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Publication Number
US-12247052-B2
Publication Date
2025-03-11
Expiration Date
Abstract
The invention provides compounds including a CpG oligodeoxynucleotide sequence linked to a lipid by a linker and related compositions and methods. The invention features a compound consisting of the nucleotide sequence of SEQ ID NO:1, at its 5′ end, bonded or linked by a linker to a lipid. Further, the invention features a method of treating a cancer in a human patient, comprising administering to the patient the compound. Further, the invention features a pharmaceutical composition including the compound and a pharmaceutically acceptable carrier. The invention features a kit including (I) the compound or a composition comprising the compound; and (ii) a protein comprising SEQ ID NO:2 or SEQ ID NO:3.
Core Innovation
The invention provides a CpG amphiphile compound defined by the nucleotide sequence 5′-TCGTCGTTTTGTCGTTTTGTCGTT-3′ (SEQ ID NO:1), positioned at its 5′ end and bonded or linked by a linker to a specified lipid, or a salt thereof. The lipid includes a structural variable X that is O or S.
The nucleotide sequence optionally includes one or more phosphorothioate bonds joining nucleotides within the sequence, including an arrangement where all internucleoside linkages are phosphorothioate linkages. This defined lipid-linked CpG construct is presented as a compound for therapeutic use.
The invention further describes treating HPV-positive cancer in a human by administering the compound together with two specific HPV protein antigens defined by SEQ ID NO:2 and SEQ ID NO:3, including HPV16 E6/E7 mutated forms as indicated in the provided content. The described therapeutic context includes HPV type 16 positive cancer and head or neck squamous cell carcinoma, with optional co-therapy with platinum-containing chemotherapy and/or anti–PD-1 antibodies.
Lipid-linked compounds bind endogenous albumin to enhance delivery to lymph nodes and promote therapeutic immune responses against the HPV proteins. The disclosed compositions and kit concepts support administration of the defined compound with the two specified HPV antigens.
Claims Coverage
The provided partial content includes one independent claim and dependent claims that refine the compound into compositions and treatment methods. Across the identified scope, the coverage centers on the defined 5′-linked CpG amphiphile structure and, in dependent claims, the inclusion of two HPV protein antigens for treating HPV-positive cancer.
5′-linked CpG amphiphile with defined lipid (X = O or S)
A compound consisting of the nucleotide sequence 5′-TCGTCGTTTTGTCGTTTTGTCGTT-3′ (SEQ ID NO:1), at its 5′ end bonded or linked by a linker to a lipid, or a salt thereof, wherein X is O or S.
Optional phosphorothioate internucleoside bonds
The nucleotides in the nucleotide sequence are optionally joined by one or more phosphorothioate bonds.
Claim coverage is directed to a defined CpG nucleotide sequence (SEQ ID NO:1) linked at its 5′ end to a lipid characterized by X = O or S, optionally including phosphorothioate bonds, with dependent claims refining into compositions and HPV antigen co-administration for treating HPV-positive cancers.
Stated Advantages
Lipid-linked compounds bind endogenous albumin to enhance delivery to lymph nodes.
Lipid-linked compounds promote therapeutic immune responses against HPV proteins.
Documented Applications
Treating HPV-positive cancer in a human by administering the lipid-linked CpG compound together with two specified HPV protein antigens (SEQ ID NO:2 and SEQ ID NO:3), including HPV type 16 positive cancer.
Treating head or neck squamous cell carcinoma using the described HPV-targeted administration context.
Using optional combination co-therapy including platinum-containing chemotherapy and/or anti–PD-1 antibody co-therapy.
Pharmaceutical composition and kit concepts for the described compound/protein antigen combination.
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