{"id":74981,"date":"2026-08-17T13:29:04","date_gmt":"2026-08-17T05:29:04","guid":{"rendered":"https:\/\/flcube.com\/?p=74981"},"modified":"2026-08-17T13:29:05","modified_gmt":"2026-08-17T05:29:05","slug":"easton-pharmaceutical-doses-first-patient-in-phase-i-ii-trial-of-hp-002-a-brain-penetrant-btk-protac-for-b-cell-non-hodgkin-lymphoma","status":"publish","type":"post","link":"https:\/\/flcube.com\/?p=74981","title":{"rendered":"Easton Pharmaceutical Doses First Patient in Phase I\/II Trial of HP\u2011002, a Brain\u2011Penetrant BTK PROTAC for B\u2011Cell Non\u2011Hodgkin Lymphoma"},"content":{"rendered":"\n<p class=\"wp-block-paragraph\"><strong>Easton Pharmaceutical Co., Ltd.<\/strong> (<a href=\"https:\/\/www.google.com\/finance\/beta\/quote\/688513:SHA\">SHA: 688513<\/a>) announced that <strong>Phase I\/II clinical trials<\/strong> are underway for <strong>HP\u2011002<\/strong>, a <strong>Class 1 innovative chemical drug<\/strong> independently developed by the company, for the treatment of <strong>relapsed or refractory B\u2011cell non\u2011Hodgkin lymphoma (B\u2011NHL)<\/strong>. The <strong>first patient dosing was recently completed<\/strong>, marking the program&#8217;s entry into clinical evaluation.<\/p>\n\n\n\n<h2 id=\"h-regulatory-amp-clinical-milestone\" class=\"wp-block-heading\">Regulatory &amp; Clinical Milestone<\/h2>\n\n\n\n<figure class=\"wp-block-table\"><table class=\"has-fixed-layout\"><thead><tr><th>Item<\/th><th>Detail<\/th><\/tr><\/thead><tbody><tr><td><strong>Developer<\/strong><\/td><td>Easton Pharmaceutical Co., Ltd. (SHA: 688513), Chengdu<\/td><\/tr><tr><td><strong>Product<\/strong><\/td><td>HP\u2011002 (Class 1 innovative chemical drug)<\/td><\/tr><tr><td><strong>Stage<\/strong><\/td><td>Phase I\/II clinical trials underway; first patient dosed<\/td><\/tr><tr><td><strong>Indication<\/strong><\/td><td>Relapsed or refractory B\u2011cell non\u2011Hodgkin lymphoma (B\u2011NHL)<\/td><\/tr><tr><td><strong>Announcement Date<\/strong><\/td><td>13 Aug 2026<\/td><\/tr><tr><td><strong>Next Steps<\/strong><\/td><td>Dose escalation and preliminary efficacy assessment in the Phase I\/II study<\/td><\/tr><\/tbody><\/table><\/figure>\n\n\n\n<h2 id=\"h-drug-profile-amp-mechanism-of-action\" class=\"wp-block-heading\">Drug Profile &amp; Mechanism of Action<\/h2>\n\n\n\n<ul class=\"wp-block-list\">\n<li><strong>Molecule:<\/strong> <strong>HP\u2011002<\/strong>, a <strong>next\u2011generation, brain\u2011penetrant PROTAC<\/strong> (proteolysis targeting chimera) molecule<\/li>\n\n\n\n<li><strong>Target:<\/strong> <strong>Bruton&#8217;s tyrosine kinase (BTK)<\/strong>, a key driver of B\u2011cell malignancies<\/li>\n\n\n\n<li><strong>Mechanism:<\/strong> As a PROTAC degrader, HP\u2011002 is designed to eliminate BTK protein rather than merely inhibit it \u2014 a strategy intended to overcome resistance mutations that limit existing covalent and non\u2011covalent BTK inhibitors<\/li>\n\n\n\n<li><strong>Differentiation:<\/strong> Combines BTK degradation with <strong>blood\u2011brain barrier penetration<\/strong>, addressing CNS involvement in B\u2011NHL where current therapies often fail<\/li>\n<\/ul>\n\n\n\n<h2 