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Restrict the search for
m ulipristal acetate
to a specific field?
Status:
Investigational
Source:
INN:sardomozide [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Sardomozide (previously known as SAM486A or CGP-48664) was developed as an inhibitor of S-adenosyl-methionine-decarboxylase, a key enzyme for polyamine biosynthesis. Sardomozide possessed the broad-spectrum antiproliferative and antitumor activity. The drug participated in a phase II clinical trial as a monotherapy in patients with refractory or relapsed non-Hodgkin's lymphoma. In Phase II clinical trial in patients with metastatic melanoma, the drug didn’t have significant therapeutic potential. The further development of this drug was discontinued.
Status:
Investigational
Source:
INN:talaglumetad [INN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Talaglumetad (also known as LY-544344) is a bicyclohexane derivative patented by Eli Lilly and Company as modulators of metabotropic glutamate receptor. Talaglumetad acts as a prodrug of Eglumegad, a selective agonist of metabotropic glutamate receptors (mGluR2/3) and metabolized to release active compound by both human jejunal homogenates and rat liver homogenates. In experiments on mice, Talaglumetad was found to be as effective as diazepam for treating anxiety symptoms in several standard tests, but without producing any of the negative side effects of diazepam such as sedation and memory impairment.
Class (Stereo):
CHEMICAL (RACEMIC)
Picenadol is a 4-phenylpiperidine derivative and a racemic mixture whose mixed agonist-antagonist properties are a consequence of the d-isomer being a potent opiate agonist, whereas the I-isomer is an opioid antagonist. In the mouse writhing and rat tail heat tests, the analgesic potency of picenadol is estimated to be 1/3 that of morphine. Picenadol itself has weak antagonist activity, whereas the antagonist potency of the l-isomer is approx. 1/10 that of nalorphine. Picenadol has high affinity for both the mu and delta receptors but a markedly lower affinity for the kappa receptor. Extensive pharmacological investigations show picenadol to have a low potential to produce opiate-like side effects, including a low liability for abuse and physical dependence. Antinociceptive properties of picenadol arise from mu agonist actions of the dextrorotatory isomer and that the levorotatory isomer acts to limit the efficacy of the racemate.
Status:
Investigational
Source:
NCT01168791: Phase 3 Interventional Completed Soft Tissue Sarcoma
(2010)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Palifosfamide or ZIO-201 (isophosphoramide mustard; IPM), a bi-functional DNA alkylator, is the active metabolite of ifosfamide (IFOS). IFOS and the related drug cyclophosphamide (CPA) are widely used anti-cancer drugs. Both are pro-drugs and need to be metabolized to be active. Their clinical use is limited by the toxicity associated with some of their metabolites. Palifosfamide has shown efficacy in diverse cancer models. ZIOPHARM Oncology Inc, under license from Dekk-Tec Inc, was developing palifosfamide, a formulation of isophosphoramide mustard with tris(hydroxymethyl)aminomethane salt-stabilization (palifosfamide-tris) and previously with lysine-stabilization (palifosfamide-lys). Preclinical studies and phase I and I/II clinical trials demonstrated that palifosfamide-tris had an antitumor efficiency comparable or superior to that of ifosfamide. To date ZIO-201 is not present in ZIOPHARM pipeline.
Class (Stereo):
CHEMICAL (ACHIRAL)
Enpiprazole is a heterocyclic three-ringed pyrazolylalkyl piperazine derivative. Enpiprazole has a cataleptic action very similar to that of neuroleptics, and its effect on muscle relaxation is comparable with that of diazepam. Enpiprazole exerts anxiolytic properties in animals.
Status:
Investigational
Source:
NCT00087061: Phase 1/Phase 2 Interventional Completed Brain and Central Nervous System Tumors
(2004)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Gimatecan is a topoisomerase I inhibitor that is presently tested in phase II of clinical trials for the treatment of different cancers: glioma, glioblastoma, epithelial ovarian cancer, fallopian tube or peritoneal cancer. The drug recieved orphan designation for the treatment of glioma.
Class (Stereo):
CHEMICAL (UNKNOWN)
Targets:
Edatrexate (10-ethyl-10-deazaaminopterin or 10-EDAM) is an analog of methotrexate with improved pre-clinical antitumor activity, more selective cellular uptake, and with the more extensive formation of intracellular polyglutamate metabolites. This drug is a new dihydrofolate reductase inhibitor, which was studied in phase II clinical trial for the patients with different cancers. The studies were discontinued, for example, in advanced renal cell carcinoma edatrexate in the investigated dose and schedule had minimal activity and was toxic. In case of non-small-cell lung cancer, the dosing schedule of edatrexate did not appear to be improved compared to other chemotherapeutic regimens. In addition, edatrexate was involved in the experiment for the treatemnt of rheumatoid arthritis, but this study was also discontinued.
Status:
Investigational
Source:
NCT01631201: Phase 2 Interventional Completed Chlamydia Trachomatis Infection
(2012)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Rifalazil (also known as KRM-1648) is a derivative of the antibiotic rifamycin. This orally administered ansamycin is under evaluation for treatment of various bacterial infections. Rifalazil kills bacterial cells by blocking off the β-subunit in RNA polymerase. This drug was originally developed as a therapeutic agent to replace rifampin in the treatment of tuberculosis. It also showed potential to treat indications caused by chlamydia trachomatis and chlamydia pneumoniae. Furthermore, it has been suggested as a potential drug in the treatment of gastric ulcer disease (which is caused by Helicobacter pylori) and antibiotic-associated colitis. Phase II studies evaluated the efficacy and safety of this drug in patients with chlamydia trachomatis and chlamydia seropositive patients. A phase 3 study was initiated including chlamydia seropositive patients. However, the development of rifalazil was terminated in 2013 due to severe side effects.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Cinoxolone is a derivative of glycyrrhetinic acid. Is is claimed to possess antiulcer properties.
Status:
Investigational
Class (Stereo):
CHEMICAL (RACEMIC)
Ibuterol, a prodrug that is rapidly hydrolyzed to form a drug, terbutaline. Terbutaline, a beta-2 adrenergic agent used to treat asthma.
