Cebranopadol hemicitrate

背景介绍（摘自专利WO2026103742 A1） Cebranopadol(西博帕多)能够激活阿片受体(尤其是-μ阿片受体，即 MOR)和/或孤啡肽(nociceptin/orphanin FQ，即 NOP)受体，从而产生广谱镇痛效果。其中，阿片受体的激活可有效抑制痛觉传导，带来显著镇痛效果;孤啡肽的激活则有助于降低成瘾性和耐受性。 与传统阿片类药物相比，Cebranopadol据信有望在癌性疼痛、神经病理性疼痛等急慢性疼痛的治疗中展现出优势，特别是预期可适用于对阿片类药物耐受或疗效不佳的患者。目前Cebranopadol仍在Ⅲ期临床研究中，尽管其具有较好的镇痛效果，但其代谢过程中产生的某些代谢产物可能引发恶心、呕吐、头晕、嗜睡等不良反应，尤其在敏感患者中更为明显。因此进一步改善 Cebranopadol的镇痛活性以及代谢特性，例如具有更加优异的安全窗和透脑效果等，延长半衰期，减少用药频率，降低不良反应，成为该领域具有重要临床价值的技术问题。 恩华专利WO2026103742 A1通过氘代对西博帕多进行了专利突破，结构如下。 中国科学院人才交流开发中心举办 “人工智能赋能药物研发全流程应用与工具实操” 高级研修班

→ It didn’t take long for Natalie Holles to rebound after the decision to wind down operations at her previous company. She has replaced Elisabet de los Pinos as CEO of Aura Biosciences , which is investigating belzupacap sarotalocan (or bel-sar ) in early choroidal melanoma. Aura indicated that it wanted to enroll 100 patients for the Phase 3 CoMpass study, and the Boston biotech says it has signed up 86 patients so far. Holles ran Audentes Therapeutics after it was purchased by Astellas and subsequently known as Astellas Gene Therapies . The company and the field itself were severely rattled by the deaths of four patients in a trial for a rare disease called X-linked myotubular myopathy. Holles launched Third Harmonic Bio in 2022 with a $105 million Series B in addition to a previously undisclosed $50 million Series A, and when nobody else dared, Third Harmonic went public six months later. But in April 2025, the biotech said it would close and sell its lead program THB335 . Holles has also jumped to the board of directors at LeonaBio , along with Fred Callori and ex- Merus COO Peter Silverman . She currently chairs the board at Renasant Bio , a kidney health biotech that raised $54.5 million in a seed round last year. → Former Celgene boss Mark Alles has handed over CEO duties to Aran Maree at Los Angeles-based ADC maker TORL BioTherapeutics . Alles will still chair the board at TORL, which has promoted Christine Loggins to COO and Steve Ritland to CSO this year while bringing in Vince Ruiz as general counsel. Maree had multiple roles over an 18-year period at J&J before taking the CMO job at TORL in October 2024. TORL has corralled more than $450 million in financing, including a $96 million Series C in October 2025 that fell short of its earlier rounds. → Pfizer has poached an obesity expert from Novo Nordisk . Rahul Ganguly has taken the role of VP and US obesity medical lead at the US giant, according to a post on LinkedIn, and will doubtless help guide development of the obesity programs Pfizer obtained when it bought Metsera last year — beating Novo to the prize . Ganguly left Novo at the end of last year, having spent over a decade at the Danish company. He initially oversaw health economic strategy for Novo’s diabetes and obesity operations, and rose to become VP of cardiovascular and emerging therapy areas. Before that, he spent 11 years at GSK . → Former Novo Nordisk exec Camilla Sylvest is on the verge of clinching a spot on the board of directors at another one of its competitors. She’s slated to become the newest board member at Zealand Pharma , which said last week that it saw comparable weight loss to Wegovy with its Boehringer Ingelheim -partnered obesity med survodutide in a Phase 3 trial. Sylvest had been EVP, commercial strategy and corporate affairs before she ended a 29-year career with Novo in April 2025. She also sits on the board at argenx , and she emphasized in a LinkedIn post that she would concentrate solely on these types of roles for the next two to three years. → The president of Merck ’s manufacturing division announced his retirement in a lengthy LinkedIn post . Sanat Chattopadhyay spent the last decade in this position, and 27-year Merck vet Dave Maraldo will take his place. Chattopadhyay came to Merck in 2009. “Together, we helped shape some of the company’s most defining chapters: transforming our vaccines operations, launching Keytruda in record time and scaling it up to be the largest monoclonal antibody ever produced for an acute care product, as well as expanding our global biologics and vaccines capabilities to reach more patients around the world,” Chattopadhyay wrote, adding, “We created a resilient manufacturing and supply network designed not just for today, but for the patients who will depend on it for decades to come.” → Astellas has found its new chief strategy officer after Adam Pearson stepped down in March. Takahiko Iwaya previously held a number of roles across Japan’s Ministry of Health, Labour and Welfare, J&J and Sanofi . He is currently president of Sanofi Japan and also chairs the European Federation of Pharmaceutical Industries and Associations in Japan. He is scheduled to step down from both roles in June. Pearson had joined Astellas in 2004, climbing to chief strategy officer in 2023. He