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ASP3082 + docetaxel

Development stage
Unknown
Lead developer
Astellas Pharma
Modality
PROTACs (E3 ligase recruitment) → Targeted Protein Degraders (TPDs) → Small Molecules, Bivalent/Multivalent Binders → Multivalent & Scaffold-Based Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

ASP3082 + docetaxel is an investigational combination regimen comprising **ASP3082**, a first-in-class KRAS G12D degrader, and **docetaxel**, a well-established microtubule inhibitor chemotherapeutic agent. ASP3082 uses proteolysis-targeting chimera (PROTAC) technology, binding specifically to KRAS G12D mutant proteins and an E3 ubiquitin ligase, inducing targeted ubiquitination and proteasome-mediated degradation of KRAS G12D, with tumor-suppressive effects in cancers harboring this mutation[2][4]. The combination is being evaluated in clinical trials for advanced solid tumors with KRAS G12D mutations, aiming to improve antitumor efficacy through synergistic targeted degradation and cytotoxic chemotherapy[1][4]. Docetaxel acts by stabilizing microtubules and inhibiting their depolymerization, leading to arrest of cell division and apoptosis.

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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