Novel il-21 prodrugs and methods of use thereof

By designing IL-21 prodrugs and utilizing the fusion of the antibody masking portion and the carrier portion, targeted activation at the tumor site was achieved, solving the problems of insufficient selectivity and severe side effects of existing IL-21 therapeutics, and improving therapeutic efficacy and PK characteristics.

CN115605504BActive Publication Date: 2026-06-09ASKGENE PHARMA INC
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
ASKGENE PHARMA INC
Filing Date
2020-08-21
Publication Date
2026-06-09

AI Technical Summary

Technical Problem

Existing IL-21 therapeutics have problems with insufficient selectivity, poor pharmacokinetic (PK) and efficacy, and serious side effects in cancer treatment.

Method used

Develop an IL-21 prodrug comprising a cytokine moiety, a masking moiety, and a carrier moiety. The masking moiety binds to an IL-21 agonist peptide via an antigen-binding fragment of an antibody and fuses with the carrier moiety via a cleavable peptide linker, enabling activation at the tumor site for targeted and localized therapy.

Benefits of technology

It improves the selectivity and PK properties of IL-21 therapy, reduces systemic side effects, achieves better therapeutic effects and a longer half-life, and enhances the targeting specificity to tumor sites.

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Abstract

The present invention provides IL-21 prodrugs and methods of making and using the same to stimulate the immune system or treat cancer or infectious disease.
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Claims

1. A prodrug comprising two identical light chains, a first heavy chain polypeptide chain, and a second heavy chain polypeptide chain, wherein the light chain has the amino acid sequence shown in SEQ ID NO: 50, the first heavy chain polypeptide chain has the amino acid sequence shown in SEQ ID NO: 48, and the second heavy chain polypeptide chain has the amino acid sequence shown in SEQ ID NO:

133.

2. A pharmaceutical composition comprising the prodrug according to claim 1 and a pharmaceutically acceptable excipient.

3. A polynucleotide encoding the prodrug of claim 1.

4. An expression vector comprising the polynucleotide according to claim 3.

5. A host cell comprising the vector according to claim 4.

6. The host cell of claim 5, wherein the gene encoding protein lyase, uPA, MMP-2 and / or MMP-9 is knocked out in the host cell.

7. A method for preparing the prodrug according to claim 1, the method comprising: The host cells according to claim 5 or 6 are cultured under conditions that allow expression of the prodrug, wherein the host cells are mammalian cells; as well as The prodrug is isolated.