IP Library Granted Patent US 12667565
Granted Patent B2
US 12667565 · App. 17/779,826 · Granted Jun 30, 2026

Use of composition for enhancing anticancer effect, comprising ERRy inhibitor as active ingredient

Inventors: Keun Gyu Park (Daegu, KR); In Kyu Lee (Daegu, KR); Sung Jin Cho (Daegu, KR); Yeon Kyung Choi (Daegu, KR); Mi Jin Kim (Daegu, KR); Jung Wook Chin (Daegu, KR); Yong Hyun Jeon (Daegu, KR); Jin A Kim (Daegu, KR); Dong Su Kim (Daegu, KR); Hoe Yune Jung (Pohang-si, KR)
Assignee: NOVMETAPHARMA CO., LTD.
A61K31/495A61K31/44A61K31/7105A61P35/00C07K16/2869C12N15/115G01N33/5758G01N33/6875
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Quick Facts
Patent No.
US 12667565
App. No.
17/779,826
Granted
Jun 30, 2026
Kind
B2
Abstract

The present invention relates to a pharmaceutical composition for inhibiting the resistance of liver cancer to sorafenib and enhancing an anticancer effect, comprising an Estrogen-related receptor γ (ERRγ) inhibitor as an active ingredient. The present invention can be effectively used as a pharmaceutical composition for treating sorafenib-resistant advanced liver cancer.

Claims (17)

1 . A method for diagnosis and treatment of sorafenib-resistant liver cancer, comprising the following steps:

(a) measuring an expression level of mRNA of an estrogen-related receptor γ (ERRγ) gene or a protein expressed therefrom in a biological sample isolated from a test patient with liver cancer;

(b) comparing the measured expression level of the ERRγ mRNA and/or the measured level of ERRγ protein of the test patient of step (a) with a reference expression level of ERRγ mRNA and/or a reference level of ERRγ protein, said reference expression level of ERRY mRNA and/or a reference level of ERRγ protein being obtained from a reference patient with a liver cancer other than sorafenib-resistant liver cancer,

wherein a higher measured expression level of the ERRγ mRNA than the reference expression level and/or a higher measured level of ERRγ protein than the reference level indicates that the test patient has sorafenib-resistant liver cancer; and

(c) administering to the test patent who is determined to have sorafenib-resistant liver cancer, (i) an agent capable of inhibiting ERRγ protein activity or ERRγ gene expression; (ii) a combination of sorafenib and an agent capable of inhibiting ERRγ protein activity or ERRγ gene expression.

2 . The method of claim 1 , wherein the biological sample comprises liver tissue, liver cells, whole blood, plasma, or serum.

3 . A method selected from the group consisting of:

(a) preventing or inhibiting a development of sorafenib resistance in a liver cancer patient who is prescribed for sorafenib treatment or underwent sorafenib treatment; and

(b) enhancing sorafenib treatment of a liver cancer patient,

said method comprising administering to the liver cancer patient an effective amount of an inverse agonist against estrogen-related receptor γ (ERRγ),

wherein the inverse agonist against ERRγ is a compound of the following Formula 1 or a pharmaceutically acceptable salt thereof:

4 . The method of claim 3 , which further comprises administering sorafenib, wherein the inverse agonist is administered simultaneously with sorafenib, separately, or sequentially.

5 . A method of treating liver cancer in a subject in need thereof, comprising:

administering an effective amount of an inverse agonist against estrogen-related receptor γ (ERRγ),

wherein the inverse agonist against ERRγ is a compound of the following Formula 1 or a pharmaceutically acceptable salt thereof:

6 . The method of claim 1 , wherein the agent is administered simultaneously with sorafenib, separately, or sequentially.

7 . The method of claim 5 , wherein the inverse agonist is administered simultaneously with sorafenib, separately, or sequentially.