Japan-based Takeda Pharmaceutical Co., Ltd’s (TYO: 4502) China unit has announced receiving marketing approval from the National Medical Products Administration (NMPA) for its lung cancer therapy mobocertinib. The drug is indicated for use in adult patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) who have progressed during or after platinum-containing chemotherapy and carry mutations in exon 20 of the epidermal growth factor receptor (EGFR).
Clinical Need and Drug Mechanism
Patients with advanced NSCLC and EGFR exon20ins mutations face a worse survival prognosis compared to those with common EGFR mutations, with a five-year survival rate of only 8%. The steric hindrance caused by the EGFR exon20ins mutant results in a smaller drug-binding pocket, and its structure is highly similar to that of wild-type EGFR, blocking traditional EGFR-targeted drug binding.
Mobocertinib is the world’s first and currently only orally targeted therapy specifically designed to treat EGFR exon20ins advanced NSCLC. Its innovative isopropyl ester structure forms a flexible single-ring core, enabling effective binding to the EGFR exon20ins mutation with accurate selection and high affinity.
Clinical Trial Results
A Phase I/II clinical study demonstrated that mobocertinib achieved a 28% overall response rate (ORR) assessed by the Independent Review Committee (IRC), a 35% ORR assessed by the investigator (INV), a 78% disease control rate (DCR), and a median duration of remission (mDoR) of 15.8 months assessed by IRC. Additionally, the median progression-free survival (mPFS) of patients increased to 7.3 months, and the median overall survival (mOS) reached 20.2 months.
Competitive Landscape
Notably, China-based Dizal Pharmaceutical Co., Ltd (SHA: 688192) filed a New Drug Application (NDA) earlier this month for its next-generation EGFR inhibitor sunvozertinib (DZD9008), also targeting approval for treating exon20 insertion mutated NSCLC. This underscores the growing interest in addressing the significant unmet need for effective treatments in this patient population.
Future Outlook
The approval of mobocertinib by the NMPA highlights Takeda’s commitment to advancing innovative therapies for patients with advanced lung cancer. With demonstrated efficacy and safety, mobocertinib is poised to make a meaningful impact on patient outcomes in EGFR exon20ins NSCLC. Takeda’s ongoing efforts in oncology underscore its dedication to addressing significant unmet needs in the treatment of lung cancer.-Fineline Info & Tech
