US 12,076,400 B2
Methods of using a bispecific antigen-binding construct targeting HER2 in combination with CDK4/6 inhibitors for the treatment of breast cancer
Nina E. Weisser, Vancouver (CA); Diana F. Hausman, Seattle, WA (US); and Patrick Kaminker, Seattle, CA (US)
Assigned to Zymeworks BC Inc., Vancouver (CA)
Filed by c/o Zymeworks BC Inc., Vancouver (CA)
Filed on May 29, 2020, as Appl. No. 16/887,460.
Claims priority of provisional application 62/944,822, filed on Dec. 6, 2019.
Prior Publication US 2021/0170023 A1, Jun. 10, 2021
Int. Cl. A61K 39/395 (2006.01); A61K 31/519 (2006.01); A61K 31/7068 (2006.01); A61K 33/243 (2019.01); A61K 47/68 (2017.01)
CPC A61K 39/3955 (2013.01) [A61K 31/519 (2013.01); A61K 31/7068 (2013.01); A61K 33/243 (2019.01); A61K 47/6817 (2017.08)] 18 Claims
 
1. A method of treating a patient with human epidermal growth factor receptor 2 (HER2)-positive, hormone receptor (HR)-positive breast cancer, the method comprising administering to the patient:
I) a palbociclib 75 mg, 100 mg or 125 mg capsule administered orally (PO) once daily (QD) for the first 21 days of each 28-day cycle;
II) 15 mg/kg to 20 mg/kg of a bispecific anti-HER2 antigen-binding construct every 2 weeks (Q2W) or 15 mg/kg to 50 mg/kg of a bispecific anti-HER2 antigen-binding construct every 3 weeks (Q3W); and
III) fulvestrant administered at 250 mg-500 mg Q2W for the first 3 doses, then once every 4 weeks (Q4W),
wherein the bispecific anti-HER2 antigen-binding construct comprises a heavy chain H1, a heavy chain H2, and a light chain L1,
wherein:
a) heavy chain H1 comprises the CDR sequences set forth in SEQ ID NO:39, SEQ ID NO:40, and SEQ ID NO:41;
b) heavy chain H2 comprises the CDR sequences set forth in SEQ ID NO:67, SEQ ID NO:68, SEQ ID NO: 69, SEQ ID NO:70, SEQ ID NO:71, and SEQ ID NO:72; and
c) light chain L1 comprises the CDR sequences set forth in SEQ ID NO:27, SEQ ID NO:28, and SEQ ID NO:29.