NEW YORK--(BUSINESS WIRE)--Inspirna, Inc., a clinical stage biopharmaceutical company developing first-in-class cancer therapeutics, announced today a licensing agreement with Merck KGaA, Darmstadt, Germany, for ompenaclid (RGX-202), a first-in-class oral inhibitor of the creatine transport channel SLC6A8, currently in development for RAS mutated (RASm) second-line (2L) advanced or metastatic colorectal cancer (mCRC) and SLC6a8 targeting follow-on compounds..

纽约--（商业新闻短讯）--Inspirna，Inc.，一家开发一流癌症治疗药物的临床阶段生物制药公司，今天宣布与德国达姆施塔特的默克KGaA就肌酸转运通道SLC6A8的一流口服抑制剂ompenaclid（RGX-202）达成许可协议，目前正在开发RAS突变（RASm）二线（2L）晚期或转移性结直肠癌（mCRC）和SLC6a8靶向后续化合物。。

“We are excited to partner with Merck KGaA, Darmstadt, Germany, a leader in the oncology field with global drug development and commercial expertise in colorectal cancer specifically, to help bring our novel therapies to more patients in need,” said Dr. Usman “Oz” Azam, M.D., Chief Executive Officer of Inspirna.

Inspirna首席执行官Usman“Oz”Azam博士说：“我们很高兴与德国达姆施塔特的默克KGaA合作，默克KGaA是肿瘤学领域的领导者，拥有全球药物开发和结肠直肠癌商业专业知识，可以帮助将我们的新疗法带给更多需要的患者。”。

“The data to date validates our belief in ompenaclid as a potential first-in-class therapy for advanced colorectal cancer and underscores the power of our proprietary target discovery platform RNA-DRIVEr™. We look forward to working closely with Merck KGaA, Darmstadt, Germany, as we continue to evaluate ompenaclid in a Phase 2 randomized controlled trial.”.

“迄今为止的数据证实了我们对ompenaclid作为晚期结直肠癌潜在的一流疗法的信念，并强调了我们专有的靶标发现平台RNA驱动程序的强大功能™. 我们期待着与德国达姆施塔特的默克公司（Merck KGaA）密切合作，因为我们将继续在2期随机对照试验中评估ompenaclid。”。

“Over the past decade, the treatment paradigm for patients with RAS-mutated CRC, accounting for approximately 45% of second-line population, has not seen major innovation,” said Victoria Zazulina, M.D., Head, Development Unit, Oncology for the Healthcare business of Merck KGaA, Darmstadt, Germany. “With our expertise in the treatment of CRC, and based on the encouraging early data for ompenaclid, this agreement with Inspirna offers the opportunity to advance a potential new first-in-class therapy that may improve outcomes for patients.”.

“在过去的十年中，RAS突变CRC患者的治疗模式（约占二线人群的45%）尚未出现重大创新，”德国达姆施塔特默克公司医疗保健业务肿瘤学发展部门负责人维多利亚·扎祖利纳（Victoria Zazulina）说。“凭借我们在CRC治疗方面的专业知识，并基于ompenaclid令人鼓舞的早期数据，与Inspirna的这项协议提供了机会，可以推进一种潜在的新的一流治疗方法，从而改善患者的预后。”。

Under the terms of the license agreement, Merck KGaA, Darmstadt, Germany will receive an exclusive license to ompenaclid outside of the United States and an option to co-develop and co-promote ompenaclid in the US. Furthermore, the parties agreed to collaborate on Inspirna’s SLC6A8 follow-on compounds for which Inspirna will retain US co-development and co-commercialization rights.

根据许可协议的条款，德国达姆施塔特的默克KGaA将获得美国境外ompenaclid的独家许可，以及在美国共同开发和共同推广ompenaclid的选择权。此外，双方同意就Inspirna的SLC6A8后续化合物进行合作，Inspirna将保留美国的共同开发和共同商业化权利。

Inspirna will receive an upfront payment of $45 million. Upon the achievement of certain development and sales milestones for ompenaclid, Inspirna is eligible to receive milestone payments with tiered royalty rates in the low teens on net sales outside of the US. Inspirna is eligible to also receive development, regulatory and sales milestone payments for each follow-on compound targeting SLC6A8 along with up to double-digit royalties on net sales outside of the US..

Inspirna将获得4500万美元的预付款。在完成ompenaclid的某些开发和销售里程碑后，Inspirna有资格获得里程碑付款，其在美国以外净销售额中的分层版税率为低青少年。Inspirna也有资格获得开发，针对SLC6A8的每个后续化合物的监管和销售里程碑付款，以及美国以外净销售额的高达两位数的版税。。

Inspirna most recently presented clinical data from the Phase 1b/2 study of ompenaclid in combination with FOLFIRI and bevacizumab at the European Society for Medical Oncology (ESMO) Congress in October 2023. Results as of the September 18, 2023 data cutoff showed encouraging efficacy and safety data, including a median progression-free survival of 10.2 months and median overall survival of 19.1 months across all 41 patients with 2L RASm mCRC.

