Immunoconjugates and methods
Inventors
Han, Xiaojun • ORR, SUVI TUULA MARJUKKA • Bunker, Kevin Duane • HUANG, Peter Qinhua • Fischer, Kimberlee
Assignees
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Publication Number
US-12274754-B2
Publication Date
2025-04-15
Expiration Date
Abstract
Immunoconjugates of the Formula (I) include a linking group for linking an antibody targeting ligand (Ab) to a drug (D). Embodiments of such immunoconjugates are useful for delivering the drug to selected cells or tissues, e.g., for the treatment of cancer. Ab-[S-L1-L2-L3-L4-L5-L6-L7-D]n (I)
Core Innovation
The invention relates to an immunoconjugate represented by a defined structure in which Ab is an antibody or an antigen-binding fragment thereof, and n is an integer from 1 to 10. The antibody component binds human receptor tyrosine kinase-like orphan receptor 1 (ROR1), and the disclosure also states anti-HER2 antibody in some embodiments.
In further embodiments, the antibody comprises variable heavy-chain and variable light-chain regions that include particular CDR1, CDR2, and CDR3 amino-acid sequences identified by SEQ ID numbers, including VLCDR2 described as AAS. The VH and VL regions have at least 80% sequence identity to specified SEQ ID amino-acid sequences while preserving the specified CDR sequence regions.
The document also describes a conjugate represented by alternative structural representations, or a pharmaceutically acceptable salt thereof. The conjugate comprises a drug moiety (D) linked via linker segments, including embodiments in which L2 is absent and where L3 is a tetrapeptide residue, with additional variability in linker segment presence or absence and defined exclusions for Formula (IV).
Claims Coverage
Three inventive feature groups are present across the input: an immunoconjugate with Ab as an antibody or antigen-binding fragment and n from 1 to 10, an antibody specifically binding human ROR1 with sequence-defined VH/VL regions, and a conjugate represented by alternative structural representations or a pharmaceutically acceptable salt thereof.
Immunoconjugate with antibody or antigen-binding fragment
An immunoconjugate represented by a defined structure, wherein Ab is an antibody or an antigen-binding fragment thereof, and n is an integer from 1 to 10.
Antibody specifically binding human ROR1
The immunoconjugate includes an antibody that specifically binds human receptor tyrosine kinase-like orphan receptor 1 (ROR1).
Specified VH and VL CDR amino-acid sequences via SEQ ID numbers
The antibody comprises variable heavy-chain and variable light-chain regions containing particular CDR1, CDR2, and CDR3 amino-acid sequences identified by SEQ ID numbers, including VLCDR2 specified as AAS.
At least 80% sequence identity while preserving specified CDRs
The antibody contains a variable heavy chain region (VH) and a variable light chain region (VL) with at least 80% sequence identity to specified SEQ ID amino acid sequences while preserving the specified CDR sequence regions.
Conjugate represented by alternative structural representations
A conjugate represented by alternative structural representations, or a pharmaceutically acceptable salt thereof.
The claim coverage centers on an immunoconjugate defined by an antibody-containing structure with n from 1 to 10, further narrowed by ROR1 binding, specified VH/VL CDR amino-acid sequences, and an at least 80% sequence identity constraint preserving those CDR regions, together with a conjugate defined by alternative structural representations or a pharmaceutically acceptable salt.
Stated Advantages
Not explicitly described in patent.
Documented Applications
Pharmaceutical compositions comprising the immunoconjugate and a pharmaceutically acceptable excipient.
Methods of treating cancer or tumor by administering the immunoconjugate or pharmaceutically acceptable salts.
Use in manufacture of medicaments.
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