US 12,403,182 B2
Liquid pharmaceutical formulations of PTH conjugates
Anja R. H. Skands, Hellerup (DK); Felix Cleemann, Heidelberg (DE); Michael Duelund Sørensen, Hellerup (DK); Julia Baron, Heidelberg (DE); Eric Hoffmann, Heidelberg (DE); and Kennett Sprogøe, Hellerup (DK)
Assigned to ASCENDIS PHARMA BONE DISEASES A/S, Hellerup (DK)
Appl. No. 17/428,608
Filed by Ascendis Pharma Bone Diseases A/S, Hellerup (DK)
PCT Filed Feb. 10, 2020, PCT No. PCT/EP2020/053316
§ 371(c)(1), (2) Date Aug. 4, 2021,
PCT Pub. No. WO2020/165087, PCT Pub. Date Aug. 20, 2020.
Claims priority of application No. 19156485 (EP), filed on Feb. 11, 2019; and application No. 19168857 (EP), filed on Apr. 12, 2019.
Prior Publication US 2022/0088149 A1, Mar. 24, 2022
Int. Cl. A61K 38/29 (2006.01); A61K 47/10 (2017.01); A61K 47/12 (2006.01); A61K 47/18 (2017.01); A61K 47/26 (2006.01); A61K 47/54 (2017.01); A61K 47/60 (2017.01)
CPC A61K 38/29 (2013.01) [A61K 47/10 (2013.01); A61K 47/12 (2013.01); A61K 47/183 (2013.01); A61K 47/26 (2013.01); A61K 47/545 (2017.08); A61K 47/60 (2017.08)] 8 Claims
 
1. A liquid pharmaceutical formulation, wherein the pharmaceutical formulation comprises a PTH conjugate of formula

OG Complex Work Unit Chemistry
or a pharmaceutically acceptable salt thereof,
wherein
the unmarked dashed line indicates attachment by an amide bond to an N-terminal amine of a PTH moiety, which is PTH1-34 (SEQ ID NO:51); and
the dashed line marked with the asterisk indicates attachment to a moiety

OG Complex Work Unit Chemistry
wherein m and p are independently an integer from 400-500,
succinic acid, D-mannitol and m-cresol, wherein the PTH moiety is at about 0.3 mg/ml mg/ml, the succinic acid is at about 1.18 mg/ml, the D-mannitol is at about 41.7 mg/ml, and the m-cresol is at about 2.5 mg/ml and wherein the pH is about 4.0, wherein about indicates variation of +/−10% of a stated value.