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US 12,447,128 B2Granted
Formulations of enzalutamide
AssigneesAstellas Pharma Inc., Medivation Prostate Therapeutics, Inc.
InventorsDouglas Alan Lorenz, Sanjay Konagurthu, Randy J. Wald, Jason A. Everett, Sheila Matz, Yuuki Takaishi, Toshiro Sakai, Ryousuke Irie, Shinsuke Oba, Hiroyasu Toyota, Koji Nishimura, Atsushi Kanbayashi
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Abstract
This disclosure provides formulations of enzalutamide and their use for treating hyperproliferative disorders.
Claims4
A method of treating prostate cancer comprising:
- orally administering to a male human in need thereof two tablets, wherein each of the two tablets comprises:
- (a) a spray-dried dispersion consisting essentially of 80 mg amorphous enzalutamide and 400 mg hydroxypropyl methylcellulose acetate succinate;
- and
- (b) one or more inactive excipients;
- wherein the two tablets, when orally dosed to a cohort of male humans each receiving a 160 mg dose of enzalutamide, results in an area under the concentration-time curve that is equivalent to the area under the concentration-time curve that results from orally dosing four capsules to a cohort of male humans, wherein each of the four capsules comprises 40 mg enzalutamide dissolved in 904.96 mg caprylocaproyl polyoxylglycerides.
2 more elements
A method of treating prostate cancer comprising:
- orally administering to a male human in need thereof two tablets, wherein each of the two tablets comprises:
- (a) a spray-dried dispersion consisting essentially of 80 mg amorphous enzalutamide and 400 mg hydroxypropyl methylcellulose acetate succinate;
- and
- (b) one or more inactive excipients;
- wherein the two tablets, when orally dosed to a cohort of male humans each receiving a single 160 mg dose of enzalutamide, result in an area under the concentration-time curve from the time of dosing to seven days after dosing that is greater than 150 μg·hr/ml.
2 more elements
A method of treating prostate cancer comprising:
- orally administering to a male human in need thereof two tablets, wherein each of the two tablets comprises:
- (a) a spray-dried dispersion consisting essentially of 80 mg amorphous enzalutamide and 400 mg hydroxypropyl methylcellulose acetate succinate;
- and
- (b) one or more inactive excipients;
- wherein the amorphous enzalutamide remains amorphous following storage of the spray-dried dispersion at 40° C. and 75% relative humidity for one month.
2 more elements
A method of treating prostate cancer comprising:
- orally administering to a male human in need thereof two tablets, wherein each of the two tablets comprises:
- (a) a spray-dried dispersion consisting essentially of 80 mg amorphous enzalutamide and 400 mg hydroxypropyl methylcellulose acetate succinate;
- and
- (b) one or more inactive excipients;
- wherein the spray-dried dispersion has a glass transition temperature greater than 50° C. following equilibration overnight at ambient temperature and 75% relative humidity.
2 more elements
Dependencies are inferred from the claim text.