led Astellas’ buyout of Iveric Bio that gave it the eye drug Izervay . In the interim, Astellas’ head of corporate strategy Peter Sandor has been serving as chief strategy officer. → This is Nathan Jorgensen ’s last day as CFO of Voyager Therapeutics , according to an SEC filing . It’s the second major resignation at Voyager in the last several months after medical chief Toby Ferguson packed his bags. Ferguson’s LinkedIn page says that he’s the new SVP of the neuroscience therapeutic area at Alnylam . The RNAi pioneer has several neuro candidates in its pipeline, including mivelsiran for Alzheimer’s and ALN-HTT02 for Huntington’s disease. Like Ferguson, Jorgensen is resigning less than two years into his tenure. → Christopher Missling has been fired as CEO of New York-based neuro biotech Anavex Life Sciences , and senior advisor Terrie Kellmeyer has stepped in as interim chief. An SEC filing says that Missling was terminated “for cause” due to “conduct that the Special Committee believed was inconsistent with company policy.” Last year around this time, Peer Review told you that Kellmeyer had joined Aardvark Therapeutics as SVP of regulatory affairs after a stint with Anavex as SVP of clinical development. Anavex has drawn criticism for altering the primary endpoints in a topline readout for its Alzheimer’s drug blarcamesine in 2022. Undeterred, Anavex said in March that it’s sent more data to the FDA to boost its NDA chances. → Halozyme Therapeutics , the drug delivery technology company , has tapped one of its partner’s executives to become its next CFO. J&J’s head of IR Darren Snellgrove will get started on June 8. Halozyme has worked with J&J for years, helping the healthcare giant deliver Darzalex Faspro under the skin, broadening its use beyond the original injectable formulation. Snellgrove was succeeded by Ryan Koors on Thursday. Koors was previously CFO for J&J Innovative Medicine ’s global R&D. → We know where Stefan Irion is headed after we told you about his departure from BlueRock Therapeutics last week. He has succeeded co-founder Alex Ng as CSO of GC Therapeutics , a stem cell startup from the lab of George Church (hence the name) that broke cover in September 2024 with $75 million in financing. Ng will still be part of the team as chief innovation officer. “Cell therapy’s first generation proved engineered cells can durably treat disease. The next generation has to do something more ambitious: not just replace cells, but reprogram sick and aged cells into young, healthy ones and reach far more patients than today’s approaches allow,” Irion wrote on LinkedIn . “That’s exactly what drew me to GCT.” → Doretta Mistras is leaving after two years as CFO of Viatris , and chief accounting officer/corporate controller Paul Campbell is taking over . Campbell was with Mylan for 18 years before the merger with Upjohn to create Viatris. The generics giant posted Q1 results on Thursday that beat consensus estimates, and shares $VTRS hit a 52-week high. → Just a dream and the wind to carry him : Flagship ’s circular RNA startup Sail Biomedicines has recruited Gene Marcantonio as CMO. Marcantonio ran what’s now known as Rycarma Therapeutics from 2022-24 after nearly five years as the Forbion -backed biotech’s president and CMO. During a decade at Merck, he was promoted to associate VP, translational lead for infectious diseases, vaccines and immunology. → California cell therapy maker Kyverna Therapeutics has another new executive, naming Nadia Dac as its chief commercial officer. Dac started Monday, as the biotech seeks the first treatment approval for stiff person syndrome . She joined from the same post at Omeros , where she led the launch of a treatment for a stem cell transplant-associated condition. Prior to that, she also led the market entry of migraine prevention drug Vyepti at Alder BioPharmaceuticals . → MBX Biosciences has also hired a chief commercial officer as it gears up for Phase 3 studies of its hypoparathyroidism drug. Mark Soued spent 20 years with Pfizer before he moved over to Alnylam as head of global commercial. He had been head of US for Yvonne Greenstreet ’s crew since March 2024. MBX’s stock $MBX doubled in September 2025, when it disclosed positive Phase 2 data for canvuparatide . → Diagonal Therapeutics is turning to a recent M&A finance whiz to lead its growth. Jonathan Piazza helped lead Orbital Therapeutics to an exit to Bristol Myers Squibb and is quickly picking up another CFO role. Diagonal noted his quarter-century of experience in “company building, strategic finance, capital markets and M&A.” He joins with a recently bolstered balance sheet, thanks to a $125 million Series B for its rare bleeding disorder drug that will be tested in additional indications down the road. → The DNA damage response experts at Artios Pharma have selected Jeremy