US 11,833,215 B2
CKIT antibody drug conjugates
Tinya Abrams, Acton, MA (US); Steven Bruce Cohen, San Diego, CA (US); Dylan Daniel, San Francisco, CA (US); Catrin Finner, Planegg (DE); Bernhard Hubert Geierstanger, Solana Beach, CA (US); Thomas Huber, Allschwil (CH); William Mallet, Redwood City, CA (US); Matthew John Meyer, Framingham, MA (US); Weijia Ou, San Diego, CA (US); Siew Ho Schleyer, El Cerrito, CA (US); and Kathrin Ulrike Tissot-Daguette, Neuried (DE)
Assigned to Novartis AG, Basel (CH)
Filed by Novartis AG, Basel (CH)
Filed on Jun. 4, 2020, as Appl. No. 16/893,359.
Application 16/893,359 is a division of application No. 15/329,818, granted, now 10,786,578, previously published as PCT/IB2015/055678, filed on Jul. 27, 2015.
Claims priority of provisional application 62/033,571, filed on Aug. 5, 2014.
Prior Publication US 2020/0405875 A1, Dec. 31, 2020
This patent is subject to a terminal disclaimer.
Int. Cl. C07K 16/00 (2006.01); A61K 39/00 (2006.01); A61K 47/68 (2017.01); C07K 16/28 (2006.01); A61K 51/10 (2006.01); A61K 49/00 (2006.01); A61P 35/02 (2006.01); A61K 39/395 (2006.01)
CPC A61K 47/6803 (2017.08) [A61K 39/39558 (2013.01); A61K 47/6849 (2017.08); A61K 49/00 (2013.01); A61K 51/103 (2013.01); A61K 51/1093 (2013.01); A61P 35/02 (2018.01); C07K 16/2803 (2013.01); A61K 2039/505 (2013.01); A61K 2039/545 (2013.01); C07K 2317/21 (2013.01); C07K 2317/24 (2013.01); C07K 2317/33 (2013.01); C07K 2317/34 (2013.01); C07K 2317/55 (2013.01); C07K 2317/565 (2013.01); C07K 2317/77 (2013.01); C07K 2317/92 (2013.01)] 17 Claims
 
1. A method of treating a cKIT positive cancer in a patient in need thereof, comprising administering to said patient an antibody drug conjugate of the formula
Ab-(L-(D)m)n
or a pharmaceutically acceptable salt thereof; wherein
Ab is an antibody or antigen binding fragment thereof that specifically binds to an epitope of human cKIT, wherein said antibody or antigen binding fragment thereof comprises:
(i) a heavy chain variable region that comprises (a) a HCDR1 (CDR-Complementarity Determining Region) of SEQ ID NO: 76, (b) a HCDR2 of SEQ ID NO: 77, (c) a HCDR3 of SEQ ID NO: 78; and a light chain variable region that comprises: (d) a LCDR1 of SEQ ID NO: 85, (e) a LCDR2 of SEQ ID NO: 86, and (f) a LCDR3 of SEQ ID NO: 87; wherein the CDRs of (a)-(f) are defined in accordance with the Kabat definition; or
(ii) a heavy chain variable region that comprises (a) a HCDR1 of SEQ ID NO: 79, (b) a HCDR2 of SEQ ID NO: 80, (c) a HCDR3 of SEQ ID NO: 81; and a light chain variable region that comprises: (d) a LCDR1 of SEQ ID NO: 88, (e) a LCDR2 of SEQ ID NO: 89, and (f) a LCDR3 of SEQ ID NO: 90; wherein the CDRs of (a)-(f) are defined in accordance with the Chothia definition;
L is a linker;
D is a drug moiety;
m is an integer from 1 to 8; and
n is an integer from 1 to 10.