Preferred Label : Acylfulvene-derived Prodrug LP-184;
NCIt synonyms : Alkylating Agent Prodrug LP-184;
NCIt definition : A tumor-site activated acylfulvene-derived prodrug and alkylating agent, with potential
antineoplastic activity. Upon administration, acylfulvene-derived prodrug LP-184 becomes
activated by prostaglandin reductase 1 (PTGR1), an oxidoreductase that is specifically
upregulated in certain tumor cell types. The active form of LP-184 covalently binds
to and alkylates DNA at N3-adenine, thereby causing double strand breaks. As tumor
cells often carry DNA damage repair (DDR) mutations and are therefore deficient in
DDR pathways, the DNA damage cannot be repaired. In turn, the damaged DNA causes apoptosis
and inhibits proliferation in susceptible DDR mutated tumor cells. PTGR1 is often
elevated in solid tumors but not in normal tissues.;
Molecule name : LP 184; LP-184;
Origin ID : C203657;
chemical_or_drug_has_mechanism_of_action
- chemical_or_drug_has_physiologic_effect
- concept_is_in_subset
