22, November 2024, Shanghai – Abbisko Therapeutics Co., Ltd. (HKD：02256) today announced that the first gastric cancer patient has been dosed in “A Phase 2， Multicenter, Open-Label Clinical Study to Evaluate the Safety and Efficacy of ABSK061 and ABSK043 with or without Chemotherapy in Patients with Metastatic/Unresectable Solid Tumors with FGFR2/3 Alterations（Protocol No: ABSK061-201）”.

ABSK061 is the world's most clinically advanced orally bioavailable, potent and selective inhibitor of FGFR2 and FGFR3. ABSK043 is a leading orally bioavailable, potent and selective inhibitor of PD-L1. In previous studies, both drugs demonstrated robust anti-tumor activity, a favorable safety profile, and low-risk of drug interaction, supporting the exploration of efficacy and safety of ABSK061 in combination with ABSK043 in advanced solid tumors with FGFR alterations.

ABSK061-201 is an open-label, multicenter, phase II clinical study designed to evaluate the safety and efficacy of the combination of ABSK061 and ABSK043 with or without chemotherapy in patients with metastatic/unresectable solid tumors harboring FGFR2/3 alterations. The study consists of two parts, a dose escalation and expansion phase. The dose escalation portion will assess safety, tolerability, preliminary efficacy, and the PK profile of ABSK061 + ABSK043 in patients with metastatic/unresectable advanced solid tumors with altered FGFR2/3 activation or overexpression to identify the recommended dose for the expansion phase.

The expansion phase will enroll tumor types with specific FGFR2/3 gene alterations, including HER2 negative gastric/gastroesophageal junction carcinoma, in multiple distinct solid tumor cohorts to evaluate the anti-tumor efficacy of ABSK061+ABSK043 with or without chemotherapy.

About ABSK061

ABSK061 is a novel, orally bioavailable, highly potent and selective small molecule inhibitor of FGFR2 and FGFR3 independently discovered and wholly owned by Abbisko Therapeutics. It is the first FGFR2/3 inhibitor to enter clinical trials globally. First-generation pan-FGFR inhibitors demonstrated clinical efficacy in multiple tumors carrying FGFR2/3 variants and have steadily gained regulatory approval globally. However, the therapeutic window of pan-FGFRs and their clinical efficacy have been limited by side effects associated with FGFR1 inhibition. By reducing FGFR1 activity while maintaining potency against FGFR2 and FGFR3, ABSK061 is expected to achieve a wider therapeutic window with improved clinical efficacy as a new-generation of FGFR inhibitors. In addition, ABSK061 has shown great potential to expand its use to a variety of non-oncology indications, including achondroplasia.

About ABSK043
ABSK043 is a novel, orally administered small molecule PD-L1 inhibitor displaying exceptional activity and high selectivity 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 restricting 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 available PD-1/PD-L1 small molecule drugs. ABSK043 is currently being studied in an ongoing Phase I clinical trial for advanced solid tumors in Australia and China.