Drug intelligence / Profile preview

sacituzumab tirumotecan + limertinib

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

Overview

This combination therapy consists of **sacituzumab tirumotecan** (sac-TMT), a TROP2-directed antibody-drug conjugate (ADC), and **limertinib**, a third-generation EGFR tyrosine kinase inhibitor (TKI). Sacituzumab tirumotecan (also known as SKB264 or MK-2870) is composed of a humanized monoclonal antibody targeting trophoblast cell-surface antigen 2 (TROP2) linked to a cytotoxic topoisomerase I inhibitor payload, tirumotecan. Limertinib is a small molecule designed to selectively inhibit mutant forms of the epidermal growth factor receptor (EGFR). The combination is being investigated in clinical trials, specifically as a neoadjuvant conversion therapy for patients with locally advanced, potentially resectable EGFR-mutant non-small cell lung cancer (NSCLC). The rationale for the combination is to provide dual targeting of TROP2-expressing tumor cells and EGFR-driven oncogenic signaling to achieve tumor downstaging and facilitate surgical resection.

Other names
sacituzumab tirumotecan and limertinibsac-TMT + limertinib
02

Targets

FcγR (Low affinity immunoglobulin gamma Fc region receptor II-c)FCGRT (Neonatal crystallizable fragment receptor)TOP1 (DNA Topoisomerase I)TACSTD2 (Tumor-associated calcium signal transducer 2)ERBB2 (Erb-b2 receptor tyrosine kinase 2)

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