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folate-conjugated antisense oligodeoxynucleotide
- Development stage
- Preclinical
- Modality
- MicroRNA (miRNA) → Small RNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics, 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, Small Interfering RNA (siRNA) → Small RNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics
- Administration
- Intravenous, Intratumoral (potential; Not Clinically Established)
01
Overview
Folate-conjugated antisense oligodeoxynucleotide is a synthetic nucleic acid drug composed of an antisense oligodeoxynucleotide (ODN) covalently linked to folic acid. This conjugation targets the ODN to cells that overexpress folate receptors, such as many epithelial cancer cells (notably ovarian cancer). The antisense ODN binds specifically to complementary mRNA (e.g., anti-c-fos), resulting in hybridization and inhibition of protein synthesis, thereby reducing gene expression. Cellular uptake and therapeutic effect are enhanced in folate receptor–overexpressing tumor cells, and the cytostatic activity is sequence-specific and mediated by binding to the folate receptor. The conjugate is under investigation for tumor-selective delivery of nucleic acids as a potential treatment for cancers with high levels of folate receptor expression[1][2][10].
- Other names
- folate-antisense oligonucleotidefolate-modified antisense ODNfolic acid-conjugated antisense oligodeoxynucleotide
02
Targets
FOLR1 (FRα)
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