway with Sonolisib leads to inhibition of cell growth and decreased activation of downstream targets in GBM, both in vitro and in vivo, using U87–tumor-bearing mice, including Akt, S6, and mTOR. Sonolisib was in phase II clinical trials by Oncothyreon for the treatment of glioblastoma multiforme and castration-resistant prostate cancer (CRPC). It was in phase I/II clinical trials for the treatment of malignant melanoma, non-small cell lung cancer and Head and neck cancer. In clinical trials, Sonolisib was well tolerated, with common side effects being diarrhea, nausea, vomiting, and elevated liver enzymes. However, no recent development has been reported.
Status:
Investigational
Source:
INN:sivifene [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Sivifene (also known as A-007), a triaryl hydrazone that produced objective responses when applied topically. During preclinical studies, sivifene was observed to upregulate both cutaneous and systemic T-lymphocytes, in particular, CD4/8+ lymphocyte subtypes. The current mechanism of action for the drug is unknown however is assumed that it can show its immunomodulating properties through the upregulation of the CD45 T lymphocyte cell surface receptor. Sivifene was being evaluated for its anticancer activities in melanoma, breast cancer, Kaposi's sarcoma, and lymphoproliferative disorders. The drug as a 0.25% gel is confirmed as an effective palliative treatment option for cutaneous metastases from cancers. Skin reactions were minimal, tolerated, and no cessation of treatment was required. However, the further development of this drug apparently has been discontinued.
Status:
Investigational
Source:
INN:tenamfetamine [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Tenamfetamine (also known as 3,4-methylenedioxyamphetamine (or MDA)) is a hallucinogen that acts as a serotonergic 5-HT2A receptor agonist and releases monoamines by interacting with monoamine plasmalemmal transporters. Tenamfetamine had no accepted medical use and it was scheduled as a controlled substance in the US in 1970. Despite appearing in illicit drug preparations, tenamfetamine has not been studied in humans in over 30 years. In 2010 was published article where was described the action of tenamfetaminea in a clinical trial in humans. In this trial was shown that the drug had induced mystical-type experiences and, in at least some individuals, closed-eye visions. However, during that experiment were impossible to provide strong evidence for changes in the efficacy of top-down influences on perception or acutely increased occipital cortex excitation.
Status:
Investigational
Source:
INN:terbogrel
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Terbogrel, an agent having two pharmacodynamic actions, namely inhibition of thromboxane A2 synthase and antagonism of the thromboxane A2 receptor. The antithrombotic effect of terbogrel was dose-dependent and was associated with enhanced prostacyclin production. The drug was studied for the treatment of peripheral vascular disorders, pulmonary hypertension, and thrombosis. Terbogrel participated in phase II clinical trial to investigate its safety and efficacy in patients with primary pulmonary hypertension, however, this study was discontinued due to terbogrel’s induction of leg pain.
Ritanserin (INN, USAN, BAN) is a serotonin receptor antagonist which was never marketed for clinical use but has been used in scientific research. In humans, ritanserin increases deep slow-wave sleep, improved liveliness in a variety of psychiatric disorders and facilitated participation in behaviour therapy. During clinical trials, unexpected observations indicated that ritanserin may be of value in treating obsessive-compulsive disorder, acute mania, negative symptoms of schizophrenia, drug addicts, etc. Clinical observations confirmed the efficacy of ritanserin in the chronic withdrawal phase after detoxification from ethanol. Ritanserin had been in phase III clinical trials by Janssen L.P. for the treatment of anxiety disorder and major depressive disorder. However, the clinical development of ritanserin was discontinued.
Status:
Investigational
Source:
INN:claficapavir [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)