IP Library Granted Patent US 10,392,667
Granted Patent B2
US 10,392,667 · App. 14/896,220 · Granted Aug 27, 2019

Methods and devices for predicting treatment efficacy of fulvestrant in cancer patients

Inventor: Steen Knudsen (Hørsholm, DK)
Assignee: Medical Prognosis Institute A/S
C12Q1/6886A61K31/138A61K31/18A61K31/4196A61K31/4535A61K31/475A61K31/517A61K31/5377A61K31/565A61K33/24C07K16/22C07K16/40C12Q2600/106C12Q2600/118C12Q2600/158
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Quick Facts
Patent No.
US 10,392,667
App. No.
14/896,220
Granted
Aug 27, 2019
Kind
B2
Abstract

The present invention features methods, devices, and kits for predicting the sensitivity of a patient to a compound or medical treatment, such as fulvestrant.

Claims (47)

1. A method of predicting the responsiveness of breast cancer in a patient to treatment with fulvestrant comprising:

a) contacting a tumor sample from the patient comprising one or more nucleic acid molecules with a device comprising:

i) single-stranded nucleic acid molecules capable of specifically hybridizing with nucleotides of a GATA3 biomarker; and

ii) single-stranded nucleic acid molecules capable of specifically hybridizing with nucleotides of an ANXA1 biomarker; and

b) quantifying a level of expression of the GATA3 biomarker and the ANXA1 biomarker by performing microarray analysis, quantitative reverse transcriptase polymerase chain reaction (qRT-PCR), or qRT-loop-mediated isothermal amplification (LAMP),

c) predicting the cancer in the patient to be responsive to the treatment with fulvestrant if the level of expression of the GATA3 and ANXA1 biomarkers in the tumor sample is equal to or above a cutoff difference level of expression of the GATA3 and ANXA1 biomarkers in a cell or tissue known to be sensitive to the treatment with fulvestrant and predicting the cancer in the patient to be non-responsive to the treatment with fulvestrant if the level of expression of the GATA3 and ANXA1 biomarkers in the tumor sample is below the cutoff difference level of expression of the GATA3 and ANXA1 biomarkers in a cell or tissue known to be resistant to the treatment with fulvestrant, wherein the cutoff difference level is obtained by subtracting the level of the ANXA1 biomarker from the level of the GATA3 biomarker, and

(d) administering an effective amount of fulvestrant to said patient, wherein the patient has been determined to be responsive to fulvestrant.

2. The method of claim 1 , wherein said method further comprises quantifying a level of a biomarker of sensitivity selected from the group consisting of CBFA2T3, SPDEF, HBA1, TFF1, CD8B1, KIAA0984, BCL2, SLC9A3R1, FBP1, ITGB7, HIST1 H3H, PDCD4, CD37, HBA2, TARP, SPI1, KIAA0182, PTP4A3, ANXA1, GPX1, SPTBN1, ANXA2, CAPN2, ZA20D2, TMSB10, PRNP, TIMP1, PSMA1, PSMB2, UGP2, CD44, TM4SF1, MCF2L2, DNAPTP6, WDR1, PSMD1, VIM, RPS6KA3, MSN, PFN1, ASPH, YWHAB, LGALS3BP, ETF1, MARCKS, CAV2, ACTG1, SEPT10, and M-RIP.

3. The method of claim 1 , wherein said cancer is a hormone positive cancer.

4. The method of claim 1 , wherein said cancer is metastatic.

5. The method of claim 1 , wherein said patient is a female.

6. The method of claim 5 , wherein said female is a postmenopausal female.

7. The method of claim 6 , wherein said cancer has progressed following anti-estrogen therapy.

8. The method of claim 1 , wherein said sample is a biopsy.

9. The method of claim 1 , wherein the expression level of said GATA3 biomarker or said ANXA1 biomarker is measured using qRT-PCR.

10. The method of claim 1 , wherein the GATA3 biomarker is an mRNA.

11. The method of claim 1 , wherein the ANXA1 biomarker is an mRNA.

12. The method of claim 1 , wherein said method comprises converting the level of expression of the GATA3 biomarker or the ANXA1 biomarker into a mean score, wherein said mean score identifies the responsiveness of said patient to fulvestrant.

13. The method of claim 1 , wherein said method comprises:

(i) converting the level of expression of said GATA3 biomarker into a first mean score;

(ii) converting the level of expression of said ANXA1 biomarker into a second mean score;

(iii) subtracting said second mean score from said first mean score to obtain a difference score,

wherein a value of said difference score that is greater than or equal to a cutoff indicates said patient is responsive to fulvestrant.

14. The method of claim 1 , wherein said GATA3 biomarker has the sequence set forth in SEQ ID NO: 415; or

wherein said ANXA1 biomarker has the sequence set forth in SEQ ID NO: 431.

