Patent SG-11201910182R-A (SG)
Title: Stable formulations of programmed death receptor 1 (pd-1) antibodies and methods of use thereof
Inventor: SHARMA MANOJ
IPC: A61K9/00
Filed: 2018-05-01
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization IiiimmomiolollmonolooloionmllooluioluovoimIE International Bureau (10) International Publication Number WO 2018/204368 Al (43) International Publication Date 08 November 2018 (08.11.2018) WIPO I PCT (51) International Patent Classification: A61K 9/00 (2006.01) A61K 39/395 (2006.01) A61K 9/08 (2006.01) A61K 47/26 (2006.01) A61K 9/19 (2006.01) C07K 16/18 (2006.01) A61K 39/00 (2006.01) (21) International Application Number: PCT/US2018/030459 (22) International Filing Date: 01 May 2018 (01.05.2018) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/500,238 02 May 2017 (02.05.2017) US (71) Applicant (for all designated States except US): MERCK SHARP & DOHME CORP. [US/US]; 126 East Lincoln Avenue, Rahway, New Jersey 07065-0907 (US). (72) Inventors; and (71) Applicants (for US only): SHARMA, Manoj, K. [US/US]; 7 Fraser Street, Littleton, Massachusetts 01460 (US). BEN- JAMIN, Wendy [US/US]; 2000 Galloping Hill Road, Kenilworth, New Jersey 07033 (US). MITTAL, Sarita [US/US]; 2000 Galloping Hill Road, Kenilworth, New Jer- sey 07033 (US). BASARKAR, Ashwin [IN/US]; 2304 Sunnyview Oval, Keasbey, New Jersey 08832 (US). NARASIMHAN, Chakravarthy Nachu [US/US]; 2000 Galloping Hill Road, Kenilworth, New Jersey 07033 (US). KASHI, Ramesh, K. [US/US]; 5 Hickory Lane, War- ren, New Jersey 07059 (US). SHAMEEM, Mohammed [US/US]; 4 Surim Court, Nanuet, New York 10954 (US). (72) Inventors; and (71) Applicants (for NZ, US only): BHATTACHARYA, Soumendu [US/US]; 2000 Galloping Hill Road, Kenil- worth, New Jersey 07033 (US). FORREST, William, P, Jr. [US/US]; 126 East Lincoln Avenue, Rahway, New Jer- sey 07065-0907 (US). (54) Title: STABLE FORMULATIONS OF PROGRAMMED DEATH RECEPTOR 1 (PD-1) ANTIBODIES AND METHODS OF USE THEREOF Pre — Pea k 1+ 2 12 10 8 — 6 — 4- 2 Oxidation by HP—HIC =T=0 • . 4 weeks 8 weeks co 00 O C 0 H1 H2 H3 H4 H5 H6 H7 H8 H9 H10 H11 H12 H13 H14 Formulation FIG.7 (57) : The invention relates to stable formulations of antibodies against human programmed death receptor PD-1, or antigen binding fragments thereof. In some embodiments the formulations of the invention comprise between 5-200 mg/mL anti- PD-1 antibody, or antigen binding fragment thereof. The invention further provides methods for treating various cancers with stable formulations of the invention. In some embodiments of the methods of the invention, the formulations are administered to a subject by intravenous or subcutaneous administration. [Continued on next page] WO 2018/204368 Al MIDEDIMIIII11111111111111111111111111111111111111111111111011110111110111111111111 (74) Common Representative: MERCK SHARP & DOHME CORP.; 126 East Lincoln Avenue, Rahway, New Jersey 07065-0907 (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 4.17(11)) as to the applicant's entitlement to claim the priority of the earlier application (Rule 4.17(iii)) Published: with international search report (Art. 21(3)) with sequence listing part of description (Rule 5.2(a))