IP Library Granted Patent US 11,291,667
Granted Patent B2
US 11,291,667 · App. 16/480,557 · Granted Apr 5, 2022

Combination therapy involving diaryl macrocyclic compounds

Inventors: Jingrong Jean Cui (San Diego, CA); Dayong Zhai (San Diego, CA)
Assignee: TURNING POINT THERAPEUTICS, INC.
A61K31/519A61K31/506A61K31/517A61K31/5377A61K39/3955A61P35/00
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Quick Facts
Patent No.
US 11,291,667
App. No.
16/480,557
Granted
Apr 5, 2022
Kind
B2
Abstract

The present disclosure relates to methods and compositions for treating cancer with a diaryl macrocycle in combination with at least one other cancer therapeutic, such as an EGFR inhibitor.

Claims (17)

1. A method for treating cancer in a patient in need thereof, the method comprising the step of administering to the patient a therapeutically effective amount of a compound having structure:

or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of an EGFR inhibitor selected from afatinib, dacomitinib, gefitinib, and osimertinib, or a pharmaceutically acceptable salt thereof,

wherein the cancer is lung cancer.

2. The method of claim 1 , wherein the lung cancer is non-small cell lung cancer (NSCLC), adenocarcinoma, lung squamous cell carcinoma, large cell carcinoma, large cell neuroendocrine tumor, or small cell lung cancer (SCLC).

3. The method of claim 1 , wherein the lung cancer is non-small cell lung cancer or metastatic non-small cell lung cancer.

4. The method of claim 1 , wherein the EGFR inhibitor is afatinib or a pharmaceutically acceptable salt thereof.

5. The method of claim 1 , wherein the EGFR inhibitor is dacomitinib or a pharmaceutically acceptable salt thereof.

6. The method of claim 1 , wherein the EGFR inhibitor is gefitinib, or a pharmaceutically acceptable salt thereof.

7. The method of claim 1 , wherein the EGFR inhibitor is osimertinib or a pharmaceutically acceptable salt thereof.

8. The method of claim 1 , comprising oral administration.

9. The method of claim 1 , comprising from 0.1 mg to 1 g daily of the compound, or a pharmaceutically acceptable salt thereof.

10. The method of claim 1 , comprising from 50 mg to 250 mg daily of the compound, or a pharmaceutically acceptable salt thereof.

11. The method of claim 1 , comprising from 50 mg to 250 mg daily of the EGFR inhibitor, or a pharmaceutically acceptable salt thereof.

12. The method of claim 1 , wherein the compound and the EGFR inhibitor are individually formulated, and administered at the same time.

13. The method of claim 1 , comprising sequential administration of the compound and the EGFR inhibitor.

14. The method of claim 13 , comprising administering the compound first, and administering the EGFR inhibitor second.

15. The method of claim 13 , comprising administering the EGFR inhibitor first, and administering the compound second.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 7, 2021
From: CUI, JINGRONG JEAN; ZHAI, DAYONG
To: TP THERAPEUTICS, INC.
Reel/Frame 058315/0466 →
CHANGE OF NAME Recorded Dec 7, 2021
From: TP THERAPEUTICS, INC.
To: TURNING POINT THERAPEUTICS, INC.
Reel/Frame 058342/0008 →
Continuity (3)
Provisional Application 62619165 · Jan 19, 2018
Provisional Application 62450455 · Jan 25, 2017
Related Publication 20190381048A1 · Dec 19, 2019