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Restrict the search for
m nalidixic acid
to a specific field?
Status:
Investigational
Source:
INN:tauroselcholic acid [INN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Nemorubicin, a doxorubicin derivative, is a DNA-intercalator, topoisomerase and RNA synthesis inhibitor that was undergoing development with Nerviano Medical Sciences (Nerviano MS; formerly Pharmacia Italia) for the treatment of solid tumours, specifically, the loco-regional treatment of primary liver tumours (hepatocellular carcinoma). The drug is active on tumors resistant to alkylating agents, topoisomerase II inhibitors and platinum derivatives. It works primarily through topoisomerase I inhibition. Of note, Nemorubicin is active in cells with upregulation of the nucleotide excision repair (NER) pathway, where current therapies fail.
Nemorubicin is biotransformed in the liver into cytotoxic metabolites that may further contribute to render this drug highly active against primary liver tumors or liver metastases. Clinical trials were conducted in Europe, US and China with Nemorubicin given at different dose-schedules and by different routes of administration: as single agent by systemic IV route, oral route and by intra-hepatic artery (IHA) infusion alone or in combination with cisplatin.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Oxetacillin was developed as an antibacterial drug that has never been marketed.
Status:
Investigational
Source:
NCT00531401: Phase 2 Interventional Completed Carcinoma, Non-Small-Cell Lung
(2007)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Salirasib or S-trans,trans-Farnesylthiosalicylic acid (FTS) is a salicylic acid derivative with potential antineoplastic activity. It acts as a potent competitive inhibitor of the enzyme prenylated protein methyltransferase (PPMTase), which methylates the carboxyl-terminal S-prenylcysteine in a large number of prenylated proteins including Ras. In such systems, Salirasib inhibits Ras methylation but not Ras farnesylation. Salirasib selectively disrupts the association of chronically active Ras proteins with the plasma membrane. Salirasib competes with Ras for binding to Ras-escort proteins, which possess putative farnesyl-binding domains and interact only with the activated form of Ras proteins, thereby promoting Ras nanoclusterization in the plasma membrane and robust signals. Salirasib was studied in the clinical trials in patients with solid tumors, however its development was discontinued.
Class (Stereo):
CHEMICAL (ACHIRAL)
Butafosfan is a phosphororganic supplement that is given, most commonly with cyanocobalamin, to cattle, swine, horses, and poultry for the prevention or treatment of phosphorus deficiencies. Butafosfan also plays a vital role in hepatic carbohydrate metabolism. In addition, butafosfan has been regarded as an antistress agent in combination with vitamin B12. Studies with butafosfan in different animals have shown that it improved general health status by stimulating feed intake, immune system, and digestive function. Butafosfan has been reported for the treatment of metabolic disorders caused by stress or nutrition problems in various species.
Class (Stereo):
CHEMICAL (ACHIRAL)
Moxastine is a diarylmethane derivative with an antihistamine and anticholinergic activities.
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Etibendazole (R34803 or methyl [5-(2-(4-fluorophenyl)-1,3-dioxolan-2-yl)-1H-benzimidazole-2-yl] carbamate), a benzimidazole derivative, is a microtubule inhibitor. Etibendazole exerts antihelmintic activity.
Status:
Investigational
Source:
NCT00743925: Phase 2 Interventional Completed Acute Coronary Syndrome
(2008)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Varespladib (LY315920; A-001) is a potent and selective inhibitor of IIa, V, and X isoforms of human non-pancreatic secretory phospholipase A2 with nM IC50. The molecule acts as an anti-inflammatory agent by disrupting the first step of the arachidonic acid pathway of inflammation. Varespladib methyl is being developed by Anthera Pharmaceuticals Inc for the potential treatment of coronary artery disease, acute coronary syndrome and inflammation. Varespladib methyl is a prodrug that is rapidly metabolized to varespladib, and both compounds are able to potently inhibit the enzymes of the human secretory phospholipase groups. Phase II clinical trials of varespladib methyl in patients with coronary artery disease, rheumatoid arthritis, asthma and ulcerative colitis revealed that the drug was well tolerated. Varespladib methyl did not demonstrate a good efficacy profile in patients with rheumatoid arthritis, asthma and ulcerative colitis; whereas in patients with coronary artery disease, varespladib methyl consistently reduced LDL-cholesterol levels, (elevated LDL-cholesterol levels are a marker of increased cardiovascular risk). Varespladib methyl could represent a novel therapy for the treatment of cardiovascular disease, although the efficacy, safety profile and advantages of this drug compared with existing therapeutic options would need to be established in upcoming phase III trials.
Status:
Investigational
Source:
NCT00233909: Phase 1/Phase 2 Interventional Completed Leukemia, Myeloid
(2005)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Zosuquidar (LY-335979) is an experimental antineoplastic drug. It is is a potent modulator of P-glycoprotein-mediated multi-drug resistance with Ki of 60 nM. Zosuqidar was initially characterized by Syntex Corporation, which was acquired by Roche in 1990. Roche licensed the drug to Eli Lilly in 1997. It was granted orphan drug status by the FDA in 2006 for AML. Zosuquidar Trihydrochloride had been in phase III clinical trials by Kanisa Pharmaceuticals for the treatment of acute myeloid leukaemia. However, this research has been discontinued.
Status:
Investigational
Source:
NCT00499499: Phase 1 Interventional Suspended Cancer
(2007)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
E7107 is a semisynthetic derivative of the natural product pladienolide B which was originally isolated from Streptomyces platensis. E7107 is the first compound a new class of anti-cancer agents targeting the spliceosome. Specifically E7107 interacts with the Splicing factor 3B subunit 1 (SF3b1) to block the normal splicing of oncogenes. Development of E7107 was suspended after Phase I clinical trials due to an unacceptable profile of adverse events.