Fitch as CBO, Michael Alrutz as general counsel, and Guy Ruble as VP, regulatory affairs. Fitch joined Eli Lilly in 1992, and he just finished his career at the Indianapolis pharma with a year as VP, corporate business development transactions, immunology. Alrutz is the latest newcomer from Chimerix , where he was general counsel, secretary and chief compliance officer. We mentioned in February that three other senior leaders followed Artios CEO Mike Andriole from Chimerix. And Ruble is a 22-year Lilly vet who had the same job title at Iovance Biotherapeutics . → OncoNano CEO Kartik Krishnan has stepped down to take the CMO post at Miami-based Pasithea Therapeutics . Krishnan was elevated to the top spot in 2024, and OncoNano formed an alliance with Gilead at the start of this year that could be worth as much as $300 million. He’s also been CMO of Gilead’s longtime partner Arcus Biosciences from 2019-22. Krishnan will draw upon his knowledge of MEK inhibitors as Pasithea’s lead program PAS-004 goes through early-stage testing. His big project at Genentech was a MEK inhibitor called cobimetinib that was approved in 2015 and marketed as Cotellic . → Robert Blaustein has been named CMO at Immutrin , a Cambridge, UK-based amyloidosis biotech that recently captured an $87 million Series A from Frazier Life Sciences , SR One and others. Blaustein had a 15-year run at Merck, working his way up to associate VP and section head for atherosclerosis. In January 2025, we informed you about his appointment as chief development officer at Edgewise Therapeutics . → Tenax Therapeutics has welcomed a new chief commercial officer after the appointment of CFO Thomas Staab last month. AbbVie vet Timothy Healey ran the commercial team at Eversana Life Science Services for six years and was SVP, commercial for Lantheus . → Tris Pharma has promoted Jim Potenziano to chief science and development officer. Potenziano had served as VP, medical science and information, and was described in a press release as “the ideal leader to bring together the full breadth of Tris’ capabilities” by CEO Ketan Mehta . An NDA is on the horizon for Tris’ acute pain drug cebranopadol . → Spruce Biosciences has lined up Brian Walls as VP, market access, and Darren Johnson as VP, commercial operations. They held the same positions at Applied Therapeutics , which was foiled by a CRL for its galactosemia drug and would later be acquired by Cycle Pharma . They also worked together at Reata Pharmaceuticals until Biogen bought the Skyclarys maker for more than $7 billion. Spruce is developing a therapy for Sanfilippo syndrome type B and hopes to submit a BLA by the fourth quarter. → Jeito Capital is padding its leadership team. Fresh off a $1.2 billion sophomore fund , the Paris-based firm is now strengthening its BD and IR functions along with its talent oversight. Former Blackstone Life Sciences deputy operating chief Elaine Caughey has joined Jeito as partner of BD and IR. Meanwhile, former Oxford Science Enterprises chief talent officer Sarah Shackelton is becoming partner of talent at the Rafaèle Tordjman -led biotech investment fund. The partners will work with portfolio companies on business development and leadership and board development, respectively. → Tim Walbert has racked up multiple board appointments since orchestrating one of the largest drugmaker M&A deals of the past five years, but the former Horizon Therapeutics CEO still hasn’t outlined a full-time executive role at a biopharma. Instead, he’s continuing to line up more advisory positions. Patient Square Capital is his next destination. “We have known Tim for a long time and believe that his depth of experience will be an exceptional resource to our team and our portfolio companies as we expand our investment activities in the therapeutics sector,” Patient Square managing partner Jim Momtazee said in a press release . Walbert has taken his industry chops to the boards of Mirum Pharmaceuticals , Latigo Biotherapeutics , BioMarin and others. → CAR-T innovator Carl June leads a cast of characters that will help out Legend Biotech as scientific advisors. Georg Schett , Renier Brentjens , Ottimo Pharma ’s Spencer Fisk , Maximilian Konig and Anthony Polverino are also involved. “These advisors bring an exceptional breadth of experience that will help guide our scientific priorities and identify new opportunities for innovation,” Legend CEO Ying Huang said in a statement . → Cancer biotech Actuate Therapeutics has added Martin Huber to its board of directors. Huber became CEO of Mersana Therapeutics at a time when the biotech hit a particularly rough patch with patient deaths and clinical failures . He then sold Mersana to Day One Biopharmaceuticals , which was scooped up by Servier for $2.5 billion. Elizabeth Cairns and Lei Lei Wu also contributed to this edition.