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Drug intelligence / Profile preview
GTI-2040 + capecitabine + oxaliplatin
- Development stage
- Phase 1
- Lead developer
- Aptose Biosciences
- Modality
- Antisense Oligonucleotides (ASOs) → Long RNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics, Single-strand DNA → Antisense DNA → DNA Therapeutics → Nucleic Acid Therapeutics, Modified DNA Oligonucleotides → Antisense DNA → DNA Therapeutics → Nucleic Acid Therapeutics, Small Molecules
- 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
DNARRM2TS (Thymidylate synthase)
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