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ASP3082 + leucovorin + fluorouracil + irinotecan + oxaliplatin
- Development stage
- Phase 3
- Lead developer
- Astellas Pharma
- Modality
- Small Interfering RNA (siRNA) → Small RNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics, MicroRNA (miRNA) → Small RNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics, Antisense Oligonucleotides (ASOs) → Long RNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics, Antisense DNA → DNA Therapeutics → Nucleic Acid Therapeutics, Small Molecules
- Administration
- Intravenous
01
Overview
ASP3082 + leucovorin + fluorouracil + irinotecan + oxaliplatin is an investigational combination regimen being evaluated for the treatment of advanced solid tumors harboring the KRAS G12D mutation, notably in pancreatic cancer. ASP3082 is a novel small-molecule proteolysis-targeting chimeric (PROTAC) degrader designed to selectively bind and degrade the mutant KRAS G12D protein via recruitment of E3 ubiquitin ligases, leading to growth inhibition of KRAS G12D-mutated cancer cells[4]. The regimen combines ASP3082 with the standard FOLFIRINOX chemotherapy protocol (leucovorin, fluorouracil, irinotecan, oxaliplatin) to potentially enhance antitumor response. The primary developer of ASP3082 is Astellas Pharma.
- Other names
- FOLFIRINOX + ASP3082
02
Targets
DNAKRASG12D (Kirsten rat sarcoma viral oncogene homolog (KRAS) G12D mutant)TS (Thymidylate synthase)VHL (Von Hippel–Lindau tumor suppressor protein)DHFR (Dihydrofolate reductase)TOP1 (DNA Topoisomerase I)
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