Combinations of an FGFR inhibitor and an IGF1R inhibitor
US-10736900-B2 · Aug 11, 2020 · US
Combination therapies for the treatment of hepatocellular carcinoma
US11833119B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-11833119-B2 |
| Application number | US-201916961292-A |
| Country | US |
| Kind code | B2 |
| Filing date | Jan 9, 2019 |
| Priority date | Jan 10, 2018 |
| Publication date | Dec 5, 2023 |
| Grant date | Dec 5, 2023 |
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- Title
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- Abstract
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Abstract
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Provided herein is a combination therapy useful for the treatment hepatocellular carcinoma. The combination comprises an FGFR4 inhibitor and lenvatinib.
First claim
Opening claim text (preview).
We claim: 1. A method of treating hepatocellular carcinoma in a patient in need thereof, comprising administering to the patient a combination of N-(2-((6-(3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-methylureido)pyrimidin-4-yl)amino)-5-(4-ethylpiperazin- 1-yl)phenyl)acrylamide or a pharmaceutically acceptable salt thereof and 4-[3-chloro-4-(N′-cyclopropylureido)phenoxy]-7-methoxyquinoline-6-carboxamide or a pharmaceutically acceptable salt thereof, wherein the N-(2-((6-(3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-methylureido)pyrimidin-4-yl)amino)-5-(4-ethylpiperazin-1-yl)phenyl)acrylamide or a pharmaceutically acceptable salt thereof is administered in a daily dosage between 50 mg to 600 mg. 2. The method of claim 1 , wherein the N-(2-((6-(3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-methylureido)pyrimidin-4-yl)amino)-5-(4-ethylpiperazin-1-yl)phenyl)acrylamide or a pharmaceutically acceptable salt thereof is administered in a daily dosage between 200 mg to 400 mg. 3. The method of claim 2 , wherein the N-(2-((6-(3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-methylureido)pyrimidin-4-yl)amino)-5-(4-ethylpiperazin-1-yl)phenyl)acrylamide or a pharmaceutically acceptable salt thereof is administered in a daily dosage of 300 mg. 4. The method of claim 1 , wherein the 4-[3-chloro-4-(N′-cyclopropylureido)phenoxy]-7-methoxyquinoline-6-carboxamide or pharmaceutically acceptable salt thereof is administered in a daily dosage of 8 mg. 5. The method of claim 1 , wherein the 4-[3-chloro-4-(N′-cyclopropylureido)phenoxy]-7-methoxyquinoline-6-carboxamide or pharmaceutically acceptable salt thereof is administered in a daily dosage of 12 mg. 6. The method of claim 1 , wherein the N-(2-((6-(3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-methylureido)pyrimidin-4-yl)amino)-5-(4-ethylpiperazin-1-yl)phenyl)acrylamide or a pharmaceutically acceptable salt thereof and the 4-[3-chloro-4-(N′-cyclopropylureido)phenoxy]-7-methoxyquinoline-6-carboxamide or a pharmaceutically acceptable salt thereof are administered as separate formulations. 7. The method of claim 1 , wherein the N-(2-((6-(3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-methylureido)pyrimidin-4-yl)amino)-5-(4-ethylpiperazin-1-yl)phenyl)acrylamide or a pharmaceutically acceptable salt thereof and the 4-[3-chloro-4-(N′-cyclopropylureido)phenoxy]-7-methoxyquinoline-6-carboxamide or a pharmaceutically acceptable salt thereof are administered as a single formulation. 8. The method of claim 1 , wherein the N-(2-((6-(3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-methylureido)pyrimidin-4-yl)amino)-5-(4-ethylpiperazin-1-yl)phenyl)acrylamide or a pharmaceutically acceptable salt thereof and the 4-[3-chloro-4-(N′-cyclopropylureido)phenoxy]-7-methoxyquinoline-6-carboxamide or a pharmaceutically acceptable salt thereof are administered sequentially. 9. The method of claim 1 , wherein the N-(2-((6-(3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-methylureido)pyrimidin-4-yl)amino)-5-(4-ethylpiperazin-1-yl)phenyl)acrylamide or a pharmaceutically acceptable salt thereof and the 4-[3-chloro-4-(N′-cyclopropylureido)phenoxy]-7-methoxyquinoline-6-carboxamide or a pharmaceutically acceptable salt thereof are administered simultaneously. 