Drug intelligence / Profile preview

SHR-A1811 + dalpiciclib

Development stage
Phase 2
Lead developer
Jiangsu HengRui Medicine Co., Ltd.
Modality
Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous, Oral
01

Overview

**SHR-A1811 + dalpiciclib** is a combination investigational oncology therapy involving an **antibody-drug conjugate (ADC)** and a **CDK4/6 inhibitor**. - **SHR-A1811** is an ADC targeting **HER2** (human epidermal growth factor receptor 2), composed of a trastuzumab backbone linked via a cleavable tetrapeptide-based linker to a topoisomerase I inhibitor payload (SHR169265). SHR-A1811 exhibits potent anti-tumor effects in HER2-expressing or mutated advanced solid tumors and has a favorable safety and pharmacokinetic profile. - **Dalpiciclib** is a highly selective, orally bioavailable small-molecule inhibitor of **cyclin-dependent kinase 4 and 6 (CDK4/6)**. It acts by inhibiting phosphorylation of retinoblastoma (Rb) protein, resulting in cell cycle arrest at the G1 phase and reduced tumor cell proliferation. Dalpiciclib has been shown to overcome endocrine resistance in breast cancer and displays significant antitumor activity, especially in HER2-positive and HR+/HER2- breast cancer. The combination is under investigation primarily for the treatment of **HER2-expressing or HER2-low breast cancer** and potentially other HER2-expressing solid tumors[1][2][3][5][6].

Brand names
AiRuiKang
Other names
dalpiciclib isethionate
02

Targets

CDK4 (Cyclin-dependent kinase 4)CDK6 (Cyclin-dependent kinase 6)ERBB2 (Erb-b2 receptor tyrosine kinase 2)

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