Cebranopadol hemicitrate

Cebranopadol is an investigational first-of-its kind dual NOP/MOP receptor (NMR) agonist which uses a novel approach of activating NOP and MOP receptors to work synergistically to modulate pain In both ALLEVIATE trials cebranopadol demonstrates significant and sustained pain reduction with a differentiated safety pro abdominoplasty and bunionectomy Human abuse-potential studies showing cebranopadol is l ess abusable than oxycodone and tramadol, further support its potential to offer strong pain relief with an improved safety profile MONMOUTH JUNCTION, N.J., March 06, 2026 (GLOBE NEWSWIRE) -- Tris Pharma, Inc. (Tris), a commercial-stage biopharmaceutical company, today announced debut data from its Phase 3 ALLEVIATE-1 and ALLEVIATE-2 studies evaluating the safety and efficacy of cebranopadol, an investigational therapy, for the treatment of moderate-to-severe acute pain in patients following abdominoplasty and bunionectomy surgery, respectively, at the American Academy of Pain Medicine (AAPM) 2026 PainConnect annual meeting. The debut abstract titled, “Results of ALLEVIATE-1 and ALLEVIATE-2 Phase 3 Trials of Cebranopadol, a First-in-Class, Dual NOP/MOP Receptor Agonist for the Treatment of Acute Pain After Abdominoplasty and Bunionectomy,” was presented by Dr. Todd Bertoch, MD, Chief Medical Officer of CenExel Clinical Research, and Principal Investigator on ALLEVIATE-2. “As pain specialists, we often see how inadequately controlled acute pain can linger long after surgery or injury,” said Dr. Todd Bertoch. “If we don’t get ahead of severe pain early, it can become chronic and much harder to treat. These Phase 3 results underscore the potential of cebranopadol to redefine the standard of care for acute pain management.” Cebranopadol is an investigational, first-in-class dual nociceptin/orphanin FQ peptide (NOP) and μ-opioid peptide (MOP) receptor agonist (dual-NMR agonist). By simultaneously activating both receptors, cebranopadol is designed to provide potent analgesia while potentially mitigating many of the risks traditionally associated with preferential MOP agonists. ALLEVIATE-1 clinical trial ( NCT06545097 ) is a Phase 3 multicenter, randomized, double-blind, placebo-controlled study. It enrolled 303 patients undergoing abdominoplasty surgery without liposuction or other collateral procedures across four U.S. sites. Eligible participants were randomized in a 1:1:1 ratio to cebranopadol 400 µg on Days 1 and 2, cebranopadol 400 µg on Day 1 and 200 µg on Day 2 or placebo all administered once daily. The first dose was administered approximately 1 hour prior to abdominoplasty and the second dose approximately 24 hours later. ALLEVIATE-2 clinical trial ( NCT06423703 ) is a Phase 3 multicenter, randomized, double-blind, placebo-and active controlled study. It enrolled 242 patients undergoing unilateral bunionectomy with first metatarsal osteotomy across ten U.S. sites. Eligible participants were randomized in a 1:1:1 ratio to a cebranopadol 400 µg, oxycodone immediate release (IR) 10 mg or placebo. Cebranopadol was administered once daily on Days 1, 2, and 3; placebo was administered at 6, 12, and 18 hours to maintain blinding. Oxycodone 10 mg and placebo were administered every 6 hours. Baseline Demographics and Allocation: In the abdominoplasty study, 303 participants were randomized to treatment at four sites in the U.S., and 292 (96.4%) completed the study. Eleven participants discontinued the study due to adverse events (AEs) (3), lost to follow-up (2), withdrawal of consent (3), and other (3). In the bunionectomy study, 242 participants were enrolled at 10 locations in the Unites States, and 236 (97.5%) completed the study. One participant was discontinued in the oxycodone