Pirtobrutinib

国产BTK赛道持续开大。根据百济神州的财报数据，2024年，泽布替尼的销售额达到26.44亿美元（约合192亿元人民币），同比增长105%，成为首个年销售额超百亿元人民币的国产BTK抑制剂。诺诚健华发布的2024年年度报告显示，其主打产品BTK抑制剂奥布替尼的全年销售收入首次突破十亿元大关，达到10.09亿元人民币，同比增长36.68%。01BTK抑制剂市场分析BTK（Bruton's tyrosine kinase，布鲁顿酪氨酸激酶）抑制剂是一类靶向药物，通过抑制BTK的活性来阻断B细胞受体下游信号通路，从而诱导恶性B细胞凋亡，主要用于治疗B细胞恶性肿瘤和某些自身免疫性疾病。自2013年首款药物伊布替尼问世以来，彻底改变了部分血液肿瘤和自身免疫性疾病的治疗格局。历经十余年的发展，BTK抑制剂领域涌现出多款创新药物，市场规模持续扩张，竞争格局日趋复杂。目前全球已上市多款BTK抑制剂，包括第一代不可逆的伊布替尼，第二代选择性更高的不可逆抑制剂如阿可替尼、泽布替尼和奥布替尼，以及第三代可逆的匹妥布替尼等。其中，第二代BTK抑制剂凭借更高的选择性和安全性，逐步蚕食第一代伊布替尼的市场份额。第三代可逆抑制剂的上市，为耐药患者提供了新的治疗选择。根据结合方式的不同，BTK抑制剂可分为共价不可逆抑制剂，如伊布替尼、阿可替尼和泽布替尼，通过与BTK的C481残基形成共价键，产生持久的抑制作用。非共价可逆抑制剂，如匹妥布替尼，与BTK的ATP结合位点形成非共价键，抑制作用是可逆的。这类抑制剂旨在克服共价抑制剂产生的C481突变耐药问题。目前，BTK抑制剂的临床研究不仅集中在已获批的血液肿瘤领域，还在积极探索在其他血液肿瘤和自身免疫性疾病中的应用。同时，BTK抑制剂与化疗、其他靶向药物和免疫疗法的联合治疗策略也备受关注。根据市场调研机构的数据显示，2024年，全球BTK抑制剂市场规模约为94亿美元。预计2025年将达到219亿美元，到2030年有望增长至251-289亿美元。中国BTK抑制剂市场增速更快，预计2025年将达到131亿元人民币，2030年将达到178-225亿元人民币。驱动市场增长的主要因素包括：广泛的适应症：BTK抑制剂已获批用于多种B细胞恶性肿瘤，并且在自身免疫性疾病领域展现出潜力。临床疗效显著：BTK抑制剂在许多患者中表现出良好的疗效，提高了患者的生存期和生活质量。新一代药物的上市：选择性更高、安全性更好的第二代和能够克服耐药性的第三代BTK抑制剂的推出，进一步推动了市场增长。联合治疗策略的进展：BTK抑制剂与其他疗法的联合应用有望扩大其治疗范围和提高疗效。本土创新药的崛起：以泽布替尼和奥布替尼为代表的国产创新BTK抑制剂凭借其疗效、安全性以及价格优势，迅速占领市场份额。未满足的临床需求：尽管已有药物上市，但在某些疾病亚型和耐药患者群体中，仍存在显著的未满足临床需求。同时仍存在一定的市场限制因素，包含以下几方面：药物价格和可及性：尽管医保政策有所改善，但BTK抑制剂的价格仍然较高，尤其是一些尚未纳入医保的进口药物，限制了部分患者的可及性。不良反应和安全性问题：第一代BTK抑制剂存在一定的脱靶毒性，新一代药物虽然有所改善，但仍可能出现不良反应，影响患者的耐受性和依从性。耐药性的产生：长期使用共价BTK抑制剂可能导致耐药性，特别是C481突变的发生，限制了药物的长期疗效。市场竞争加剧：随着更多BTK抑制剂和同靶点药物的上市，市场竞争日益激烈，对新进入者的市场份额构成挑战。02BTK抑制剂竞争格局分析全球BTK抑制剂市场的主要参与者包括艾伯维/强生的伊布替尼（Imbruvica），是首个上市的BTK抑制剂，拥有广泛的适应症和较长的市场积累。然而，其脱靶毒性和耐药性问题以及专利即将到期是其面临的主要挑战。阿斯利康的阿可替尼（Calquence），一种选择性更高的第二代共价BTK抑制剂，在特定适应症上展现出优势。百济神州的泽布替尼（Brukinsa），一款具有高选择性的第二代共价BTK抑制剂，在全球市场表现强劲，尤其在中国市场后来居上。礼来的匹妥布替尼（Jaypirca），首个获批的非共价可逆BTK抑制剂，为C481突变耐药患者提供了新的治疗选择。诺诚健华的奥布替尼（Orelabrutinib），一款国产第二代共价BTK抑制剂，在中国市场取得了显著的商业化成功。中国BTK抑制剂市场竞争格局正在经历深刻的变化，主要特点是本土创新药的快速崛起，其中伊布替尼最早进入中国市场，曾占据主导地位。目前，国产创新药正在强势崛起，泽布替尼和奥布替尼凭借其临床数据、价格优势以及医保支持，迅速抢占市场份额，2023年其全球销售额突破13亿美元大关，成为首个国产“十亿美元分子”。泽布替尼已在多个适应症上获得批准，并在头对头临床试验中展现出优于伊布替尼的疗效。奥布替尼在边缘区淋巴瘤等适应症上具有独特优势，并实现了快速放量。匹妥布替尼进入耐药市场，作为首个在中国获批的非共价BTK抑制剂，匹妥布替尼有望在经历过其他BTK抑制剂治疗的复发或难治性MCL患者中占据市场份额。此外，伊布替尼的专利即将到期，预计将有大量仿制药上市，进一步加剧市场竞争。国内多家药企正在积极研发新一代BTK抑制剂，未来市场竞争将更加激烈。随着BTK抑制剂市场的持续发展和竞争的加剧，未来几年将呈现以下趋势：新一代BTK抑制剂持续涌现：更多具有更高选择性、更好安全性和克服耐药性潜力的BTK抑制剂将进入市场。如蛋白水解靶向嵌合体（PROTACs）是一种新兴的药物研发策略，它通过招募E3泛素连接酶到靶蛋白附近，诱导靶蛋白的泛素化和蛋白酶体降解。BTK-PROTACs有望实现对BTK的更深层次抑制，并可能克服传统小分子抑制剂的耐药性问题。目前，一些公司正在积极探索BTK-PROTACs的研发。联合治疗成为趋势：BTK抑制剂与其他靶向药物、免疫疗法等的联合应用将成为重要的研究方向，以期提高疗效和克服耐药性。自身免疫性疾病领域潜力巨大：目前获批的BTK抑制剂主要集中在血液肿瘤领域，但在类风湿关节炎、系统性红斑狼疮等自身免疫性疾病中也显示出治疗潜力，未来有望成为新的增长点。国际化进程加速：以泽布替尼为代表的国产BTK抑制剂已开始走向国际市场，未来将有更多中国创新药参与全球竞争。结论BTK抑制剂行业正处于快速发展和变革的时期。随着对BTK在疾病发生发展中作用的深入理解和技术的不断进步，新一代BTK抑制剂和创新的治疗策略将持续涌现，为B细胞恶性肿瘤和自身免疫性疾病患者带来更多希望。市场竞争将日益激烈，但同时也为具有创新能力和差异化优势的企业提供了广阔的发展空间。期待下一个国产BTK抑制剂大药。识别微信二维码，添加抗体圈小编，符合条件者即可加入抗体圈微信群！请注明：姓名+研究方向！本公众号所有转载文章系出于传递更多信息之目的，且明确注明来源和作者，不希望被转载的媒体或个人可与我们联系(cbplib@163.com)，我们将立即进行删除处理。所有文章仅代表作者观点，不代表本站立场。

