Lutetium Lu 177 Rofapitide Tetraxetan

**Semantic type:** Indicator, Reagent, or Diagnostic Aid|Pharmacologic Substance

**Definition:** A radioconjugate composed of rofapitide tetraxetan, a fibroblast activation protein (FAP)-targeted peptide, attached to the chelating agent 1,4,7,10-tetraazacyclododecane-N,N',N'',N''-tetraacetic acid (DOTA), and radiolabeled with the beta-emitting radioisotope lutetium Lu 177, with potential antineoplastic activity. Upon administration of lutetium Lu 177 rofapitide tetraxetan, rofapitide tetraxetan targets and binds to FAP-expressing cancer-associated fibroblasts (CAFs) and FAP-expressing tumor cells. Upon binding and internalization, this radioconjugate specifically delivers a cytotoxic dose of beta radiation to CAFs and tumor cells. FAP, a cell surface protein, is overexpressed on CAFs in the tumor microenvironment (TME) and certain tumor cells.

**Synonyms:** - 177Lu Labeled DOTA-conjugated Peptide FAP-2286 - 177Lu-FAP-2286 - LUTETIUM (177LU) ROFAPITIDE TETRAXETAN - Lutetium Lu 177-FAP-2286 - Lutetium-177-FAP-2286