IP Library › Granted Patent US 12,390,458
Granted Patent B2
US 12,390,458 · App. 17/260,398 · Granted Aug 19, 2025

Therapeutic combination of quinoline derivative and antibody

Inventors: Xin Tian (Nanjing, CN); Chen Shen (Nanjing, CN); Peng Lyu (Nanjing, CN); Xiangjian Wang (Nanjing, CN); Xiquan Zhang (Nanjing, CN); Zheng Liu (Nanjing, CN); Yu Xia (Zhongshan, CN); Xiaoping Jin (Zhongshan, CN); Baiyong Li (Zhongshan, CN); Zhongmin Maxwell Wang (Zhongshan, CN); Baohui Han (Shanghai, CN); Tianqing Chu (Shanghai, CN); Hua Zhong (Shanghai, CN); Rong Li (Shanghai, CN)
Assignee: CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LTD.
A61K31/4709A61K39/3955A61P35/00
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Quick Facts
Patent No.
US 12,390,458
App. No.
17/260,398
Granted
Aug 19, 2025
Kind
B2
Abstract

The present application provides a therapeutic combination of a quinoline derivative and an antibody, which comprises an immune checkpoint inhibitor and a tyrosine kinase inhibitor, wherein the tyrosine kinase inhibitor is a compound of formula I or a pharmaceutically acceptable salt thereof. The therapeutic combination in the present application shows good activity against lung tumor and liver tumor.

Claims (16)

1. A therapeutic combination, comprising:

a) an inhibitor for the interaction between PD-1 and its ligand PD-L1, wherein the inhibitor is an anti-PD-1 antibody or an antigen-binding fragment thereof, and wherein the anti-PD-1 antibody is sintilimab and

b) a tyrosine kinase inhibitor, wherein the tyrosine kinase inhibitor is a compound of formula I or a pharmaceutically acceptable salt thereof,

2. The therapeutic combination according to claim 1 , wherein the pharmaceutically acceptable salt of the compound of formula I is 1-[[[4-(4-fluoro-2-methyl-1H-indol-5-yl)oxy-6-methoxyquinolin-7-yl]oxy]methyl]cyclopropylamine hydrochloride.

3. The therapeutic combination according to claim 1 , comprising: a dihydrochloride of the compound of formula I; and sintilimab or an antigen-binding fragment thereof.

4. A method for treating cancer in an entity, comprising administering to the entity the therapeutically effective amount of a therapeutic combination according to claim 1 , wherein the cancer is non-small cell lung cancer.

5. The method according to claim 4 , wherein the anti-PD-1 antibody is administered about once a week (q1w), about once every 2 weeks (q2w), about once every 3 weeks (q3w), or about once every 4 weeks (q4w).

6. The method according to claim 4 , wherein the non-small cell lung cancer is driver gene-negative.

7. The method according to claim 6 , wherein 1, 2 or 3 of EGFR, ALK and ROS1 genes are mutation-negative.

8. The method according to claim 6 , wherein the cancer is recurrent and/or metastatic non-small cell lung cancer or locally advanced non-small cell lung cancer.

9. The method according to claim 4 , wherein the method is a first-line treatment for recurrent or metastatic non-small cell lung cancer.

10. The method according to claim 8 , wherein the non-small cell lung cancer is lung adenocarcinoma, squamous cell carcinoma of lung, or large cell lung carcinoma.

11. The method according to claim 4 , wherein the compound of formula I or the pharmaceutically acceptable salt thereof is administered according to a treatment cycle of 2 weeks (14 days) of treatment plus 1 week (7 days) of interruption.

12. The method according to claim 4 , wherein the therapeutic combination administered per treatment cycle comprises about 84-168 mg of the compound of formula I or the pharmaceutically acceptable salt thereof.

13. The method according to claim 4 , wherein 100-600 mg of the anti-PD-1 antibody is administered about once every 2 weeks (q2w) or about once every 3 weeks (q3w).

14. The method according to claim 4 , wherein the anti-PD-1 antibody or the antigen-binding fragment thereof and the tyrosine kinase inhibitor are each in the form of a pharmaceutical composition and can be administered simultaneously, sequentially, or at intervals.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 14, 2021
From: TIAN, XIN; SHEN, CHEN; LYU, PENG; WANG, XIANGJIAN; ZHANG, XIQUAN; LIU, ZHENG; XIA, YU; JIN, XIAOPING; LI, BAIYONG; WANG, ZHONGMIN MAXWELL; HAN, BAOHUI; CHU, TIANQING; ZHONG, HUA; LI, RONG
To: CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LTD.
Reel/Frame 055000/0009 →
Priority Claims (3)
CN 201810790198.6 · Jul 18, 2018 · national
CN 201811346173.6 · Nov 13, 2018 · national
CN 201910149525.4 · Feb 28, 2019 · national
Continuity (1)
Related Publication 20220160700A1 · May 26, 2022
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