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Gapmer-90
- Development stage
- Preclinical
- Lead developer
- Georgetown University
- 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
- Administration
- Intraperitoneal
01
Overview
Gapmer-90 is a target-specific locked nucleic acid (LNA) gapmer antisense oligonucleotide designed to target gastrin mRNA. Developed by researchers at Georgetown University, Gapmer-90 is modified via thiol-maleimide click chemistry to conjugate an amino acid ligand that selectively binds to the cholecystokinin-B receptor (CCKBR / CCK-BR). This modification enables receptor-mediated internalization and selective delivery of the antisense oligonucleotide to CCKBR-expressing cancer cells, disrupting the autocrine CCKBR-gastrin signaling axis. Gapmer-90 is under preclinical investigation for the treatment of recalcitrant cancers, including pancreatic ductal adenocarcinoma (PDAC) and hepatocellular carcinoma (HCC), where it has demonstrated the ability to downregulate gastrin expression, inhibit tumor cell growth, reduce tumor fibrosis, and improve survival in animal models.
- Other names
- LNA gapmer-90anti-gastrin LNA gapmer-90
02
Targets
CCK2R (Cholecystokinin 2 Receptor)
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