Drug intelligence / Profile preview

rociletinib

Development stage
Discontinued
Lead developer
Clovis Oncology
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

Rociletinib is an orally available, small molecule, third-generation tyrosine kinase inhibitor (TKI) that irreversibly inhibits the epidermal growth factor receptor (EGFR), specifically targeting both common activating mutations (L858R, Del19) and the T790M resistance mutation in EGFR. It was developed for the treatment of patients with non-small cell lung cancer (NSCLC) harboring EGFR mutations who have progressed on prior EGFR-targeted therapies. Rociletinib demonstrated antitumor activity in clinical trials but was associated with notable adverse effects such as hyperglycemia and QT prolongation. Development was discontinued after regulatory review due to concerns over efficacy and safety[2][4][5][6].

Brand names
Xegafri
Other names
rociletinibCO1686CO-1686CO 1686
02

Targets

EGFR T790M (Epidermal growth factor receptor T790M mutant)

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