December 11, 2024, Abbisko Therapeutics Co., Ltd. (HKD: 02256) today announced that it has dosed its first patient in a phase II, open-label study to evaluate the efficacy and safety of ABSK043 in combination with furmonertinib patients with EGFR-mutated, locally advanced or metastatic NSCLC. ABSK043 is an orally bioavailable, highly selective and potent small molecule PD-L1 inhibitor independently developed by Abbisko Therapeutics and is currently being explored for the treatment of malignant neoplasms. Furmonertinib, also known as firmonertinib, is a Class I New Drug that is a novel irreversible, selective third-generation EGFR TKI independently developed by Shanghai Allist Pharmaceuticals. The combination of ABSK043 and furmonertinib is expected to improve clinical anti-tumor efficacy for patients with advanced lung cancer with EGFR mutations.

The ongoing study is divided into two parts: a dose escalation and expansion phase. The dose escalation phase will evaluate the safety and tolerability of ABSK043 in combination with furmonertinib in Chinese patients with previously treated, EGFR-mutant, locally advanced or metastatic NSCLC who are recommend a combination regimen, and will conduct a preliminary assessment of anti-tumor activity. The expansion phase will evaluate the efficacy of ABSK043 in combination with furmonertinib as a first-line treatment for patients with EGFR-mutant locally advanced or metastatic NSCLC at the one or more recommended doses, and will further assess the safety, tolerability and PK profile of the combination regimens.

About ABSK043
ABSK043 is a novel, orally bioavailable, highly selective small molecule PD-L1 inhibitor wholly-owned by Abbisko Therapeutics. Tumor cells can exploit immune checkpoints such as PD-1 and its ligand PD-L1 to evade immune detection and clearance, thereby suppressing or limiting T-cell responses. ABSK043 selectively binds to the PD-L1 receptor and induces its internalization from the cell surface, effectively inhibiting the PD-1/PD-L1 interaction and alleviating PD-L1-mediated suppression of T-cell activation. In preclinical models, ABSK043 has demonstrated anti-tumor efficacy comparable to approved PD-L1 antibodies. While several PD-1/PD-L1 monoclonal antibodies have been approved worldwide, there are currently no approved orally bioavailable PD-1/PD-L1 small molecule drugs. ABSK043 is currently being explored in an ongoing Phase I clinical trial for advanced solid tumors in Australia and China.

About Furmonertinib

Furmonertinib is a self-developed 3rd generation of EGFR-TKI with independent IP from China. It is approved by CDE for the second-line and first-line treatment of adult patients with locally advanced or metastatic NSCLC with EGFR mutations in March 2021 and June 2022, respectively, both of which are included in the National Reimbursement Drug List. Thus far, the global multi-center (including China, the United States, the United Kingdom, France, Japan, South Korea, etc.), registrational Phase III clinical study of Furmonertinib is well advanced, which is used for the first-line treatment of NSCLC patients harboring EGFR Exon 20 insertion mutations. In addition, Furmonertinib has been granted as Breakthrough Therapy Designation in China and the United States for the treatment of NSCLC with EGFR Exon 20 insertion mutations. The phase III clinical studies for adjuvant treatment of NSCLC with EGFR-sensitive mutations and for the first-line treatment of NSCLC with uncommon EGFR mutations are also progressing smoothly.