Pharmaceutical composition for preventing or treating liver cancer

Inventors

WON, Cheolhee

Assignees

Lemonex Inc

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Publication Number

US-12076336-B2

Patent

Publication Date

2024-09-03

Expiration Date


Abstract

The present invention provides siRNA or dsRNA, which can effectively inhibit the expression of three highly expressed markers in liver cancer, and a pharmaceutical composition including the same can obtain excellent effects of preventing or treating liver cancer through RNAi. A pharmaceutical composition for preventing or treating liver cancer according to an embodiment of the present invention includes at least one of siRNA which includes a sense RNA having at least one sequence selected from the group consisting of sequences of SEQ ID NOs: 5 to 157, and an antisense RNA having a complementary sequence thereto and dsRNA having at least one sequence selected from the group consisting of sequences of SEQ ID NOs: 158 to 310.

Core Innovation

The disclosed subject matter relates to a pharmaceutical composition for preventing or treating liver cancer, including hepatocellular carcinoma (HCC), by using RNA interference (RNAi) with siRNA or dsRNA loaded on a porous silica particle. The siRNA includes a sense RNA having at least one sequence selected from the group consisting of sequences of SEQ ID NOs: 121 to 157 and 635 and an antisense RNA having a complementary sequence thereto, and the dsRNA has at least one sequence selected from the group consisting of sequences of SEQ ID NOs: 274 to 310.

The invention links selected target genes including BANF1, PLOD3, and SF3B4 with processes such as EMT and changes associated with E-cadherin, N-cadherin, and Slug, supporting selection of nucleic acid therapeutics intended to suppress those targets. The composition comprises a porous silica particle loaded with at least one of siRNA and dsRNA.

A central feature is characterization of the porous silica particle by a biodegradation parameter t defined by an absorbance ratio in Equation 1, using a dialysis-based measurement framework. The porous silica particle is characterized in that when a ratio of absorbance in Equation 1 becomes 1/2, t is 20 or more, and dependent claims further refine hydrophilic substituents, positive charge at neutral pH, and particle and pore size ranges.

Claims Coverage

The consolidated claim coverage includes one independent pharmaceutical composition for preventing or treating liver cancer using a porous silica particle loaded with specified siRNA and/or dsRNA sequences, together with an absorbance-based biodegradation parameter t threshold. Dependent claims refine the sequence selections and porous silica properties.

Porous silica particle loaded with siRNA or dsRNA for liver cancer prevention or treatment

A pharmaceutical composition for preventing or treating liver cancer comprising a porous silica particle and at least one of siRNA and dsRNA loaded on the porous silica particle.

Specified sense and antisense siRNA sequences

The siRNA includes a sense RNA having at least one sequence selected from SEQ ID NOs: 121 to 157 and 635, and an antisense RNA having a complementary sequence thereto.

Specified dsRNA sequence selections

The dsRNA has at least one sequence selected from the group consisting of sequences of SEQ ID NOs: 274 to 310.

Porous silica biodegradation parameter t threshold

The porous silica particle is characterized in that when a ratio of absorbance in Equation 1 becomes 1/2, t is 20 or more.

Overall, the claims center on a liver cancer pharmaceutical composition combining porous silica particle loading with specified siRNA/dsRNA sequence selections and an absorbance-based particle characterization parameter t. Dependent claims further refine hydrophilic substituents, charge at neutral pH, and particle and pore diameter ranges.

Stated Advantages

Documented Applications

Preventing or treating liver cancer, including hepatocellular carcinoma (HCC).

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