# US 2021/0330696 A1 · A high capacity platform for immunogenic cancer cell death

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- Number: US 2021/0330696 A1
- Document ID: US20210330696A1
- Status: Published application
- Kind: A1
- Application number: 16/978,418
- Filed: 2019-03-05
- Published: 2021-10-28
- Earliest claimed: 2018-03-06
- Inventors: Rita Elena Serda; Achraf Noureddone
- Web page: https://patentgrep.com/patent/US20210330696A1

## CPC

- A61K 31/739: Lipopolysaccharides
- A61P 35/00: Antineoplastic agents
- A61K 9/1271: Non-conventional liposomes, e.g. PEGylated liposomes or liposomes coated or grafted with polymers (liposomes as conjugates {A61K47/6911})
- A61K 31/555: containing heavy metals, e.g. hemin, hematin, melarsoprol
- A61K 31/704: attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin {(digitoxin A61K31/7048)}
- A61K 33/243: Platinum; Compounds thereof
- A61K 38/208: {IL-12}
- A61K 39/39558: {against tumor tissues, cells, antigens}
- C07K 16/2818: {against CD28 or CD152}
- B82Y 5/00: Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- C07K: PEPTIDES (peptides in foodstuffs A23; obtaining protein compositions for foodstuffs, working-up proteins for foodstuffs A23J; preparations for medicinal purposes A61K; peptides containing beta-lactam rings C07D; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, C07D; ergot alkaloids of the cyclic peptide type C07D519/02; macromolecular compounds having statistically distributed amino acid units in their molecules, i.e. when the preparation does not provide for a specific; but for a random sequence of the amino acid units, homopolyamides and block copolyamides derived from amino acids C08G69/00; macromolecular products derived from proteins C08H1/00; preparation of glue or gelatine C09H; single cell proteins, enzymes C12N; genetic engineering processes for obtaining peptides C12N15/00; compositions for measuring or testing processes involving enzymes C12Q; investigation or analysis of biological material G01N33/00)
- B82Y: SPECIFIC USES OR APPLICATIONS OF NANOSTRUCTURES; MEASUREMENT OR ANALYSIS OF NANOSTRUCTURES; MANUFACTURE OR TREATMENT OF NANOSTRUCTURES

## Abstract

Compositions comprising, and methods of using, mesoporous hybrid siliceous nanoparticles comprising a TLR ligand or other immune stimulant(s), and an agent to induce immunogenic cell death.

## Claims

### Claim 1

A mesoporous hybrid siliceous nanoparticle comprising an immune stimulant and an agent to induce immunogenic cell death (ICD).

### Claim 2 (depends on 1)

The nanoparticle of claim 1 wherein the immune stimulant comprises a TLR4 ligand.

### Claim 3

(canceled)

### Claim 4 (depends on 2)

The nanoparticle of claim 2 further comprising a TLR9 ligand.

### Claim 5 (depends on 4)

The nanoparticle of claim 4 wherein the TLR9 ligand comprises CpG oligonucleotides, SD-101AS15, GNKG168, PF-3512676, ISS 1018, IMO-2055, CpG-28, EMD120108, or BCG.

### Claim at position 6

6-8. (canceled)

### Claim 9 (depends on 2)

The nanoparticle of claim 2 wherein the TLR4 ligand comprises monophosphoryl lipid (MPL)-A, aminoalkyl glucosaminide phosphate (AGP), glucopyranosyl LPS, beta-defensin 2, fibronectin EDA, HMGB1, AS15, snapin, tenascin C, ER111232, ER111233, ER112040, ER111230, ER112231, ER112093, ER112049, ER112047, ER112066, ER113651, ER119327, ER803022, ER803732, or ER803789.

### Claim 10 (depends on 1)

The nanoparticle of claim 1 wherein the agent that induces ICD comprises an anthracycline, R2016 (3-(4-chlorophenylamino)-6-hydroxy-9-methyl-9H-carbazole-1,4-dione), an anthracenedione, a platinin, an alkylating agent, proteasomal inhibitor, or immunogenic cell-killing RNA.

### Claim at position 9

11-12. (canceled)

### Claim 13 (depends on 1)

The nanoparticle of claim 1 wherein the agent that induces ICD is linked to the silaceous core.

### Claim 14 (depends on 13)

The nanoparticle of claim 13 wherein the linker is pH sensitive, light sensitive, redox sensitive or comprises a hydrazine or benzene-bridged silsesquioxane.

### Claim 15 (depends on 1)

The nanoparticle of claim 1 which has a diameter of about 50 nm to about 150 nm or about 75 um to about 300 nm or which has pores of about 5 to 20 nm in diameter or about 8 to 15 nm in diameter.

### Claim at position 13

16-18. (canceled)

### Claim 19 (depends on 1)

The nanoparticle of claim 1 further comprising a lipid layer.

### Claim at position 15

20-27. (canceled)

### Claim 28 (depends on 1)

A method to stimulate antitumor immunity, activate dendritic cells (DCs), or stimulate antigen processing presentation in a mammal, comprising administering to the mammal an effective amount of a composition comprising a plurality of the nanoparticles of claim 1, and a checkpoint inhibitor.

### Claim 29 (depends on 28)

The method of claim 28 wherein the checkpoint inhibitor is an anti-PD1 agent.

### Claim 30 (depends on 28)

The method of claim 28 wherein the mammal is a human.

### Claim 31 (depends on 28)

The method of claim 28, wherein the mammal has cancer.

### Claim 32 (depends on 31)

The method of claim 31 wherein the cancer is kidney, liver, lung, ovary, pancreas, breast, brain, bladder, stomach, or prostate cancer, leukermia or lymphoma.

### Claim 33

(canceled)

### Claim 34 (depends on 29)

The method of claim 29 wherein the anti-PD1 agent comprises dinaciclib, nivolumab, pembrolizumab, pidilizumab, BMS-936559, MPDL3280A, MEDI4736, MSB0010718C, avelumab, durvalumab, or atezolizumab

### Claim 35 (depends on 28)

The method of claim 28 further comprising administering IL-12.

### Claim 36 (depends on 28)

The method of claim 28 wherein the composition is injected.

### Claim 37 (depends on 28)

The method of claim 28 wherein the composition is subcutaneously or intratumorally administered.

### Claim 38 (depends on 28)

The method of claim 28 wherein the composition is systemically administered.

### Claim at position 27

39-40. (canceled)