SAN FRANCISCO and SUZHOU, China, March 30, 2025 /PRNewswire/ -- Innovent Biologics, Inc. ("Innovent") (HKEX: 01801), a world-class biopharmaceutical company that develops, manufactures and commercializes high-quality medicines for the treatment of oncology, cardiovascular and metabolic, autoimmune, ophthalmology and other major diseases, announced that the Center for Drug Evaluation (CDE) of China's National Medical Products Administration (NMPA) has granted Breakthrough Therapy Designation (BTD) for IBI363, a first-in-class PD-1/IL-2α-bias bispecific antibody fusion protein, as monotherapy for the treatment of unresectable locally advanced or metastatic mucosal or acral melanoma who have not received prior systemic therapy. Recently, Innovent initiated and dosed the first patient for IBI363 in its first pivotal study to evaluate the efficacy and safety of IBI363 monotherapy versus pembrolizumab (Keytruda®) monotherapy in patients with unresectable, locally advanced or metastatic mucosal or acral melanoma who have not received prior systemic therapy. Furthermore, IBI363 has received two fast track designations (FTD) from the U.S. Food and Drug Administration (FDA), for the treatment of squamous non-small cell lung cancer and melanoma, respectively. IBI363 has demonstrated outstanding efficacy signals in immunotherapy (IO)-naïve melanoma patients across two earlier clinical trials (Phase 1a/1b study NCT05460767 and Phase 2 study NCT06081920), which enrolled a total of 26 patients with advanced acral or mucosal melanoma: The overall objective response rate (ORR) was 61.5%, and the disease control rate (DCR) was 84.6%—significantly higher than current domestic immunotherapy standards. Prolonged follow-up revealed sustained tumor responses and long-term benefits, suggesting the potential superiority of IBI363 over existing standard therapies. Dr. Hui Zhou, Senior Vice President of Innovent, said, "As Innovent's first-in-class next-generation IO therapy, IBI363 simultaneously and selectively inhibits the PD-1/PD-L1 pathway and activates the IL-2 pathway. IBI363 has recently received multiple FTD and BTD designations, signifying regulatory recognition of its clinical value in addressing unmet medical needs. Non-cutaneous melanoma subtypes like mucosal melanoma—which are more prevalent in China—are particularly resistant to immunotherapy with limited clinical benefits[i]. We aim to validate IBI363's potential in its first pivotal trial, through a head-to-head comparison with pembrolizumab, as a superior treatment option for melanoma patients over the current standard-of-care. We are also accelerating the global development of IBI363 across multiple tumor types, with the goal of extending the benefits of China's innovation to patients worldwide." NMPA Breakthrough Therapy Designation is intended to facilitate and expedite the development and review of investigational drugs for serious diseases or conditions when preliminary clinical evidence indicates substantial improvement over current therapies. BTD qualifies a drug candidate for accelerated review by the CDE and provides the sponsor with timely advice and