Patent SG-11201907505T-A (SG)
Title: Low-viscosity, high-concentration evolocumab formulations and methods of making the same
Inventor: SLOEY CHRISTOPHER JAMES
IPC: C07K16/40
Filed: 2018-02-22
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 30 August 2018 (30.08.2018) WIP0 I PCT 0111111010 0111 °nolo moll loon En oimIE (10) International Publication Number WO 2018/156741 Al (51) International Patent Classification: C07K 16/40 (2006.01) A61K 47/18 (2017.01) A61K 39/395 (2006.01) (21) International Application Number: PCT/US2018/019189 (22) International Filing Date: 22 February 2018 (22.02.2018) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/462,266 22 February 2017 (22.02.2017) US (71) Applicant: AMGEN INC. [US/US]; One Amgen Center Drive, Thousand Oaks, California 91320-1799 (US). (72) Inventors: SLOEY, Christopher James; 474 Calle Ver- acruz, Newbury Park, California 91320 (US). KANAPU- RAM, Sekhar; 5675 Via Bonita, Thousand Oaks, Califor- nia 91320 (US). CUI, Huanchun; St. Jakobstrasse 68, 4147 Aesch, Basel Land (CH). CHAN, Chio Mui; 1180 NE 63rd Way, Unit 1010, Hillsboro, Oregon 97124 (US). BINABA- JI, Elaheh; 11734 Wilshire Blvd., Apt. C1501, Los Ange- les, California 90025 (US). (74) Agent: ZINKL, Gregory M.; One Amgen Center Drive, Thousand Oaks, California 91320-1799 (US). (81) Designated States (unless otherwise indicated, for every kind of national protection available): AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (84) Designated States (unless otherwise indicated, for every kind of regional protection available): ARIPO (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG). Declarations under Rule 4.17: as to applicant's entitlement to apply for and be granted a patent (Rule 4.1700) Published: — with international search report (Art. 21(3)) with amended claims (Art. 19(1)) with sequence listing part of description (Rule 5.2(a)) N (54) Title: LOW-VISCOSITY, HIGH-CONCENTRATION EVOLOCUMAB FORMULATIONS AND METHODS OF MAKING THE SAME 00 (57) : Provided herein are formulations of PCSK9-binding polypeptides, such as those comprising evolocumab, that comprise O N-acetyl arginine and have reduced viscosities when compared to formulations lacking N-acetyl arginine. Provided herein are also methods of formulating such compositions that are advantageous in that they conserve certain components. Such formulations com- C prising PCSK9-binding polypeptides can be administered to patients to treat and/or prevent PCSK9-related diseases, conditions, and disorders.