Patent SG-11201804839W-A (SG)
Title: Bispecific molecules having immunoreactivity with pd-1 and ctla-4, and methods of use thereof
Inventor: JOHNSON LESLIE
IPC: C07K16/46
Filed: 2016-12-12
Abstract: DAPC + D36774 CD4+ T-cells lo 11 [1[1 IFN-y a t 72 h, pg /m L W O 20 17 / 10606 1 Al (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (10) International Publication Number (43) International Publication Date WO 2017/106061 Al 22 June 2017 (22.06.2017) WIPO I PCT 111111111111110110101011111 010 11111 0111010 1101 100 1101E1101111111111111 0111111 (51) International Patent Classification: A61K 39/395 (2006.01) C07K 16/30 (2006.01) C07K 16/28 (2006.01) C07K 16/46 (2006.01) (21) International Application Number: PCT/US2016/066060 (22) International Filing Date: 12 December 2016 (12.12.2016) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/266,944 14 December 2015 (14.12.2015) US (71) Applicant: MACROGENICS, INC. [US/US]; 9704 Med- ical Center Drive, Rockville, MD 20850 (US). (72) Inventors: JOHNSON, Leslie, S.; 14411 Poplar Hill Road, Darnestown, MD 20874 (US). CHICHILI, Gurun- adh, Reddy; 13926 Lullaby Road, Germantown, MD 20874 (US). SHAH, Kalpana; 13013 Ethel Rose Way, Boyds, MD 20841 (US). LA MOTTE-MOHS, Ross; 16000 Schaeffer Road, Boyds, MD 20841 (US). MOORE, Paul, A.; 10 Turley Court, North Potomac, MD 20878 (US). BONVINI, Ezio; 11136 Powder Horn Drive, Potom- ac, MD 20854 (US). KOENIG, Scott; 10901 Ralston Road, Rockville, MD 20852 (US). (74) Agents: AUERBACH, Jeffrey, I. et al.; AuerbachSchrot LLC, 2200 Research Blvd., Suite 560, Rockville, MD 20850 (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, 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). Published: with international search report (Art. 21(3)) [Continued on next page] (54) Title: BISPECIFIC MOLECULES HAVING IMMUNOREACTIVITY WITH PD-1 AND CTLA-4, AND METHODS OF USE THEREOF „R N. Q t•V 3'. x, co 0 - c° V - ‘c. ;•0 .0t . \" e's 4 C, Concentration Concentration (nM): 10.016 10.0810.412110150 Figure 18 (57) : The present invention is directed to bispecific molecules (e.g., diabodies, bispecific antibodies, trivalent binding mo - lecules, etc.) that possess at least one epitope-binding site that is immunospecific for an epitope of PD-1 and at least one epi- tope-binding site that is immunospecific for an epitope of CTLA-4 (i.e., a \"PD-1 x CTLA-4 bispecific molecule\"). The PD-1 x CTLA-4 bispecific molecules of the present invention are capable of simultaneously binding to PD-1 and to CTLA-4, particularly as such molecules are arrayed on the surfaces of human cells. The invention is directed to pharmaceutical compositions that contain such PD-1 x CTLA-4 bispecific molecules, and to methods involving the use of such bispecific molecules in the treatment of cancer and other diseases and conditions. The present invention also pertains to methods of using such PD-1 x CTLA-4 bispecific mo- lecules to stimulate an immune response. WO 2017/106061 Al MIDEDIMO110101011111010101110101101100110110110EMOVOIMIE — with sequence listing part of description (Rule 5.2(a))