communication to expedite the approval process, helping to address the unmet clinical needs of patients more swiftly. About IBI363 (First-in-class PD-1/IL-2α-bias bispecific antibody fusion protein) IBI363 is a first-in-class drug candidate independently developed by Innovent Biologics. It is a PD-1/IL-2 bispecific antibody fusion protein designed to enhance efficiency while minimizing toxicity. The IL-2 arm of IBI363 has been engineered to optimize therapeutic effects with reduced side effects, while the PD-1 binding arm enables PD-1 blockade and selective IL-2 delivery. By simultaneously inhibiting the PD-1/PD-L1 pathway and activating the IL-2 pathway, IBI363 facilitates more precise and efficient targeting and activation of tumor specific T cells. Preclinical studies have shown that IBI363 exhibits strong anti-tumor activity across multiple tumor-bearing pharmacological models, including those resistant to PD-1 inhibitors and metastatic models. Additionally, it has demonstrated a favorable safety profile in preclinical models. Clinical trials of IBI363 are currently underway in China, the United States, and Australia to evaluate its safety, tolerability and preliminary efficacy in subjects with advanced malignancies. The first pivotal study of IBI363 has been initiated, for the treatment of IO-naive mucosal or acral melanoma. Furthermore, IBI363 has received two fast track designations (FTD) from the U.S. FDA, for the treatment of melanoma and squamous NSCLC, respectively. IBI363 has also received breakthrough therapy designation from the NMPA of China for the treatment of melanoma. About Melanoma Melanoma is a malignant tumor that develops from melanocytes. Although melanoma accounts for only 3% of all types of skin cancer, it has the highest mortality rate of all types and is the most likely to metastasize. In China, the incidence and mortality rate of melanoma continue to rise. Melanoma is classified into three main subtypes: cutaneous, acral and mucosal. The characteristics of melanoma in Chinese patients differs greatly from those seen in European and American Caucasian populations in terms of pathogenesis, biological behavior, histological morphology, treatment response and prognosis[i]. For advanced cutaneous and acral melanomas, patients with the BRAF V600 mutation typically receive BRAF inhibitor combined with MEK inhibitors as the preferred molecular targeted therapy. For those without the BRAF V600 mutation, chemotherapy combined with anti-angiogenic drugs can be is a first-line treatment option. Notably, pembrolizumab has been approved as the first-line treatment indication for advanced melanoma in September 2024 in China, although clinical benefits are limited. For second-line treatment, therapies not previously used in first-line settings are recommended. Patients who have not received PD-1 monoclonal antibody in the first-line setting may be treated with PD-1 inhibitors as a second-line option. For advanced mucosal melanoma -which are more prevalent in China-are