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HRS-1358

Development stage
Phase 1
Lead developer
Shandong Suncadia Medicine
Modality
PROTACs (E3 ligase recruitment) → Targeted Protein Degraders (TPDs) → Small Molecules, Bivalent/Multivalent Binders → Multivalent & Scaffold-Based Small Molecules → Small Molecules
Administration
Oral
01

Overview

HRS-1358 is an oral small molecule proteolysis targeting chimera (PROTAC) protein degrader that selectively targets estrogen receptor alpha (ERα) for degradation. It is being developed primarily for the treatment of breast cancer, particularly in patients with locally advanced or metastatic disease who have received at least one line of endocrine therapy. The drug acts as an estrogen receptor alpha degradation enhancer, aiming to overcome resistance to standard endocrine therapies by promoting the targeted destruction of ERα in tumor cells. HRS-1358 is a new molecular entity and has reached phase I/II clinical trials in China, both as monotherapy and in combination with other agents such as dalpiciclib isethionate[1][2][3][5].

02

Targets

ESR1 (ERα)

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