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Restrict the search for
colchicine
to a specific field?
Status:
Investigational
Source:
NCT00054262: Phase 2 Interventional Completed Liver Cancer
(2002)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
T-900607 is a pentafluorophenylsulphonamide derivative patented by Tularik Inc. as antiproliferative agent. Antitumor mechanism of T900607 is similar to the vinca alkaloids in terms of disruption of microtubule polymerization but uniquely causes a specific covalent modification of β-tubulin. In preclinical studies, T900607 was shown to bind irreversibly and specifically to the β1, β2, and β4 isotypes of β-tubulin is not a substrate for p-glycoprotein drug pump and has activity in the preclinical setting in MDR models. T900607 was evaluated in human tumor xenografts and showed activity in MX-1, MCF-7, and MCF-7/ADR mammary, C13 ovarian, HT 29 colon, and Caki-1 renal carcinoma as well as lymphoblastic leukemia, with equal or more efficacious effects compared to vinblastine, doxorubicin and paclitaxel. In a clinical trial, T-900607 shows significant toxicity, consisting of thrombocytopenia, nausea/vomiting, fatigue, and apparent cardiac toxicity.
Status:
Investigational
Source:
NCT00960557: Phase 1 Interventional Completed Neoplasm Metastasis
(2009)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Oxi0-4503 (now known as combretastatin A1 phosphate), a diphosphate prodrug of combretastatin A1, was developed by Mateon therapeutics as a second-generation, dual-mechanism vascular disrupting agent from the combretastatin family. On November 21, 2012, Oxi-4503 has been granted orphan designation by the US Food and Drug Administration for the treatment of acute myelogenous leukemia. It is known that the orphan drug designation qualifies a company for several benefits, including the potential for market exclusivity, development grants, and tax credits. Oxi0-4503 is currently participating in phase I/II clinical trial the treatment of patients with acute myelogenous leukemia or myelodysplastic syndrome. In addition, phase I clinical trial was successfully completed where was studied the safety of Oxi0-4503 in patients with advanced solid tumors.
Status:
Investigational
Source:
NCT00113438: Phase 2 Interventional Completed Cancer
(2005)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Combretastatin is a phenol derivative isolated from the bark of Combretum caffrum, commonly known as South African Bush Willow. Combretastatin is an effective antimitotic agent, and like colchicine, inhibited tubulin polymerization and stimulated tubulin-dependent GTP hydrolysis.
Status:
Investigational
Source:
JAN:OMBRABULIN HYDROCHLORIDE [JAN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Ombrabulin is an experimental drug candidate discovered by Ajinomoto and further developed by Sanofi-Aventis for cancer treatment.
Ombrabulin is a synthetic water-soluble analog of combretastatin A4, derived from the South African willow bush (Combretum caffrum), with potential vascular-disrupting and antineoplastic activities. Ombrabulin binds to the colchicine binding site of endothelial cell tubulin, inhibiting tubulin polymerization and inducing mitotic arrest and apoptosis in endothelial cells. As apoptotic endothelial cells detach from their substrate, tumor blood vessels collapse; the acute disruption of tumor blood flow may result in tumor necrosis. Ombrabulin has been used in trials studying the treatment of Sarcoma, Neoplasms, Solid Tumor, Neoplasms, Malignant, and Advanced Solid Tumors, among others. In January 2013, Sanofi said it discontinued development of Ombrabulin after disappointing results from phase III clinical trials.
Status:
Investigational
Source:
INN:fosbretabulin [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Fosbretabulin (Combretastatin A4 phosphate, CA4P) is the lead compound of a relatively new class of agents termed vascular disrupting agents that target existing tumor blood vessels. Rapid tumor blood flow shutdown has been demonstrated in preclinical models and patients by various techniques such as dynamic contrast-enhanced MRI, perfusion computed tomography and PET scans following CA4P infusion. CA4P typically induces rapid tumor necrosis in the center of the tumor and leaves a rim of viable cells in the periphery. In oncology, CA4P does not appear to be that active by itself, but may be more efficacious when combined with chemotherapy, antiangiogenic therapy and radiation therapy. Combretastatin was initially isolated from the
root bark of the South African Bush willow
Combretum caffrum in 1982 by Pettit and colleagues
at the Arizona State University (AZ, USA). Combretastatin A4 phosphate binds avidly to tubulin at the colchicine-binding site to inhibit microtubule assembly and destabilize the cytoskeleton. CA4P is a tubulin-binding agent that binds at or near the colchicine binding site of β-tubulin (Kd = 0.40 uM), inhibits tubulin assembly with IC50 of 2.4 uM. Fosbretabulin has orphan drug status in the EU and the US for the treatment of ATC (Anaplastic Thyroid Cancer). Later the development of this drug was discontinued.
Status:
Investigational
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Taltobulin, also known as HTI-286 and SPA-110, is a fully synthetic analog of the natural tripeptide hemiasterlin, inhibits tubulin polymerization and circumvents transport-based resistance to taxanes. Taltobulin was a potent inhibitor of proliferation (mean IC50 = 4 nm in 18 human tumor cell lines) and had substantially less interaction with multidrug resistance protein (P-glycoprotein) than currently used antimicrotubule agents, including paclitaxel, docetaxel, vinorelbine, or vinblastine. Taltobulin showed strong antitumor activity both in androgen-dependent and androgen- independent tumors and may be a promising agent in second- line treatment strategies for patients suffering from docetaxel- refractory prostate cancer.
Status:
Investigational
Source:
NCT00003709: Phase 1 Interventional Completed Unspecified Adult Solid Tumor, Protocol Specific
(1998)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Carbendazim is a broad-spectrum benzimidazole antifungal with potential antimitotic and antineoplastic activities widely used as a fungicide in agriculture and home gardening, and as an antihelminthic in veterinary medicine. As a fungicide, carbendazim used for controls Ascomycetes, Fungi Imperfecti, and Basidiomycetes on a wide variety of crops, including bananas, cereals, cotton, fruits, grapes, mushrooms, ornamentals, peanuts, sugarbeet, soybeans, tobacco, and vegetables. Carbendazim is a chemically stable and relatively persistent fungicide which only metabolizes to a limited extent in plants and in soil. The only detected metabolite is 2-aminobenzimidazole, which constitutes less than 5% of the total residues in leaves. Carbendazim may be anticipated to metabolize in the animal into hydroxylated analogues which may appear in meat and milk products. Carbendazim acts as a mitotic poison by altering tubulin binding and microtubule formation. This has been proposed as a possible mechanism of action for the developmental abnormalities seen in animal studies with high concentrations.
Status:
Designated
Source:
EU-Orphan Drug:EU/3/16/1618
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
