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AssigneeMerck Sharp & Dohme Corp.
InventorsMinilik ANGAGAW, Edward Paul BOWMAN, Ming-Tang CHEN, Laurence FAYADAT-DILMAN, Malgorzata A. GIL, Marlene C. HINTON, Zhong HUA, Rebecca Elizabeth JOHNSON, Simon B. LANG, W. Michael SEGANISH, Andrew B. WAIGHT
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Anti-TROP2 antibody-drug conjugates comprising derivatives of the anthracycline metabolite PNU-159682 conjugated to an antibody that preferentially binds high-expressing TROP2 cells over low-expressing TROP2 cells are disclosed.
An antibody drug conjugate (ADC) comprising an antibody or antigen binding fragment thereof that specifically binds to human TROP2 conjugated to a linker-PNU (linker-PNU) payload, wherein the antibody comprises two heavy chains, each heavy chain comprising a variable domain and a constant domain, the variable domain comprising a CDRH1, a CDRH2, and a CDRH3, and two light chains, each light chain comprising a variable domain and a constant domain, the variable domain comprising a CDRL1, a CDRL2, and a CDRL3, wherein the CDRH1, CDRH2, CDRH3, CDRL1, CDRL2, and CDRL3, respectively, comprise the amino acid sequence of NYGMN (SEQ ID NO:
3-5. (canceled)
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An antibody-drug conjugate (ADC) comprising an antibody that specifically binds to human TROP2 conjugated to a linker-anthracycline derivative (linker-PNU) payload, wherein the antibody comprises two heavy chains, each heavy chain comprising a variable domain and a constant domain, the variable domain comprising the amino acid sequence of SEQ ID NO:
34-53. (canceled)
Dependencies are inferred from the claim text.