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Restrict the search for
m sacubitril
to a specific field?
Status:
Investigational
Source:
INN:darovasertib [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
FGF-401 is an inhibitor of human fibroblast growth factor receptor 4 (FGFR4), with potential antineoplastic activity. Upon administration, FGF401 binds to and inhibits the activity of FGFR4, which leads to an inhibition of tumor cell proliferation in FGFR4-overexpressing cells. FGFR4 is a receptor tyrosine kinase upregulated in certain tumor cells and involved in tumor cell proliferation, differentiation, angiogenesis, and survival. FGF-401 is an FGFR4 inhibitor in phase I/II clinical studies at Novartis for the treatment of positive FGFR4 and KLB expression solid tumors and hepatocellular carcinoma.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
CX-5461 represents an innovative-targeted agent with numerous differentiating features when compared to current options for treatment of hematologic cancers. CX-5461 is a first-in-class small molecule inhibitor of RNA polymerase I (Pol I) that triggers the nucleolar stress surveillance pathways to activate p53, without causing direct DNA damage. Molecular studies demonstrate that CX-5461 inhibits the initiation stage of rRNA synthesis and induces both senescence and autophagy, but not apoptosis, through a p53-independent process in solid tumor cell lines. Currently, CX-5461 is in clinical trial for patients with advanced hematological malignancies.
Status:
Investigational
Source:
JAN:TERALLETHRIN [JAN]
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Terallethrin is an insecticide that controls flying insects including houseflies, wasps and mosquitoes.
Status:
Investigational
Source:
NCT01724320: Phase 1 Interventional Unknown status Solid Tumors
(2012)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
PTX-008 (OTX008) is a calixarene-based compound and galectin-1 (Gal-1) inhibitor with potential anti-angiogenic and antineoplastic activities. Upon subcutaneous administration, galectin-1 inhibitor OTX008 binds Gal-1 which leads to Gal-1 oxidation and proteosomal degradation through a not yet fully elucidated mechanism, and eventually downregulates Gal-1. This decreases tumor cell growth and inhibits angiogenesis. Gal-1, a multifunctional carbohydrate-binding protein, is often overexpressed on tumor cells and plays a key role in cancer cell proliferation, apoptosis, tumor angiogenesis and evasion of immune responses. PTX-008 had been in phase I clinical trials for the treatment of solid tumours. This compound was originally discovered by University of Minnesota and PepTx, then licensed to OncoEthix (acquired by Merck Sharp & Dohme in 2014). However, no recent developments has been reported.
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.
