Nilotinib Hydrochloride

▎药明康德内容团队编辑 Azurity Pharmaceuticals日前宣布，美国FDA已批准Danziten（nilotinib）用于治疗新确诊的费城染色体阳性慢性髓系白血病（Ph+ CML）慢性期（CP）成年患者，以及对包括伊马替尼（imatinib）在内的既往疗法有耐药或不耐受的慢性期和急性期（AP）成年患者。根据新闻稿，这是FDA批准的首个无需用餐限制的nilotinib药物。 Nilotinib是一款BCR-ABL激酶抑制剂，该药物能与ABL蛋白激酶域的非活性构象结合并稳定其构象。体外实验中，nilotinib可抑制BCR-ABL介导的小鼠白血病细胞系和Ph+ CML患者衍生的人类细胞系的增殖。在测试的33种BCR-ABL激酶突变中，nilotinib对32种伊马替尼耐药性突变仍具有活性。 过去试验显示，nilotinib对新确诊的Ph+CML-CP和耐药性或不耐受Ph+CML-CP和CML-AP成人有效。然而，在此之前的获批疗法的生物利用度不稳定，尤其是在与食物一起服用时更为显著。分析显示，在与食物一起不当服用时，过往获批的nilotinib会以浓度依赖性方式，显著延长体表心电图（ECG）上的QT间期。因此，服用该疗法期间时严格禁食对于避免心脏毒性至关重要。 Danziten是nilotinib的重新设计的配方，不受进餐时间限制，并与以往获批疗法具有相似的疗效，但生物利用度更高，可以更低的剂量来服用。Danziten表现出一致的药代动力学，无论患者空腹状态或进餐类型如何，Danziten暴露量均无临床显著差异。Danziten由于取消了禁食要求，有潜力改善患者的治疗依从性。 ▲欲了解更多前沿技术在生物医药产业中的应用，请长按扫描上方二维码，即可访问“药明直播间”，观看相关话题的直播讨论与精彩回放 参考资料： [1] AZURITY PHARMACEUTICALS, INC. ANNOUNCES FDA APPROVAL OF DANZITEN™ (nilotinib) tablets, THE FIRST AND ONLY NILOTINIB WITH NO MEALTIME RESTRICTIONS. Retrieved November 15, 2024 from https://azurity.com/azurity-pharmaceuticals-inc-announces-fda-approval-of-danziten-nilotinib-tablets-the-first-and-only-nilotinib-with-no-mealtime-restrictions/ [2] Danziten Prescribing Information. Retrieved November 15, 2024 from https://azurity.com/wp-content/uploads/2024/11/Danziten-Prescribing-Information.pdf 免责声明：药明康德内容团队专注介绍全球生物医药健康研究进展。本文仅作信息交流之目的，文中观点不代表药明康德立场，亦不代表药明康德支持或反对文中观点。本文也不是治疗方案推荐。如需获得治疗方案指导，请前往正规医院就诊。 版权说明：本文来自药明康德内容团队，欢迎个人转发至朋友圈，谢绝媒体或机构未经授权以任何形式转载至其他平台。转载授权请在「药明康德」微信公众号回复“转载”，获取转载须知。 分享，点赞，在看，聚焦全球生物医药健康创新

Danziten is set to be available soon via Biologics by McKesson and Limited Specialty Distribution. Credit: Motortion Films via Shutterstock. The US Food and Drug Administration (FDA) has approved Azurity Pharmaceuticals’ Danziten (nilotinib), the first and only nilotinib formulation that does not require mealtime restrictions, to treat chronic myeloid leukaemia (CML). It is indicated for adults with newly diagnosed Philadelphia chromosome-positive (Ph+) CML in the chronic phase, as well as those who are resistant or intolerant to previous therapies that included imatinib. Danziten’s reengineered formulation is said to provide equivalent efficacy to Tasigna but with enhanced bioavailability, enabling a lower dosage. Its approval is expected to enhance patient adherence to treatment, as it eliminates the need for fasting, which has been a challenge with current therapies. While Tasigna, the existing nilotinib treatment, has proven efficacy for Ph+ CML in chronic and acute phases, its bioavailability is affected by food intake, necessitating strict fasting to prevent cardiotoxicity. An optimal tyrosine kinase inhibitor therapy may lead to deep molecular responses, and for some patients, even treatment-free remission, the company noted. Azurity Pharmaceuticals CEO Richard Blackburn said: “Danziten offers a new nilotinib treatment option with the equivalent efficacy to Tasigna, but without the fasting requirements of Tasigna. “Unlike Tasigna, the boxed warning on the Danziten label has no requirement for patients to take their medication in a fasted state, liberating CML patients from mealtime restrictions.” Danziten is set to be shortly available via Biologics by McKesson and Limited Specialty Distribution. In September this year, the FDA approved the company’s Nymalize , an oral solution provided in a 5ml prefilled ENFit syringe as an alternative for adult subarachnoid haemorrhage patients. In 2022, it received approval for Konvomep, a treatment for active benign gastric ulcers and risk reduction of upper gastrointestinal bleeding in critically ill patients.