A bispecific ligand-drug conjugate composed of dual ligands that target human folate receptor alpha (FRa; FolRa; FOLR1) and transient receptor potential cation channel subfamily V member 6 (TRPV6; CaT1; CATL), conjugated to the camptothecin analog and topoisomerase 1 inhibitor exatecan, with potential antineoplastic activity. Upon administration of FRa/TRPV6 bispecific ligand-drug conjugate CBP-1019, the dual ligands target and bind to FRa and/or TRPV6 expressed on tumor cells. Upon binding and internalization, exatecan is released and inhibits DNA topoisomerase 1 activity, thereby inhibiting DNA replication and resulting in cell cycle arrest and apoptosis in tumor cells expressing FRa and/or TRPV6. FRa is a glycosylphosphatidylinositol linked cell-surface glycoprotein that is widely expressed in certain cancers while its expression is limited in normal tissues. The TRPV6 ion channel plays a key role in calcium homeostasis and is highly selective for calcium compared to other cations; it is overexpressed in a variety of tumors and initiates tumor cell growth, proliferation and metastases.