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ASP3082 + nab-paclitaxel + gemcitabine
- Development stage
- Unknown
- Lead developer
- Astellas Pharma
- Modality
- Recombinant Proteins and Enzymes, PROTACs (E3 ligase recruitment) → Targeted Protein Degraders (TPDs) → Small Molecules, Bivalent/Multivalent Binders → Multivalent & Scaffold-Based Small Molecules → Small Molecules
- Administration
- Intravenous
01
Overview
A combination regimen consisting of **ASP3082**, a novel KRAS G12D-targeted protein degrader, **nab-paclitaxel** (a nanoparticle albumin-bound formulation of the microtubule inhibitor paclitaxel), and **gemcitabine** (a nucleoside analog and DNA synthesis inhibitor). ASP3082 utilizes proteolysis-targeting chimera (PROTAC) technology to selectively degrade the mutant KRAS G12D protein, thereby inhibiting its downstream oncogenic signaling. nab-paclitaxel disrupts microtubule dynamics, leading to mitotic arrest and cancer cell death, while gemcitabine interferes with DNA replication in rapidly dividing tumor cells. This triple-drug combination is under investigation for the treatment of advanced solid tumors harboring KRAS G12D mutations, including pancreatic and other cancers, to potentially enhance anti-tumor efficacy via complementary mechanisms of action[2][4][6].
- Other names
- nab-paclitaxel + gemcitabine
02
Targets
TUBB (Tubulin (alpha and beta subunits))KRASG12D (Kirsten rat sarcoma viral oncogene homolog (KRAS) G12D mutant)VHL (Von Hippel–Lindau tumor suppressor protein)
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