{"id":2700,"date":"2023-07-31T10:00:12","date_gmt":"2023-07-31T08:00:12","guid":{"rendered":"https:\/\/www.fondazionebonadonna.eu\/?p=2700"},"modified":"2023-07-31T10:09:08","modified_gmt":"2023-07-31T08:09:08","slug":"a-new-fgfr2-inhibitor-with-activity-across-fgfr2-alterations","status":"publish","type":"post","link":"https:\/\/www.fondazionebonadonna.eu\/en\/a-new-fgfr2-inhibitor-with-activity-across-fgfr2-alterations\/","title":{"rendered":"A new FGFR2 inhibitor with activity across FGFR2 alterations"},"content":{"rendered":"<div class=\"wpb-content-wrapper\"><p>[vc_row][vc_column][vc_custom_heading text=&#8221;By targeting primary alterations and resistance mutations, the highly selective, irreversible FGFR2 inhibitor RLY4008 shows a broad therapeutic potential in multiple tumors&#8221; font_container=&#8221;tag:h3|text_align:left&#8221; use_theme_fonts=&#8221;yes&#8221;][\/vc_column][\/vc_row][vc_row][vc_column width=&#8221;1\/2&#8243;][vc_column_text]<a href=\"https:\/\/aacrjournals.org\/cancerdiscovery\/article\/doi\/10.1158\/2159-8290.CD-23-0475\/727134\/RLY-4008-the-first-highly-selective-FGFR2\" target=\"_blank\" rel=\"noopener\">A new study recently published on Cancer Discovery<\/a>\u00a0shows that RLY 4008, a highly selective, irreversible FGFR2 inhibitor, targets FGFR2 primary alterations and resistance mutations inducing regression in multiple xenograft models, thus confirming the broad therapeutic potential of selective FGFR2 targeting.<\/p>\n<p>Oncogenic activation of FGFR2 drives multiple cancers and represents a broad therapeutic opportunity, yet selective targeting of FGFR2 has not been achieved and patients with FGFR2-driven cancers derive limited benefit from pan-FGFR inhibitors due to multiple FGFR1\u20134 mediated toxicities and acquired FGFR2 resistance mutations. The new study describes RLY-4008, the first highly selective, irreversible, small-molecule FGFR2 inhibitor specifically designed to overcome the limitations of pan-FGFR inhibitors via targeting of oncogenic FGFR2 alterations and resistance mutations.\u00a0 Preclinical characterization in biochemical assays, cell-based assays and in vivo cancer models validate RLY4008 mechanism of action; moreover, three case studies from the ongoing phase 1\/2, first-in-human study of RLY-4008 (ReFocus) shows high response rates with RLY-4008 in patients with FGFR inhibitors-nai\u0308ve cholangiocarcinoma harboring an FGFR2 fusion or rearrangement as well as responses in patients with other FGFR2-altered tumors and activity against common FGFR2 resistance mutations. The case studies demonstrate that RLY- 4008 induces durable radiographic response in pan-FGFR inhibitors-naive and pre-treated patients without clinically significant off-isoform toxicity. Taken together, these data demonstrate that RLY-4008 is a highly selective FGFR2 inhibitor that targets primary alterations and resistance mutations and induces tumor regression while sparing other FGFRs, suggesting it may have broad therapeutic potential.[\/vc_column_text][\/vc_column][vc_column width=&#8221;1\/2&#8243;][vc_single_image image=&#8221;2319&#8243; img_size=&#8221;large&#8221;][\/vc_column][\/vc_row]<\/p>\n<\/div>","protected":false},"excerpt":{"rendered":"<p>[vc_row][vc_column][vc_custom_heading text=&#8221;By targeting primary alterations and resistance mutations, the highly selective, irreversible FGFR2 inhibitor RLY4008 shows a broad therapeutic potential in multiple tumors&#8221; font_container=&#8221;tag:h3|text_align:left&#8221; use_theme_fonts=&#8221;yes&#8221;][\/vc_column][\/vc_row][vc_row][vc_column width=&#8221;1\/2&#8243;][vc_column_text]A<span class=\"excerpt-hellip\"> [\u2026]<\/span><\/p>\n","protected":false},"author":2,"featured_media":2319,"comment_status":"open","ping_status":"closed","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[39,21],"tags":[],"class_list":["post-2700","post","type-post","status-publish","format-standard","has-post-thumbnail","hentry","category-events","category-uncategorized"],"yoast_head":"<!-- This site is optimized with the Yoast SEO plugin v28.5 - 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