Dosage forms of an estrogen receptor antagonist
Patent Information
- Application Number
- HK62026121803
- Authority / Receiving Office
- HK · HK
- Patent Type
- Applications
- Current Assignee / Owner
- Priority Date
- 2022-12-09
- Filing Date
- 2026-04-14
- Publication Date
- 2026-07-31
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Abstract
Description
S61-411 En + Ch DOSAGE FORMS OF AN ESTROGEN RECEPTOR ANTAGONIST The present disclosure provides unit dosage forms comprising Compound 1 (I) or a pharmaceutically acceptable salt thereof, that are useful for treatment of estrogen receptor mediator diseases, disorders, and conditions. The presently described unit dosage forms are suitable for oral administration. Abstract
Claims
CLAIMS1. A unit dosage form comprising Compound 1 :Compound 1 or a pharmaceutically acceptable salt thereof; a first diluent; a second diluent; and a disintegrant.
2. The unit dosage form of claim 1, wherein the unit dosage form comprises about 10% to about 20% by weight of Compound 1, or a pharmaceutically acceptable salt thereof, calculated as a free base.
3. The unit dosage form of claims 1 or 2, wherein the unit dosage form comprises about 10%> to about 15% by weight of Compound 1, or a pharmaceutically acceptable salt thereof, calculated as a free base.
4. The unit dosage form of any one of claims 1-3, wherein the unit dosage form comprises about 10% to about 80% by weight of the first diluent.
5. The unit dosage form of any one of claims 1-4, wherein the unit dosage form comprises about 10% to about 20% by weight of the second diluent.
6. The unit dosage form any one of claims 1-5, wherein a weight ratio of the first diluent to the second diluent is from about 3 : 1 to about 4: 1.
7. The unit dosage form of any one of claims 1-6, wherein the first diluent and the second diluent are different.
8. The unit dosage form of any one of claims 1-7, wherein the unit dosage form comprises about 5 to about 10% by weight of the disintegrant.
9. The unit dosage form of any one of claims 1-8, wherein the first diluent is selected from the group consisting of lactose monohydrate, microcrystalline cellulose, mannitol, calcium phosphate, lactose anhydrate, calcium silicate, and pregelatinized starch.
10. The unit dosage form of any one of claims 1-9, wherein the first diluent is selected from the group consisting of lactose monohydrate and mannitol.
11. The unit dosage form of any one of claims 1-10, wherein the first diluent is lactose monohydrate.
12. The unit dosage form of any one of claims 1-11, wherein the second diluent is selected from the group consisting of microcrystalline cellulose, lactose monohydrate, calcium phosphate, lactose anhydrate, calcium silicate, and pregelatinized starch.
13. The unit dosage form of any one of claims 1-12, wherein the second diluent is microcrystalline cellulose.
14. The unit dosage form of any one of claims 1-13, wherein the disintegrant is selected from the group consisting of croscarmellose sodium, sodium starch glycolate, crospovidone, and hydroxypropyl cellulose.
15. The unit dosage form of any one of claims 1-14, wherein the disintegrant is croscarmellose sodium.
16. The unit dosage form of any one of claims 1-15, wherein the unit dosage form comprises:about 12% by weight of Compound 1, or a pharmaceutically acceptable salt thereof, calculated as a free base; about 60% by weight of the first diluent; about 19% by weight of the second diluent; and about 8% by weight of the disintegrant.
17. The unit dosage form of any one of claims 1-16, further comprising a lubricant.
18. The unit dosage form of claim 17, wherein the unit dosage form comprises about 0.1 to about 1.5% by weight of the lubricant.
19. The unit dosage form of claims 17 or 18, wherein the lubricant is magnesium stearate.
20. The unit dosage form of any one of claims 1-19, wherein the unit dosage form comprises about 10 mg to about 120 mg of Compound 1, or a pharmaceutically acceptable salt thereof, calculated as a free base.
