Tilatamig samrotecan  (Synonyms: AZD9592)

Tilatamig samrotecan (AZD9592) is an anti-EGFR/c-MET antibody-drug conjugate (ADC). Tilatamig samrotecan consists of an anti-EGFR/c-MET antibody with the drug-linker conjugate being AZ14170133 (HY-145399) (a topoisomerase I (TOP1i) inhibitor payload). Tilatamig samrotecan induces multiple DNA damage response pathway markers (like ATM, ATR, γH2AX). Tilatamig samrotecan selectively binds to EGFR and c-MET, delivering the cytotoxic payload. Tilatamig samrotecan exerts anti-tumor activity in vivo. Tilatamig samrotecan can be used for non-small cell lung cancer (NSCLC) and head and neck squamous cell carcinoma (HNSCC) research^[1][2][3].

Tilatamig samrotecan induces a dose-dependent increase in the expression of DNA damage markers γH2AX and phosphorylated RAD-50 (pRAD50), elevates levels of cleaved caspase-3 (CC3) and reduces tumor volume (TV), in NSCLC-derived xenograft models^[1].
Tilatamig samrotecan (8 mg/kg, once) achieves tumor growth inhibition (TGI) in 73% (16/22) of models, with tumor volume reduction ≥30% from baseline in EGFR-mutant non-small cell lung cancer (NSCLC) models (heterogeneous EGFR and c-MET expression levels, and regardless of prior EGFR tyrosine kinase inhibitor treatment)^[1].
Tilatamig samrotecan (8 mg/kg, once) shows TGI in 60% (12/20) and 44% (4/9) of models in PDX models of EGFR wild-type NSCLC and head and neck squamous cell carcinoma (HNSCC), respectively^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

151659 (average)

Liquid

Colorless to light yellow

[Tilatamig samrotecan]

Shipping with dry ice.

-80°C, protect from light

• [1]. Lara McGrath, et al. Abstract 5737: Evaluation of the relationship between target expression and in vivo anti-tumor efficacy of AZD9592, an EGFR/c-MET targeted bispecific antibody drug conjugate. Cancer research. (2023) 83 (7_Supplement): 5737.

  [2]. Kinsley Wang, et al. Anti-MET Antibody Therapies in Non-Small-Cell Lung Cancer: Current Progress and Future Directions. Antibodies (Basel). 2024 Oct 18;13(4):88.  [Content Brief]

  [3]. Frank Comer; et al. Abstract 5736: AZD9592: An EGFR-cMET bispecific antibody-drug conjugate (ADC) targeting key oncogenic drivers in non-small-cell lung cancer (NSCLC) and beyond. Cancer Res (2023) 83 (7_Supplement): 5736.