group for hypersensitivity, which was considered a severe and serious AE. No other participants discontinued or experienced a severe or serious AE. Across the two trials, baseline characteristics were similar among groups. More participants in the abdominoplasty study had a history of substance abuse. Efficacy and Safety Results The primary endpoints in both trials were met, demonstrating an acceptable benefit-risk pro cebranopadol for the treatment of acute pain following abdominoplasty and bunionectomy: In ALLEVIATE-1, the average total pain score area under the curve (AUC 4-48) for patients dosed with 400 µg cebranopadol was significantly less than placebo (LS mean difference 59.2; SE 10.14; p<0.001). In ALLEVIATE-2, the average total pain score area under the curve (AUC 2-48) for patients dosed with cebranopadol was significantly less than placebo (LS mean difference 56.1; SE 13.49; p<0.001) Following abdominoplasty, a significantly greater proportion of patients receiving cebranopadol 400 µg required no opioid rescue medication compared with those receiving placebo (34.7% vs 9.9%; p<0.001). Following bunionectomy, a significantly higher proportion of patients receiving cebranopadol 400 µg required no opioid rescue medication compared with those receiving placebo (57.5% vs 28.4%; p=0.006) Cebranopadol was generally well tolerated and exhibited a favorable safety profile. Nausea was the most common AE across study groups with exception of placebo group in the bunionectomy study. Other AEs included vomiting, constipation, headache, dizziness, hypertension and pruritus. Ketan Mehta, founder and CEO at Tris Pharma added, “Acute postoperative pain remains a significant clinical challenge, and the standard of care has serious associated risks. With our first-in-class dual NOP/MOP receptor agonist, we are taking a fundamentally new approach to pain relief, one that simultaneously targets two distinct pathways of pain modulation to deliver meaningful pain relief with a reduced risk of side effects associated with preferential MOP agonists. These data validate this mechanism of action and reinforce the potential of cebranopadol to address a critical need for safe and effective treatment options.” About Acute Pain Approximately 80 million adults in the U.S. are treated for acute pain every year 1,2 . Acute pain can be caused by injury, invasive surgery, illness, major trauma and burns. It can last up to three months and typically resolves once the underlying cause is treated or healed. Moderate-to-severe acute pain can often only be effectively treated with opioid analgesics, which, while effective, are associated with risks including respiratory depression, tolerance, dependence, misuse, and overdose. However, undertreating severe pain in the immediate period after onset can increase the risk of a patient developing chronic pain 3,4 . About Cebranopadol Cebranopadol is a first-in-class investigational therapy that targets two key receptors, the nociceptin/orphanin FQ peptide (NOP) and µ-opioid peptide (MOP) receptors (a dual-NMR agonist), for the treatment of moderate-to-severe pain, as well as opioid use disorder (OUD). These receptors are partially homologous to each other, and they play both complementary and distinct roles to modulate pain biology pathways. Studied in over 33 clinical trials in more than 2,200 subjects, cebranopadol’s pro been well characterized in pain management studies. It has demonstrated positive clinical results in acute pain, chronic pain, and diabetic neuropathic pain with a favorable safety profile. The FDA granted Fast Track Designation to cebranopadol for chronic low back pain, and if approved, it could become the first dual-NMR pain-relief therapy with the potential to provide efficacy equivalent to selective MOP agonists such as oxycodone with less risk of misuse or physical dependence, addiction or overdose.  