21. The unit dosage form of any one of claims 1-20, wherein the unit dosage form is in the form of a tablet.
22. The unit dosage form of any one of claims 1-21, characterized in that the unit dosage form, when stored at 40 °C / 75% RH for 1 month or more, exhibits greater than 80% dissolution in about 30 minutes or less using suitable dissolution conditions.
23. A unit dosage form comprising granules, wherein the granules comprise Compound 1 :Compound 1 or a pharmaceutically acceptable salt thereof; a first diluent; a second diluent; and a disintegrant.
24. The unit dosage form of claim 23, wherein the granules comprise Compound 1, or a pharmaceutically acceptable salt thereof, in an amount that is about 15% to about 20% of the total weight of the unit dosage form, calculated as a free base of Compound 1.
25. The unit dosage form of claims 23 or 24, wherein the granules comprise the first diluent in an amount that is about 5% to about 20% of the total weight of the unit dosage form.
26. The unit dosage form of any one of claims 23-25, wherein the granules comprise the second diluent in an amount that is about 50% to about 60% of the total weight of the unit dosage form.
27. The unit dosage form of any one of claims 23-26, wherein the granules comprise the disintegrant in an amount that is about 1% to about 5% of the total weight of the unit dosage form.
28. The unit dosage form of any one of claims 23-27, wherein the first diluent is selected from lactose monohydrate, microcrystalline cellulose, mannitol, calcium phosphate, lactose anhydrate, calcium silicate, and pregelatinized starch.
29. The unit dosage form of any one of claims 23-28, wherein the second diluent is selected from microcrystalline cellulose, lactose monohydrate, mannitol, calcium phosphate, lactose anhydrate, calcium silicate, and pregelatinized starch.
30. The unit dosage form of any one of claims 23-29, wherein the disintegrant selected from the group consisting of is croscarmellose sodium, sodium starch glycolate, crospovidone, and hydroxypropyl cellulose.
31. The unit dosage form of any one of claims 23-30, further comprising one or more extra- granular excipients.
32. The unit dosage form of any one of claims 23-31, wherein the unit dosage form is in the form of a tablet.
33. A method of treating an estrogen-receptor mediated disease, disorder, or condition, comprising administering to a subject in need thereof, the unit dosage form of any one of claims 1-32.
34. The method of claim 33, wherein the estrogen-receptor mediated disease, disorder, or condition is a cancer.
35. The method of claim 34, wherein the cancer is a breast cancer.
36. The method of claim 34, wherein the cancer is a breast cancer that has metastasized to the lungs, liver, bones, or brain.
37. The method of any one of claims 33-36, further comprising administering a secondary anti- cancer agent.
38. The method of claim 37, wherein the secondary anti-cancer agent is a CDK 4 / 6 inhibitor, a PI3KCA inhibitor, or an mTOR inhibitor.
39. The method of claim 38, wherein the secondary anti-cancer agent is a CDK 4 / 6 inhibitor.
40. The method of claim 39, wherein the CDK 4 / 6 inhibitor is selected from the group consisting of palbociclib, ribociclib, abemaciclib, lerociclib, trilaciclib, and SHR6390.
41. The method of claim 38, wherein the secondary anti-cancer agent is a PIK3CA inhibitor.
42. The method of claim 41, wherein the PIK3CA inhibitor is selected from the group consisting of alpelisib, taselisib, and LY3023414.
43. The method of claim 38, wherein the secondary anti-cancer agent is an mTOR inhibitor.
44. The method of claim 43, wherein the mTOR inhibitor is selected from the group consisting of sirolimus, temsirolimus, everolimus, and LY3023414.
45. The method of claim 38, wherein the secondary anti-cancer agent is a HER2 inhibitor.
46. The method of claim 45, wherein the HER2 inhibitor is selected from the group consisting of tucatinib, pertuzumab, lapatinib, trastuzumab, ado-trastuzumab emtansine, trastuzumab deruxtecan, and neratinib.