Rolinsatamab Talirine

**Semantic type:** Pharmacologic Substance

**Definition:** An antibody-drug conjugate (ADC) composed of rolinsatamab, a humanized immunoglobulin G1 (IgG1) monoclonal antibody against the prolactin receptor (PRLR), linked, via a maleimidocaproyl-valine-alanine dipeptide protease-cleavable linker, to talirine, a cytotoxic DNA minor groove crosslinking agent and pyrrolobenzodiazepine (PBD) dimer, with potential antineoplastic activity. Upon intravenous administration of rolinsatamab talirine, the rolinsatamab moiety targets and binds to PRLR expressed on tumor cells. Upon binding, internalization and linker cleavage, talirine is released and the imine groups of the PBD moiety bind to the N2 positions of guanines on opposite strands of DNA. This induces DNA strand breaks and inhibits DNA replication, and results in G2/M cell cycle arrest and cell death, and inhibits the proliferation of PRLR-expressing tumor cells. PRLR, a tumor-associated antigen (TAA), is overexpressed by a variety of tumor cell types.

**Synonyms:** - ABBV 176 - ABBV-176 - ABBV176 - ADC ABBV-176 - ROLINSATAMAB TALIRINE