SG11201910134SA - Stable formulations of anti-ctla4 antibodies alone and in combination with programmed death receptor 1 (pd-1) antibodies and methods of use thereof - Google Patents

Abstract

INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 08 November 2018 (08.11.2018) WIPO I PCT Iiiimmomiolollmonolooloionmilmilonomom (10) International Publication Number WO 2018/204343 Al (51) International Patent Classification: A61K 39/395 (2006.01) C07K 16/30 (2006.01) CO7K 16/28 (2006.01) (21) International Application Number: PCT/US2018/030420 (22) International Filing Date: 01 May 2018 (01.05.2018) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/500,268 02 May 2017 (02.05.2017) US (71) Applicant: MERCK SHARP & DOHME CORP. [US/US]; 126 East Lincoln Avenue, Rahway, New Jersey 07065-0907 (US). (72) Inventors; and (71) Applicants (for US only): BHATTACHARYA, Soumen- du [US/US]; 2000 Galloping Hill Road, Kenilworth, New Jersey 07033 (US). DE, Arnab [IN/US]; 2000 Gallop- ing Hill Road, Kenilworth, New Jersey 07033 (US). NARASIMHAN, Chakravarthy Nachu [US/US]; 2000 Galloping Hill Road, Kenilworth, New Jersey 07033 (US). SHARMA, Manoj, K. [US/US]; 7 Fraser St., Littleton, Massachusetts 01460 (US). YANG, Xiaoyu [US/US]; 2000 Galloping Hill Road, Kenilworth, New Jersey 07033 (US). (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). (54) Title: STABLE FORMULATIONS OF ANTI-CTLA4 ANTIBODIES ALONE AND IN COMBINATION WITH PRO- = GRAMMED DEATH RECEPTOR 1 (PD-1) ANTIBODIES AND METHODS OF USE THEREOF Formulation Al: UV A350 0.300 a. =3 0.200 —*-5C —M-25C --k-40C 5 0.100 0.000 O 00 O C 6 10 Time (weeks) FIG.1 A (57) : The invention relates to stable formulations comprising antibodies or antigen binding fragments thereof that bind to cytotoxic T lymphocyte associated antigen 4 (CTLA4), optionally further containing an anti-human programmed death receptor 1 (PD-1) antibody or antigen binding fragment thereof. Also provided are methods of treating various cancers and chronic infections with the formulations of the invention. [Continued on next page] WO 2018/204343 Al MIDEDIMOMOIDEIRDERIHIMINIMIIMIERVOIMIE 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))