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untargeted anti-gastrin LNA Gapmer
- Development stage
- Preclinical
- Lead developer
- Georgetown University
- Modality
- Antisense Oligonucleotides (ASOs) → Long RNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics, Modified DNA Oligonucleotides → Antisense DNA → DNA Therapeutics → Nucleic Acid Therapeutics, Single-strand DNA → Antisense DNA → DNA Therapeutics → Nucleic Acid Therapeutics
- Administration
- Intraperitoneal
01
Overview
The untargeted anti-gastrin LNA Gapmer is an experimental antisense oligonucleotide (ASO) designed to selectively downregulate the expression of gastrin mRNA. Gastrin is known to stimulate the growth of pancreatic cancer through an autocrine mechanism, and this Gapmer aims to inhibit that growth by reducing gastrin levels. The molecule utilizes Locked Nucleic Acid (LNA) technology, which provides enhanced stability and a longer half-life in vivo compared to traditional RNAi techniques. In preclinical studies presented at AACR 2024, the untargeted Gapmer demonstrated the ability to significantly decrease metastases in human pancreatic cancer orthotopic mouse models, although it was less potent in reducing primary tumor mass compared to a version targeted specifically to the cholecystokinin-B receptor (CCK-BR). The research was conducted by investigators at Georgetown University and the National Cancer Institute.
- Other names
- anti-gastrin Gapmeruntargeted LNA-Gapmer
02
Targets
GAST (Gastrin)
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