Products and
Pipeline

Overview¹

Mobocertinib is an orally active epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) uniquely designed to optimize affinity and selectivity for EGFR Exon 20 insertions over wild type EGFR

MOA^1,2

- Mobocertinib was uniquely designed as a potent inhibitor of EGFR and HER2 exon 20 insertions, with selectivity over wild type EGFR

- Mobocertinib binds to mutant EGFR and HER2 via irreversible covalent binding of EGFR-Cys797/HER2-Cys805²

Clinical Trials

Study Name

A Randomized Phase 3 Multicenter Open-label Study to Compare the Efficacy of TAK-788 as First-line Treatment Versus Platinum-Based Chemotherapy in Patients With Non-Small Cell Lung Cancer With EGFR Exon 20 Insertion Mutations

Study Name

A Phase 1/2 Study of the Safety, Pharmacokinetics, and Anti-Tumor Activity of the Oral EGFR/HER2 Inhibitor TAK-788 in Non-Small Cell Lung Cancer

Study Name

A Phase 1/2 Study of the Oral EGFR/HER2 Inhibitor TAK-788 in Japanese Non-Small Cell Lung Cancer Patients

Study Name

A Phase 1 Pharmacokinetic Study of Oral Mobocertinib in Subjects With Severe Renal Impairment and Normal Renal Function

Study Name

Phase 1 Pharmacokinetics and Safety Study of Oral Mobocertinib in Subjects With Moderate or Severe Hepatic Impairment and Normal Hepatic Function

References

1. Gonzalvez, et al. AACR 2016.

2. Chouitar J, et al. J Thorac Oncol. 2018:13:S811 [abstract P2.13-32].