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Restrict the search for
m ceftaroline
to a specific field?
Status:
Investigational
Source:
NCT00084812: Phase 1 Interventional Completed Unspecified Adult Solid Tumor, Protocol Specific
(2004)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Safingol, the synthetic L-threo-stereoisomer of endogenous (D-erythro-) sphinganine, is an inhibitor of protein kinase C and sphingosine kinase in vitro, and in some cell types has been implicated in ceramide generation and induction of apoptosis. Safingol inhibits enzymatic activity and 3H-phorbol dibutyrate binding of purified rat brain PKC (IC50 = 37.5 uM and 31uM, respectively). Inhibits human PKCα, the major overexpressed isoenzyme in MCF-7 DOXR cells (IC50 = 40 uM). Safingol enhances the cytotoxic effect of the chemotherapeutic agent Mitomycin C (MMC) in gastric cancer cells by promoting drug-induced apoptosis. Safingol is an inhibitor of SphK (Sphingosine kinase). Safingol has been shown to act synergistically with other chemotherapeutic agents and may potentiate chemotherapy drug-induced apoptosis in vitro and in vivo.
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.
Class (Stereo):
CHEMICAL (RACEMIC)
Nitramisole, an imidazothiazole derivative, is an anthelmintic. Nitramisole was effective against migrating Strongylus vulgaris larvae in ponies. Treatment of infected ponies with Nitramisole resulted both a clinical and radical cure.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Ciprefadol is an opioid analgesic drug. It binds with a high affinity to mu (Ki 4.2 nM) and kappa (Ki 2.5 nM) opioid receptors. In vivo, ciprefadol displays mixed antagonist/agonist activity in the mouse writhing and the rat tail heat tests: in low doses, the compound inhibits the analgesic effect of morphine, while at higher doses it displays analgesic effect. Chronic administration of ciprefadol to rhesus monkeys produced a marked physical dependence more severe than that of morphine, and its effect was consistent with what would be expected of a potent, long-lasting morphine-like agonist.
Status:
Investigational
Source:
NCT01746979: Phase 3 Interventional Completed Metastatic or Locally Advanced Unresectable Pancreatic Adenocarcinoma
(2012)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Evofosfamide, also formerly known as TH-302, is an investigational hypoxia-activated prodrug and is used to target cancerous cells under hypoxic conditions, which is a feature possessed by multiple solid tumors including glioblastoma and pancreatic cancer. Within regions of tumor hypoxia, evofosfamide releases bromo isophosphoramide mustard (Br-IPM), a potent DNA alkylating agent that kills tumor cells by forming DNA crosslinks. Once activated in hypoxic tissues, Br-IPM can also diffuse into surrounding oxygenated regions of the tumor and kill cells there via a “bystander effect”. Because of its preferential activation in the targeted hypoxic regions of solid tumors, evofosfamide may be less likely to produce broad systemic toxicity seen with untargeted cytotoxic chemotherapies.
Status:
Investigational
Source:
NCT00195325: Phase 1 Interventional Terminated Tumors
(2005)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Cevipabulin is a synthetic, water-soluble tubulin-binding agent with potential antineoplastic activity. Cevipabulin appears to bind at the vinca-binding site on tubulin but seems to act more similar to taxane-site binding agents in that it enhances tubulin polymerization and does not induce tubulin depolymerization. The disruption in microtubule dynamics may eventually inhibit cell division and reduce cellular growth.
Status:
Investigational
Source:
NCT00003359: Phase 1 Interventional Completed Unspecified Adult Solid Tumor, Protocol Specific
(1998)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Batabulin or T138067 (2-fluoro-1-methoxy-4-pentafluorophenylsulfonamidobenzene) covalently and selectively modifies the beta1, beta2, and beta4 isotypes of beta-tubulin at a conserved cysteine residue, thereby disrupting microtubule polymerization. Cells exposed to batabulin become altered in shape, indicating a collapse of the cytoskeleton, and show an increase in chromosomal ploidy. Batabulin is equally efficacious in inhibiting the growth of sensitive and multidrug-resistant human tumor xenografts in athymic nude mice. Batabulin has been in clinical trials for the treatment of cancers (breast cancer, colorectal cancer, glioma, hepatocellular carcinoma, non-small cell lung cancer). It does not have clinical activity in the treatment of colorectal cancer and glioma. Batabulin development was discontinued.
Status:
Class (Stereo):
CHEMICAL (ACHIRAL)
ISOMETAMIDIUM (as a chloride salt) is widely used in tropical countries as an antiprotozoal agent to control animal trypanosomiasis. It is used principally in cattle but also in sheep, goats, buffalos, donkeys, horses, camels and dogs.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Cyprenorphine is a mixed agonist-antagonist of opioid receptors. In clinical trials, administration of cyprenorphine induced psychotomimetic effects in pre-operative patients.
Status:
Investigational
Source:
NCT00394628: Phase 1/Phase 2 Interventional Unknown status Glioblastoma Multiforme
(2006)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Banoxantrone (formally known as AQ4N), a bioreductive drug that is irreversibly converted to AQ4, a stable DNA affinic cytotoxic compound. Banoxantrone is activated by haem-containing reductases such as inducible nitric oxide synthase (iNOS). In hypoxic cells, AQ4N is reduced to the topoisomerase II inhibitor AQ4. By inhibition of topoisomerase II within these hypoxic areas, AQ4N has been shown to sensitize tumors to existing chemo- and radiotherapy treatments. Novacea, the company which was responsible for clinical trials for banoxantrone had decided to scale back on its clinical development, including discontinuing the clinical trial in acute lymphoblastic leukemia and delaying the planned clinical trial in B-cell lymphoma. The company decided to continue enrollment in an ongoing Phase 1b/2a clinical trial in patients with glioblastoma multiforme. However, further information about these clinical trials are not available. Some recent experiments have shown that targeting hypoxic tumors with high levels of iNOS with a combination of AQ4N and radiotherapy could be a useful clinical therapeutic strategy.
