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Petosemtamab

Names

[ CAS No. ]:
2213450-26-9

[ Name ]:
Petosemtamab

Biological Activity

[Description]:

Petosemtamab (MCLA 158) is an anti- EGFR (Kd: 0.22 nM) and anti-LGR5 (Kd: 0.86 nM) monoclonal antibody (mAb). Petosemtamab leads to EGFR signaling blockade and receptor degradation in LGR5+ cancer cells. Petosemtamab can be used in the research of solid tumors, such as head and neck squamous cell carcinoma (HNSCC), metastatic colorectal cancer (CRC)[1][2].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> JAK/STAT Signaling >> EGFR
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> EGFR

[Target]

EGFR:0.22 nM (Kd)

LGR5:0.85 nM (Kd)


[In Vitro]

MCLA-158 (1 µg/mL, 24 or 72 h) leads to EGFR degradation in EGFR+/LGR5+ colorectal cancer organoids[2]. Western Blot Analysis[2] Cell Line: P18T (KRAS WT), C55T (KRAS G12V) and C82N (normal) organoids Concentration: 1 µg/mL Incubation Time: 1, 6, 24, 72 h Result: Time-dependently degraded EGFR.

[In Vivo]

MCLA-158 (25 mg/kg/week, i.v., for 6 weeks) leads to tumor regression in esophageal squamous, gastric adenocarcinoma and head & neck PDX models[2]. Animal Model: Esophageal squamous, gastric adenocarcinoma and head & neck PDX models[2] Dosage: 25 mg/kg/week Administration: Intravenous injection (i.v.) for 6 weeks. Result: Inhibited tumor growth.

[References]

[1]. Antoine Hollebecque, et al. Abstract P185: Preliminary antitumor activity of MCLA-158, an IgG1 bispecific antibody targeting EGFR and LGR5, in advanced head and neck squamous cell carcinoma. Mol Cancer Ther (2021) 20 (12_Supplement): P185.

[2]. Guillem Argiles, et al. Phase I dose-escalation study of MCLA-158, a first-in-class bispecific antibody targeting EGFR and LGR5, in metastatic colorectal cancer (CRC). Journal of Clinical Oncology 39, no. 3_suppl

Chemical & Physical Properties

No Any Chemical & Physical Properties

Related Compounds