Composition for preventing or treating metastatic ovarian cancer, endometrial cancer or breast cancer

Inventors

Lee, Jae HoWON, Cheolhee

Assignees

Lemonex Inc

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Publication Number

US-11779582-B2

Patent

Publication Date

2023-10-10

Expiration Date


Abstract

A method for treatment of cancer selected from the group consisting of metastatic ovarian cancer, endometrial cancer, and breast cancer includes administering a composition comprising a compound represented by Formula 1, a pharmaceutically acceptable salt thereof to a subject in need thereof: The composition can efficiently kill cancer cells present in a spheroid form, thereby being usefully applied as novel medicament for metastatic ovarian cancer, endometrial cancer or breast cancer.

Core Innovation

The invention relates to pharmaceutical compositions that comprise at least one compound represented by Formula 1 and/or a pharmaceutically acceptable salt thereof, for treatment of cancer in a spheroid form. The cancer is selected from metastatic ovarian cancer, endometrial cancer, and breast cancer, and the composition is administered to a subject in need thereof.

The document describes the use of a Formula 1 compound exemplified by BGJ398 as a pan-FGFR1-4 inhibitor. It links treatment of spheroid-form (3D) metastatic cancer cells to reduced cell survival signaling and states that the compound degrades spheroids and inhibits survival signaling via reduced phosphorylation of FGFR, AKT, and STAT3, leading to cell apoptosis.

The document further discloses combination therapy with chemical anticancer agents to address chemo-resistant cancer, including paclitaxel and other antimitotic or alkylating agents such as cisplatin. It reports comparison between 2D monolayer and 3D sphere culture models and indicates enhanced sensitivity and apoptosis in combination settings, including in paclitaxel-resistant cell lines.

Claims Coverage

The partial claim set provided contains three independent method claims. Across these claims, the coverage centers on treating spheroid-form cancers by administering a Formula 1 compound or pharmaceutically acceptable salt alone or in combination with paclitaxel, with additional limitations directed to paclitaxel resistance and paclitaxel-resistant cancer selection.

Spheroid-form cancer treatment with Formula 1 composition

Administering to a subject in need a composition comprising at least one compound represented by Formula 1 and a pharmaceutically acceptable salt thereof for treatment of cancer in a spheroid form selected from metastatic ovarian cancer, endometrial cancer, and breast cancer.

Paclitaxel-resistant spheroid-form cancer treatment with Formula 1 composition

Administering to a subject in need a composition comprising at least one compound represented by Formula 1 and a pharmaceutically acceptable salt thereof for treatment of spheroid-form cancer selected from metastatic ovarian cancer, endometrial cancer, and breast cancer, wherein the cancer is resistant to paclitaxel.

Combination of Formula 1 composition with paclitaxel for spheroid-form cancer

Administering to a subject in need a composition comprising at least one compound represented by Formula 1 and a pharmaceutically acceptable salt thereof and paclitaxel for treatment of spheroid-form cancer selected from metastatic ovarian cancer, endometrial cancer, and breast cancer.

The independent claims collectively cover methods for treating spheroid-form metastatic ovarian, endometrial, and breast cancers using a Formula 1 compound or pharmaceutically acceptable salt, including versions limited to paclitaxel-resistant cancer and a combination approach that includes paclitaxel.

Stated Advantages

Degrades spheroids and inhibits cell survival signaling via reduced phosphorylation of FGFR, AKT, and STAT3, leading to cell apoptosis.

Enhanced sensitivity and apoptosis in combination settings, including in paclitaxel-resistant cell lines.

Documented Applications

Preventing or treating metastatic ovarian, endometrial, and breast cancers in spheroid (3D) form using a Formula 1 compound composition administered to a subject in need.

Treatment of paclitaxel-resistant spheroid-form cancers selected from metastatic ovarian cancer, endometrial cancer, and breast cancer using a Formula 1 compound composition.

Combination treatment of spheroid-form metastatic ovarian, endometrial, and breast cancers using a Formula 1 compound composition together with paclitaxel.

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