Claims for Patent: 12,611,397

Summary for Patent: 12,611,397

Title:	Pharmaceutical composition of darolutamide
Abstract:	The present invention relates to a pharmaceutical composition for oral administration, particularly in the form of a tablet, comprising darolutamide or a pharmaceutically acceptable salt thereof as an active ingredient. Darolutamide is a potent androgen receptor (AR) modulator useful in the treatment of cancer, particularly AR dependent cancer such as prostate cancer, and other diseases where AR antagonism is desired.
Inventor(s):	Susanna ILMONEN, Juha LINTUNEN, Petteri LYYTINEN, Marko Saalasti
Assignee:	Orion Oyj
Application Number:	US19/182,859
Patent Claims:	1. A pharmaceutical composition in the form of a tablet comprising (a) 45-80%, per weight of the composition, of darolutamide or a pharmaceutically acceptable salt thereof; (b) 5-60%, per weight of the composition, of a filler; (c) 0.5-10%, per weight of the composition, of a disintegrant; (d) 0.5-10%, per weight of the composition, of a binder; and (e) 0.2-5%, per weight of the composition, of a lubricant; wherein the darolutamide or pharmaceutically acceptable salt thereof is present in an amount of 300 mg or 600 mg, wherein the tablet comprises an intragranular part and an extragranular part, and wherein the intragranular part comprises darolutamide or a pharmaceutically acceptable salt thereof, the filler, the binder and a portion of the disintegrant and the extragranular part comprises the lubricant and the rest of the disintegrant, and wherein the tablet has a compact tensile strength of at least about 3.5 MPa at average punch pressure of 200 MPa. 2. The pharmaceutical composition according to claim 1, wherein the filler comprises calcium hydrogen phosphate in combination with lactose and/or microcrystalline cellulose. 3. The pharmaceutical composition according to claim 1, wherein the disintegrant is croscarmellose sodium. 4. The pharmaceutical composition according to claim 1, wherein the binder is polyvinylpyrrolidone. 5. The pharmaceutical composition according to claim 1, wherein the lubricant is magnesium stearate. 6. The pharmaceutical composition according to claim 1, wherein the tablet is wet-granulated. 7. The pharmaceutical composition according to claim 1, wherein the pharmaceutical composition is in the form of a tablet, which provides a dissolution of at least 80% of darolutamide or a pharmaceutically acceptable salt thereof after 60 minutes in 0.01 M hydrochloric acid with 1.0% of sodium lauryl sulfate using paddle apparatus (USP apparatus 2) with paddle speed of 75 rpm at room temperature. 8. A tablet composition comprising a tablet core and a film coating, wherein the tablet core comprises: (a) about 300 mg of darolutamide or a pharmaceutically acceptable salt thereof; (b) about 60 mg of calcium hydrogen phosphate; (c) about 180 mg of lactose monohydrate; (d) about 30 mg of croscarmellose sodium; (e) about 24 mg of polyvinylpyrrolidone; and (f) about 5.4 mg of magnesium stearate, wherein the tablet core comprises an intragranular part and an extragranular part, and wherein the intragranular part comprises the darolutamide or a pharmaceutically acceptable salt thereof, the calcium hydrogen phosphate, the lactose monohydrate, the polyvinylpyrrolidone and a portion of the croscarmellose sodium and the extragranular part comprises the magnesium stearate and the rest of the croscarmellose sodium, and wherein the tablet composition has a compact tensile strength of at least about 3.5 MPa at average punch pressure of 200 MPa. 9. The pharmaceutical composition according to claim 1, wherein the pharmaceutical composition is in the form of an immediate release tablet. 10. A tablet composition comprising a tablet core and a film coating, wherein the tablet core comprises: (a) 300 mg of darolutamide or a pharmaceutically acceptable salt thereof; (b) 60 mg of calcium hydrogen phosphate; (c) 180 mg of lactose monohydrate; (d) 30 mg of croscarmellose sodium; (e) 24 mg of polyvinylpyrrolidone; and (f) 5.4 mg of magnesium stearate, wherein the tablet core comprises an intragranular part and an extragranular part, and wherein the intragranular part comprises the darolutamide or a pharmaceutically acceptable salt thereof, the calcium hydrogen phosphate, the lactose monohydrate, the polyvinylpyrrolidone and a portion of the croscarmellose sodium and the extragranular part comprises the magnesium stearate and the rest of the croscarmellose sodium.