Drug intelligence / Profile preview

prt3789 + docetaxel

Development stage
Unknown
Lead developer
Prelude Therapeutics
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

**PRT3789 + docetaxel** is an investigational combination therapy being studied for the treatment of advanced or metastatic solid tumors, specifically those harboring loss-of-function mutations in the SMARCA4 gene. PRT3789 is a highly selective, first-in-class small molecule proteolysis-targeting chimera (PROTAC) designed to degrade SMARCA2, which compensates for loss of SMARCA4 in tumor cells. Docetaxel is a well-established cytotoxic chemotherapeutic agent that inhibits microtubule disassembly, promoting cancer cell death. The combination aims to selectively target cancer cells with SMARCA4 mutations using PRT3789 and enhance cytotoxicity with docetaxel, with the rationale that SMARCA2 degradation may sensitize tumors to chemotherapy or act synergistically in this genetically defined population. The therapy is currently undergoing Phase 1 dose-escalation trials to determine safety, tolerability, pharmacokinetics, recommended dosing, and preliminary efficacy in targeted patient populations[1][2][3][8].

Other names
PRT-3789 + docetaxelPRT 3789 + docetaxel
02

Targets

VHL (Von Hippel–Lindau tumor suppressor protein)TUBB (Tubulin (alpha and beta subunits))SMARCA2 (SWI/SNF related, matrix associated, actin dependent regulator of chromatin subfamily A member 2)

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