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Ref Type Abstract
Authors J. Zhu Z. Song Y. Zhao J. Zhang Y. Li D. Li R. Schneider Y. Ding Z. Sun Y. Qin Z-W. Chang Z. Wang Z. Zhang P. Zhang Y. Wang J. Zhang
Title 45O First-in-human study of ABSK061: A selective fibroblast growth factor receptor (FGFR) 2/3 inhibitor for treating patients with advanced solid tumors
Abstract Text Background Aberrant activation of FGFR signaling promotes cancer cell proliferation and tumor growth. Targeting FGFR2/3 selectively may alleviate FGFR1-dependent hyperphosphatemia and could provide better efficacy. Here, we evaluated the safety and pharmacokinetics of a selective and potent FGFR2/3 inhibitor ABSK061 in advanced solid tumors in a phase 1 open-label study (NCT05244551). Methods As of November 2023, a total of 28 patients with advanced solid tumors were enrolled in the escalation part of the study. These patients were treated with ABSK061 twice daily (5mg-100mg BID) or once daily (150mg QD) in 28-day cycles. 75mg BID and 150mg QD were selected to explore the recommended doses for expansion. Results Among the 28 patients, the mean age was 53.5 years with 54% males. When comparing 150mg QD with 75mg BID, 150mg QD resulted in ∼50% higher Cmax,ss, ∼50% lower Ctrough,ss and similar AUC0-24h,ss. No dose-limiting toxicity was observed. The most common treatment-related adverse events (TRAEs) (≥15%) included alanine aminotransferase (ALT) increase, aspartate aminotransferase (AST) increase, and anaemia. Grade ≥3 TRAE was reported in 5 patients, including anaemia, ALT increase, AST increase, bilirubin conjugated increase, blood bilirubin increase, gamma-glutamyltransferase increase, and pulmonary embolism. Hyperphosphatemia was reported in only 11% (3/28) of patients, and all were grade 1. One patient on 75mg BID experienced pulmonary embolism with a prior history, discerned as an unlikely related serious adverse event (SAE) by the investigators. Among the 5 patients with prior treatments and FGFR2 fusion/amplification or FGFR3 fusion, 2 achieved partial response (PR) and 2 achieved stable disease (SD). Objective response rate was 40%. All 4 patients are continuing treatment. Disease control rate was 80%. PR was observed in non-small cell lung cancer (FGFR2 fusion) and urothelial carcinoma (FGFR3 fusion). Conclusions This study demonstrated the anti-tumor activity of ABSK061 in patients with FGFR2/3 alterations and its favorable safety profile, which warrants further investigation.


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Molecular Profile Treatment Approach
Gene Name Source Synonyms Protein Domains Gene Description Gene Role
Therapy Name Drugs Efficacy Evidence Clinical Trials
ABSK061 ABSK061 2 1
Drug Name Trade Name Synonyms Drug Classes Drug Description
ABSK061 ABSK-061|ABSK 061 FGFR2 Inhibitor 23 FGFR3 Inhibitor 19 ABSK061 inhibits FGFR2 and FGFR3, potentially leading to antitumor activity (ESMO Open 9 (2024): 102274).
Gene Variant Impact Protein Effect Variant Description Associated with drug Resistance
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
FGFR2 fusion lung non-small cell carcinoma predicted - sensitive ABSK061 Case Reports/Case Series Actionable In a Phase I trial, ABSK061 treatment resulted in a partial response in a patient with non-small cell lung cancer harboring an FGFR2 fusion (ESMO Open 9 (2024): 102274); NCT05244551). detail...
FGFR3 fusion transitional cell carcinoma predicted - sensitive ABSK061 Case Reports/Case Series Actionable In a Phase I trial, ABSK061 treatment resulted in a partial response in a patient with urothelial carcinoma harboring an FGFR3 fusion (ESMO Open 9 (2024): 102274); NCT05244551). detail...