Drug intelligence / Profile preview

GTI-2040 + capecitabine + oxaliplatin

Development stage
Preclinical
Lead developer
Aptose Biosciences
Modality
Antisense Oligonucleotides (ASOs) → Long RNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics, Modified DNA Oligonucleotides → Antisense DNA → DNA Therapeutics → Nucleic Acid Therapeutics, Small Molecules, Single-strand DNA → Antisense DNA → DNA Therapeutics → Nucleic Acid Therapeutics
Administration
Intravenous, Oral
01

Overview

GTI-2040 + capecitabine + oxaliplatin is a combination therapy that has been investigated for the treatment of locally advanced or metastatic colorectal cancer and other solid tumors. GTI-2040 (also known as LOR-2040) is an antisense oligonucleotide that specifically targets the R2 component of ribonucleotide reductase, which is required for DNA synthesis and cell proliferation. This enzyme is elevated in a wide range of tumors and can enhance tumor growth and metastatic potential. Capecitabine is an oral fluoropyrimidine that is converted to 5-fluorouracil in tumor tissue, while oxaliplatin is a platinum-based chemotherapeutic agent. The combination aims to leverage the different mechanisms of action of these agents to improve efficacy against cancer.

02

Targets

TS (Thymidylate synthase)DNARRM2

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