IP Library Granted Patent US 11,497,733
Granted Patent B2
US 11,497,733 · App. 15/549,866 · Granted Nov 15, 2022

Combination therapy of HSP90 inhibitors and PD-1 inhibitors for treating cancer

Inventors: David A. Proia (Newton, MA); Patricia E. Rao (Acton, MA)
Assignee: Synta Pharmaceuticals Corp.
A61K31/4196A61K31/6615A61K31/675A61K39/3955A61K39/39558C07K16/2818C07K16/2827C07K16/3046A61K2039/505A61K2039/545C07K2317/24C07K2317/76
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Quick Facts
Patent No.
US 11,497,733
App. No.
15/549,866
Granted
Nov 15, 2022
Kind
B2
Abstract

A pharmaceutical composition comprising a PD-1 inhibitor and a Hsp90 inhibitor, or a tautomer, or a pharmaceutically acceptable salt thereof, wherein the Hsp90 inhibitor is 3-(2,4-dihydroxy-5-isopropyl-phenyl)-4-(1-methyl-indol-5-yl)-5-hydroxy-[1,2,4] triazole or 5-hydroxy-4-(5-hydroxy-4-(1-methyl-1H-indol-5-yl)-4H-1,2,4-triazol-3-yl)-2-isopropylphenyl dihydrogen phosphate. Also provided is a method for treating cancer in a subject in need thereof, using the pharmaceutical composition described herein.

Claims (13)

1. A method of treating cancer in a subject in need thereof, comprising administering to the subject an effective amount of a PD-1 inhibitor and an effective amount of a Hsp90 inhibitor, or a tautomer, or a pharmaceutically acceptable salt thereof, wherein the Hsp90 inhibitor is 3-(2,4-dihydroxy-5-isopropyl-phenyl)-4-(1-methyl-indol-5-yl)-5-hydroxy-[1,2,4] triazole or 5-hydroxy-4-(5-hydroxy-4-(1-methyl-1H-indol-5-yl)-4H-1,2, 4-triazol-3-yl)-2-isopropylphenyl dihydrogen phosphate; wherein the PD-1 inhibitor is nivolumab, pembrolizumab, pidilizumab, BMS 936559, MPDL3280A, MSB0010718C or MEDI4736; wherein the Hsp90 inhibitor is administered to the subject in a dose of about 125 mg/kg; and wherein the cancer is colon cancer or melanoma.

2. The method of claim 1 , wherein the cancer is melanoma.

3. The method of claim 1 , wherein the cancer is colon cancer.

4. The method of claim 1 , wherein the PD-1 inhibitor binds PD-L1.

5. The method of claim 1 , wherein the Hsp90 inhibitor is administered IV once weekly or twice weekly.

6. The method of claim 1 , wherein the Hsp90 inhibitor is 3-(2,4-dihydroxy-5-isopropyl-phenyl)-4-(1-methyl-indol-5-yl)-5-hydroxy-[1,2,4] triazole, or a pharmaceutically acceptable salt thereof.

7. The method of claim 1 , wherein the Hsp90 inhibitor is 5-hydroxy-4-(5-hydroxy-4-(1-methyl-1H-indol-5-yl)-4H-1,2,4-triazol-3-yl)-2-isopropylphenyl dihydrogen phosphate, or a pharmaceutically acceptable salt thereof.

8. The method of claim 1 , wherein the PD-1 inhibitor is nivolumab.

9. The method of claim 1 , wherein the PD-1 inhibitor is pembrolizumab.

10. The method of claim 1 , wherein the PD-1 inhibitor and the Hsp90 inhibitor are administered separately.

11. The method of claim 1 , wherein the PD-1 inhibitor and the Hsp90 inhibitor are administered simultaneously.

12. A method of treating cancer in a subject in need thereof, comprising administering to the subject an effective amount of a PD-1 inhibitor and an effective amount of a Hsp90 inhibitor, or a tautomer, or a pharmaceutically acceptable salt thereof, wherein the Hsp90 inhibitor is 3-(2,4-dihydroxy-5-isopropyl-phenyl)-4-(1-methyl-indol-5-yl)-5-hydroxy-[1,2,4] triazole or 5-hydroxy-4-(5-hydroxy-4-(1-methyl-1H-indol-5-yl)-4H-1,2,4-triazol-3-yl)-2-isopropylphenyl dihydrogen phosphate; wherein the PD-1 inhibitor is nivolumab, pembrolizumab, pidilizumab, BMS 936559, MPDL3280A, MSB0010718C or MEDI4736; wherein the Hsp90 inhibitor is administered to the subject in a dose of about 125 mg/kg; and wherein the cancer is colon cancer.

13. A method of treating cancer in a subject in need thereof, comprising administering to the subject an effective amount of a PD-1 inhibitor and an effective amount of a Hsp90 inhibitor, or a tautomer, or a pharmaceutically acceptable salt thereof, wherein the Hsp90 inhibitor is 3-(2,4-dihydroxy-5-isopropyl-phenyl)-4-(1-methyl-indol-5-yl)-5-hydroxy-[1,2,4] triazole or 5-hydroxy-4-(5-hydroxy-4-(1-methyl-1H-indol-5-yl)-4H-1,2,4-triazol-3-yl)-2-isopropylphenyl dihydrogen phosphate; wherein the PD-1 inhibitor is nivolumab, pembrolizumab, pidilizumab, BMS 936559, MPDL3280A, MSB0010718C or MEDI4736; wherein the Hsp90 inhibitor is administered to the subject in a dose of about 125 mg/kg; and wherein the cancer is melanoma.

Assignments (2)
SECURITY INTEREST Recorded Jul 17, 2025
From: MADRIGAL PHARMACEUTICALS, INC.
To: LSI FINANCING LLC, AS ADMINISTRATIVE AGENT
Reel/Frame 072038/0693 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 5, 2017
From: PROIA, DAVID A.; RAO, PATRICIA E.
To: SYNTA PHARMACEUTICALS CORP.
Reel/Frame 043793/0627 →
Continuity (2)
Provisional Application 62113807 · Feb 9, 2015
Related Publication 20180064689A1 · Mar 8, 2018