Drug intelligence / Profile preview

CS5001 + lenalidomide

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

Overview

**CS5001 + lenalidomide** is an experimental combination therapy under investigation primarily for advanced lymphomas and solid tumors. - **CS5001** is a novel antibody-drug conjugate (ADC) targeting receptor tyrosine kinase-like orphan receptor 1 (ROR1), a protein overexpressed in multiple malignancies but largely absent from adult normal tissues. CS5001 comprises a monoclonal antibody against ROR1, a proprietary tumor-cleavable linker, and a pyrrolobenzodiazepine (PBD) cytotoxic prodrug payload; it is designed for selective release and activation within tumor tissue, enabling targeted cytotoxicity with improved safety over traditional PBD payloads. - **Lenalidomide** is an oral immunomodulatory drug with anti-neoplastic, pro-apoptotic, and anti-angiogenic activity; it is approved for various hematologic malignancies, including multiple myeloma and lymphomas, often in combination with other agents. The combination is being evaluated in relapsed/refractory lymphoma and solid tumor settings, where CS5001 offers direct tumoricidal action and lenalidomide contributes immunomodulation and anti-tumor efficacy[1][2][3][4][7].

02

Targets

ROR1 (Receptor tyrosine kinase-like orphan receptor 1)CK1α (Casein kinase I alpha)CRBN (Cereblon)IKZF3 (Zinc finger protein Aiolos)IKZF1 (Ikaros family zinc finger protein 1)

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