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Restrict the search for
vitamin a
to a specific field?
Status:
Investigational
Source:
NCT02272478: Phase 2/Phase 3 Interventional Unknown status Acute Myeloid Leukaemia
(2014)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Ganetespib (formerly called STA-9090) is a novel, injectable resorcinolic triazolone small molecule inhibitor of Hsp90, developed by Synta Pharmaceuticals. Ganetespib inhibits the growth of many tumor types in vitro and in vivo including AML, ALL, CML, NHL, neuroblastoma, Ewing sarcoma, rhabdoid cancer, rhabdomyosarcoma, melanoma, and carcinomas of the breast, lung, prostate, bladder and colon7-10,14-27. Ganetespib has being studied in multiple adult oncology indications. The 50% inhibitory concentrations (IC50) for Ganetespib against malignant mast cell lines are 10-50 times lower than that for 17-AAG, indicating that triazolone class of HSP90 inhibitors likely exhibits greater potency than geldanamycin based inhibitors. Ganetespib inhibits MG63 cell lines with IC50 of 43 nM. Ganetespib binds to the ATP-binding domain at the N-terminus of Hsp90 and serves as a potent Hsp90 inhibitor by causing degradation of multiple oncogenic Hsp90 client proteins including HER2/neu, mutated EGFR, Akt, c-Kit, IGF-1R, PDGFRα, Jak1, Jak2, STAT3, STAT5, HIF-1α, CDC2 and c-Met as well as Wilms' tumor 1. Ganetespib, at low nanomolar concentrations, potently arrests cell proliferation and induces apoptosis in a wide variety of human cancer cell lines, including many receptor tyrosine kinase inhibitor- and tanespimycin-resistant cell lines. Ganetespib exhibits potent cytotoxicity in a range of solid and hematologic tumor cell lines, including those that express mutated kinases that confer resistance to small-molecule tyrosine kinase inhibitors. Ganetespib has been studied in 5 completed Synta-sponsored clinical trials (Studies 9090-02, 9090-03, 9090-04, 9090-05, and 9090-07) and 3 completed Synta-sponsored studies in normal healthy volunteers (9090-12, 9090-13, and 9090-15). Ganetespib is currently being studied in 6 Synta-sponsored clinical trials. Studies include: one Phase 1 study, three Phase 2 studies, one Phase 2b study, and one Phase 3 study. Ganetespib is also being studied in 24 Investigator Sponsored Trials (ISTs)
Status:
Investigational
Source:
INN:tocofenoxate [INN]
Source URL:
Class (Stereo):
CHEMICAL (MIXED)
Tocofenoxate is a semisynthetic tocopherol derivative. Vitamin E supplement.
Status:
Investigational
Source:
NCT04028492: Phase 3 Interventional Recruiting Idiopathic Gastroparesis
(2019)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Tradipitant is a neurokinin 1 receptor antagonist. The dose of 50 mg of tradipitant given orally for 4 weeks was not superior to placebo in reducing itch intensity in patients with atopic dermatitis. However, in a subsequent study, in which a higher dose (85 mg) was administered for 8 weeks, significant antipruritic effect compared with placebo was recorded. Tradipitant is in phase III clinical trial for the treatment of atopic dermatitis and gastroparesis. Vanda Pharmaceuticals plans a phase III trial in Motion Sickness in 2019.
Status:
Investigational
Source:
NCT00830154: Phase 2/Phase 3 Interventional Completed Stuttering
(2009)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Pagoclone is an anxiolytic agent from the cyclopyrrolone family, related to better-known drugs such as the sleeping medication zopiclone. It binds with the roughly equivalent high affinity (0.7–9.1 nM) to the benzodiazepine binding site of human GABAA receptors containing either a α1, α2, α3 or α5 subunit. It is a partial agonist at α1-, α2- and α5-containing GABAA receptors and a full agonist at receptors containing a α3 subunit. Pagoclone produces anxiolytic effects with little sedative or amnestic actions at low doses.
Status:
Investigational
Source:
NCT00820079: Phase 2 Interventional Completed Gastroesophageal Reflux
(2008)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
ADX 10059 is a first-in-class reflux inhibitor that works by reducing activation of the metabotropic glutamate receptor 5 (mGluR5) through negative allosteric modulation (NAM). This approach may lead to a new class of drugs that addresses the causes of GERD rather than just the symptoms. ADX 10059 is a potent selective NAM of the mGluR5, with
an IC50 of 17.1 nM on hmGluR5 showing good selectivity
compared with > 65 other receptors, transporters, ion
channels and enzymes. ADX 10059 completed Phase IIb testing in gastroesophageal reflux disease (GERD) and migraine prevention, demonstrated significant potential in a non-human primate model of Parkinson's disease levodopa induced dyskinesia (PD-LID). However, Addex Pharmaceuticals announced the discontinuation of development of ADX 10059 in December 2009 due to liver enzyme changes.
Class (Stereo):
CHEMICAL (RACEMIC)
Acridorex (BS 7573a) is an anorectic agent.
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Ocfentanil, a compound structurally similar to the opioid analgesic fentanyl, was developed in the early 1990’s with the hope that it would provide a better clinical safety profile than fentanyl. The receptor pharmacology of ocfentanil appears to share pharmacodynamic effects with fentanyl and other μ opioid agonists, including analgesia, sedation, and respiratory depression. In rodents, ocfentanil was approximately 2.5 times more potent as an analgesic than fentanyl and had a shorter duration of action. Because the preclinical research suggested that ocfentanil had a better safety profile than fentanyl, it was selected for clinical evaluation. Like other μ opioid agonists, ocfentanil has been reported to produce itching, nausea, sedation, and severe respiratory depression. Chest pain, psychosis, and agitation have also been reported. In humans, however, ocfentanil had a similar potency (3 ug/kg ocfentanil produced effects that were comparable to 5 ug/kg fentanyl) and side-effects profile as fentanyl so further clinical development was discontinued. Ocfentanil is not approved in any country for medical useand is under national control in Canada, the United Kingdom, and China.
Class (Stereo):
CHEMICAL (ACHIRAL)
Recainam is an investigational Class I anti-arrhythmic agent that has been studied for its potential in treatment of heart rhythm disorders. No severe adverse events of intravenous recainam adminstration were reported in a study in patients with frequent ventricular premature complexes (extra heart beats) and nonsustained ventricular tachycardia (abnormally fast heartbeat).
Status:
Investigational
Source:
NCT02342249: Phase 2 Interventional Completed Influenza A
(2014)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
JNJ-872 is an inhibitor of influenza virus replication that offers a potential for the treatment of pandemic and seasonal influenza.
Class (Stereo):
CHEMICAL (MIXED)
Odalprofen was used as an analgesic. Information about the current use of this compound is not available.
