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Patexia Research
Patent No. US 11273171
Issue Date Mar 15, 2022
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Patent 11273171 - Methods for treating or preventing ophthalmological conditions > Claims

  • 1. A method of treating geographic atrophy in a human subject in need thereof, the method comprising administering via intravitreal injection to said subject about 2 mg/eye of a pegylated aptamer in an amount sufficient to reduce growth of a lesion associated with geographic atrophy in the subject, wherein the aptamer comprises the sequence fCmGfCfCGfCmGmGfUfCfUfCmAmGmGfCGfCfUmGmAmGf UfCfUmGmAmGfUfUfUAfCfCfUmGfCmG-3T (SEQ ID NO:26),wherein fC and fU=2′ fluoro nucleotides, mG and mA=2′-OMe nucleotides, all other nucleotides are 2′-OH, and 3T indicates an inverted deoxythymidine, or a salt thereof, andwherein the pegylated aptamer is administered to the subject biweekly, monthly, or quarterly.
    • 2. The method according to claim 1, wherein the pegylated aptamer is provided as a pegylated moiety conjugated to the aptamer via a linker.
      • 3. The method according to claim 2, wherein the pegylated moiety is conjugated to the 5′ end of the aptamer.
      • 4. The method according to claim 2, wherein the pegylated moiety is a branched PEG.
      • 5. The method according to claim 2, wherein the pegylated moiety has a molecular weight greater than about 10 kDA.
      • 6. The method according to claim 2, wherein the pegylated moiety has a molecular weight of about 40 kDa.
    • 7. The method according to claim 1, wherein the pegylated moiety has the following structure:embedded image
    • 8. The method according to claim 1, wherein the growth of the GA lesion in the subject in need thereof is reduced by at least 10%, as compared to a subject who is not administered the anti-C5 agent.
    • 9. The method according to claim 1, wherein the anti-C5 agent is administered monthly.
      • 10. The method according to claim 9, wherein the anti-C5 agent is administered monthly for three injections, and the fourth and fifth injections are administered three or four months after the third injection.
    • 11. The method according to claim 1, wherein the anti-C5 agent is administered bimonthly.
    • 12. The method according to claim 1, wherein the anti-C5 agent is administered quarterly.
    • 13. The method according to claim 1, wherein the growth of the GA lesion in the subject in need thereof is reduced by at least 20% as compared to a subject who is not administered the anti-C5 agent.
    • 14. The method according to claim 1, wherein the growth of the GA lesion in the subject in need thereof is reduced by at least 30% as compared to a subject who is not administered the anti-C5 agent.
    • 15. The method according to claim 1, wherein the growth of the GA lesion in the subject in need thereof is reduced by at least 40% as compared to a subject who is not administered the anti-C5 agent.
    • 16. The method according to claim 1, wherein the growth of the GA lesion in the subject in need thereof is reduced by at least 50% as compared to a subject who is not administered the anti-C5 agent.
    • 17. The method according to claim 1, wherein growth of the lesion is assessed using autofluorescence imaging or optical coherence tomography.
  • 18. A method of treating geographic atrophy in a human subject in need thereof, the method comprising administering via intravitreal injection to said subject about 2 mg/eye of a pegylated aptamer in an amount sufficient to reduce growth of a lesion associated with geographic atrophy in the subject, wherein the aptamer comprises the sequence fCmGfCfCGfCmGmGfUfCfUfCmAmGmGfCGfCfUmGmAmGf UfCfUmGmAmGfUfUfUAfCfCfUmGfCmG-3T (SEQ ID NO:26),wherein fC and fU=2′ fluoro nucleotides, mG and mA=2′-OMe nucleotides, all other nucleotides are 2′-OH, and 3T indicates an inverted deoxythymidine, or a salt thereof, andwherein the pegylated aptamer is administered to the subject biweekly, monthly, or quarterly,wherein the pegylated moiety is a branched PEG and has a molecular weight greater than about 10 kDA, andwherein the growth of the GA lesion in the subject in need thereof is reduced by at least 30% as compared to a subject who is not administered the anti-C5 agent.
  • 19. A method of treating geographic atrophy in a human subject in need thereof, the method comprising administering via intravitreal injection to said subject about 2 mg/eye of a pegylated aptamer in an amount sufficient to reduce growth of a lesion associated with geographic atrophy in the subject, wherein the aptamer comprises the sequence fCmGfCfCGfCmGmGfUfCfUfCmAmGmGfCGfCfUmGmAmGf UfCfUmGmAmGfUfUfUAfCfCfUmGfCmG-3T (SEQ ID NO:26),wherein fC and fU=2′ fluoro nucleotides, mG and mA=2′-OMe nucleotides, all other nucleotides are 2′-OH, and 3T indicates an inverted deoxythymidine, or a salt thereof, andwherein the pegylated aptamer is administered to the subject biweekly, monthly, or quarterly,wherein the pegylated moiety is a branched PEG and has a molecular weight greater than about 10 kDA, andwherein the growth of the GA lesion in the subject in need thereof is reduced by at least 40% as compared to a subject who is not administered the anti-C5 agent.
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