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TKM-080301
- Development stage
- Phase 2
- Lead developer
- Arbutus Biopharma
- 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, Lipid-based Nanoparticles → Nanoparticles → Drug Delivery Systems
- Administration
- Intravenous
01
Overview
TKM-080301 is a lipid nanoparticle (LNP) formulation containing small interfering RNA (siRNA) specifically targeting polo-like kinase 1 (PLK1), a serine/threonine kinase that regulates key aspects of cell cycle progression and mitosis. PLK1 is highly expressed in malignant cells and has been validated as a molecular target and prognostic factor in various cancers. Inhibition of PLK1 activity by TKM-080301 induces mitotic arrest and apoptosis in proliferating cancer cells. The drug uses stable nucleic acid lipid particles (SNALP) to protect the siRNA from degradation, enhance tumor accumulation via the enhanced permeation and retention effect, and enable effective intracellular delivery. Developed for intravenous administration, TKM-080301 has been evaluated primarily for advanced solid tumors, including liver cancer, adrenocortical carcinoma (ACC), neuroendocrine tumors, hepatocellular carcinoma (HCC), as well as other refractory or metastatic cancers[1][2][3][5][6].
- Other names
- polo-like kinase 1 small interfering RNAPLK1 siRNAPLK-1 siRNAPLK 1 siRNASNALP-siPLK1SNALP-siPLK-1SNALP-siPLK 1
02
Targets
PLK1 (Polo like kinase 1)
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