Patent SG-11201905622V-A (SG)
Title: Subcutaneous her2 antibody formulations
Inventor: ENG-WONG JENNIFER
IPC: A61K47/26
Filed: 2018-01-16
Abstract: Cohortn=6) Perjeta 420 mg IV Cohort 2 (n=6) Perjeta 400 mg SC Cohort 3 (n=6) Perjeta 600 mg SC Cohort 4 (n=6) Perjeta 1200 mg SC Cohort 6 (n=6)• •, Perjeta 400 mg S . C.+.' \"Herceptin 600 mg SC. 8030185 study schema Target SC Dose(s)b of Perjeta Determined? No Possible Additional ' Cohorts • . „ . +3 If pertgzumab , • exposure different frorn target • \". concentration; only if FDC not feasible OR . Cohort B (n=20) '. Co-mixed .Perjeta SC Target Dose+. ••• Herpeptirt 600 mg SC Ohort eijota SC.: , :arget pose+,•: HergetitiTE.Iop • • '•\", Part 2: Dose Confirmation and Bridging ‘— Patients with Early Breast Cancer Yes 'b Calculated to deliver a s'milar exposure ac a 420-mg IV dose a No additional rHoPh120 concentration = 667 U/m Part 1: Dose Finding Single Dose in Healthy Male Volunteers— . 0 Perjeta alone/separately Herceptin alone/separately 0 Perjeta + Herceptin co-mixed Perjeta + Herceptin FDC Cohort 8 (n=6)• • • Perjeta 1200 mg Herceptin .600 mg Sc FIG. 6 c Cohort A - Co-admifi, Perjeta SC Target Dose ohQ/1.•5An7.6; ehtir. 300'Mg1s1. • • Cohort 7 (n=6) Perjeta 1200 mg SC + Herceptin 600 md SC: . • (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 26 July 2018 (26.07.2018) WI P0 I PC T omit Ill °nolo Oil 1111E1111°111 (10) International Publication Number WO 2018/136412 A3 (51) International Patent Classification: A61K 39/395 (2006.01) A61K 47/42 (2017.01) A61K 9/00 (2006.01) C07K 16/32 (2006.01) A61K 47/26 (2006.01) A61K 39/00 (2006.01) (21) International Application Number: PCT/US2018/013854 (22) International Filing Date: 16 January 2018 (16.01.2018) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/447,359 17 January 2017 (17.01.2017) US (71) Applicants: GENENTECH, INC. [US/US]; 1 DNA Way, South San Francisco, CA 94080 (US). F. HOFF- MANN-LA ROCHE AG [CH/CH]; Grenzacherstrasse 124, 4070 Basel (CH). (72) Inventors: ENG-WONG, Jennifer; c/o Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080 (US). KIRSCHBROWN, Whitney; c/o Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080 (US). KHAN, Tarik; c/o F. Hoffmann-La Roche AG, Grenzacherstrasse 124, 4070 Basel (CH). LIN, Jasper; c/o Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080 (US). ALAVAT- TAM, Sreedhara; c/o Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080 (US). GARG, Amit; c/ o Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080 (US). HEESON, Sarah; c/o Roche Products Limit- ed, Hexagon Place, 6 Falcon Way, Shire Park, Welwyn Gar- den City, Greater London AL71TW (GB). BADOVINAC- CRNJEVIC, Tanja; c/o F. Hoffmann-La Roche AG, Gren- zacherstrasse 124, 4070 Basel (CH). WURTH, Christine; c/o F. Hoffmann-La Roche AG, Grenzacherstrasse 124, 4070 Basel (CH). (74) Agent: LEE, Wendy, M. et al.; c/o Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080 (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, (54) Title: SUBCUTANEOUS HER2 ANTIBODY FORMULATIONS (57) : Fixed dose HER2 antibody formulations for subcutaneous administration are provided along with their use in the O treatment of cancer. The formulations include fixed dose subcutaneous formulations of pertuzumab and subcutaneous co-formulations of pertuzumab and trastuzumab, and their use in the treatment of cancer. C [Continued on next page] WO 2018/136412 A3 IIIIII1111Il 011101010111 VIIIIIOIIIIII0111VIII VIIIVIIIVIIIIIII1111111IIIIIIIIIIII 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(U)) 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)) before the expiration of the time limit for amending the claims and to be republished in the event of receipt of amendments (Rule 48.2(h)) with sequence listing part of description (Rule 5.2(a)) (88) Date of publication of the international search report: 15 November 2018 (15.11.2018)