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Restrict the search for
m didanosine
to a specific field?
Status:
Investigational
Source:
INN:mavelertinib [INN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
PF-06747775 is an irreversible pyrrolopyrimidine inhibitor of epidermal growth factor receptor (EGFR) T790M mutants which provides potent EGFR activity against the four common mutants (exon 19 deletion (Del), L858R, and double mutants T790M/L858R and T790M/Del), selectivity over wild-type EGFR, and desirable ADME properties. The third-generation class of EGFR tyrosine kinase inhibitors PF-06747775 is a clinical candidate drug for treatment of non-small-cell lung cancer (NSCLC) driven by mutant EGFR.
Status:
Investigational
Source:
INN:icosabutate [INN]
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Icosabutate (also known as PRC-4016 or NST-4016), a cholesterol ester transfer protein inhibitor was developed by NorthSea Therapeutics for the treatment of combined dyslipidemias and hypertriglyceridemia. Icosabutate successfully completed phase II clinical trial for hypertriglyceridemic subjects, where was studied the drug efficacy and safety. In April 2018 NorthSea Therapeutics announced that its lead product, icosabutate would be further developed as an effective and safe therapeutic approach to treating both non-alcoholic steatohepatitis and its associated comorbidities.
Status:
Class (Stereo):
CHEMICAL (ACHIRAL)
Monophosphothiamine is thiamine derivative used for the treatment of neuritis, polyneuritis, asthenic conditions (weakness), as an additional remedy for chronic blood circulation insufficiency, chronic gastritis accompanied by motor and secretory disorders functions of the stomach. Monophosphothiamine underwent metabolic phosphorylation to active metabolite thiamine pyrophosphate, that acts as a coenzyme in the different metabolic process.
Status:
Investigational
Source:
NCT00103350: Phase 1/Phase 2 Interventional Completed Myocardial Infarction
(2005)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
TG-100115 is a potent dual inhibitor of PI3K-gamma and PI3K-delta. TG-100115 has broad anti-inflammatory activities. TG-100115 provided potent cardioprotection, reducing infarct development and preserving myocardial function. In murine models of asthma and acute stages of chronic obstructive pulmonary disease, aerosolized TG100-115 demonstrated not only markedly inhibited anti-inflammatory activity but also, in the case of the asthma model, improved functional outcome for the test animals. TG-100115 can be used as a potent TRPM7 kinase inhibitor and a potent inhibitor of breast cancer cell migration.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
TAK-063 is a highly potent, selective, and orally active phosphodiesterase 10A (PDE10A) inhibitor with IC50 of 0.30 nM; >15000-fold selectivity over other PDEs. TAK-063 is currently being evaluated in clinical trials for the treatment of schizophrenia. Phosphodiesterase 10A (PDE10A) is a cAMP/cGMP phosphodiesterase highly expressed in medium spiny neurons (MSNs) in the striatum. TAK-063 represents a promising drug for the treatment of schizophrenia with potential for superior safety and tolerability profiles.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
RRX-001, also known as ABDNAZ, is a dinitroazetidine derivative with potential radiosensitizing activity. Upon administration, RRx-001 is able to dilate blood vessels, thereby increasing tumor blood flow and thus improving oxygenation to the tumor site. By increasing oxygen levels, these tumor cells may be more susceptible to radiation therapy. Tumor hypoxia is correlated with tumor aggressiveness, metastasis and resistance to radiotherapy. In mouse models, RRx-001 administered intravenously as a single agent was equipotent to cisplatin while better tolerated. RRx-001 also showed activity as a radiosensitizer in both in vitro and in vivo models. The activity of RRx-001 is thought to be associated with a nucleophilic substitution by circulating thiol compounds and covalent binding of RRx-001 to cysteinyl residues in Hb, followed by the generation of nitrogen oxides. During 2014-2015 EpicentRx has launched Phase 2 trials in brain, colorectal, non-small cell lung, small cell lung and cholangiocarcinoma both alone and in combination. The anti-proliferative effects of RRx-001 are not explainable via a single mechanism. RRx-001 exerts its anti-proliferative effect, at least partially, through interference with glucose 6 phosphate dehydrogenase (G6PD), a key enzyme in the pentose phosphate pathway, responsible for maintaining adequate levels of the major cellular reductant, NADPH.
Status:
Investigational
Source:
INN:seltorexant [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
2-(4,6-DIMETHYLPYRIMIDIN-2-YL)-5-((2-FLUORO-6-(2H-1,2,3-TRIAZOL-2-YL)PHENYL)CARBONYL)OCTAHYDROPYRROLO(3,4-C)PYRROLE (Seltorexant, MIN 202), a small molecule, selective orexin receptor type-2 antagonist, is being developed by Minerva Neurosciences and Janssen Research & Development for the treatment of insomnia and major depressive disorder. Seltorexant has shown high in vitro affinity
(affinity pKi =8.0 and 6.1 for OX2R and OX1R respectively) for the
human OX2R and approximates two logs selectivity ratio versus
its affinity for the OX1R. Seltorexant demonstrated a dose-dependent normalization of sleep and a trend towards improvement of subjective depressive symptoms in antidepressant-treated MDD
patients with residual insomnia. Additionally, seltorexant’s
favorable PK profile as a potential sedative-hypnotic drug was
confirmed in a MDD population and did not demonstrate unacceptable adverse events or unwanted next-day CNS effects. Seltorexant is in phase II clinical trials for both insomnia and MDD.
Status:
Class (Stereo):
CHEMICAL (ACHIRAL)
Allocupreide is a copper(l) complex used as an antiinflammatory drug and antiarthritic agent. It was used for the treatment of trigeminal neuralgia.
Status:
Investigational
Source:
INN:trempamotide [INN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Trempamotide immunological agent used for active immunization. It is an antineoplastic drug.
Status:
Investigational
Source:
NCT03189992: Phase 1 Interventional Unknown status Malignant Tumor of Small Intestine Metastatic to Liver
(2014)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Cinobufotalin, the bufadienolide isolated from toad venom,
has displayed antitumor activities in many in vitro systems. It has been shown that cinobufotalin induced significant apoptosis in cultured human lymphoma U-937 cells. It induced DNA fragmentation, mitochondrial membrane
potential decrease, and reactive oxygen species (ROS)
production in U-937 cells. Cinobufotalin induces cytotoxic effect in cultured lung cancer cells. Cinobufotalin (1/5 mg/kg, i.p. twice
daily, for 7 days) significantly inhibited A549 xenograft growth in
mice. Further, same cinobufotalin administration improved mice
survival at week five. Cinobufotalin administration didn’t
significantly affect mice body weight, indicating the relative safety
of this regimen. Thus, cinobufotalin inhibits A549 xenograft
growth in vivo and improves mice survival.
