IP Library Granted Patent US 12,458,630
Granted Patent B2
US 12,458,630 · App. 17/792,387 · Granted Nov 4, 2025

Combination therapy for cancer

Inventors: Michael Karin (La Jolla, CA); Hua Su (La Jolla, CA)
Assignee: The Regents of the University of California
A61K31/427A61K31/137A61K31/366A61P35/00
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Quick Facts
Patent No.
US 12,458,630
App. No.
17/792,387
Granted
Nov 4, 2025
Kind
B2
Abstract

Provided herein are methods and compositions for treating cancer through a combination of an inhibitor of macropinocytosis upregulation and an autophagy inhibitor. Also provided are methods and compositions for inducing cell death of cancer cells, and transgenic animal models regarding same.

Claims (9)

1. A method of inducing cell death of a cancer cell, the method comprising, contacting the cancer cell with:

(1) an inhibitor of macropinocytosis upregulation, wherein the inhibitor of macropinocytosis upregulation is an inhibitor of:

(a) NRF2 activity or expression selected from ML385 or Brusatol; or

(b) p62 activity or expression is selected from LP1-106 or XRK3F2;

and

(2) an autophagy inhibitor, wherein the autophagy inhibitor is selected from 3-Methyladenine (3-MA), LY294002, Bafilomycin A1 (Baf A1), Chloroquine (CQ), hydroxychloroquine (HCQ), ABT-737, an IKKα downregulator, obatoclax, Clarithromycin, Resveratrol, Quinacrine, 4-Acetylantroquinonol B, antroquinonol, Epigallocatechin gallate (EGCG), MRT68921 dihydrochloride, ULK1 inhibitors, MRT67307, SBI-0206965, ULK-100, ULK-101, DCC-3116, SAR405, Vps34-IN1 (PIK-III), SU1261, Vps34 inhibitors, or a combination thereof, thereby inducing cell death of the cancer cell.

2. The method of claim 1 , wherein the cancer cell is breast cancer, triple negative breast cancer, non-small-cell lung cancer, pancreatic cancer, leukemia, melanoma, colorectal cancer, bladder cancer, lung cancer, or pancreatic ductal adenocarcinoma (PDAC) cell.

3. The method of claim 1 , wherein the autophagy inhibitor is an inhibitor of ULK1, MRT68921 dihydrochloride, ULK-100, ULK-101, DCC-3116, or SBI-0206965.

4. The method of claim 1 , wherein contacting the cancer cell with the inhibitor of macropinocytosis upregulation and the autophagy inhibitor is sequential or concurrent.

Assignments (2)
CONFIRMATORY LICENSE Recorded Aug 2, 2023
From: UNIVERSITY OF CALIFORNIA SAN DIEGO
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 064476/0036 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 12, 2022
From: KARIN, MICHAEL; SU, HUA
To: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
Reel/Frame 060489/0575 →
Continuity (2)
Provisional Application 62960832 · Jan 14, 2020
Related Publication 20230068698A1 · Mar 2, 2023
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