Formulations of enzalutamide

Patent metadata

Field	Value
Publication number	US-12447128-B2
Application number	US-202217985220-A
Country	US
Kind code	B2
Filing date	Nov 11, 2022
Priority date	Sep 11, 2012
Publication date	Oct 21, 2025
Grant date	Oct 21, 2025

Abstract

This disclosure provides formulations of enzalutamide and their use for treating hyperproliferative disorders.

First claim

The invention claimed is:

1. 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. 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.

3. 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.

4. 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.

Assignees

• Astellas Pharma Inc
• Medivation Prostate Therapeutics Llc

Inventors

• Lorenz Douglas Alan
• Konagurthu Sanjay
• Wald Randy J
• Everett Jason A
• Matz Sheila
• Takaishi Yuuki
• Sakai Toshiro
• Irie Ryousuke
• Oba Shinsuke
• Toyota Hiroyasu
• Nishimura Koji
• Kanbayashi Atsushi

Classifications

• A61K31/4164 Primary

  1,3-Diazoles · CPC title

• A61K9/2095

  Tabletting processes · CPC title

• A61K9/1652

  Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin (homeopathic globules A61K9/1623) · CPC title

• A61K9/16

  Agglomerates; Granulates; Microbeadlets {; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction (A61K9/20 takes precedence if the final form is a tablet; microspheres with drug-free outer coating, microcapsules A61K9/50; mixture of different granules, microcapsules, (coated) microparticles A61K9/5084; nanoparticles A61K9/51)} · CPC title

• A61K47/38

  Cellulose; Derivatives thereof · CPC title