U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 111 - 120 of 1114 results

Status:
Investigational
Source:
NCT00458744: Phase 1 Interventional Withdrawn Brain and Central Nervous System Tumors
(2007)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Talotrexin (also known as PT-523) was developed as a nonpolyglutamatable antifolate drug for the treatment of various types of tumors. It is known that antifolates are a class of cytotoxic or antineoplastic agents, which inhibit or prevent the maturation and proliferation of malignant cells. Talotrexin was studied in clinical trials for the treatment of brain and central nervous system tumors, leukemia, lymphoma, unspecified childhood solid tumor. However, this study was withdrawn because of toxicity. In addition, was studied in phase I/II multicenter clinical trial in patients with non-small-cell Lung carcinoma, this study was also withdrawn. The withdrawal was related to incidences of dose-limiting mucositis and myelosuppression. However, on May 22, 2006, was announced that the U.S. Food and Drug Administration has granted orphan drug designation for talotrexin in patients with acute lymphoblastic leukemia (ALL).
Status:
Investigational
Source:
NCT01037556: Phase 1/Phase 2 Interventional Unknown status Acute Myelogenous Leukemia
(2010)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

PR-104 is a phosphate ester dinitrobenzamide mustard pre-prodrug that is rapidly hydrolyzed systemically to PR-104A, a bioreductive prodrug. PR-104A is in turn activated via reduction by NADPH:cytochrome P450 oxidoreductase and other one-electron reductases in hypoxic cells, and by aldo-keto reductase 1C3 (AKR1C3) independently of oxygen, to the corresponding hydroxylamine (PR-104H) and amine (PR-104M) metabolites. Subsequently, these reactive nitrogen mustards crosslink DNA and cause cytotoxicity in cells. PR-104 is known to have preclinical anti-tumor activity in human tumor xenograft models as mono-therapy and in combination with radiotherapy and chemotherapy. Thrombocytopenia, and to a lesser extent neutropenia, was the dose-limiting toxicity of weekly PR-104. Combination of PR-104 with docetaxel or gemcitabine caused dose-limiting and severe myelotoxicity in patients with advanced solid tumors. PR-104 had been in phase II clinical trial for the treatment of acute myeloid leukemia.
Status:
Investigational
Source:
INN:benclonidine
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
INN:oxazafone
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Oxazafone was studied as an anticonvulsant and anxiolytic agent. Information about the further development of this compound is not available.
Status:
Investigational
Source:
INN:lamifiban
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


LAMIFIBAN is a potent and selective nonpeptide glycoprotein IIb/IIIa antagonist. It inhibits platelet aggregation and thrombus formation by preventing the binding of fibrinogen to platelets. It was in clinical development as an injectable antithrombotic agent for treating and preventing acute coronary syndromes but showed no significant effects on clinical outcomes.
Status:
Investigational
Source:
INN:naroparcil [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Naroparcil [LF 90055], the lead compound in a series of orally-active antithrombotics, is an analogue of LF 1351, a compound shown to have antithrombotic action. Antithrombotic activity of naroparcil is dependent on modification in the plasma GAG profile which inactivates thrombin via heparin cofactor II (HCII).
Status:
Investigational
Source:
INN:oxindanac
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Oxindanac, a non-steroidal anti-inflammatory drug, and is a weak cyclooxygenase inhibitor possessed antipyretic activity. This drug is used as a veterinary inflammatory drug. In addition, oxindanac was studied in phase III clinical trials for the treatment of rheumatic disorders. However, this study was discontinued.
Status:
Investigational
Source:
INN:metamfepramone [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Metamfepramone (dimethylcathinone, dimethylpropion, and dimepropion) was synthesized by various routes in the 1930s and 1940s and clinically evaluated as anorectic as well as a treatment of hypotension and symptoms of the common cold. It was widely used for the treatment of the common cold or hypotonic conditions. Due to its stimulating properties and its rapid metabolism resulting in major degradation products such as methylpseudoephedrine and methcathinone, it has been considered relevant for doping controls by the World Anti-Doping Agency (WADA). Metamfepramone was marketed as an appetite suppressant, but was made illegal in 2006.
Status:
Investigational
Source:
NCT00431912: Phase 2 Interventional Completed Cutaneous T-cell Lymphoma
(2007)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Daporinad is an inhibitor of nicotinamide phosphoribosyltransferase (NMPRTase), an enzyme that participates in the biosynthesis of nicotinamide adenine dinucleotide (NAD+) from niacinamide (vitamin B3). Inhibition of NMPRTase may deplete energy reserves in metabolically active tumor cells and induce tumor cell apoptosis. In addition, this agent may inhibit tumor cell production of vascular endothelial growth factor (VEGF), resulting in the inhibition of tumor angiogenesis. Daporinad was investigated as a treatment of B-cell chronic lymphocytic leukemia, melanoma, and cutaneous T-cell lymphoma. Clinical trials have shown that drug has low efficacy when used alone.
Status:
Investigational
Source:
INN:ketotrexate
Source URL:

Class (Stereo):
CHEMICAL (EPIMERIC)

KETOTREXATE is an antifolate developed to overcome methotrexate (MTX) resistance. However, it demonstrated such potential only in MTX-resistant sensitive L1210/FR8 leukemia cells and its clinical development was discontinued. Unlike MTX, KETOTREXATE exhibited minimal inhibition of purified dihydrofolate reductase, which implies that it does not act as a classical antifolate.