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GTI-2040 + docetaxel
- Development stage
- Phase 2
- 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
01
Overview
GTI-2040 + docetaxel is an investigational combination therapy for cancer. GTI-2040 is a 20-mer antisense oligonucleotide that specifically targets the mRNA of the R2 small subunit of human ribonucleotide reductase, an enzyme essential for DNA synthesis and cell proliferation. By binding to this mRNA, GTI-2040 decreases both mRNA and protein levels of R2, thereby inhibiting tumor cell proliferation[1][6][10]. Docetaxel is a well-established chemotherapeutic agent that stabilizes microtubules and inhibits cell division. The combination aims to enhance antitumor efficacy by simultaneously disrupting DNA synthesis (via ribonucleotide reductase inhibition) and mitosis (via microtubule stabilization). This regimen has been explored in clinical trials for various solid tumors.
02
Targets
TUBB (Tubulin (alpha and beta subunits))RRM2
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