id=\"h-preclinical-evidence\" class=\"wp-block-heading\">Preclinical Evidence<\/h2>\n\n\n\n<figure class=\"wp-block-table\"><table class=\"has-fixed-layout\"><thead><tr><th>Element<\/th><th>Result (HP\u2011002)<\/th><\/tr><\/thead><tbody><tr><td><strong>Anti\u2011Proliferative Activity<\/strong><\/td><td>Potent activity against various BTK\u2011mutant cell lines<\/td><\/tr><tr><td><strong>In Vitro Profile<\/strong><\/td><td><strong>Best\u2011in\u2011class<\/strong> activity against multiple BTK mutations<\/td><\/tr><tr><td><strong>In Vivo Efficacy<\/strong><\/td><td>Significantly outperformed clinical\u2011stage control molecule <strong>NX\u20115948<\/strong> (Nurix Therapeutics) in two distinct animal models<\/td><\/tr><tr><td><strong>Pharmacokinetics<\/strong><\/td><td>Superior oral bioavailability and blood\u2011brain barrier penetration vs. control<\/td><\/tr><\/tbody><\/table><\/figure>\n\n\n\n<p class=\"wp-block-paragraph\">Preclinical studies demonstrated that <strong>HP\u2011002<\/strong> exhibits best\u2011in\u2011class in vitro activity against multiple BTK mutations. In two distinct in vivo efficacy animal models, its activity significantly outperformed <strong>NX\u20115948<\/strong>, the clinical\u2011stage BTK degrader from <strong>Nurix Therapeutics<\/strong>, while pharmacokinetic evaluations showed superior oral bioavailability and blood\u2011brain barrier penetration.<\/p>\n\n\n\n<h2 id=\"h-market-impact-amp-outlook\" class=\"wp-block-heading\">Market Impact &amp; Outlook<\/h2>\n\n\n\n<ul class=\"wp-block-list\">\n<li><strong>Resistance\u2011Driven Unmet Need:<\/strong> Patients with B\u2011NHL who relapse after covalent BTK inhibitors such as ibrutinib often carry resistance mutations; BTK degraders are designed to address precisely this population, making the segment one of the most closely watched in hematologic oncology.<\/li>\n\n\n\n<li><strong>Competitive Benchmarking:<\/strong> Head\u2011to\u2011head preclinical superiority over <strong>NX\u20115948<\/strong>, the leading clinical\u2011stage BTK PROTAC, positions <strong>HP\u2011002<\/strong> as a potentially differentiated entrant in the BTK degrader race.<\/li>\n\n\n\n<li><strong>CNS Opportunity:<\/strong> Brain penetrance is rare among BTK\u2011targeted therapies and could open treatment options for patients with CNS involvement \u2014 a significant differentiator if confirmed clinically.<\/li>\n\n\n\n<li><strong>Platform Validation:<\/strong> The first\u2011patient dosing of a proprietary Class 1 PROTAC validates <strong>Easton Pharmaceutical&#8217;s<\/strong> targeted protein degradation platform and extends Chengdu&#8217;s growing footprint in innovative oncology drug development.<\/li>\n<\/ul>\n\n\n\n<p class=\"wp-block-paragraph\"><strong>Forward-Looking Statements<\/strong><br>This brief contains forward\u2011looking statements regarding clinical trial progress, efficacy outcomes, and commercial potential for HP\u2011002. Actual results may differ due to risks including Phase I\/II safety and efficacy data, regulatory decisions, and competitive dynamics in the BTK degrader market.