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AssigneeBioNTech SE
InventorsGonçalo Bernardes, Nuno Prego Ramos, Mariangela Natale
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An antibody-drug conjugate (ADC) is provided and comprises an antibody which binds to sialyl Tn (STn) or a glycan terminated by an alpha 2,6-linked sialic acid, conjugated to a drug via a linker, wherein the linker comprises a cleavable linker, and the drug comprises a growth inhibitory agent which is exatecan, deruxtecan, or a derivative thereof. The antibody-drug conjugate (ADC) of the invention comprises a linker cleavable by glucuronidase, for examples the linker comprises a β-glucuronide moiety, such as shown in formula I: Formula (I). The antibody-drug conjugate (ADC) comprises a linker which is linked to, or is modified to link to, the drug via a carbamate linkage, or a linker which is linked to, or is modified to link to, the drug via a quaternary ammonium salt linkage. The antibody-drug conjugate (ADC) may comprise a linker which is PEGylated with a group comprising polyethylene glycol (PEG). Novel linkers for use in ADCs are also described.
An antibody-drug conjugate (ADC) comprising an antibody which binds to sialyl Tn (STn) or a glycan terminated by an alpha 2,6-linked sialic acid, conjugated to a drug via a linker, wherein the linker comprises a linker cleavable by glucuronidase, and the drug comprises a growth inhibitory agent.
An antibody-drug conjugate (ADC) according to any preceding claim wherein the linker is linked to, or is modified to link to, the drug via a carbamate linkage.
An antibody-drug conjugate (ADC) according to any preceding claim wherein the sialyl Tn (STn) or a glycan terminated by an alpha 2,6-linked sialic acid is a human or animal protein.
An antibody-drug conjugate (ADC) according to any preceding claim wherein the drug is exatecan, or deruxtecan, or a derivative thereof.
An antibody-drug conjugate (ADC) according to any preceding claim wherein the antibody is an antibody fragment.
An antibody-drug conjugate (ADC) according to any preceding claim wherein the antibody is a human or animal antibody.
An antibody-drug conjugate (ADC) according to any preceding claim wherein the antibody comprises:
An antibody-drug conjugate (ADC) according to any preceding claim wherein the glycans terminated by alpha 2,6-linked sialic acids comprise STn, 2,6-sialyl T, di-sialyl T, or 2,6-sialolactosamine.
An antibody-drug conjugate (ADC) according to any preceding claim wherein the antibody is subject to glycan changes at glycosylation sites.
An antibody-drug conjugate (ADC) according to any preceding claim wherein the antibody is a monoclonal antibody, chimeric antibody, or a humanized antibody.
An antibody-drug conjugate (ADC) according to any preceding claim wherein the antibody is a functional antibody fragment that binds STn and a group of glycans terminated by alpha 2,6-linked sialic acids.
A linker cleavable by glucuronidase, wherein the linker is configured to be coupled to a drug via a quaternary ammonium salt linkage, and is PEGylated with a group comprising polyethylene glycol (PEG).
A linker cleavable by glucuronidase, wherein the linker is configured to be coupled to a drug via a carbamate linkage, and does not include an alkyne moiety.
A linker cleavable by glucuronidase, wherein the linker is configured to be coupled to a drug via a carbamate linkage and terminates in a maleimide moiety.
A drug-linker payload, as shown in formula V′:
A drug-linker payload, as shown in formula VI′:
An exatecan derivative compound with a handle moiety covalently bonded to said exatecan parent molecule at a position that does not significantly affect the therapeutic or pharmacokinetic properties of the parent molecule, wherein said handle moiety comprises a quaternary ammonium salt of the formula:
An exatecan derivative compound having the following general structure:
Dependencies are inferred from the claim text.