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US 2022/0023433 A1Published application
Saponin Conjugates
AssigneesSapreme Technologies B.V., Charite-Universitatsmedizin Berlin
InventorsRuben Postel, Hendrik Fuchs
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AssigneesSapreme Technologies B.V., Charite-Universitatsmedizin Berlin
InventorsRuben Postel, Hendrik Fuchs
Estimating the term…
The current invention relates to an effector moiety capable of inducing an intracellular effect when present inside a mammalian cell, the effector moiety comprising a payload conjugated with at least one saponin. The invention also relates to an antibody-drug conjugate comprising the effector moiety according to the invention, or a ligand-drug conjugate comprising the effector moiety of the invention, the effector moiety comprising covalently coupled saponin. The invention also relates to a therapeutic combination comprising: (a) the effector moiety of the invention, comprising at least one saponin, and optionally a pharmaceutically acceptable excipient; and (b) an antibody-drug conjugate or a ligand-drug conjugate, and optionally a pharmaceutically acceptable excipient. Further, the invention relates to a pharmaceutical composition comprising the effector moiety of the invention or the antibody-drug conjugate of the invention or the ligand-drug conjugate of the invention, comprising at least one saponin covalently linked to the effector molecule, and optionally a pharmaceutically acceptable excipient. The invention also relates to the effector moiety of the invention or the antibody-drug conjugate of the invention or the therapeutic combination of the invention or the ligand-drug conjugate of the invention or the pharmaceutical composition of the invention, for use as a medicament. Finally, the invention also relates to the effector moiety of the invention or the antibody-drug conjugate of the invention or the therapeutic combination of the invention or the ligand-drug conjugate of the invention or the pharmaceutical composition of the invention, for use in the treatment or prevention of a cancer or an autoimmune disease.
An effector moiety capable of inducing an intracellular effect when present inside a mammalian cell, the effector moiety conjugated with at least one saponin, wherein the at least one saponin is covalently bound to the effector moiety via at least one linker, or is covalently bound directly to said effector moiety.
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The effector moiety of 14, wherein the cleavable bond is subject to cleavage in vivo under acidic conditions as present in endosomes and/or in lysosomes of mammalian cells, preferably of human cells, preferably at pH 4.0-6.5, and more preferably at pH≤5.5.
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Dependencies are inferred from the claim text.