Crystalline forms of 5-chloro-N4-[-2-(dimethylphosphoryl) phenyl]-N2-{2-methoxy-4-[4-(4-methylpiperazin-1-yl) piperidin-1-yl] phenyl} pyrimidine-2,4-diamine
View Patent ↗Novel crystalline forms of brigatinib, pharmaceutical compositions comprising the same, and methods of their preparation and use of the same are disclosed herein.
1. Crystalline Form H of brigatinib having the structure:
wherein the crystalline form has an x-ray powder diffraction pattern with peaks at 4.2, 5.2, 8.4, 10.9, 12.7, and 21.3° 2θ, with a variance of ±0.2° 2θ.
2. The crystalline Form H of claim 1 having an x-ray powder diffraction pattern as shown in FIG. 25 .
3. The crystalline Form H of claim 1 having an x-ray powder diffraction pattern with characteristic peaks at 4.2, 5.2, 8.4, 10.9, 12.7, 15.0, 15.7, 16.5, 17.2, 18.4, 19.5, and 21.3° 2θ, with a variance of ±0.2° 2θ.
4. A pharmaceutical composition comprising the crystalline Form H of brigatinib of claim 1 and at least component chosen from pharmaceutically acceptable carriers, pharmaceutically acceptable vehicles, and pharmaceutically acceptable excipients.
5. A method for treating non-small cell lung cancer in a subject in need thereof comprising administering to the subject the crystalline Form H of brigatinib of claim 1 .
6. The method of claim 5 , wherein the non-small cell lung cancer is ALK-positive non-small cell lung cancer.
7. The method of claim 6 , wherein the non-small cell lung cancer is ALK-positive metastatic non-small cell lung cancer.
8. The method of claim 7 , wherein the subject has been previously treated with crizotinib.