15. The method of claim 1 , wherein said breast cancer is hormone receptor positive breast cancer.

16. The method of claim 1 , wherein:

i) the single-stranded nucleic acid molecules capable of specifically hybridizing with nucleotides of the GATA3 biomarker have the sequence of any one of SEQ ID NO: 1-3 and 415, or a complement thereof; or

ii) the single-stranded nucleic acid molecules capable of specifically hybridizing with nucleotides of the ANXA1 biomarker have the sequence of any one of SEQ ID NO: 104 and 431, or a complement thereof.

17. The method of claim 16 , wherein said device comprises two or more of said single-stranded nucleic acid molecules of i) and ii).

18. The method of claim 1 , wherein said one or more single-stranded nucleic acid molecules have a length in the range of 10-100 nucleotides in length.

19. The method of claim 1 , wherein said device allowing, when contacted with a diverse population of nucleic acid molecules prepared from a sample under conditions allowing hybridization to occur, the quantification of the level of expression of the GATA3 and ANXA1 biomarkers.

20. The method of claim 1 , wherein said method further comprises quantifying a level of a biomarker of resistance selected from the group consisting of GPX1, SPTBN1, ANXA2, CAPN2, ZA20D2, TMSB10, PRNP, TIMP1, PSMA1, PSMB2, UGP2, CD44, TM4SF1, and ACTN4.

21. The method of claim 1 , wherein the expression level of said GATA3 biomarker or said ANXA1 biomarker is measured using microarray analysis.

22. The method of claim 1 , wherein the expression level of said GATA3 biomarker or said ANXA1 biomarker is measured using qRT-LAMP.

23. A method comprising administering an effective amount of fulvestrant to a patient with breast cancer, wherein the patient has a level of a GATA3 biomarker and an ANXA1 biomarker in a tumor sample that is equal to or above a cutoff difference level of a GATA3 biomarker and an ANXA1 biomarker in a cell or tissue known to be sensitive to treatment with fulvestrant, wherein the cutoff difference level is obtained by subtracting the level of the ANXA1 biomarker from the level of the GATA3 biomarker, thereby identifying the patient as responsive to fulvestrant.

24. The method of claim 23 , wherein the level of the GATA3 biomarker and the ANXA1 biomarker is determined by

a) contacting a tumor sample from the patient comprising one or more nucleic acid molecules with a device comprising:

i) single-stranded nucleic acid molecules capable of specifically hybridizing with nucleotides of the GATA3 biomarker; and

ii) single-stranded nucleic acid molecules capable of specifically hybridizing with nucleotides of the ANXA1 biomarker; and

b) quantifying the level of the GATA3 biomarker and the ANXA1 biomarker by performing microarray analysis, quantitative reverse transcriptase polymerase chain reaction (qRT-PCR), or qRT-loop-mediated isothermal amplification (LAMP).

25. A method of treating a patient with breast cancer, said method comprising:

a) contacting a tumor sample from the patient comprising one or more nucleic acid molecules with a device comprising:

i) single-stranded nucleic acid molecules capable of specifically hybridizing with nucleotides of a GATA3 biomarker; and

ii) single-stranded nucleic acid molecules capable of specifically hybridizing with nucleotides of an ANXA1 biomarker; and

b) quantifying a level of expression of the GATA3 biomarker and the ANXA1 biomarker by performing microarray analysis, quantitative reverse transcriptase polymerase chain reaction (qRT-PCR), or qRT-loop-mediated isothermal amplification (LAMP), and

c) administering an effective amount of fulvestrant to said patient having a level of expression of the GATA3 and ANXA1 biomarkers in the tumor sample that is equal to or above a cutoff difference level of expression of the GATA3 and ANXA1 biomarkers in a cell or tissue known to be sensitive to treatment with fulvestrant, wherein the cutoff difference level is obtained by subtracting the level of the ANXA1 biomarker from the level of the GATA3 biomarker, thereby identifying the patient as responsive to fulvestrant.

Assignments (4)
CHANGE OF NAME Recorded May 18, 2022
From: ONCOLOGY VENTURE PRODUCT DEVELOPMENT APS
To: ALLARITY THERAPEUTICS EUROPE APS
Reel/Frame 060107/0429 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 11, 2022
From: ALLARITY THERAPEUTICS A/S
To: ONCOLOGY VENTURE PRODUCT DEVELOPMENT APS
Reel/Frame 059888/0812 →
CHANGE OF NAME Recorded Apr 1, 2022
From: MEDICAL PROGNOSIS INSTITUTE A/S
To: ALLARITY THERAPEUTICS A/S
Reel/Frame 059569/0092 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 23, 2016
From: KNUDSEN, STEEN
To: MEDICAL PROGNOSIS INSTITUTE A/S
Reel/Frame 039843/0714 →
Priority Claims (1)
DK 2013 00348 · Jun 7, 2013 · national
Continuity (1)
Related Publication 20160138111A1 · May 19, 2016