Drug intelligence / Profile preview

mobocertinib

Development stage
Discontinued
Lead developer
Takeda
Modality
Bivalent/Multivalent Binders → Multivalent & Scaffold-Based Small Molecules → Small Molecules, Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Reversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules, Fragment-Derived Small Molecules → Multivalent & Scaffold-Based Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Mobocertinib is an oral small molecule kinase inhibitor specifically designed to target epidermal growth factor receptor (EGFR) exon 20 insertion mutations in non-small cell lung cancer (NSCLC). These mutations are associated with resistance to standard EGFR inhibitors and a poorer prognosis. Mobocertinib binds irreversibly to the mutant EGFR at cysteine 797 in the active site, leading to sustained inhibition of EGFR enzymatic activity and suppression of tumor cell proliferation. It was developed for use in adults with locally advanced or metastatic NSCLC harboring EGFR exon 20 insertion mutations whose disease has progressed on or after platinum-based chemotherapy. Mobocertinib received accelerated approval from the US FDA in 2021 but was voluntarily withdrawn worldwide following results from a phase III trial that did not meet its primary endpoint.

Brand names
Exkivity
Other names
mobocertinibTAK-788TAK788TAK 788Exkivity
02

Targets

Epidermal growth factor receptor (EGFR) exon 20 insertion mutantEGFR T790M (Epidermal growth factor receptor T790M mutant)ERBB2 (Erb-b2 receptor tyrosine kinase 2)ABCB1 (P-glycoprotein)ABCG2 (ATP-binding cassette sub-family G member 2)

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