10. The method of claim 1 , wherein the N-(2-((6-(3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-methylureido)pyrimidin-4-yl)amino)-5-(4-ethylpiperazin-1-yl)phenyl)acrylamide is in free base form. 11. The method of claim 1 , wherein the pharmaceutically acceptable salt of N-(2-((6-(3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-methylureido)pyrimidin-4-yl)amino)-5-(4-ethylpiperazin-1-yl)phenyl)acrylamide is a free base form of N-(2-((6-(3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-methylureido)pyrimidin-4-yl)amino)-5-(4-ethylpiperazin-1-yl)phenyl)acrylamide. 12. The method of claim 1 , wherein the pharmaceutically acceptable salt of 4-[3-chloro-4-(N′-cyclopropylureido)phenoxy]-7-methoxyquinoline-6-carboxamide is a mesylate salt of 4-[3-chloro-4-(N′-cyclopropylureido)phenoxy]-7-methoxyquinoline-6-carboxamide. 13. The method of claim 1 , wherein the pharmaceutically acceptable salt of N-(2-((6-(3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-methylureido)pyrimidin-4-yl)amino)-5-(4-ethylpiperazin-1-yl)phenyl)acrylamide is a free base form of N-(2-((6-(3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-methylureido)pyrimidin-4-yl)amino)-5-(4-ethylpiperazin-1-yl)phenyl)acrylamide, and wherein the pharmaceutically acceptable salt of 4-[3-chloro-4-(N′-cyclopropylureido)phenoxy]-7-methoxyquinoline-6-carboxamide is a mesylate salt of 4-[3-chloro-4-(N′-cyclopropylureido)phenoxy]-7-methoxyquinoline-6-carboxamide. 14. A pharmaceutical formulation comprising N-(2-((6-(3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-methylureido)pyrimidin-4-yl)amino)-5-(4-ethylpiperazin-1- yl)phenyl)acrylamide or a pharmaceutically acceptable salt thereof, 4-[3-chloro-4-(N′-cyclopropylureido)phenoxy]-7-methoxyquinoline-6-carboxamide or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. 15. The pharmaceutical formulation of claim 14 , comprising a free base form of N-(2-((6-(3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-methylureido)pyrimidin-4-yl)amino)-5-(4- ethylpiperazin-1-yl)phenyl)acrylamide. 16. The pharmaceutical formulation of claim 14 , wherein the pharmaceutically acceptable salt of N-(2-((6-(3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-methylureido)pyrimidin-4-yl)amino)-5-(4-ethylpiperazin-1-yl)phenyl)acrylamide is a free base form of N-(2-((6-(3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-methylureido)pyrimidin-4-yl)amino)-5-(4-ethylpiperazin-1-yl)phenyl)acrylamide. 17. The pharmaceutical formulation of claim 14 , wherein the pharmaceutically acceptable salt of 4-[3-chloro-4-(N′-cyclopropylureido)phenoxy]-7-methoxyquinoline-6-carboxamide is a mesylate salt of 4-[3-chloro-4-(N′-cyclopropylureido)phenoxy]-7-methoxyquinoline-6-carboxamide. 18. The pharmaceutical formulation of claim 14 , wherein the pharmaceutically acceptable salt of N-(2-((6-(3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-methylureido)pyrimidin-4-yl)amino)-5-(4-ethylpiperazin-1-yl)phenyl)acrylamide is a free base form of N-(2-((6-(3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-methylureido)pyrimidin-4-yl)amino)-5-(4-ethylpiperazin-1-yl)phenyl)acrylamide, and wherein the pharmaceutically acceptable salt of 4-[3-chloro-4-(N′-cyclopropylureido)phenoxy]-7-methoxyquinoline-6-carboxamide is a mesylate salt of 4-[3-chloro-4-(N′-cyclopropylureido)phenoxy]-7-methoxyquinoline-6-carboxamide.
Assignees
Inventors
Classifications
Antineoplastic agents · CPC title
- A61K31/496Primary
Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin · CPC title
the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine · CPC title
- A61K31/47Primary
Quinolines; Isoquinolines · CPC title
- A61K31/506Primary
not condensed and containing further heterocyclic rings · CPC title
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- What does patent US11833119B2 cover?
- Provided herein is a combination therapy useful for the treatment hepatocellular carcinoma. The combination comprises an FGFR4 inhibitor and lenvatinib.
- Who is the assignee on this patent?
- Eisai R&D Man Co Ltd
- What technology area does this patent fall under?
- Primary CPC classification A61K31/496. Mapped technology areas include Human Necessities.
- When was this patent published?
- Publication date Tue Dec 05 2023 00:00:00 GMT+0000 (Coordinated Universal Time) (B2). Legal status and post-grant events are not shown on this page.
- What related patents are in patentsdb?
- We list 5 related publications on this page (citations in our corpus or others sharing the same primary CPC).