Pasifolate Exatecan

**Semantic type:** Pharmacologic Substance

**Definition:** A conjugate composed of folic acid analogs and exatecans covalently bound by linkers to the ultrasmall silica-based nanoparticle carrier C'Dot, with potential antineoplastic activity. Upon administration, pasifolate exatecan targets and binds to the human folate receptor 1 (FOLR1; FR-alpha) on FR-alpha-expressing tumor cells. Upon internalization, the camptothecin analog exatecan is released via proteolytic cleavage of the linker and inhibits DNA topoisomerase 1 activity, thereby inhibiting DNA replication and resulting in cell cycle arrest and apoptosis in tumor cells expressing FR-alpha. FR-alpha is a high-affinity folate-binding protein and a member of the folate receptor family; it is overexpressed in various cancer cell types.

**Synonyms:** - EC112002 - ELU 001 - ELU-001 - ELU001 - FA-CDC ELU001 - FR-alpha-targeting CDC ELU001 - FR-alpha-targeting Ultrasmall Silica Nanoparticle-drug Conjugate ELU001 - Folate-receptor Alpha-targeting C'Dot-drug Conjugate ELU001 - Folate-receptor Alpha-targeting Ultrasmall Silica Nanoparticle-drug Conjugate ELU001 - Folic-acid Functionalized C'Dot-drug-conjugate ELU001 - PASIFOLATE EXATECAN