Drug intelligence / Profile preview

EO1001

Development stage
Unknown
Lead developer
Apollomics
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
Administration
Oral
01

Overview

EO1001 (also known as APL-122) is a first-in-class, oral, irreversible pan-ErbB tyrosine kinase inhibitor developed for the treatment of advanced solid tumors. It targets multiple members of the ErbB receptor family—specifically Epidermal growth factor receptor (EGFR), Receptor protein-tyrosine kinase erbB-2 (HER2), and Receptor protein-tyrosine kinase erbB-4 (HER4)—and has demonstrated potent inhibition against these receptors in preclinical studies. Notably, EO1001 is designed to penetrate the central nervous system and has shown activity against both intracellular and extracellular domain mutations of Epidermal growth factor receptor that are commonly found in non-small cell lung cancer and glioblastoma. The drug is being evaluated in Phase 1/2 clinical trials for patients with ErbB-positive cancers who have progressed after standard therapies, including those with CNS involvement. Preclinical data indicate a favorable pharmacokinetic profile and tolerability[1][4][5][6].

Other names
EO1001EO-1001EO 1001
02

Targets

BLK (B lymphoid tyrosine kinase)ERBB2 (Erb-b2 receptor tyrosine kinase 2)ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)ERBB4 (Erb-b2 receptor tyrosine kinase 4)EGFR T790M (Epidermal growth factor receptor T790M mutant)

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