Claims for Patent: 12,383,503

Summary for Patent: 12,383,503

Title:	Adagrasib solid pharmaceutical compositions
Abstract:	Pharmaceutical compositions in solid form comprising adagrasib, suitable for oral dosage to treat subjects having cancer; as well as methods of manufacturing the compositions, and methods of treating cancer.
Inventor(s):	Cletus NUNES, Mehrdad KHEIRIPOUR, Monika GAVIREDDI
Assignee:	Mirati Therapeutics Inc
Application Number:	US18/794,390
Patent Claims:	1. A tablet formulation for oral administration in a human comprising (1) adagrasib; (2) one or more diluents selected from the group consisting of microcrystalline cellulose, mannitol, and a combination thereof; (3) crospovidone; (4) colloidal silicon dioxide; and (5) magnesium stearate; wherein a single oral dose of the tablet formulation provides a Cmax for adagrasib in the human that is lower as compared to a Cmax for adagrasib in the human provided by a single oral dose of a capsule formulation comprising the same amount of adagrasib. 2. The tablet formulation of claim 1, wherein the Cmax for adagrasib in the tablet formulation is about 13% lower than the Cmax of the capsule formulation when the human is under fasted conditions. 3. The tablet formulation of claim 1, wherein a side effect of nausea in the human is lower as compared to the side effect of nausea in humans administered the capsule formulation. 4. The tablet formulation of claim 1, wherein a side effect of vomiting in the human is lower as compared to the side effect of vomiting in humans administered the capsule formulation. 5. The tablet formulation of claim 1, wherein a side effect of diarrhea in the human is less as compared to the side effect of diarrhea in humans administered the capsule formulation. 6. The tablet formulation of claim 1, wherein a side effect of nausea in the human occurs in less than 17% of the total subject population. 7. The tablet formulation of claim 1, wherein a side effect of vomiting in the human occurs in less than 5% of the total subject population. 8. The tablet formulation of claim 1, wherein a side effect of diarrhea in the human occurs in less than 20% of the total subject population. 9. The tablet formulation of claim 1, wherein adagrasib constitutes about 30-67% of the tablet formulation; crospovidone constitutes about 2% to about 5% of the tablet formulation; colloidal silicon dioxide constitutes 0.5-2% of the tablet formulation; and magnesium stearate constitutes about 1-3% of the tablet formulation, wherein all percentages are percentages by weight. 10. The tablet formulation of claim 1, wherein adagrasib constitutes about 30-35% of the tablet formulation; the crospovidone constitutes about 2% to about 5% of the tablet formulation; the colloidal silicon dioxide constitutes up to about 0.5-1.5% of the tablet formulation; and the magnesium stearate constitutes about 1-2% of the tablet formulation, wherein all percentages are percentages by weight. 11. A tablet formulation for oral administration in a human comprising (1) adagrasib; (2) one or more diluents selected from the group consisting of microcrystalline cellulose, mannitol, and a combination thereof; (3) crospovidone; (4) colloidal silicon dioxide; and (5) magnesium stearate; wherein a single oral dose of the tablet formulation provides an AUC0→∞ for adagrasib in the human that is lower as compared to the AUC0→∞ for adagrasib in the human provided by a single oral dose of a capsule formulation comprising the same amount of adagrasib. 12. The tablet formulation of claim 11, wherein the AUC0→∞ for adagrasib in the tablet formulation is about 10% lower than the AUC0→∞ of the capsule formulation when the human is under fasted conditions. 13. The tablet formulation of claim 11, wherein a side effect of nausea in the human is lower as compared to the side effect of nausea in humans administered the capsule formulation. 14. The tablet formulation of claim 11, wherein a side effect of vomiting in the human is lower as compared to the side effect of vomiting in humans administered the capsule formulation. 15. The tablet formulation of claim 11, wherein a side effect of diarrhea in the human is less as compared to the side effect of diarrhea in humans administered the capsule formulation. 16. The tablet formulation of claim 11, wherein a side effect of nausea in the human occurs in less than 17% of the total subject population. 17. The tablet formulation of claim 11, wherein a side effect of vomiting in the human occurs in less than 5% of the total subject population. 18. The tablet formulation of claim 11, wherein a side effect of diarrhea in the human occurs in less than 20% of the total subject population. 19. The tablet formulation of claim 11, wherein adagrasib constitutes about 30-67% of the tablet formulation; the crospovidone constitutes about 2% to about 5% of the tablet formulation; the colloidal silicon dioxide constitutes 0.5-2% of the tablet formulation; and the magnesium stearate constitutes about 1-3% of the tablet formulation, wherein all percentages are percentages by weight. 20. The tablet formulation of claim 11, wherein adagrasib constitutes about 30-35% of the tablet formulation; the crospovidone constitutes about 2% to about 5% of the tablet formulation; the colloidal silicon dioxide constitutes up to about 0.5-1.5% of the tablet formulation; and the magnesium stearate constitutes about 1-2% of the tablet formulation, wherein all percentages are percentages by weight. 21. The tablet formulation of claim 1, wherein the one or more diluents comprise mannitol. 22. The tablet formulation of claim 1 wherein the mannitol comprises about 0-10% of the tablet formulation by weight percentage. 23. The tablet formulation of claim 1, wherein the one or more diluents comprise microcrystalline cellulose. 24. The tablet formulation of claim 23, wherein the microcrystalline cellulose comprises about 20-55% of the tablet formulation by weight percentage. 25. The tablet formulation of claim 1, further comprising a film coat. 26. The tablet formulation of claim 11, wherein the one or more diluents comprise mannitol. 27. The tablet formulation of claim 11, wherein the mannitol comprises about 0-10% of the tablet formulation by weight percentage. 28. The tablet formulation of claim 11, wherein the one or more diluents comprise microcrystalline cellulose. 29. The tablet formulation of claim 28, wherein the microcrystalline cellulose comprises about 20-55% of the tablet formulation by weight percentage. 30. The tablet formulation of claim 11, further comprising a film coat.