particularly resistant to immunotherapy with limited clinical benefits, in urgent need of new treatment options. About Innovent Innovent is a leading biopharmaceutical company founded in 2011 with the mission to empower patients worldwide with affordable, high-quality biopharmaceuticals. The company discovers, develops, manufactures and commercializes innovative medicines that target some of the most intractable diseases. Its pioneering therapies treat cancer, cardiovascular and metabolic, autoimmune and eye diseases. Innovent has launched 15 products in the market. It has 3 new drug applications under regulatory review, 4 assets in Phase III or pivotal clinical trials and 15 more molecules in early clinical stage. Innovent partners with over 30 global healthcare companies, including Eli Lilly, Sanofi, Incyte, Adimab, LG Chem and MD Anderson Cancer Center. Guided by the motto, "Start with Integrity, Succeed through Action," Innovent maintains the highest standard of industry practices and works collaboratively to advance the biopharmaceutical industry so that first-rate pharmaceutical drugs can become widely accessible. For more information, visit , or follow Innovent on Facebook and LinkedIn. Statement: （1）Innovent does not recommend the use of any unapproved drug (s)/indication (s). （2）Ramucirumab (Cyramza), Selpercatinib (Retsevmo) and Pirtobrutinib (Jaypirca) were developed by Eli Lilly and Company. Forward-Looking Statements This news release may contain certain forward-looking statements that are, by their nature, subject to significant risks and uncertainties. The words "anticipate", "believe", "estimate", "expect", "intend" and similar expressions, as they relate to Innovent, are intended to identify certain of such forward-looking statements. Innovent does not intend to update these forward-looking statements regularly. These forward-looking statements are based on the existing beliefs, assumptions, expectations, estimates, projections and understandings of the management of Innovent with respect to future events at the time these statements are made. These statements are not a guarantee of future developments and are subject to risks, uncertainties and other factors, some of which are beyond Innovent's control and are difficult to predict. Consequently, actual results may differ materially from information contained in the forward-looking statements as a result of future changes or developments in our business, Innovent's competitive environment and political, economic, legal and social conditions. Innovent, the Directors and the employees of Innovent assume (a) no obligation to correct or update the forward-looking statements contained in this site; and (b) no liability in the event that any of the forward-looking statements does not materialize or turn out to be incorrect. References: [i] CSCO黑色素瘤诊疗指南（2023年版） SOURCE Innovent Biologics WANT YOUR COMPANY'S NEWS FEATURED ON PRNEWSWIRE.COM? 440k+ Newsrooms & Influencers 9k+ Digital Media Outlets 270k+ Journalists Opted In GET STARTED