{"id":5608,"date":"2023-11-09T16:33:56","date_gmt":"2023-11-09T15:33:56","guid":{"rendered":"https:\/\/beigen.vipdev.lndo.site\/?post_type=compound&#038;p=5608"},"modified":"2024-04-24T14:51:26","modified_gmt":"2024-04-24T13:51:26","slug":"bgb-16673","status":"publish","type":"compound","link":"http:\/\/beonemedaffairs.com\/begenius\/compound\/5608\/bgb-16673\/","title":{"rendered":"BGB-16673"},"content":{"rendered":"","protected":false},"template":"","meta":{"_acf_changed":false,"editor_notices":[]},"post-tag":[],"class_list":["post-5608","compound","type-compound","status-publish","hentry"],"acf":{"header_text":"","summary":"BGB-16673 is a BTK-targeted protein degrader.<sup>1<\/sup>","tags":false,"text":"<strong>Mechanism of action<\/strong>\r\n\r\nBruton\u2019s tyrosine kinase (BTK) is a component of the B-cell receptor (BCR) signaling pathway and is an important regulator of cell proliferation and cell survival in various B-cell malignancies including chronic lymphocytic leukemia\/small lymphocytic lymphoma (CLL\/SLL), Waldenstr\u00f6m\u2019s macroglobulinemia (WM), marginal zone lymphoma (MZL), mantle cell lymphoma (MCL) and follicular lymphoma (FL).<sup>2<\/sup>\r\n\r\nBGB-16673 is an orally available BTK-targeting chimeric degradation activating compound (CDAC) with demonstrated preclinical degradation activity against both wildtype BTK and multiple mutant forms commonly identified in patients who have progressed on BTK inhibitors.<sup>1<\/sup> BGB-16673 triggers selective BTK degradation via the intracellular ubiquitin-proteasome system. By degrading BTK, BGB-16673 blocks BCR-induced BTK activation and its downstream signaling in a rapid and sustained manner, leading to growth inhibition and cell death in B-cells.\r\n\r\nTargeting BTK via an alternative mechanism may overcome the current challenges of BTK inhibitors and may allow continued targeting of a critical pathway in B-cell malignancies.\r\n\r\n<img class=\"aligncenter wp-image-5615 size-full\" src=\"https:\/\/beonemedaffairs.com\/wp-content\/uploads\/2023\/11\/BGB-16673_Compound.png\" alt=\"BGB-16673_Compound\" width=\"3508\" height=\"3525\" \/>\r\n\r\n<strong>BGB-16673 in clinical trials<\/strong>\r\n\r\nBGB-16673 is currently being investigated as monotherapy in two Phase 1 dose-escalation\/expansion studies in adult patients with relapsed\/refractory (R\/R) B-cell malignancies.<sup>3<\/sup>\r\n\r\nFor an exhaustive list of BGB-16673 clinical trials, view the development program.\r\n\r\n<em>BGB-16673 is an <\/em><em>investigational compound for which safety and efficacy have not been established. <\/em><em>B<\/em><em>ecause of the<\/em><em> uncertainty of clinical trials, there is no guarantee that BGB-16673 will receive regulatory approval and become commercially available for the uses being investigated.<\/em>\r\n\r\n<strong>References<\/strong>\r\n<ol>\r\n \t<li>Wang, H., et al. Abstract P1219: BGB-16673, a BTK degrader, overcomes on-target resistance from BTK inhibitors and presents sustainable long-term tumor regression in lymphoma xenograft models. <em>Hemasphere<\/em> 2023; 7(Suppl):<\/li>\r\n \t<li>Singh, S. P., Dammeijer, F. &amp; Hendriks, R. W. Role of Bruton's tyrosine kinase in B cells and malignancies. <em>Mol Cancer<\/em> 2018; 17(1):57.<\/li>\r\n \t<li>Tam, C.S, et al. Abstract P686: A Phase 1 first-in-human study of BGB-16673, a Bruton\u2019s tyrosine kinase protein degrader, in patients with B-cell malignancies (trial in progress). <em>Hemasphere<\/em> 2022; 6:582-583.<\/li>\r\n<\/ol>","approval_status_for_filter":"","accordion_presentation":"expanded","overview":"","mechanism_of_action":"","approval_status":"","other_resources":null},"_links":{"self":[{"href":"http:\/\/beonemedaffairs.com\/begenius\/wp-json\/wp\/v2\/compound\/5608","targetHints":{"allow":["GET"]}}],"collection":[{"href":"http:\/\/beonemedaffairs.com\/begenius\/wp-json\/wp\/v2\/compound"}],"about":[{"href":"http:\/\/beonemedaffairs.com\/begenius\/wp-json\/wp\/v2\/types\/compound"}],"wp:attachment":[{"href":"http:\/\/beonemedaffairs.com\/begenius\/wp-json\/wp\/v2\/media?parent=5608"}],"wp:term":[{"taxonomy":"post-tag","embeddable":true,"href":"http:\/\/beonemedaffairs.com\/begenius\/wp-json\/wp\/v2\/post-tag?post=5608"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}