TK-216

精彩内容近日，上海医药枸橼酸托法替布片获批上市，旗下10款中成药获推荐“抗疫”。目前上海医药有23款创新药（17款1类新药）处于获批临床及以上阶段，4款处于III期临床阶段，上市可期；60个品种过评（16个首家），16个品种中标国家集采；中医药底蕴深厚，超10款中成药获推荐“抗疫”。拿下6大重磅品种！60个过评品种亮眼12月15日，上海医药发布公告称，控股子公司上海上药中西制药的枸橼酸托法替布片获批上市，并视同通过一致性评价。枸橼酸托法替布片是全球首个治疗类风湿关节炎的小分子靶向JAK激酶抑制剂，米内网数据显示，2021年中国三大终端6大市场（统计范围详见本文末）枸橼酸托法替布片销售额超过5亿元，同比增长58.92%。今年以来，上海医药已有6个新分类报产品种获批上市，包括枸橼酸托法替布片、拉考沙胺片、阿立哌唑口服溶液、替格瑞洛片、阿哌沙班片、盐酸胺碘酮注射液。米内网数据显示，2021年中国三大终端6大市场阿立哌唑销售额超过14亿元、替格瑞洛销售额超过10亿元、胺碘酮销售额超过4亿元。2022年至今上海医药获批品种来源：米内网中国申报进度（MED）数据库一致性评价方面，目前上海医药已有60个品种通过/视同通过一致性评价。其中，16个品种为国内首家过评，阿普唑仑片、阿立哌唑胶囊、盐酸度洛西汀肠溶片、硫酸羟氯喹片等4个品种为独家过评。上海医药通过/视同通过一致性评价品种从治疗领域上看，60个品种涵盖11个治疗大类，主要集中在心脑血管系统药物（17个）、神经系统药物（15个）。米内网数据显示，2021年中国三大终端6大市场心脑血管系统药物、神经系统药物销售规模均超过1000亿元。自国家第三批化药集采开始，上海医药便陆续有产品中标，累计16个品种中选国家集采。随着集采常态化推进，仿制药以价换量，药企更加注重院外市场的开发，同时也逐步向壁垒较高、竞争格局较好的品种倾斜，加速向创新转型。17款1类新药在研！4款创新药上市可期以科技创新为驱动，近年来上海医药加速创新转型，持续加大研发投入。2022年前三季度公司研发投入16.92亿元，其中费用化的研发投入13.89亿元，同比增长1.63%。公司已有安柯瑞（重组人5型腺病毒）、凯力康（尤瑞克林）、培菲康（双歧杆菌三联活菌）3款1类新药上市。目前上海医药主要有23款创新药处于获批临床及以上阶段，主要聚焦肿瘤及自身免疫领域，其中1类创新药有17个。从药品类型来看，小分子1类创新药有11个、大分子创新药有9个、中药创新药有2个。上海医药主要在研创新药来源：米内网中国药品临床试验公示库23款创新药中，SPH3127片、X842、Prolgolimab注射液、Netakimab注射液均已有适应症处于Ⅲ期临床阶段，上市可期；注射用百纳培南、藿苓生肌颗粒、B013注射液、羟基雷公藤内酯醇片、TK216注射液、注射用重组抗HER2人源化单克隆抗体-MCC-DM1偶联剂等处于Ⅱ期临床阶段。1类创新药SPH3127片是新一代口服非肽类小分子肾素抑制剂，先后获批开展原发性高血压、糖尿病肾病、炎症性肠炎等适应症的临床试验。米内网数据显示，2021年中国三大终端6大市场高血压用药销售额超过720亿元。作为新作用机制的降压药物，SPH3127片有望为广大的原发性轻、中度高血压患者提供一种有效的治疗途径和更丰富的治疗手段。X842是新一代钾离子竞争性酸阻断剂（P-CAB）口服药物，从机理上讲在起效时间、个体差异、服用顺应性方面皆好于PPI药物，且市场竞争格局较好。其针对反流性食管炎的Ⅲ期临床试验已达到主要终点指标且显示了良好的安全性，预计于今年年底递交NDA，有望于2023Q4-2024Q1获批上市。疫情防控新阶段！10余款中成药“抗疫”作为国内大型医药产业集团，上海医药在中医药领域也有深厚的积淀。上海医药中药产品资源丰富，旗下拥有7家中药重点企业、9个广受认可的核心品牌以及八宝丹、六神丸等多项保密配方和胃复春等独家品种，中药销售收入约为工业板块总体收入的三分之一，其中14种产品于2021年的销售收入逾1亿元。12月8日，国务院联防联控机制发布了《新冠病毒感染者居家治疗常用药参考表》，8款中成药获得推荐，上海雷允上的六神丸入选。12月10日，国家中医药局发布了《新冠病毒感染者居家中医药干预指引》（《指引》），60款中成药获得推荐。上海医药旗下10款产品六神丸、通宣理肺颗粒、桑菊感冒片、感冒退热颗粒、银翘解毒颗粒、小柴胡颗粒、通宣理肺丸、藿香正气丸、防风通圣丸、小儿止咳糖浆等入选。上海医药旗下入选《指引》产品除了入选常用药参考表或《指引》，上海医药旗下产品小儿肺热咳喘颗粒及独家产品八宝丹、苦甘颗粒等也被列为多地新型冠状病毒防治推荐用药。资料来源：米内网数据库、公司公告等注：米内网《中国三大终端6大市场药品竞争格局》，统计范围是：城市公立医院和县级公立医院、城市社区中心和乡镇卫生院、城市实体药店和网上药店，不含民营医院、私人诊所、村卫生室，不含县乡村药店；上述销售额以产品在终端的平均零售价计算。数据统计如有疏漏，欢迎指正！本文为原创稿件，转载请注明来源和作者，否则将追究侵权责任。投稿及报料请发邮件到872470254@qq.com稿件要求详询米内微信首页菜单栏商务及内容合作可联系QQ：412539092●温馨提示●因为微信公众号修改了推送规则，最近很多读者反映没有及时看到推文。把米内网设为“星标”，就能每天与我们不见不散啦，具体操作如下：【分享、点赞、在看】点一点不失联哦

SAN DIEGO, Nov. 15, 2021 (GLOBE NEWSWIRE) -- Oncternal Therapeutics, Inc. (Nasdaq: ONCT), a clinical-stage biopharmaceutical company focused on the development of novel oncology therapies, today announced updated interim clinical data from the Phase 2 expansion cohort of its ongoing Phase 1/2 clinical trial evaluating ONCT-216 (formerly TK216), an investigational, potentially first-in-class, targeted small-molecule inhibitor of the E26 transformation-specific (ETS) family of oncoproteins, in patients with relapsed or refractory Ewing sarcoma. The data update was delivered in an oral presentation at the Connective Tissue Oncology Society (CTOS) 2021 Virtual Annual Meeting. Session Title: Session 12: Ultra-Rare and Translocation Sarcomas Session Date: Saturday, November 13, 2021 Presentation Title: Paper 74 - TK216 FOR EWING SARCOMA- INTERIM PHASE 1/2 RESULTS A copy of the presentation will be accessible on the Events & Presentations page of the Investors section on the Company’s website at investor.oncternal.com. “We remain encouraged by the two complete responses to ONCT-216 in heavily pre-treated patients with relapsed or refractory Ewing sarcoma, including one patient who had a durable CR for 24 months on treatment, and remains with no evidence of disease off of all treatments for several months,” said James Breitmeyer, M.D., Ph.D., Oncternal’s President and CEO. “We believe that an intensified dosing schedule, which we are investigating in a new study