Complexes of IL-15 and IL-15Ralpha and uses thereof

Inventors

Felber, Barbara K.Finkielsztein, SergioPavlakis, George N.VOURNAKIS, John V.

Assignees

Novartis AGUS Department of Health and Human Services

Publication Number

US-10265382-B2

Publication Date

2019-04-23

Expiration Date

2028-06-27

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Abstract

The present invention relates to agents that modulate interleυkin-15 (“IL-15”) signal transduction or function (“Therapeutic Agents”) and the use ol” those agents to modulate immune function. The Therapeutic Agents target the interaction between IL-15 and its receptor and modulate IL-15-induced signal transduction. The Therapeutic Agents may be formulated with polymers, such as poly-β-1-♦4-N-acetylglucosamine. for administration to a human subject to modulate IL-15-mediated immune function.

Core Innovation

The invention provides agents, termed Therapeutic Agents, that modulate interleukin-15 (IL-15) signal transduction or function, targeting the interaction between IL-15 and its receptor. These Therapeutic Agents modulate IL-15-induced signal transduction and can be formulated with polymers such as poly-β-1→4-N-acetylglucosamine for administration to human subjects to modulate IL-15-mediated immune function.

The Therapeutic Agents are divided into Agonistic Therapeutic Agents that induce IL-15 signal transduction and enhance IL-15-mediated immune function, and Antagonistic Therapeutic Agents that reduce or inhibit IL-15 signal transduction and suppress IL-15-mediated immune function. The Agonistic Therapeutic Agents include complexes comprising IL-15 covalently or noncovalently bound to interleukin-15 receptor alpha (IL-15Ra), nucleic acids encoding IL-15 and IL-15Ra, and cells engineered to express IL-15/IL-15Ra complexes. These are useful for prevention, treatment, and management of disorders benefitting from enhanced IL-15-mediated immune function such as cancer and infectious diseases. The Antagonistic Therapeutic Agents include antibodies that specifically bind IL-15/IL-15Ra complexes and prevent binding to the beta/gamma receptor complex, useful for disorders where suppression of IL-15-mediated immune function is beneficial, such as autoimmune disorders, graft versus host disease, transplantation rejection, and inflammatory disorders.

Significant aspects of the invention describe engineering IL-15Ra derivatives to inhibit cleavage by endogenous proteases or substituting cleavage sites, facilitating formation of stable complexes with IL-15. The IL-15/IL-15Ra complexes may include heterologous molecules, such as disease-associated antigens or antibodies, which can be conjugated to IL-15 or IL-15Ra without interfering with receptor binding. The use of polymers, specifically poly-β-1→4-N-acetylglucosamine, is emphasized to formulate these complexes or cells expressing IL-15/IL-15Ra for administration. Additionally, methods include generating irradiated cancer cells engineered to co-express IL-15 and IL-15Ra as Therapeutic Agents to enhance immune responses against cancer.

Claims Coverage

The patent discloses a method comprising seven main inventive features related to producing and purifying codon optimized human IL-15 and IL-15Ra complexes using engineered cells.

Recombinant production of codon optimized human IL-15 and IL-15Ra complex

A method of culturing cells expressing codon optimized human IL-15 encoded by nucleic acid sequences with at least 95% identity to specific regions of SEQ ID NOs: 9, 11, or 17, and human IL-15Ra encoded by nucleic acid sequences with at least 95% identity to specific regions of SEQ ID NOs: 13 or 15, followed by purification of the IL-15/IL-15Ra complex.

Specific nucleic acid combinations for IL-15 and IL-15Ra expression

Variants of the above method employing specific combinations of nucleic acid sequences from the named SEQ IDs to encode human IL-15 and IL-15Ra.

Selection of cell lines for production

Use of specific mammalian cell lines such as 293 or CHO cells for expressing the IL-15 and IL-15Ra nucleic acids to produce the complex.

High expression levels of IL-15

The method ensures cells express at least 0.15 pg (up to 2 pg) of human IL-15 per day in serum-free media as measured by ELISA, indicating high production yield.

The claims cover recombinant methods using codon optimized IL-15 and IL-15Ra nucleic acids expressed in mammalian cells to produce and purify IL-15/IL-15Ra complexes with defined nucleic acid sequences and high expression levels, focusing on specific nucleic acid sequence identities and cell line selection.

Stated Advantages

Therapeutic Agents enhance or suppress IL-15-mediated immune function depending on the therapeutic goal.

Formulation with polymers like poly-β-1→4-N-acetylglucosamine improves administration and stability of Therapeutic Agents.

Use of IL-15/IL-15Ra complexes or engineered cells enables stable expression and production of bioactive agents for therapy.

Methods enable targeting specific diseases by modulating IL-15 signaling, with applications in cancer, infectious, autoimmune, and inflammatory diseases.

Documented Applications

Treatment, prevention, and management of diseases involving modulation of IL-15-mediated signaling including cancer, infectious diseases, autoimmune diseases, inflammatory disorders, graft versus host disease, and transplantation rejection.

Use of agonistic Therapeutic Agents to enhance IL-15-mediated immune function for cancer and infectious disease therapy.

Use of antagonistic Therapeutic Agents to suppress IL-15-mediated immune function in autoimmune, inflammatory, graft versus host, and transplant rejection conditions.

Use of irradiated cancer cells engineered to express IL-15 and IL-15Ra as Therapeutic Agents to induce or enhance immune responses against tumors.

Formulation of therapeutic complexes or cells with polymers such as poly-β-1→4-N-acetylglucosamine for improved delivery.

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