<a href=\"https:\/\/flcube.com\/\">-Fineline Info &amp; Tech<\/a><\/p>\n\n\n\n<div data-wp-interactive=\"core\/file\" class=\"wp-block-file\"><object data-wp-bind--hidden=\"!state.hasPdfPreview\" hidden class=\"wp-block-file__embed\" data=\"https:\/\/flcube.com\/wp-content\/uploads\/2026\/08\/12489793.pdf\" type=\"application\/pdf\" style=\"width:100%;height:600px\" aria-label=\"Embed of 12489793.\"><\/object><a id=\"wp-block-file--media-4bd7eeab-c894-49dd-ad5f-074a394a4e00\" href=\"https:\/\/flcube.com\/wp-content\/uploads\/2026\/08\/12489793.pdf\">12489793<\/a><a href=\"https:\/\/flcube.com\/wp-content\/uploads\/2026\/08\/12489793.pdf\" class=\"wp-block-file__button wp-element-button\" download aria-describedby=\"wp-block-file--media-4bd7eeab-c894-49dd-ad5f-074a394a4e00\">Download<\/a><\/div>\n","protected":false},"excerpt":{"rendered":"<p>Easton Pharmaceutical Co., Ltd. (SHA: 688513) announced that Phase I\/II clinical trials are underway for&#8230;<\/p>\n","protected":false},"author":1,"featured_media":0,"comment_status":"open","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"googlesitekit_rrm_CAownpewDA:productID":"","_jetpack_newsletter_access":"","_jetpack_dont_email_post_to_subs":false,"_jetpack_newsletter_tier_id":0,"_jetpack_memberships_contains_paywalled_content":false,"_jetpack_feature_clip_id":0,"_jetpack_memberships_contains_paid_content":false,"footnotes":"","jetpack_publicize_message":"","jetpack_publicize_feature_enabled":true,"jetpack_social_post_already_shared":true,"jetpack_social_options":{"image_generator_settings":{"template":"highway","default_image_id":0,"font":"","enabled":false},"version":2},"jetpack_post_was_ever_published":false},"categories":[7,11],"tags":[16,62,557,1008,70],"class_list":["post-74981","post","type-post","status-publish","format-standard","hentry","category-company","category-drug","tag-cancer","tag-clinical-trial-approval-initiation","tag-easton-pharmaceutical","tag-sha-688513","tag-tpd"],"yoast_head":"<!-- This site is optimized with the Yoast SEO Premium plugin v27.5 (Yoast SEO v28.2) - https:\/\/yoast.com\/product\/yoast-seo-premium-wordpress\/ -->\n<title>Easton Pharmaceutical Doses First Patient in Phase I\/II Trial of HP\u2011002, a Brain\u2011Penetrant BTK PROTAC for B\u2011Cell Non\u2011Hodgkin Lymphoma - Insight, China&#039;s Pharmaceutical Industry<\/title>\n<meta name=\"description\" content=\"Easton Pharmaceutical Co., Ltd. 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(SHA: 688513) announced that Phase I\/II clinical trials are underway for HP\u2011002, a Class 1 innovative chemical drug independently developed by the company, for the treatment of relapsed or refractory B\u2011cell non\u2011Hodgkin lymphoma (B\u2011NHL). The first patient dosing was recently completed, marking the program's entry into clinical evaluation.","breadcrumb":{"@id":"https:\/\/flcube.com\/?p=74981#breadcrumb"},"inLanguage":"en-US","potentialAction":[{"@type":"ReadAction","target":["https:\/\/flcube.com\/?p=74981"]}]},{"@type":"BreadcrumbList","@id":"https:\/\/flcube.com\/?p=74981#breadcrumb","itemListElement":[{"@type":"ListItem","position":1,"name":"Home","item":"https:\/\/flcube.com\/"},{"@type":"ListItem","position":2,"name":"Easton Pharmaceutical Doses First Patient in Phase I\/II Trial of HP\u2011002, a