China-based Haisco Pharmaceutical Group Co., Ltd (SHE: 002653) has announced that its clinical trial filing for the oral small molecule EGFR-PROTAC HSK40118 has been accepted for review by the National Medical Products Administration (NMPA). The targeted indication is EGFR mutant advanced non-small cell lung cancer (NSCLC). This marks a significant step forward in the development of this innovative therapy.
Mechanism and Development
HSK40118 is a Category 1 drug and a proteolysis-targeting chimeric (PROTAC) small-molecule inhibitor that targets the EGFR protein. The drug recruits the ligand of E3 ubiquitin ligase, with a linker connecting the two parts. This mechanism allows for the degradation of the EGFR protein, offering a novel approach to treating EGFR mutant NSCLC. Haisco’s first PROTAC product, HSK29116, a small-molecule BTK inhibitor, obtained clinical trial approval in China in April 2021 for the treatment of recurrent/refractory B-cell lymphoma.
Market and Clinical Need
Lung cancer is one of the most prevalent cancers in China, with NSCLC accounting for approximately 85% of cases. Among Chinese NSCLC patients, the most common type of gene mutation is the epidermal growth factor receptor (EGFR) gene mutation, which is present in about 50% of cases. EGFR-TKI is currently the most effective therapy for this type of disease. The EGFR-targeted drug market, valued at RMB 10.8 billion (USD 1.568 billion) in 2020, has grown significantly from RMB 2.2 billion (USD 319.4 million) in 2016 and is expected to reach RMB 36.8 billion (USD 5.344 billion) by 2025.
Future Outlook
The acceptance of the clinical trial filing for HSK40118 by the NMPA highlights Haisco Pharmaceutical Group’s commitment to advancing innovative treatments for advanced non-small cell lung cancer. With its novel PROTAC mechanism and demonstrated potential in preclinical studies, HSK40118 is poised to address significant unmet needs in the treatment of EGFR mutant NSCLC. Haisco’s ongoing efforts in clinical development underscore its dedication to improving patient outcomes in oncology.-Fineline Info & Tech
