GTI-2501

Identification

Generic Name
GTI-2501
DrugBank Accession Number
DB05406
Background

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.

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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

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

Categories

Drug Categories
Classification
Not classified
Affected organisms
Not Available

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. [Article]
  2. Tu GC, Tu X: GTI-2501. Lorus Therapeutics. Curr Opin Investig Drugs. 2001 Oct;2(10):1467-70. [Article]
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
Chromatographic Properties
Collision Cross Sections (CCS)
Not Available

Drug created at November 18, 2007 18:24 / Updated at June 12, 2020 16:52