Drug intelligence / Profile preview

SHR2554 + SHR-A2102

Development stage
Unknown
Lead developer
Hengrui Pharmaceutical
Modality
Small Molecules, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Oral, Intravenous
01

Overview

**SHR2554 + SHR-A2102** is a combination of two investigational oncology drugs, developed by Jiangsu Hengrui Pharmaceuticals, and evaluated as a combination therapy in clinical trials for advanced solid tumors and other malignancies. \n- **SHR2554** is a selective, orally bioavailable inhibitor of *enhancer of zeste homolog 2* (EZH2), a histone methyltransferase that is implicated in the epigenetic silencing of tumor suppressor genes and is a rational target in lymphoid neoplasms and potentially other cancers. It has demonstrated clinical activity and acceptable safety in phase 1 studies involving relapsed or refractory lymphomas[2][4][8]. \n- **SHR-A2102** is an antibody-drug conjugate (ADC) targeting *Nectin-4*, utilizing a novel topoisomerase I inhibitor payload (rezetecan). SHR-A2102 is being studied in advanced solid tumors that express Nectin-4, particularly in second-line urothelial carcinoma, in phase 3 clinical trials. Unlike other Nectin-4 ADCs that use auristatin payloads, SHR-A2102’s rezetecan payload differentiates its mechanism[5][10]. \nThe two agents are evaluated together in specific clinical protocols, likely to leverage the epigenetic modulation by SHR2554 and the tumor-targeted cytotoxic activity of SHR-A2102.

02

Targets

TOP1 (DNA Topoisomerase I)PVRL4 (Nectin cell adhesion molecule 4)EZH2 (Histone-lysine N-methyltransferase EZH2)

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