Drug intelligence / Profile preview

MRG003 + dalpiciclib

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

Overview

MRG003 + dalpiciclib is an investigational combination therapy for cancer, currently being studied in recurrent or metastatic tumors such as head and neck squamous cell carcinoma. MRG003 is an antibody-drug conjugate (ADC) consisting of a humanized IgG1 monoclonal antibody targeting the epidermal growth factor receptor (EGFR), conjugated to the cytotoxic agent monomethyl auristatin E via a valine-citrulline linker. It delivers targeted cytotoxicity to EGFR-expressing tumor cells[4][9]. Dalpiciclib is an orally administered, selective small molecule inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), which blocks cell cycle progression from G1 to S phase by inhibiting phosphorylation of retinoblastoma protein, leading to cell cycle arrest and reduced tumor proliferation[5][8][10]. The combination aims to enhance antitumor efficacy through dual targeting of EGFR signaling and CDK-mediated cell cycle progression.

Brand names
AiRuiKang
Other names
Dalpiciclib isethionateDalpicicilib
02

Targets

EGFR T790M (Epidermal growth factor receptor T790M mutant)CDK6 (Cyclin-dependent kinase 6)CDK4 (Cyclin-dependent kinase 4)

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