IP Library Granted Patent US 11,312,772
Granted Patent B2
US 11,312,772 · App. 16/635,059 · Granted Apr 26, 2022

Combinations of PD-1 antagonists and benzo [b] thiophene STING agonists for cancer treatment

Inventors: Saso Cemerski (Norfolk, MA); Jared N. Cumming (Winchester, MA); Johnny E. Kopinja (Newton, MA); Samanthi A. Perera (Lexington, MA); Benjamin Wesley Trotter (Medfield, MA); Archie Ngai-Chiu Tse (Long Island City, NY)
Assignee: MERCK SHARP & DOHME CORP.
C07K16/2818A61K31/381A61P35/00A61K2039/505
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Quick Facts
Patent No.
US 11,312,772
App. No.
16/635,059
Granted
Apr 26, 2022
Kind
B2
Abstract

Therapeutic combinations that comprise at least one antagonist of the Programmed Death 1 receptor (PD-1) and at least one benzo[b]thiophene compound that activates the Stimulator of Interferon Genes (STING) pathway are disclosed herein. Also disclosed is the use of such therapeutic combinations for the treatment of cancers.

Claims (17)

1. A method of treating cancer, said method comprising administering to a subject in need thereof a combination therapy that comprises

a) a PD-1 antagonist; and

b) a benzo[b]thiophene STING agonist; wherein

the PD-1 antagonist is administered once every 21 days; and

the benzo[b]thiophene STING agonist is administered once every 3 to 28 days; and

the benzo[b]thiophene STING agonist is selected from the group consisting of:

or a pharmaceutically acceptable salt thereof.

2. The method according to claim 1 , wherein the cancer occurs as one or more solid tumors or lymphomas.

3. The method according to claim 1 , wherein the cancer is selected from the group consisting of advanced or metastatic solid tumors and lymphomas.

4. The method according to claim 1 , wherein the cancer is selected from the group consisting of malignant melanoma, head and neck squamous cell carcinoma, breast adenocarcinoma, and lymphoma.

5. The method according to claim 2 , wherein the lymphoma is selected from the group consisting of diffuse large B-cell lymphoma, follicular lymphoma, mantle cell lymphoma, small lymphocytic lymphoma, mediastinal large B-cell lymphoma, splenic marginal zone B-cell lymphoma, extranodal marginal zone B-cell lymphoma of mucosa-associated lymphoid tissue (malt), nodal marginal zone B-cell lymphoma, lymphoplasmacytic lymphoma, primary effusion lymphoma, Burkitt lymphoma, anaplastic large cell lymphoma (primary cutaneous type), anaplastic large cell lymphoma (systemic type), peripheral T-cell lymphoma, angioimmunoblastic T-cell lymphoma, adult T-cell lymphoma, nasal type extranodal NK/T-cell lymphoma, enteropathy-associated T-cell lymphoma, gamma/delta hepatosplenic T-cell lymphoma, subcutaneous panniculitis-like T-cell lymphoma, mycosis fungoides, and Hodgkin lymphoma.

6. The method according to claim 1 , wherein the cancer has metastasized.

7. The method according to claim 1 , wherein the PD-1 antagonist is an anti-PD-1 monoclonal antibody.

8. The method according to claim 7 , wherein the PD-1 antagonist is selected from the group consisting of nivolumab, pembrolizumab, pidilizumab, and AMP-224.

9. The method according to claim 8 , wherein the PD-1 antagonist is nivolumab.

10. The method according to claim 8 , wherein the PD-1 antagonist is pembrolizumab.

11. The method of claim 1 , wherein the PD-1 antagonist is administered by intravenous infusion, and the benzo[b]thiophene STING agonist is administered orally, by intravenous infusion, by intertumoral injection or by subcutaneous injection.

Assignments (3)
MERGER Recorded Aug 8, 2022
From: MERCK SHARP & DOHME CORP.
To: MERCK SHARP & DOHME LLC
Reel/Frame 061102/0145 →
CORRECTIVE ASSIGNMENT TO CORRECT SPELLING OF THE FOURTH ASSIGNOR'S FIRST NAME ON THE COVER SHEET PREVIOUSLY RECORDED AT REEL/FRAME 052782/0665 ASSIGNOR HEREBY CONFIRMS THE ASSIGNMENT. Recorded Aug 12, 2020
From: CEMERSKI, SASO; CUMMING, JARED N.; KOPINJA, JOHNNY E.; PERERA, SAMANTHI A.; TROTTER, BENJAMIN WESLEY; TSE, ARCHIE NGAI-CHIU
To: MERCK SHARP & DOHME CORP.
Reel/Frame 053480/0880 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 29, 2020
From: CEMERSKI, SASO; CUMMING, JARED N.; KOPINJA, JOHNNY E.; PERERA, SAMANTHA A.; TROTTER, BENJAMIN WESLEY; TSE, ARCHIE NGAI-CHIU
To: MERCK SHARP & DOHME CORP.
Reel/Frame 052782/0665 →