Desidustat particles and compositions thereof

Desidustat particles, wherein at least 90% of the desidustat particles are less than about 250 μm.

Desidustat particles, wherein

• at least 90% of the desidustat particles are less than about 175 μm,
• at least 50% of the desidustat particles are less than about 75 μm, and
• at least 10% of the desidustat particles are less than about 10 μm.

Desidustat particles having specific surface area value of at least 0.75 m2/g.

A pharmaceutical composition comprising a therapeutically effective amount of desidustat particles and at least one pharmaceutically acceptable excipient, wherein at least 90% of the desidustat particles are less than about 250 μm, and wherein the composition provides a serum or plasma profile for desidustat comprising:

• (i) a mean of Cmax of from about 1,500 ng/ml to about 15,000 ng/ml, when administered to a patient in need thereof, or
• (ii) a mean of AUClast of from about 10,000 hr*ng/ml to about 75,000 hr*ng/ml, when administered to a patient in need thereof, or
• (iii) a Tmax of from about 0.5 hr to about 7.0 hr, when administered to a patient in need thereof.

A pharmaceutical composition comprising a therapeutically effective amount of desidustat particles and at least one pharmaceutically acceptable excipient, wherein at least 90% of the desidustat particles are less than about 250 μm, and wherein the composition does not contain 1-(but-3-en-1-yloxy)-4-hydroxy-2-oxo-1,2-dihydroquinoline-3-carbonyl) glycine more than 0.5% by weight of desidustat, as measured by HPLC, after storage for 3 months at 40°±2° C. and 75±5% relative humidity.

A pharmaceutical composition comprising a therapeutically effective amount of desidustat particles and at least one pharmaceutically acceptable excipient, wherein at least 90% of the desidustat particles are less than about 250 μm, and wherein the composition retains at least 95% of the desidustat after storage for 3 months at 40°±2° C. and 75±5% relative humidity.