Fusion comprising a cell penetrating peptide, a multi epitope and a TLR peptide agonist for treatment of cancer

Inventors

Derouazi, MadihaBELNOUE, Elodie

Assignees

Amal Therapeutics SA

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Publication Number

US-12220387-B2

Patent

Publication Date

2025-02-11

Expiration Date


Abstract

The present invention provides a complex for use in the prevention and/or treatment of cancer, the complex comprising a) a cell penetrating peptide, b) at least one antigen or antigenic epitope, and c) at least one TLR peptide agonist, wherein the components a)-c) are covalently linked. In particular, compositions for use in the prevention and/or treatment of cancer, such as a pharmaceutical compositions and vaccines are provided.

Core Innovation

The invention relates to eliciting or improving an immune response against one or more antigens selected from survivin, carcino-embryonic antigen (CEA) and achaete-scute homolog 2 (ASCL2) in a subject. The immune response comprises presentation of multiple epitopes of the antigen(s) by MHC class I and/or MHC class II molecules. The method is based on administering a complex that is covalently linked so that multiple components function together in vivo to drive the epitope presentation.

The complex comprises a cell penetrating peptide, at least three antigenic peptides, and at least one TLR peptide agonist. The antigenic peptides include peptides having amino acid sequences according to SEQ ID NO:95, SEQ ID NO:96 and SEQ ID NO:97. The TLR peptide agonist supports immune activation, with preferred TLR peptide agonists corresponding to TLR2 and TLR4.

The components a)-c) are covalently linked, optionally using cleavable linkers/spacers, to support multi-component covalent fusion protein designs. The document also describes antigen-presenting cells loaded with the complexes, and compositions, kits, vaccines, and pharmaceutical formulations comprising the complexes.

Claims Coverage

The independent claim coverage centers on a covalently linked complex that combines a cell penetrating peptide, at least three antigenic peptides, and at least one TLR peptide agonist to elicit or improve an immune response via MHC class I and/or MHC class II presentation of multiple epitopes. The provided claim excerpts identify 2 inventive features in the independent claim, with additional dependent-claim refinements in the excerpts.

Antigen-epitope immune response using MHC class I/II presentation

A method for eliciting or improving an immune response against one or more antigens selected from survivin, carcino-embryonic antigen (CEA) and achaete-scute homolog 2 (ASCL2) in a subject, wherein the immune response comprises presentation of multiple epitopes of the antigen(s) by MHC class I and/or MHC class II molecules.

Covalently linked multi-component vaccine complex

Administering a complex comprising a cell penetrating peptide, at least three antigenic peptides comprising peptides having amino acid sequences according to SEQ ID NO:95, SEQ ID NO:96, and SEQ ID NO:97, and at least one TLR peptide agonist, wherein the components are covalently linked.

The claim coverage is directed to a covalently linked CPP–multi-epitope–TLR peptide agonist complex for presentation of multiple epitopes by MHC class I and/or MHC class II. The excerpts also refer to dependent-claim restrictions involving peptide identity, sequence arrangement, linker use, and colorectal cancer co-agent contexts.

Stated Advantages

Increased multimer-positive antigen-specific T cells versus controls.

Provides antigen-specific immune responses characterized by presentation of multiple epitopes by MHC class I and/or MHC class II molecules.

Improved immune potency and construct efficacy in downstream immunotherapy comparisons.

Tumor growth/survival outcomes are reported in EG.7-OVA and MC38 models.

Repeated vaccination durability is reported.

Homing to tumor sites is reported.

Cytokine secretion and functional T-cell responses are reported.

Maturation of human dendritic cells is reported.

Antigen processing/presentation by human DCs with HLA I/II peptides identified by mass spectrometry is reported.

Synergy with PD-1 blockade (anti-PD1) together with ATP128/antigenic cargo construct vaccination is reported.

DC Activation Index measurements and human-construct activation data for multiple ATP series variants are reported.

Documented Applications

In vivo vaccination regimens in C57BL/6 mice evaluating CPP variants (Z14 or Z18) with MAD5 and the TLR4 agonist EDA (EDAZ14Mad5 and EDAZ18Mad5), showing increased multimer-positive antigen-specific T cells.

Downstream immunotherapy examples comparing construct efficacy and immune potency across additional antigenic cargos (including Z13Mad8Anaxa, Z13Mad11Anaxa, Z13Mad9Anaxa, and Z13Mad12Anaxa).

Tumor growth/survival studies in EG.7-OVA and MC38 models, including effects on tumor control and/or survival outcomes.

Repeated vaccination durability and homing to tumor sites as measured outcomes.

Human dendritic cell maturation and antigen processing/presentation by human DCs, with HLA I/II peptides identified by mass spectrometry.

Combination immunotherapy showing synergy with PD-1 blockade (anti-PD1) together with ATP128/antigenic cargo construct vaccination (e.g., Z13Mad12Anaxa + anti-PD1 synergy).

Human-construct activation measurements for multiple ATP series variants (ATP110/ATP112/ATP115/ATP117/ATP118/ATP119/ATP120/ATP122/ATP123/ATP125/ATP128) including DC Activation Index measurements.

Colorectal cancer context, including administration prior to, at the same time as, or sequentially with a co-agent for treating or stabilizing colorectal cancer.

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