LP-184

LP-184 is a clinical-stage, next-generation acylfulvene small molecule prodrug developed for the treatment of multiple cancers, including central nervous system (CNS) tumors and solid tumors. It is bioactivated inside cancer cells by the enzyme prostaglandin reductase 1 (PTGR1), which is overexpressed in certain tumor types. Upon activation, LP-184 generates cytotoxic metabolites that form adducts with DNA, leading to irreparable DNA damage and subsequent tumor cell death. This mechanism makes it particularly effective against cancers with epigenetic dysregulation or defects in DNA damage repair pathways. Preclinical studies have shown potent anti-tumor activity across various cancer models—including glioblastoma multiforme (GBM), malignant gliomas, triple-negative breast cancer (TNBC), pancreatic cancer, and atypical teratoid rhabdoid tumors (ATRT)—with strong blood-brain barrier penetrance and favorable tolerability profiles[1][4][6]. The drug has received Orphan Drug Designation for malignant gliomas/GBM and pancreatic cancer as well as Rare Pediatric Disease Designation for ATRT from the FDA[1][3]. Clinical development includes monotherapy trials and combination regimens with agents such as PARP inhibitors or spironolactone to enhance therapeutic response[2][4].

Brand names

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Other names

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