HER2-targeted antibody-drug conjugate composed of a humanized anti-HER2 monoclonal antibody linked via a cleavable linker to an exatecan-derived topoisomerase I inhibitor; after HER2 binding and internalization, the payload is released to induce Topo I–mediated DNA damage, S-phase arrest, apoptosis, and a bystander effect.
HER2-targeted antibody–drug conjugate linking a humanized anti‑HER2 monoclonal antibody via a cleavable linker to an exatecan-derived topoisomerase I inhibitor; after HER2 binding and internalization, the linker is cleaved to release the payload, which inhibits Topo I to induce DNA damage, S‑phase arrest, apoptosis, and a bystander cytotoxic effect.
YES
DIRECT
The ADC binds HER2 on target cells, is internalized, and releases an exatecan-derived topoisomerase I inhibitor via a cleavable linker, causing DNA damage, S-phase arrest, and apoptosis (with potential bystander killing).
HER2-targeted antibody-drug conjugate composed of a humanized anti-HER2 monoclonal antibody linked via a cleavable linker to an exatecan-derived topoisomerase I inhibitor; after HER2 binding and internalization, the payload is released to induce Topo I–mediated DNA damage, S-phase arrest, apoptosis, and a bystander effect.
HER2-targeted antibody–drug conjugate linking a humanized anti‑HER2 monoclonal antibody via a cleavable linker to an exatecan-derived topoisomerase I inhibitor; after HER2 binding and internalization, the linker is cleaved to release the payload, which inhibits Topo I to induce DNA damage, S‑phase arrest, apoptosis, and a bystander cytotoxic effect.
NO
INDIRECT
The ADC binds HER2 on target cells, is internalized, and releases an exatecan-derived topoisomerase I inhibitor that causes DNA damage, S-phase arrest, and apoptosis (with possible bystander effect). Expression of Topoisomerase I alone does not direct the drug to kill the cell.
CD19-directed antibody–drug conjugate (ADCT-402) that delivers a pyrrolobenzodiazepine (PBD) dimer payload to crosslink DNA and induce cell death.
Humanized anti‑CD19 monoclonal antibody linked via a cleavable valine‑alanine linker to a pyrrolobenzodiazepine (PBD) dimer. After binding CD19 and internalization, the linker is cleaved to release the PBD payload, which binds the DNA minor groove at N2‑guanine positions to form interstrand crosslinks, blocking DNA replication and inducing cell death in CD19‑expressing B‑cell malignancies.
YES
DIRECT
Anti-CD19 ADC binds CD19, is internalized, and releases a PBD dimer that forms DNA interstrand crosslinks, blocking replication and causing cell death in CD19+ cells.
CD19-directed antibody–drug conjugate (ADCT-402) that delivers a pyrrolobenzodiazepine (PBD) dimer payload to crosslink DNA and induce cell death.
Humanized anti‑CD19 monoclonal antibody linked via a cleavable valine‑alanine linker to a pyrrolobenzodiazepine (PBD) dimer. After binding CD19 and internalization, the linker is cleaved to release the PBD payload, which binds the DNA minor groove at N2‑guanine positions to form interstrand crosslinks, blocking DNA replication and inducing cell death in CD19‑expressing B‑cell malignancies.
NO
INDIRECT
Loncastuximab tesirine targets CD19 on B cells, is internalized, and releases a PBD payload that crosslinks DNA at the N2 of guanine in the minor groove, blocking replication and causing cell death. DNA is the intracellular pharmacologic site, not the selecting target; only CD19+ cells are killed.
Anti-CD20 monoclonal antibody that induces ADCC, CDC, and direct apoptosis of CD20-positive B cells.
Chimeric anti-CD20 monoclonal antibody that binds CD20 on B cells and induces cell death via antibody-dependent cellular cytotoxicity (ADCC), complement-dependent cytotoxicity (CDC), and direct apoptosis, depleting CD20-positive B lymphocytes.
YES
DIRECT
Binds CD20 on B cells and eliminates them via Fc-mediated ADCC (engaging NK cells/macrophages), complement-dependent cytotoxicity, and direct apoptotic signaling.