On February 11, Wayshine announced that its novel EGFR inhibitor WSD0922 had been granted Breakthrough Therapy Designation by the Center for Drug Evaluation (CDE) of China’s National Medical Products Administration (NMPA). The indication is for advanced or metastatic non?small cell lung cancer (NSCLC) with EGFR C797S mutation (cysteine at position 797 of the EGFR gene is replaced by serine) following disease progression on first?line third?generation EGFR inhibitors, including osimertinib, furmonertinib, aumolertinib, and befotertinib.

According to Wayshine’s press release, WSD0922 is a fourth?generation EGFR/EGFRvIII targeted inhibitor independently developed by the company, with the potential to penetrate the blood?brain barrier. It is intended for the treatment of central nervous system metastases from NSCLC and brain tumors. The drug has the potential to overcome multiple resistance mechanisms to first?line third?generation EGFR inhibitors and may be used for the treatment of EGFRvIII?driven glioblastoma multiforme (GBM) and anaplastic astrocytoma (AA).

The CDE Breakthrough Therapy Designation was based on “a multicenter, open?label, single?arm Phase 1/2 clinical study evaluating the safety, tolerability, pharmacokinetics, and efficacy of WSD0922?FU in patients with advanced NSCLC”. The trial aims to assess the efficacy and safety of WSD0922 in patients with advanced or metastatic NSCLC harboring EGFR C797S mutation whose disease progressed after first?line treatment with third?generation EGFR inhibitors (including osimertinib, furmonertinib, aumolertinib, befotertinib, etc.).

The clinical trial showed that WSD0922 achieved a high objective response rate (ORR >60%) and durable progression?free survival (approximately 10 months) in patients with advanced or metastatic NSCLC with C797S mutation after progression on first?line third?generation EGFR inhibitors.

As stated in the press release, the designation of WSD0922 as a breakthrough therapy is of great significance to the ongoing international multicenter Phase 2 clinical trial in NSCLC patients with C797S mutation following disease progression on first?line osimertinib.

Wayshine focuses on the research and development of targeted drugs for brain tumors with unmet clinical needs. In addition to WSD0922, the company’s WSD0628 is a blood?brain barrier?penetrating ATM targeted inhibitor, intended for use in combination with radiotherapy for brain tumors. It has received IND clearance from the U.S. FDA and is undergoing Phase 1 and Phase 2a clinical trials in the United States. Furthermore, the company has a strategic pipeline of drug candidates. For instance, WSD1227, which can be used as monotherapy or in combination for the treatment of brain tumors, is currently in preclinical IND?enabling studies.