Inspirna最近于2023年10月在欧洲肿瘤内科学会（ESMO）大会上提交了来自ompenaclid联合FOLFIRI和贝伐单抗的1b/2期研究的临床数据。结果截至2023年9月18日，数据截止显示令人鼓舞的疗效和安全性数据，包括所有41例2L RASm mCRC患者的中位无进展生存期为10.2个月，中位总生存期为19.1个月。

Of the 30 evaluable patients for response, the objective response rate was 37%, with 11 partial responses. Ompenaclid was well-tolerated, with no dose-limiting toxicities observed in the dose-escalation cohort and combination safety profile comparable to FOLFIRI plus bevacizumab backbone treatment..

在30名可评估的患者中，客观缓解率为37%，其中11名部分缓解。Ompenaclid耐受性良好，在剂量递增队列中未观察到剂量限制性毒性，联合安全性与FOLFIRI加贝伐单抗骨架治疗相当。。

Inspirna has initiated a Phase 2 double-blind randomized controlled trial in 2L RAS mutant advanced or metastatic mCRC comparing ompenaclid versus placebo plus FOLFIRI and bevacizumab.

Inspirna已经在2L RAS突变晚期或转移性mCRC中启动了一项2期双盲随机对照试验，比较了ompenaclid与安慰剂加FOLFIRI和贝伐单抗。

About Inspirna

关于Inspirna

Inspirna, Inc., is a privately-held clinical-stage biopharmaceutical company focused on the discovery and development of novel cancer drugs that target key pathways in cancers of high unmet need. The company is pursuing several first-in-class drug candidates. Inspirna’s lead drug candidate, ompenaclid (RGX-202), is an orally-administered small molecule that targets the CKB/SLC6A8 pathway.

Inspirna，Inc.是一家私营临床阶段生物制药公司，专注于发现和开发新型癌症药物，这些药物针对高度未满足需求的癌症的关键途径。该公司正在寻找几名一流的候选药物。Inspirna的主要候选药物ompenaclid（RGX-202）是一种口服小分子，靶向CKB/SLC6A8途径。

This pathway becomes activated in the tumors of select patients where it enables the generation of the energy molecule ATP in response to tumor hypoxia. Ompenaclid is currently being tested in multiple mid stage clinical trials in patients with advanced or metastatic RAS mutant colorectal cancer..

该途径在选定患者的肿瘤中被激活，从而能够响应肿瘤缺氧产生能量分子ATP。Ompenaclid目前正在对晚期或转移性RAS突变型结直肠癌患者进行多项中期临床试验。。

Inspirna’s second clinical stage drug candidate, abequolixron (RGX-104), is an oral small molecule activator of LXR/APOE that inhibits angiogenesis and tumor myeloid derived suppressor cells to enhance the immune response against tumors. Abequolixron is currently being tested in a Phase 1b/2 clinical trial in patients with advanced or metastatic lung cancer in combination with docetaxel and endometrial cancer in combination with ipilimumab through a clinical collaboration with Bristol Myers Squibb..

Inspirna的第二临床阶段候选药物abequolixron（RGX-104）是LXR/APOE的口服小分子激活剂，可抑制血管生成和肿瘤骨髓来源的抑制细胞，以增强对肿瘤的免疫应答。Abequolixron目前正在与百时美施贵宝（Bristol-Myers Squibb）进行临床合作，对晚期或转移性肺癌患者联合多西紫杉醇和子宫内膜癌联合ipilimumab进行1b/2期临床试验。。

Inspirna identifies novel cancer targets using its microRNA-based target discovery platform, RNA-DRIVEr, which was originally developed by Inspirna’s scientific co-founders at The Rockefeller University and exclusively licensed to Inspirna. The Company brings together distinguished scientific founders, a seasoned board of directors, and a leadership team comprised of experienced drug developers.

Inspirna使用其基于microRNA的靶标发现平台RNA驱动程序识别新的癌症靶标，该平台最初由洛克菲勒大学Inspirna的科学联合创始人开发，并独家授权给Inspirna。该公司汇集了杰出的科学创始人，经验丰富的董事会以及由经验丰富的药物开发人员组成的领导团队。

The Company is funded by leading biotechnology investors, including Novo Holdings A/S, Sofinnova Partners, Sands Capital, Vivo Capital, Lepu Holdings Limited, Sixty Degree Capital, Silicon Valley Bank, K2 HealthVentures, Oceanpine Capital, WuXi PharmaTech Healthcare Fund I, LP, Alexandria Venture Investments, LLC, Dreavent 6, Exor Seeds, and the Partnership Fund for New York City.

该公司由领先的生物技术投资者资助，包括Novo Holdings A/S，Sofinnova Partners，Sands Capital，Vivo Capital，Lepu Holdings Limited，Sixty Degree Capital，硅谷银行，K2 HealthVentures，Oceanpine Capital，无锡PharmaTech Healthcare Fund I，LP，Alexandria Venture Investments，LLC，Dreavent 6，Exor Seeds和纽约市合伙基金。

For more information, please visit https://inspirna.com/..

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