cohort that is now enrolling, holds promise to address the significant unmet needs for patients suffering from this devastating disease.” ONCT-216 remains generally well tolerated. As of the October 1, 2021 data cutoff date, the most common drug-related adverse events included myelosuppression, fatigue, alopecia, nausea, pyrexia, and decreased appetite. The myelosuppression was primarily neutropenia, which was transient and readily managed. No unexpected off-target toxicities have been observed. About Ewing sarcoma Ewing sarcoma is the second most common bone tumor among children and adolescents. The median age at diagnosis of patients with Ewing sarcoma is 15, the incidence is about 3 cases per 1 million per year in children under the age of 20 and about 1.3 cases per 1 million overall in the U.S. and prevalence is about 12 per million people overall in the US. Nearly all Ewing sarcoma cases are driven by translocations of ETS family oncogenes, including 85-90% of cases driven by the EWS-FLI1 fusion, and approximately 10% by EWS-ERG. Patients diagnosed with metastatic disease have five-year survival rates between 18% and 30%. The prognosis for patients with recurrent Ewing sarcoma is particularly poor, and five-year survival after recurrence is approximately 10 to 15%. About ONCT-216 ONCT-216 is an investigational, potentially first-in-class, targeted small-molecule inhibitor of the E26 transformation-specific (ETS) family of oncoproteins including fusion proteins. Tumorigenic fusion proteins involving the EWS protein and an ETS protein can be found in most cases of Ewing sarcoma. ETS-related translocations or overexpression are also found in many other tumors such as diffuse large B-cell lymphoma (DLBCL), prostate cancer and acute myeloid leukemia (AML). ONCT-216 was developed based on discoveries in the laboratory of Jeffrey Toretsky, M.D., at Georgetown Lombardi Comprehensive Cancer Center, who discovered inhibitors of EWS-FLI1 using a novel chemical screening assay. In preclinical models, ONCT-216 was observed to bind to EWS-FLI1, blocking the interaction between this fusion protein and other transcriptome proteins such as RNA helicase A, leading to tumor cell apoptosis and inhibiting tumor growth in animal models. The U.S. Food and Drug Administration (FDA) has granted Rare Pediatric Disease Designation, Orphan Drug Designation and Fast Track Status to ONCT-216 for the treatment of Ewing sarcoma. ONCT-216 is an investigational medication that has not been approved by the FDA for any indication. About the Study ONCT-216 is being evaluated in a Phase 1/2 clinical study as a single agent and in combination with vincristine in heavily pretreated patients with relapsed or refractory Ewing sarcoma, a rare pediatric cancer with no standard treatment available after first-line chemotherapy. The current Phase 2 expansion cohort targeting up to 21 evaluable Ewing sarcoma patients is active and enrolling patients, designed to evaluate clinical responses to single agent ONCT-216 using an optimized dosing regimen, treating for 28 days per cycle, to intensify the amount of ONCT-216 administered over time. This multi-center study is currently enrolling patients at nine clinical trial centers across the U.S. Additional information about the ONCT-216 study may be accessed at ClinicalTrials.gov (NCT02657005). About Oncternal Therapeutics Oncternal Therapeutics is a clinical-stage biopharmaceutical company focused on the development of novel oncology therapies for the treatment of cancers with critical unmet medical need. Oncternal focuses drug development on promising, yet untapped biological pathways implicated in cancer generation or progression. The clinical pipeline includes zilovertamab (formerly cirmtuzumab) an