Drug intelligence / Profile preview

siRNA (KRAS)

Development stage
Unknown
Lead developer
Silexion Therapeutics
Modality
Chemically Modified siRNA → Small Interfering RNA (siRNA) → Small RNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics, Conjugated siRNA → Small Interfering RNA (siRNA) → Small RNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics
Administration
Intratumoral, Intravenous
01

Overview

siRNA (KRAS) refers to a class of RNA interference (RNAi)-based therapeutic agents designed to silence the expression of the KRAS oncogene, a critical driver in many human cancers. These drugs utilize small interfering RNA (siRNA) molecules that are complementary to the KRAS messenger RNA (mRNA). Upon delivery into tumor cells, the siRNA is incorporated into the RNA-induced silencing complex (RISC), which then binds to and cleaves the target KRAS mRNA, preventing the translation of the KRAS protein. This approach is particularly significant because KRAS has historically been considered "undruggable" by traditional small molecules. Development efforts, most notably by Silexion Therapeutics (formerly Silenseed), have produced candidates like siG12D-LODER, which uses a biodegradable PLGA microparticle system for local, sustained delivery in pancreatic cancer, and SIL-204, which targets specific mutations such as G12D and G12V.

Other names
KRAS siRNAsiRNA targeting KRASsiRNA-KRAS
02

Targets

AGO2 (Argonaute RISC catalytic component 2)Kirsten rat sarcoma virus oncogene homolog mRNA (KRAS mRNA)

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