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Publication Number
US-12134646-B2
Publication Date
2024-11-05
Expiration Date
Abstract
The present invention relates to a novel anti-C-KIT antibody or an antibody fragment thereof. In addition, the present invention relates to a composition for preventing or treating angiogenesis-related diseases comprising the anti-C-KIT antibody or an antibody fragment thereof, or a kit for diagnosing angiogenesis-related diseases.
Core Innovation
The invention provides an anti-C-KIT antibody or antibody fragment thereof that specifically binds to domain II of C-KIT. The antibody or fragment comprises a light chain variable region defined by a light chain CDR1, CDR2, and CDR3 corresponding to SEQ ID NO: 1, SEQ ID NO: 2, and SEQ ID NO: 3, and a heavy chain variable region defined by a heavy chain CDR1, CDR2, and CDR3 corresponding to SEQ ID NO: 4, SEQ ID NO: 5, and SEQ ID NO: 6.
Embodiments further specify additional variable-region definitions and a human IgG1-derived constant region. Nucleic acid, vector, and transformed-cell embodiments are described for encoding the anti-C-KIT antibody or antibody fragment thereof, providing the antibody-related constructs across antibody, genetic, and cellular forms.
The invention addresses angiogenesis-related diseases by targeting C-KIT via binding to domain II and inhibiting SCF/C-KIT downstream signaling. Reported effects include inhibition of C-KIT phosphorylation, AKT phosphorylation, ERK1/2 phosphorylation, and β-catenin, together with effects on angiogenesis-related cellular functions and in vivo efficacy in mouse and rat disease models.
Claims Coverage
The independent claim defines an anti-C-KIT antibody or antibody fragment that specifically binds domain II of C-KIT with sequence-specified light-chain and heavy-chain CDRs. Coverage includes antibody and fragment structure, with dependent claims extending to additional sequence identifiers, a human IgG1-derived constant region, nucleic acid, diagnostic kit use, and treatment of angiogenesis-related diseases.
Domain II binding anti-C-KIT antibody with specified light- and heavy-chain CDRs
An anti-C-KIT antibody or antibody fragment thereof specifically binding to domain II of C-KIT, comprising a light chain variable region with a light chain CDR1 of SEQ ID NO: 1, a light chain CDR2 of SEQ ID NO: 2, and a light chain CDR3 of SEQ ID NO: 3; and a heavy chain variable region with a heavy chain CDR1 of SEQ ID NO: 4, a heavy chain CDR2 of SEQ ID NO: 5, and a heavy chain CDR3 of SEQ ID NO: 6.
Alternative CDR-defined variable regions using SEQ ID NOs 7 and 8
The anti-C-KIT antibody or fragment includes a light chain variable region with the amino acid sequence of SEQ ID NO: 7 and a heavy chain variable region with the amino acid sequence of SEQ ID NO: 8.
Human IgG1-derived constant region
The anti-C-KIT antibody or fragment includes a human IgG1-derived constant region.
Nucleic acid encoding the anti-C-KIT antibody or fragment
A nucleic acid encodes the anti-C-KIT antibody or antibody fragment thereof.
Diagnostic kit for angiogenesis-related diseases
A diagnostic kit for angiogenesis-related diseases comprising the anti-C-KIT antibody or antibody fragment thereof.
Treatment of selected angiogenesis-related diseases by administering the antibody
A method of treating an angiogenesis-related disease by administering the anti-C-KIT antibody or antibody fragment thereof to a patient in need, wherein the disease is selected from an enumerated group including cancer and ophthalmic vascular diseases.
Overall, claim coverage centers on an anti-C-KIT antibody or fragment that binds domain II of C-KIT and is defined by specific light-chain and heavy-chain CDR sequence identifiers, with dependent coverage adding alternative variable-region identifiers, a human IgG1-derived constant region, nucleic acid encoding, diagnostic kit use, and patient treatment methods for angiogenesis-related diseases.
Stated Advantages
Strong C-KIT affinity was reported (SPR, KD).
Domain-mapping results confirmed binding to domain II of C-KIT.
Reported cross-reactivity in mice/rats.
Reported inhibition of tube formation in vitro.
Reported in vivo efficacy in mouse oxygen-induced retinopathy (OIR) and Brown Norway rat CNV models versus Eylea.
Reported inhibition of SCF/C-KIT downstream signaling pathways including AKT phosphorylation, ERK1/2 phosphorylation, C-KIT phosphorylation, and β-catenin.
Reported inhibition of cell proliferation in HUVEC and TF-1 cells.
Documented Applications
Pharmaceutical composition and methods for preventing or treating angiogenesis-related diseases, including cancer and ophthalmic vascular diseases.
Diagnostic kit using the anti-C-KIT antibody in immunoassays/immunostaining formats.
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