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Showing 501 - 510 of 4342 results

Status:
Investigational
Source:
INN:lanproston
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

LANPROSTON is an analog of prostaglandin F2 alpha. It is used as veterinary medicament.
Status:
Investigational
Source:
INN:lamtidine
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

LAMTIDINE is an irreversible and specific gastric histamine H2-receptor antagonist.
Status:
Investigational
Source:
INN:colfenamate
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Colfenamate is an antypyretic and antiinflammatory compound developed by the German company Tropon, GmbH.
Status:
Investigational
Source:
INN:iodetryl
Source URL:

Class (Stereo):
CHEMICAL (MIXED)

Iodetryl is fatty acid derivative patented by Russian company OOO "Nauchno-Proizvodstvennaya Firma "I. M. A." as a colloidal contrast agent.
Status:
Investigational
Source:
INN:liarozole
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Liarozole is an imidazole-containing compound that inhibits the cytochrome P-450-dependent metabolism of all-trans-retinoic acid (RA). Liarozole, a retinoic acid (RA) metabolism-blocking agent (RAMBA) in clinical development, has been granted orphan drug designation for congenital ichthyosis by the European Commission and the U.S. Food and Drug Administration. Later, based on the mixed results from a phase II/III trial of liarozole for the treatment of ichthyosis, Barrier decided to discontinue the development of liarozole. Liarozole displays antitumor activity against androgen-dependent and independent rat prostate carcinomas.A large phase III international study was completed comparing liarozole 300 mg twice daily with cyproterone acetate (CPA) 100 mg twice daily in a total of 321 patients with metastatic prostate cancer in relapse after first-line endocrine therapy. The results indicate that liarozole might be a possible treatment option for prostate cancer (PCA) following failure of first-line endocrine therapy.
Vadimezan (5,6-dimethyl(xanthenone-4-acetic acid), ASA404, DMXAA) is a fused tricyclic analogue of flavone acetic acid with potential antineoplastic activity. In pre-clinical mouse tumour models it was demonstrated that administration of Vadimezan rapidly leads to disruption of the existing vasculature in the tumour and consequent haemorrhagic necrosis of the tumour. This was consistent with the finding that a single dose of Vadimezan induced a prolonged reduction in the growth of xenografted tumours in animal models. The ability to disrupt the vasculature in these pre-clinical models has been attributed to a rapid induction of cytokines, particularly TNFα (tumour necrosis factor α), serotonin and nitric oxide, resulting in hemorrhagic necrosis and a decrease in angiogenesis. Despite the fact that the molecular targets for the drug remained unknown, the promising pre-clinical results led to Vadimezan being selected for clinical development. Results of Phase I trials showed some restriction of tumour blood flow within 24 h of treatment, although this was not as dramatic as seen in pre-clinical models. Unlike the animal models, there was also very little evidence for the rapid death of blood vessels or for increases in TNFα levels in human tumors. No difference in antitumour activity, cytokine induction or toxicity was observed between two parallel Phase I trials, one dosed weekly and the other dosed every 3 weeks. Therefore the drug proceeded to Phase II clinical trials, dosed every 21 days in combination with chemotherapeutic agents. These trials indicated the drug had small benefits in the treatment of non-small-cell lung cancer and prostate cancer. However, a subsequent Phase III clinical trial was not able to reproduce this response and clinical development was halted.
Status:
Investigational
Source:
INN:fosbretabulin [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Targets:


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
Source:
INN:ambamustine
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Ambamustine (PTT-119) is a bifunctional alkylating agent. Its antitumour effect is reported to mainly be through alkylation and interstrand cross-linkage of DNA. The drug was awaiting registration in Italy for the treatment of non-Hodgkin's lymphoma, and was also in phase-II clinical trial for small cell lung cancer, but was discontinued.
Status:
Investigational
Source:
INN:ditiocarb sodium [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Targets:

Ditiocarb, the sodium salt of diethyldithiocarbamate, is a drug with strong antioxidant capacity and chelating activities. It improves the depressed immune responses of newborn and aged mice and mice that are treated with chemotherapy or irradiation. Ditiocarb prevents cisplatin nephrotoxicity in animals without reducing the drug's antitumor activity. Ditiocarb has therapeutic activity in the LP-BM5 murine retrovirus-induced immunodeficiency disease. In that AIDS model, it reduces lymphadenopathy and hypergammaglobulinemia, restores immunocompetence, and prolongs survival. Ditiocarb was safe and reduced the incidence of opportunistic infections in patients with symptomatic HIV infection but ditiocarb had no positive effect on HIV patients. The administration of ditiocarb did not induce any major adverse clinical or biological reactions. Sixty-four patients with nonmetastatic high-risk breast cancer were randomized in a double-blind trial of adjuvant immunotherapy with sodium ditiocarb (DDC) versus placebo. At 6 years, overall survival was 81% in DDC group versus 55%.
Status:
Investigational
Source:
INN:brosuximide [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Brosuximide is longer-lasting anticonvulsant that has been studied as an antiepileptic drug.