The University of Texas MD Anderson Cancer Center, Houston, TX, USA.
Fondazione IRCCS Istituto Nazionale dei Tumori, Milan, Italy.
Nat Med. 2024 Jun;30(6):1645-1654. doi: 10.1038/s41591-024-02934-7. Epub 2024 May 6.
Fibroblast growth factor receptor (FGFR) alterations drive oncogenesis in multiple tumor types. Here we studied pemigatinib, a selective, potent, oral FGFR1-FGFR3 inhibitor, in the phase 2 FIGHT-207 basket study of FGFR-altered advanced solid tumors. Primary end points were objective response rate (ORR) in cohorts A (fusions/rearrangements, n = 49) and B (activating non-kinase domain mutations, n = 32). Secondary end points were progression-free survival, duration of response and overall survival in cohorts A and B, and safety. Exploratory end points included ORR of cohort C (kinase domain mutations, potentially pathogenic variants of unknown significance, n = 26) and analysis of co-alterations associated with resistance and response. ORRs for cohorts A, B and C were 26.5% (13/49), 9.4% (3/32) and 3.8% (1/26), respectively. Tumors with no approved FGFR inhibitors or those with alterations not previously confirmed to be sensitive to FGFR inhibition had objective responses. In cohorts A and B, the median progression-free survival was 4.5 and 3.7 months, median duration of response was 7.8 and 6.9 months and median overall survival was 17.5 and 11.4 months, respectively. Safety was consistent with previous reports. The most common any-grade treatment-emergent adverse events were hyperphosphatemia (84%) and stomatitis (53%). TP53 co-mutations were associated with lack of response and BAP1 alterations with higher response rates. FGFR1-FGFR3 gatekeeper and molecular brake mutations led to acquired resistance. New therapeutic areas for FGFR inhibition and drug failure mechanisms were identified across tumor types. ClinicalTrials.gov identifier: NCT03822117 .
成纤维细胞生长因子受体 (FGFR) 改变驱动多种肿瘤类型的肿瘤发生。在这里,我们研究了 pemigatinib,一种选择性、有效、口服的 FGFR1-FGFR3 抑制剂,用于 FGFR 改变的晚期实体瘤的 FIGHT-207 篮子研究 2 期试验。主要终点是队列 A(融合/重排,n=49)和队列 B(激活非激酶结构域突变,n=32)的客观缓解率 (ORR)。次要终点是队列 A 和 B 的无进展生存期、缓解持续时间和总生存期,以及安全性。探索性终点包括队列 C(激酶结构域突变、可能具有未知意义的致病性变异,n=26)的 ORR 以及与耐药性和反应相关的共改变分析。队列 A、B 和 C 的 ORR 分别为 26.5%(49/185)、9.4%(32/340)和 3.8%(26/686)。没有批准的 FGFR 抑制剂的肿瘤或以前未证实对 FGFR 抑制敏感的改变的肿瘤有客观反应。在队列 A 和 B 中,无进展生存期的中位数分别为 4.5 个月和 3.7 个月,缓解持续时间的中位数分别为 7.8 个月和 6.9 个月,总生存期的中位数分别为 17.5 个月和 11.4 个月。安全性与之前的报告一致。最常见的任何级别治疗相关不良事件是高磷血症(84%)和口腔炎(53%)。TP53 共突变与无反应相关,BAP1 改变与更高的反应率相关。FGFR1-FGFR3 门控和分子制动器突变导致获得性耐药。在各种肿瘤类型中确定了新的 FGFR 抑制治疗领域和药物失败机制。临床试验.gov 标识符:NCT03822117。