US 12,453,754 B2
Leuprolide acetate compositions and methods of using the same to treat breast cancer
John Middleton, Fort Collins, CO (US); Avinash Nangia, Fort Collins, CO (US); John Arthur Mclane, Loveland, CO (US); and Terri L. Morton, Loveland, CO (US)
Assigned to Tolmar International Limited, Dublin (IE)
Appl. No. 17/614,312
Filed by TOLMAR INTERNATIONAL LIMITED, Dublin (IE)
PCT Filed May 26, 2020, PCT No. PCT/IB2020/054984
§ 371(c)(1), (2) Date Nov. 24, 2021,
PCT Pub. No. WO2020/240417, PCT Pub. Date Dec. 3, 2020.
Claims priority of provisional application 62/853,153, filed on May 27, 2019.
Prior Publication US 2022/0265760 A1, Aug. 25, 2022
Int. Cl. A61K 9/00 (2006.01); A61K 31/138 (2006.01); A61K 31/4196 (2006.01); A61K 31/566 (2006.01); A61K 38/09 (2006.01); A61K 47/22 (2006.01); A61K 47/34 (2017.01); A61P 35/00 (2006.01)
CPC A61K 38/09 (2013.01) [A61K 9/0024 (2013.01); A61K 31/138 (2013.01); A61K 31/4196 (2013.01); A61K 31/566 (2013.01); A61K 47/22 (2013.01); A61K 47/34 (2013.01); A61P 35/00 (2018.01)] 20 Claims
 
1. A method of suppressing ovarian function during treatment of hormone receptor-positive breast cancer in a subject comprising
subcutaneously administering to the subject in need thereof about every three months a therapeutically effective amount of a flowable, extended release composition comprising
a) N-methyl-2-pyrrolidone,
b) leuprolide or a pharmaceutically acceptable salt thereof, present in an amount to provide about 26 mg to about 30 mg of a free base equivalent of leuprolide, and
c) a biodegradable polymer comprising co-polymer segments of poly (lactide-co-glycolide) (PLG), wherein a molar ratio of lactide to glycolide monomers is about 75:25, wherein the biodegradable polymer has substantially no titratable carboxylic acid groups, and wherein at least one distal end group of the biodegradable polymer is hydroxyl-terminated, and
wherein upon contact of the flowable, extended release composition with a bodily fluid, the organic solvent dissipates and an in situ solid or semi-solid depot forms.