IP Library › Granted Patent US 10,449,187
Granted Patent B2
US 10,449,187 · App. 16/040,450 · Granted Oct 22, 2019

Formulations of 2-(4-chlorophenyl)-N-((2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-5-yl)methyl)-2,2-difluoroacetamide

Inventors: Ho-Wah Hui (Basking Ridge, NJ); Yu Pu (East Hanover, NJ)
Assignee: Celgene Corporation
A61K31/454A61K9/0019A61K9/0095A61K9/08A61K9/19A61K39/395A61K47/12A61K47/40C07K16/00A61K47/18A61K2039/505
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Quick Facts
Patent No.
US 10,449,187
App. No.
16/040,450
Granted
Oct 22, 2019
Kind
B2
Abstract

Provided herein are lyophilized formulations of 2-(4-chlorophenyl)-N-((2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-5-yl)methyl)-2,2-difluoroacetamide or a stereisomer or mixture of stereisomers, pharmaceutically acceptable salt, tautomer, prodrug, solvate, hydrate, co-crystal, clathrate, or polymorph thereof. Methods of using the formulations and dosage forms for treating, managing, and/or preventing cancer are also provided herein.

Claims (13)

1. A method of treating a cancer comprising administering to a mammal having cancer a lyophilized formulation comprising: Compound 1 (2-(4-chlorophenyl)-N-((2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-5-yl)methyl)-2,2-difluoroacetamide), or a stereoisomer or mixture of stereoisomers, pharmaceutically acceptable salt, tautomer, prodrug, solvate, hydrate, co-crystal, clathrate, or polymorph thereof, a buffer and a bulking agent, wherein the cancer is a solid tumor and the method further comprises administering calcium, calcitriol, and vitamin D supplementation.

2. The method of claim 1 , further comprising administering a therapeutically effective amount of a second active agent or a support care therapy.

3. The method of claim 2 , wherein the second active agent is 1) a therapeutic antibody that specifically binds to a cancer antigen or a pharmacologically active mutant thereof, 2) a hematopoietic growth factor, 3) a cytokine, 4) an anti-cancer agent, 5) an antibiotic, 6) a cox-2 inhibitor, 7) an immunomodulatory agent, 8) an immunosuppressive agent, or 9) a corticosteroid.

4. A method of treating a cancer comprising administering to a mammal having cancer a reconstituted formulation obtained from a lyophilized formulation and a diluent, wherein the lyophilized formulation comprises: Compound 1 (2-(4-chlorophenyl)-N-((2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-5-yl)methyl)-2,2-difluoroacetamide), or a stereoisomer or mixture of stereoisomers, pharmaceutically acceptable salt, tautomer, prodrug, solvate, hydrate, co-crystal, clathrate, or polymorph thereof, a buffer and a bulking agent, wherein the cancer is a solid tumor and the method further comprises administering calcium, calcitriol, and vitamin D supplementation.

5. The method of claim 4 , wherein the method comprises administering the formulation intravenously.

6. The method of claim 4 , further comprising administering a therapeutically effective amount of a second active agent or a support care therapy.

7. The method of claim 6 , wherein the second active agent is 1) a therapeutic antibody that specifically binds to a cancer antigen or a pharmacologically active mutant thereof, 2) a hematopoietic growth factor, 3) a cytokine, 4) an anti-cancer agent, 5) an antibiotic, 6) a cox-2 inhibitor, 7) an immunomodulatory agent, 8) an immunosuppressive agent, or 9) a corticosteroid.

8. The method of claim 1 , wherein the cancer is a cancer of bladder, bone, brain, breast, cervix, chest, colon, endrometrium, esophagus, eye, head, kidney, liver, lymph nodes, lung, mouth, neck, ovaries, pancreas, prostate, rectum, stomach, testis, throat, or uterus.

9. The method of claim 1 comprising administering calcium, calcitriol, and vitamin D supplementation with the lyophilized formulation.

10. The method of claim 1 comprising administering calcium, calcitriol, and vitamin D supplementation prior to the lyophilized formulation.

11. The method of claim 4 , wherein the cancer is a cancer of bladder, bone, brain, breast, cervix, chest, colon, endrometrium, esophagus, eye, head, kidney, liver, lymph nodes, lung, mouth, neck, ovaries, pancreas, prostate, rectum, stomach, testis, throat, or uterus.

12. The method of claim 4 comprising administering calcium, calcitriol, and vitamin D supplementation with the reconstituted formulation.

13. The method of claim 4 comprising administering calcium, calcitriol, and vitamin D supplementation prior to the reconstituted formulation.

Continuity (3)
Continuation 15400791 · Jan 6, 2017
Provisional Application 62276756 · Jan 8, 2016
Related Publication 20180353496A1 · Dec 13, 2018
Cited By (1)
US 12,577,223