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Restrict the search for
m cariprazine
to a specific field?
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.
Status:
Investigational
Source:
NCT00803556: Phase 1 Interventional Completed Solid Tumor
(2006)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Alvespimycin (17-desmethoxy-17-N,N-dimethylaminoethylamino-geldanamycin) (17-DMAG; NSC 707545) is an inhibitor of the molecular chaperone heat shock protein HSP90. Alvespimycin is a derivative of antineoplastic benzoquinone antibiotic geldanamycin. Alvespimycin binds to HSP90, a chaperone protein that aids in the assembly, maturation and folding of proteins. Subsequently, the function of Hsp90 is inhibited, leading to the degradation and depletion of its client proteins such as kinases and transcription factors involved with cell cycle regulation and signal transduction. Alvespimycin was studied in clinical trials for the treatment of solid tumors and hematologic malignancies however its development was discontinued.
Class (Stereo):
CHEMICAL (ACHIRAL)
Nitraquazone (TVX 2706) is an phosphodiesterase inhibitor with antiinflammatory action. It strongly enhances the increase in intracellular levels of cyclic AMP caused by appropriate effectors in all systems tested so far. EC50 values are in the submicromolar range. The effect is apparently neither due to an increased responsiveness of the hybrid cells for an effector like prostaglandin E1 nor to an increased activity of adenylate cyclase, but to an inhibition of both low and high affinity cyclic AMP phosphodiesterases. Half-maximal inhibition of enzyme activity is obtained at 10 uM TVX 2706. TVX 2706 does not interfere with the calmodulin activation of phosphodiesterase. Nitraquazone affected cytokine production by PHA-stimulated human blood cells. Nitraquazone was active in reducing the production of IL-5 (IC50 = 0.8 uM), while its potency against IL-2, GM-CSF and IFN-gamma was 3-6 times lower.
Status:
Investigational
Source:
NCT00000763: Phase 1 Interventional Completed Sarcoma, Kaposi
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
TNP-470 (AGM-1470, (3R,4S,5S,6R)-5-methoxy-4- [(2R,3R)-2-methyl-3-(3-methyl-2-butenyl) -oxiranyl]-1-oxaspiro[2,5]oct-6-yl(chloroacetyl) carbamate) is an anti-angiogenic, semisynthetic analogue of fumagillin, a known antibiotic secreted by the fungus Aspergillus fumigatus fresenius, which is under clinical development for the treatment of cancer by Takeda Chemical Industries Ltd. in Japan and TAP Pharmaceuticals, Inc. in the United States. TNP-470 binds to and irreversibly inactivates methionine aminopeptidase-2 (MetAP2), resulting in endothelial cell cycle arrest late in the G1 phase and inhibition of tumor angiogenesis. This agent may also induce the p53 pathway, thereby stimulating the production of cyclin-dependent kinase inhibitor p21 and inhibiting angiogenesis. In early clinical reports, TNP-470 is tolerated up to 177 mg/m(2) with neurotoxic effects (fatigue, vertigo, ataxia, and loss of concentration) being the principal dose-limiting toxicity (DLT). TNP-470 is being evaluated in Phase I-II trials in the US in patients with Kaposi’s sarcoma, cervical cancer, breast cancer, brain cancer, prostate cancer and renal cell carcinoma.
Status:
Investigational
Source:
NCT03504423: Phase 3 Interventional Completed Pancreatic Cancer Metastatic
(2018)
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
CPI-613 is a lipoate derivative synthesized to be catalytically inert but to potentially mimic lipoate catalytic intermediates. The drug is in phase II of clinical trials for the treatment of Myelodysplastic syndromes; Pancreatic cancer; Small cell lung cancer; Solid tumors; Bile duct cancer; Acute Myeloid leukemia. The mechanism of CPI-613 action can be explained by (I) inhibition of tumor cell pyruvate dehydrogenase complex (PDC) through activation of pyruvate dehydrogenase kinases leading to inactivating phosphorylation of the E1alpha-subunit of PDC; and (II) inhibition of alpha-ketoglutarate dehydrogenase.
Class (Stereo):
CHEMICAL (RACEMIC)
In the early stages of testing was shown that it is about 4 times more potent than gallopamil and 12 times more potent than verapamil in its effects on smooth muscle tone and labeled calcium uptake.
Class (Stereo):
CHEMICAL (RACEMIC)
Divabuterol or terbutaline dipivalate is a prodrug of terbutaline. The half-life of terbutaline dipivalate in human plasma is less than five minutes. Therapeutically, most forms of terbutaline can be used as bronchodilators in antiasthmatic treatment, as smooth muscle relaxants to treat premature labour (uterine relaxant) and for a number of other indications.
Class (Stereo):
CHEMICAL (ACHIRAL)
Niludipine (Bay-a-7168) is a potent calcium antagonistic coronary vasodilator with less cardiodepressant effect than nifedipine. Niludipine is a safe antianginal Ca2+-antagonist with broad effectiveness for various types of angina pectoris. Niludipine is clinically useful as coronary vasodilator and hypotensive agent.
Class (Stereo):
CHEMICAL (ACHIRAL)
Etofenprox is a synthetic pyrethroid insecticide compound used in agricultural production. Etofenprox acts on the nervous system of insects by disrupting their neuron sodium channels. Etofenprox is a contact-kill adulticide used to control a wide variety of insects including weevils, beetles, aphids, moths, whiteflies, thrips, borers, fleas and mosquitoes. Etofenprox is well tolerated by mammals, including cats, and is environmentally friendly.
Status:
Investigational
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Icomucret (15(S)-HETE) is an hydroxyeicosatetraenoic acid developed by Alcon Research, Ltd for treatment Ophthalmic Disorders. In vitro Icomucret has been shown to inhibit LTB4 formation, 12-HETE formation and specifically inhibits the neutrophil chemotactic effect of LTB4. The inhibition of LTB4 formation is probably due to modulation of the 5- lipoxygenase (LO) because no changes in PGE2 formation have been determined. In vivo, Icomucret inhibits LTB4-induced erythema and edema, and reduces LTB4 in the synovial fluid of carragheenan-induced experimental arthritis in dogs. Icomucret has also some immunomodulatory effects. It inhibits the mixed lymphocyte reaction, induces generation of murine cytotoxic suppressor T cells, and it decreases interferon production by murine lymphoma cells. Furthermore, IL-4 and IL-13 have recently been shown to be potent activators of the 15-LO in mononuclear cells. Icomucret induces the secretion of membrane-bound mucins from human conjunctival and corneal epithelial cells. Icomucret was evaluated in clinical trials for Dry Eye Syndrome treatment. However from 2007 no future development reported, and Icomucret development sims to be discontinued.
