Claims for Patent: 10,869,928

Summary for Patent: 10,869,928

Title:	Lyophilized preparation of cytotoxic dipeptides
Abstract:	The present invention is directed to novel lyophilized pharmaceutical preparations comprising a cytotoxic dipeptides such as melphalan flufenamide and one or more excipient(s) selected from the group comprising a polysorbate; a polyethylene glycol; .beta.-cyclodextrin; ocyclodextrin; hydroxypropyl-.beta.-cyclodextrin; sulfobutylether-.beta.-cyclodextrin; lactose; benzyl alcohol; disodium succinate; propylene glycol; Cremophor EL; Dimethyl sulfoxide; D-mannitol; Trehalose; Sucrose and an amino acid. This preparation may be further formulated and is useful in cancer therapy.
Inventor(s):	Spira; Jack (Tyreso, SE), Lehmann; Fredrik (Knivsta, SE)
Assignee:	ONCOPEPTIDES AB (Stockholm, SE)
Application Number:	16/721,639
Patent Claims:	1. A lyophilized pharmaceutical preparation which is directly soluble in a physiologically acceptable aqueous solution, comprising melphalan flufenamide, or a pharmaceutically acceptable salt thereof, and sucrose. 2. The lyophilized pharmaceutical preparation according to claim 1, wherein the amount of sucrose is 10-100% by weight of the melphalan flufenamide or pharmaceutically acceptable salt thereof. 3. The lyophilized pharmaceutical preparation according to claim 1, which is free, or substantially free from organic solvents. 4. The lyophilized pharmaceutical preparation according to claim 2, which is free, or substantially free from organic solvents. 5. A pharmaceutical composition consisting of the lyophilized pharmaceutical preparation of claim 1 and a physiologically acceptable solution, wherein said physiologically acceptable solution is a glucose solution. 6. A pharmaceutical composition consisting of the lyophilized pharmaceutical preparation of claim 2 and a physiologically acceptable solution, wherein said physiologically acceptable solution is a glucose solution. 7. A pharmaceutical composition consisting of the lyophilized pharmaceutical preparation of claim 3 and a physiologically acceptable solution, wherein said physiologically acceptable solution is a glucose solution. 8. A pharmaceutical composition consisting of the lyophilized pharmaceutical preparation of claim 4 and a physiologically acceptable solution, wherein said physiologically acceptable solution is a glucose solution. 9. The lyophilized pharmaceutical preparation according to claim 1, in which sucrose is the sole excipient. 10. The lyophilized pharmaceutical preparation according to claim 9, which contains trace amounts of an organic solvent. 11. The lyophilized pharmaceutical preparation according to claim 1, which consists essentially of melphalan flufenamide, or a pharmaceutically acceptable salt thereof, and sucrose. 12. The lyophilized pharmaceutical preparation according to claim 11, which contains trace amounts of an organic solvent. 13. The lyophilized pharmaceutical preparation according to claim 9, which consists essentially of melphalan flufenamide, or a pharmaceutically acceptable salt thereof, and sucrose. 14. The lyophilized pharmaceutical preparation according to claim 13, which contains trace amounts of an organic solvent. 15. The lyophilized pharmaceutical preparation according to any one of claims 1 to 4, which is obtained by lyophilizing a solution comprising melphalan flufenamide, or a pharmaceutically acceptable salt thereof, sucrose, an organic solvent and water. 16. The lyophilized pharmaceutical preparation according to any one of claims 9 to 14, which is obtained by lyophilizing a solution of melphalan flufenamide, or a pharmaceutically acceptable salt thereof, sucrose, an organic solvent and water.