GTI-2501

Identification

Name
GTI-2501
Accession Number
DB05406
Description

GTI-2501 is a novel antisense drug which has shown a favorable safety profile in preclinical studies, and in a phase I clinical trial. The drug is in a phase II clinical trial in combination with docetaxel for the treatment of hormone refractory prostate cancer. Initial testing has demonstrated strong antitumor activity in preclinical studies in prostate cancer and a variety of other tumor types.

Type
Small Molecule
Groups
Investigational
Synonyms
Not Available

Pharmacology

Indication

Investigated for use/treatment in prostate cancer and solid tumors.

Contraindications & Blackbox Warnings
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Pharmacodynamics
Not Available
Mechanism of action

GTI-2501 is an antisense oligonucleotide complementary to the R1 component of ribonucleotide reductase, which component is essential for DNA replication and tumor cell proliferation. GTI-2501 is designed to exert its activity by specific downregulation of the R1 component of ribonucleotide reductase. In preclinical studies, GTI-2501 showed significant antitumor activity against prostate cancer and a variety of other tumor types including colon, pancreas, NSCLC, breast, ovary, melanoma, brain (glioblastoma-astrocytoma), renal, cervical, lymphoma and leukemia.

Absorption
Not Available
Volume of distribution
Not Available
Protein binding
Not Available
Metabolism
Not Available
Route of elimination
Not Available
Half-life
Not Available
Clearance
Not Available
Adverse Effects
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Toxicity
Not Available
Affected organisms
Not Available
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Not Available
Food Interactions
Not Available

Products

Categories

Drug Categories
Classification
Not classified

Chemical Identifiers

UNII
G9AU73Z0Y0
CAS number
Not Available
InChI Key
Not Available
InChI
Not Available
IUPAC Name
Not Available
SMILES
Not Available

References

General References
  1. Lee Y, Vassilakos A, Feng N, Jin H, Wang M, Xiong K, Wright J, Young A: GTI-2501, an antisense agent targeting R1, the large subunit of human ribonucleotide reductase, shows potent anti-tumor activity against a variety of tumors. Int J Oncol. 2006 Feb;28(2):469-78. [PubMed:16391803]
  2. Tu GC, Tu X: GTI-2501. Lorus Therapeutics. Curr Opin Investig Drugs. 2001 Oct;2(10):1467-70. [PubMed:11890367]
PubChem Substance
347910122

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
Not Available
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Drug created on November 18, 2007 11:24 / Updated on June 12, 2020 10:52

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