# US 12,000,833 B2 · Marker for predicting the sensitivity to PI3K inhibitors

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- Number: US 12,000,833 B2
- Document ID: US12000833B2
- Status: Granted
- Kind: B2
- Application number: 16/765,345
- Filed: 2018-11-22
- Published: 2020-11-12
- Granted: 2024-06-04
- Earliest claimed: 2017-11-23
- Assignees: Inserm (Institut National De La Sante Et De La Recherche Medicale); Universite Paul Sabatier Toulouse III; Centre National de la Recherche Scientifique (CNRS)
- Applicants: Inserm (Institut National De La Sante Et De La Recherche Medicale); Université Paul Sabatier Toulouse III; Centre National De La Recherche Scientifique (Cnrs)
- Inventors: Julie Guillermet-Guibert; Thibaut Douche; Emmanuelle Mouton-Barbosa; Odile Schiltz; Marie-Pierre Bousquet; Célia Cintas
- Web page: https://patentgrep.com/patent/US12000833B2

## CPC

- C07K 14/4748: {Tumour specific antigens; Tumour rejection antigen precursors [TRAP], e.g. MAGE}
- G01N 33/57525: of the liver or pancreas
- C07K 14/47: from mammals
- C07K 16/303: {Liver or Pancreas}
- C07K 16/32: against translation products of oncogenes
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- C07K 7/08: having 12 to 20 amino acids (gastrins C07K14/595; somatostatins C07K14/655; melanotropins C07K14/68)
- 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)
- G01N: INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES (measuring or testing apparatus or processes other than immunoassay, involving enzymes or microorganisms C12M, C12Q)
- 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)

## Abstract

PI3K signalling is the most increased pathway in human cancers. The four isoforms of PI3K are thought to be activated by different redundant mechanisms leading to a common downstream signalling. However, the mutational pattern of PI3K pathway or its level of expression is not sufficient to predict the sensitivity to PI3K inhibitors. By identifying for the first time a phosphopeptide that predict the sensitivity to p110α and/or p110γ inhibitors, the inventors provide insight in how to handle heterogeneity of PI3K expression patterns in tumoral samples for the choice of available PI3K-targetting drugs. Accordingly, the present relates to a phosphopeptide characterized by the amino acid sequence as set forth in SEQ ID NO:1 (PGTPSDHQSQEASQFER) wherein the threonine residue at position 3 is phosphorylated.

## Claims

### Claim 1

A method of treating pancreatic cancer in a subject in need thereof comprising
i) detecting a phosphopeptide having the amino acid sequence as set forth in SEQ ID NO:1 (PGTPSDHQSQEASQFER) wherein the threonine residue at position 3 is phosphorylated in a tumor tissue obtained from the subject and
ii) administering to the subject a therapeutically effective amount of a small molecule p110α and/or small molecule p110γ inhibitor when the phosphopeptide is detected at step i),
wherein the step of detecting is performed by SILAC based LC-MS/MS.