Drug intelligence / Profile preview

datopotamab deruxtecan + pembrolizumab + cisplatin

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

Overview

A combination regimen composed of **datopotamab deruxtecan**, **pembrolizumab**, and **cisplatin**, being investigated primarily as a first-line treatment for advanced or metastatic non-small cell lung cancer (NSCLC), specifically in cases without actionable genomic alterations. - **Datopotamab deruxtecan** (Dato-DXd) is an antibody-drug conjugate (ADC) comprising a humanized anti-TROP2 IgG1 monoclonal antibody linked to a topoisomerase I inhibitor derivative via a cleavable tetrapeptide-based linker. It targets the TROP2 antigen on cancer cells, delivering cytotoxic payload to induce DNA damage and cell death. - **Pembrolizumab** is a monoclonal antibody that blocks PD-1 (programmed death-1) on T cells, thereby enhancing T cell–mediated immune responses against tumor cells. - **Cisplatin** is a platinum-based chemotherapeutic that forms DNA crosslinks, inhibiting DNA replication and transcription, resulting in impaired cancer cell proliferation and survival. This combination aims to leverage targeted cytotoxicity (via datopotamab deruxtecan), immune checkpoint inhibition (via pembrolizumab), and cytotoxic chemotherapy (via cisplatin) for synergistic anti-tumor effects.

02

Targets

TOP1 (DNA Topoisomerase I)TACSTD2 (Tumor-associated calcium signal transducer 2)PDCD1 (Programmed cell death protein 1 receptor)DNA

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