investigational monoclonal antibody designed to inhibit the ROR1 pathway, a type I tyrosine kinase-like orphan receptor, that is being evaluated in a Phase 1b/2 clinical trial in combination with ibrutinib for the treatment of patients with mantle cell lymphoma (MCL) and chronic lymphocytic leukemia (CLL) and in an investigator-sponsored, Phase 1b clinical trial in combination with paclitaxel for the treatment of women with HER2-negative metastatic or locally advanced, unresectable breast cancer, as well as a Phase 2 clinical trial of zilovertamab in combination with venetoclax, a Bcl-2 inhibitor, in patients with relapsed/refractory CLL. Oncternal is also developing ONCT-808, a chimeric antigen receptor T cell (CAR-T) therapy that targets ROR1, which is currently in preclinical development as a potential treatment for hematologic cancers and solid tumors. The clinical pipeline also includes ONCT-216 (formerly TK216), an investigational targeted small-molecule inhibitor of the ETS family of oncoproteins, that is being evaluated in a Phase 1/2 clinical trial for patients with Ewing sarcoma alone and in combination with vincristine chemotherapy. The early-stage pipeline also includes ONCT-534 (formerly GTX-534), a dual-action androgen receptor inhibitor, that is in pre-clinical development as a potential treatment for castration resistant prostate cancer and other androgen-receptor dependent diseases. More information is available at . Forward-Looking Information Oncternal cautions you that statements included in this press release that are not a description of historical facts are forward-looking statements. In some cases, you can identify forward-looking statements by terms such as “may,” “will,” “should,” “expect,” “plan,” “anticipate,” “could,” “intend,” “target,” “project,” “contemplates,” “believes,” “estimates,” “predicts,” “potential” or “continue” or the negatives of these terms or other similar expressions. These statements are based on Oncternal’s current beliefs and expectations. Forward-looking statements include statements regarding the potential for ONCT-216 dosing changes to address unmet medical needs. Forward-looking statements are subject to risks and uncertainties inherent in Oncternal’s business, including risks associated with the clinical development and process for obtaining regulatory approval of Oncternal’s product candidates, such as potential delays in the commencement, enrollment and completion of clinical trials; the risk that results seen in a case study of one patient likely will not predict the results seen in other patients in the clinical trial; the risk that interim results of a clinical trial do not predict final results and that one or more of the clinical outcomes may materially change as patient enrollment continues, following more comprehensive reviews of the data, as follow-up on the outcome of any particular patient continues, and as more patient data become available; and other risks described in Oncternal’s filings with the U.S. Securities and Exchange Commission. All forward-looking statements in this press release are current only as of the date hereof and, except as required by applicable law, Oncternal undertakes no obligation to revise or update any forward-looking statement, or to make any other forward-looking statements, whether as a result of new information, future events or otherwise. All forward-looking statements are qualified in their entirety by this cautionary statement. This caution is made under the safe harbor provisions of the Private Securities Litigation Reform Act of 1995. Investors Richard Vincent Chief Financial Officer 858-434-1113 rvincent@oncternal.com Media Corey Davis LifeSci Advisors 212-915-2577 cdavis@lifesciadvisors.com