Combination of BCL-2/BCL-XL inhibitors and chemotherapeutic agent and use thereof

Patent metadata

Field	Value
Publication number	US-12083136-B2
Application number	US-201916630855-A
Country	US
Kind code	B2
Filing date	Jul 31, 2019
Priority date	Jul 31, 2018
Publication date	Sep 10, 2024
Grant date	Sep 10, 2024

Abstract

The present disclosure provides a pharmaceutical composition comprising a Bcl-2/Bcl-xL inhibitor, a chemotherapeutic agent, and a pharmaceutically acceptable carrier. The present disclosure also provides a method of treating cancer, comprising administering to a subject in need thereof a therapeutically effective amount of a Bcl-2/Bcl-xL inhibitor and a therapeutically effective amount of a chemotherapeutic agent. The present disclosure also provides use of a combination of a Bcl-2/Bcl-xL inhibitor and a chemotherapeutic agent in the manufacture of an anti-tumor medicament. In the present disclosure, a significantly enhanced anti-tumor effect can be achieved by administration of a Bcl-2/Bcl-xL inhibitor in combination with a chemotherapeutic agent.

First claim

What is claimed is:

1. A method of treating cancer comprising administering to a subject in need thereof a therapeutically effective amount of a Bcl-2/Bcl-xL inhibitor and a therapeutically effective amount of a chemotherapeutic agent, wherein the Bcl-2/Bcl-xL inhibitor is

or a pharmaceutically acceptable salt thereof,
wherein the chemotherapeutic agent is docetaxel or paclitaxel, and
wherein the cancer is small cell lung cancer.

2. The method according to claim 1 , wherein the cancer is a metastatic solid tumor.

3. The method according to claim 1 , wherein the cancer is Bcl-2/Bcl-xL and Bax positive.

4. The method according to claim 1 , wherein the Bcl-2/Bcl-xL inhibitor is administered at an amount from about 0.005 to about 500 mg/day, from about 0.05 to about 250 mg/day or from about 0.5 to about 100 mg/day.

Assignees

• Ascentage Pharma Suzhou Co Ltd

Inventors

• Yang Dajun
• Zhai Yifan
• Wang Guangfeng
• Fang Douglas Dong
• Deng Jing
• Qiu Miaozhen
• Zhang Lin

Classifications

• A61K31/513

  having oxo groups directly attached to the heterocyclic ring, e.g. cytosine · CPC title

• A61K31/496

  Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin · CPC title

• A61K31/4745

  condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines (yohimbine derivatives, vinblastine A61K31/475; ergoline derivatives A61K31/48) · CPC title

• A61K31/4045

  Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin · CPC title

• A61K31/337 Primary

  having four-membered rings, e.g. taxol · CPC title