Conjugate of immune-stimulating il-2 analog and preparation method thereof
AssigneeHanmi Pharm. Co., Ltd.
InventorsYong Ho Heo, Euh Lim Oh, Da Hyeon Park, Jin Young Kim, Jun Sub Park, Yu Yon Kim, A Ram Lee, Sang Yun Kim
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Abstract
The present invention relates to a long-acting conjugate of an interleukin-2 analog with altered binding affinity for interleukin-2 receptors.
Claims12
A method for treating cancer, comprising administering to a human cancer patient in need thereof a pharmaceutical composition comprising a pharmaceutically effective amount of a long-acting conjugate and a pharmaceutically acceptable excipient,
- wherein the long-acting conjugate comprises an interleukin-2 analog, and is represented by Chemical Formula 1 below:
- X—La—F [Chemical Formula 1]
- wherein, X is an interleukin-2 analog having an increased binding affinity for interleukin-2 beta receptors compared to aldesleukin under a same condition;
- L is a polyethylene glycol linker;
- a is 0 or a natural number, with the proviso that when a is 2 or more, each L is independent of each other;
- F is an immunoglobulin Fc region in the form of a dimer;
- and
- — indicates a covalent linkage between X and L and between L and F;
- wherein the interleukin-2 analog comprises the amino acid sequence of SEQ ID NO:
- 87,
- wherein the cancer is selected from the group consisting of metastatic renal cell cancer, metastatic melanoma, colorectal cancer, pancreatic cancer, kidney cancer, lung cancer, melanoma, and breast cancer.
A method for treating cancer, comprising administering to a human cancer patient in need thereof a pharmaceutical composition comprising a pharmaceutically effective amount of a long-acting conjugate and a pharmaceutically acceptable excipient,
- wherein the long-acting conjugate comprises an interleukin-2 analog, and is represented by Chemical Formula 1 below:
- X—La—F [Chemical Formula 1]
- wherein, X is an interleukin-2 analog having an increased binding affinity for interleukin-2 beta receptors compared to aldesleukin under a same condition;
- L is a polyethylene glycol linker;
- a is 0 or a natural number, with the proviso that when a is 2 or more, each L is independent of each other;
- F is an immunoglobulin Fc region in the form of a dimer;
- and
- — indicates a covalent linkage between X and L and between L and F;
- wherein the interleukin-2 analog comprises the amino acid sequence selected from the group consisting of SEQ ID NO:
- 22, 42, and 53,
- wherein the cancer is selected from the group consisting of metastatic renal cell cancer, metastatic melanoma, and colorectal cancer.
Dependencies are inferred from the claim text.