Combination product of a Bcl-2/Bcl-xL inhibitor and a chemotherapeutic agent and use thereof in the prevention and/or treatment of diseases

Patent metadata

Field	Value
Publication number	US-12370197-B2
Application number	US-202017282024-A
Country	US
Kind code	B2
Filing date	Jul 30, 2020
Priority date	Jul 31, 2019
Publication date	Jul 29, 2025
Grant date	Jul 29, 2025

Abstract

Provided herein is a combination product comprising a Bcl-2/Bcl-xL inhibitor and a chemotherapeutic agent, in particular a Bcl-2/Bcl-xL inhibitor of formula (I-A) and homoharringtonine or an active derivative thereof, in free or pharmaceutically acceptable salt or solvate form. Provided herein is also the use of the aforementioned combination for the preparation of a medicament for the prevention and/or treatment of cancer, in particular of hematological malignancies, and to a method for the prevention and/or treatment of cancer, in particular of hematological malignancies, using the aforementioned combination.

First claim

The invention claimed is:

1. A combination product for the treatment of acute myeloid leukemia (AML) or myelodysplastic syndrome (MDS) comprising a Bcl-2/Bcl-xL inhibitor and a chemotherapeutic agent, wherein the Bcl-2/Bcl-xL inhibitor is a compound having the following formula:

or a pharmaceutically acceptable salt thereof;
wherein the chemotherapeutic agent is homoharringtonine or a pharmaceutically acceptable salt thereof.

2. The combination product according to claim 1 , wherein the combination product is in the form of a pharmaceutical composition, optionally comprising a pharmaceutically acceptable carrier, diluent or excipient; or the Bcl-2/Bcl-xL inhibitor and the chemotherapeutic agent are each in separate formulations.

3. The combination product according to claim 2 wherein the Bcl-2/Bcl-xL inhibitor and the chemotherapeutic agent each in separate formulations are administered simultaneously or sequentially.

4. The combination product according to claim 1 , wherein the combination product is in the form of tablets, capsules, granules, syrups, powders, lozenges, sachets, cachets, elixirs, suspensions, emulsions, solutions, syrups, aerosols, ointments, creams and injections.

5. A method of treating, reducing the frequency of symptoms of, or delaying the onset of symptoms of acute myeloid leukemia (AML) or myelodysplastic syndrome (MDS) in a patient in need thereof comprising administering a combination product according to claim 1 .

6. The method according to claim 5 , wherein the acute myeloid leukemia (AML) or myelodysplastic syndrome (MDS) is resistant to chemotherapy.

7. The method according to claim 5 , wherein the Bcl-2/Bcl-xL inhibitor or pharmaceutically acceptable salt thereof in the combination product is administered in an amount of about 0.0025-1500 mg/day.

8. The method according to claim 5 , wherein the chemotherapeutic agent or a pharmaceutically acceptable salt thereof in the combination product is administered in an amount of from about 0.005 mg/day to about 1000 mg/day.

Assignees

• Ascentage Pharma Suzhou Co Ltd
• Ascentage Pharma Group Corp Ltd

Inventors

• Yang Dajun
• Zhai Yifan
• Fang Douglas Dong
• Tang Qiuqiong

Classifications

• A61K45/06 Primary

  Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca · CPC title

• A61K31/675

  having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate · CPC title

• A61K31/635

  having a heterocyclic ring, e.g. sulfadiazine · CPC title

• A61K31/496

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

• A61P35/02

  specific for leukemia · CPC title