Brain\u2011Penetrant BTK PROTAC for B\u2011Cell Non\u2011Hodgkin Lymphoma"}]},{"@type":"WebSite","@id":"https:\/\/flcube.com\/#website","url":"https:\/\/flcube.com\/","name":"Insight, China's Pharmaceutical Industry","description":"Fineline Insights, Pharma Clarity","publisher":{"@id":"https:\/\/flcube.com\/#organization"},"potentialAction":[{"@type":"SearchAction","target":{"@type":"EntryPoint","urlTemplate":"https:\/\/flcube.com\/?s={search_term_string}"},"query-input":{"@type":"PropertyValueSpecification","valueRequired":true,"valueName":"search_term_string"}}],"inLanguage":"en-US"},{"@type":"Organization","@id":"https:\/\/flcube.com\/#organization","name":"Fineline Infomation and Technology","alternateName":"Fineline Info & Tech","url":"https:\/\/flcube.com\/","logo":{"@type":"ImageObject","inLanguage":"en-US","@id":"https:\/\/flcube.com\/#\/schema\/logo\/image\/","url":"https:\/\/flcube.com\/wp-content\/uploads\/2024\/11\/Fineline-info-tech-scaled.jpg","contentUrl":"https:\/\/flcube.com\/wp-content\/uploads\/2024\/11\/Fineline-info-tech-scaled.jpg","width":2560,"height":1894,"caption":"Fineline Infomation and Technology"},"image":{"@id":"https:\/\/flcube.com\/#\/schema\/logo\/image\/"},"sameAs":["https:\/\/www.facebook.com\/profile.php?id=61566606313834"]},{"@type":"Person","@id":"https:\/\/flcube.com\/#\/schema\/person\/19ad11870d326204db8524d3c3c5e66a","name":"Fineline Cube","image":{"@type":"ImageObject","inLanguage":"en-US","@id":"https:\/\/secure.gravatar.com\/avatar\/89f733aaed3d2d91d7d6f45d0e9ab509e3004e8243c6e57620b36380684657f2?s=96&d=mm&r=g","url":"https:\/\/secure.gravatar.com\/avatar\/89f733aaed3d2d91d7d6f45d0e9ab509e3004e8243c6e57620b36380684657f2?s=96&d=mm&r=g","contentUrl":"https:\/\/secure.gravatar.com\/avatar\/89f733aaed3d2d91d7d6f45d0e9ab509e3004e8243c6e57620b36380684657f2?s=96&d=mm&r=g","caption":"Fineline Cube"},"sameAs":["https:\/\/flcube.com"],"url":"https:\/\/flcube.com\/?author=1"}]}},"jetpack_publicize_connections":[],"jetpack_sharing_enabled":true,"jetpack_featured_media_url":"","_links":{"self":[{"href":"https:\/\/flcube.com\/index.php?rest_route=\/wp\/v2\/posts\/74981","targetHints":{"allow":["GET"]}}],"collection":[{"href":"https:\/\/flcube.com\/index.php?rest_route=\/wp\/v2\/posts"}],"about":[{"href":"https:\/\/flcube.com\/index.php?rest_route=\/wp\/v2\/types\/post"}],"author":[{"embeddable":true,"href":"https:\/\/flcube.com\/index.php?rest_route=\/wp\/v2\/users\/1"}],"replies":[{"embeddable":true,"href":"https:\/\/flcube.com\/index.php?rest_route=%2Fwp%2Fv2%2Fcomments&post=74981"}],"version-history":[{"count":1,"href":"https:\/\/flcube.com\/index.php?rest_route=\/wp\/v2\/posts\/74981\/revisions"}],"predecessor-version":[{"id":74984,"href":"https:\/\/flcube.com\/index.php?rest_route=\/wp\/v2\/posts\/74981\/revisions\/74984"}],"wp:attachment":[{"href":"https:\/\/flcube.com\/index.php?rest_route=%2Fwp%2Fv2%2Fmedia&parent=74981"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/flcube.com\/index.php?rest_route=%2Fwp%2Fv2%2Fcategories&post=74981"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/flcube.com\/index.php?rest_route=%2Fwp%2Fv2%2Ftags&post=74981"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}