ELBIO LTD.

Development

siRNA Anti-Cancer Drug

"under nonclinical tests"

Characteristics

As cancer cells proliferate very fast due to short cell cycle, the synthesis of the DNA proceeds fast. The thymine base among four bases of DNA essentially requires a SHMT enzyme based on Vit. Bx. The Vit.Bx-coupled vector(VBPdXYP) targets cancer cells, especially SHMT enzymes.

The siRNA-loaded vector targets cancer cells and inhibit SHMT enzymes in the thymidylate synthase cycle of cancer cells. It leads to apoptosis of cancer cells as targetd gene therapy (Fig. 6).

The special peptide TR7-coupled vector(VBPdXYP-P) tagets cancer stem cells of cancer cells. Another siRNA-loaded vector coupled with TR7 targets cancer stem cells and inhibits the self-renewal of cancer stem cells. So it lead to apoptosis of cancer stem cells.

Items

siRNA Anti-Cancer Drug for Brain Tumor (ACD-01)

Patients with brain tumor occurs in about 12,000 patients/year in Korea, but there is only some medicines to extend life without medicines to cure it,

Glioblastoma multiforme(GBM) of brain tumor is malignant. 5-year cancer relative survival rate of GBM is about 7%.

siRNA(small interfering RNA) gene degrades the corresponding mRNA and inhibits the synthesis of the corresponding special protein. siRNA anti-cancer drug of nano particles reduced tumor volume size by ave. 65% and siRNA drug of nanochain type reduced tumor size by ave. 87% after 2 week treatment in mouse brain tumor(GBM) models (Fig. 7).

siRNA anti-cancer drug for lung cancer (ACD-02)

Patients of lung cancer occurs in about 30,000 patients/year in Korea. The death rate of lung cancer among all cancers is the highest in Korea.

Immune therapy is effectively used for cancers, but the efficacy is less than about 30%. So new siRNA anti-cancer drugs with high efficacy are required for all cancers.

siRNA anti-cancer drug of nano particles reduced tumor volume size by about 80% after 30 day intratumoral treatment in the mouse human lung cancer xenograft models.

siRNA Anti-Cancer Drug for Cancer Stem Cells (ACD-03)

The TR-7 peptide coupled vector targets cancer stem cells, and then the siRNA-loaded vector inhibits the self-renewal of cancer stem cells. It leads to apoptosis of cancer stem cells.

ELBIO can simultaneously treat cancer cells and cancer stem cells with combination treatment of both the drug of VBPdXYP/siRNA for cancer cells and the drug of VBPdXYP-P/siRNA1 for cancer stem cells(Fig. 9 and 10). Hence, ELBIO can completedly heal cancers including cancer stem cells. This combination treatment can prevent a recurrence of cancer.

siRNA Anti-Cancer Drug of Nanochain Type (ACD-04)

3~5 nano particles of siRNA-loaded anti-cancer drug can be connected each other by a lingker. Anti-cancer drug of nanochain type is formed by the connection of nano particles.

As the transfection efficiency of siRNA anti-cancer drug of nanochain type is 6% higher than that of siRNA anti-cancer drug of nano particles type, siRNA anti-cancer drug of nanochain type can improve the treatment effect of cancer from 10% to 20%. Please refer to Fig. 7.

CRISPR Anti-Cancer Drug (ACD-05)

CRISPR anti-cancer drug is CRISPR-Cas9 loaded drug instead of siRNA, namely vector/CRISPR complex of nano particles.

If the safety of CRISPR-Cas9 is confirmed, the treatment effect of cancers can be improved, and the treatment period can be reduced by only 3~4 IV injections. It is also expected that this CRISPR drug can be very helpful for cancer patients in the final stage.

The combination treatment on cancer cells and cancer stem cells of GBM reduced tumor volume size of 81% after 5 week treatment by (VBXYP/siRNA + VBXYP-P/CRISPR) in the mouse GBM xenograft models(Fig. 11). CRISPR-Cas9 gene was used for apoptosis of cancer stem cells, and siRNA was used for apoptosis of cancer cells of GBM.

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