Cebranopadol’s novel mechanism of action has potential in treating patients with substance use disorders (SUDs). Tris plans to continue to evaluate cebranopadol’s potential to help patients break the cycle of opioid addiction.  The National Institute on Drug Abuse (NIDA), part of the National Institutes of Health (NIH), has awarded Tris a five-year grant of up to $16.6 million to study cebranopadol’s potential to treat OUDs and SUDs.  About Tris Pharma Tris Pharma is a privately held, innovation-driven biopharmaceutical company that is applying its drug development capabilities and proprietary technologies to transform the treatment of ADHD, pain, addiction and disorders of the central nervous system. Tris markets a portfolio of best-in-class ADHD products and is developing a promising pipeline of differentiated near-term drug candidates. More information is available at  and on LinkedIn  @TrisPharma .  Media Contact Jonathan Pappas  LifeSci Communication  jpappas@lifescicomms.com Company Contact Cheryl Patnick  Tris Pharma, Inc.  cpatnick@trispharma.com ________________________ Banerjee S, Argaez C. Multidisciplinary Treatment Programs for Patients with Acute or Subacute Pain: A Review of Clinical Effectiveness, Cost-Effectiveness, and Guidelines [Internet]. Canadian Agency for Drugs and Technologies in Health. 2019 May 7; PMID: 31498579 Lopez A, Menzie AM, Kenderes M, Rubin JL. A real-world database analysis of the prevalence of pain medication use in the United States. PAIN Reports. 2026 February; DOI: 10.1097/PR9.0000000000001396 McGreevy K, Bottros MM, Raja SN. Preventing Chronic Pain following Acute Pain: Risk Factors, Preventive Strategies, and their Efficacy. European Journal of Pain Supplements. 2012 Nov 11; PMID: 22102847 Sinatra, R. (2010). “Causes and Consequences of Inadequate Management of Acute Pain.” Pain Medicine, 11(12), 1859–1871. doi:10.1111/j.1526-4637.2010.00983.x

1、研究进展：艾伯维生物制药（非积极）、Forest Laboratories（非积极）、阿特维斯制药公司（非积极）、格兰泰、Assertio Therapeutics、Tris Pharma 2、别名：GRT-6005、TRN-228、西博帕多、塞雷帕多、PRK-101、cebranopadolum 3、靶点：DOR、KOR、MOR、NOP 4、剂型及给药途径：普通胶囊剂; 口服给药；口服溶液剂; 口服给药；普通片剂; 口服给药；鼻用制剂(剂型未知); 鼻腔给药 5、结构式： （推测） 6、适应症及进展 适应症 进展 最新进展日期 术后疼痛 III期 2025-08-28 急性疼痛 III期 2026-01-09 疼痛 II期 2025-06-12 阿片成瘾 I期 2025-09-06 7、交易： 交易名称 交易类型 转让方 受让方 交易时研发状态 权益类型 权益地区 权益适应症 交易金额 交易时间 Tris Pharma® Announces Acquisition of Park Therapeutics – Pain Company with First-in-class, Phase III-Ready New Chemical Entity (NCE) 转让/收购 Park Therapeutics Tris Pharma 临床III期 开发/商业化权 全球 2021-04-29 Depomed Announces Closing of Acquisition of U.S. Rights to Cebranopadol From Grunenthal 授权/许可 格兰泰 Assertio Therapeutics 临床III期 开发/商业化权 美国，其他 2015-12-30 Grünenthal Announces Termination of License Agreement with Actavis for the Development of Cebranopadol as of October 1, 2014交易终止 授权/许可 格兰泰 Forest Laboratories 临床III期 开发/商业化权 美国，其他 2014-12-01 Actavis' subsidiary Forest Laboratories Ireland Limited and Grünenthal GmbH had entered into a license agreement on Cebranopadol in December 2010. 授权/许可 格兰泰 Forest Laboratories 临床III期 开发/商业化权 美国，其他 2010-12-01 The NCE cebranopadol has been granted Fast Track status by the FDA and was initially developed by Grünenthal, a German company which specializes in pain. 授权/许可 格兰泰 Park Therapeutics 临床III期 开发/商业化权 全球 8、专利布局 公开（公告）号 专利主题 发明名称 申请日 法律状态 CN100577664C 化合物 螺环环己烷衍生物 2003-11-05 期限届满 CN103179953A 制剂 含6’-氟-(N-甲基-或N,N-二甲基-)-4-苯基-4’,9’-二氢-3’H-螺[环己烷-1,1’-吡喃并[3,4,B]吲哚]-4-胺的药物剂型 2011-08-04 驳回 CN103649094B 晶型 晶态的(1r,4r)‑6'‑氟‑n,n‑二甲基‑4‑苯基‑4',9'‑二氢‑3'h‑螺[环己烷‑1,1'‑吡喃并[3,4,b]吲哚]‑4‑胺 2012-07-06 CN104105699B 晶型 (1r,4r)-6'-氟-n,n-二甲基-4-苯基-4',9'-二氢-3'h-螺[环己烷-1,1'-吡喃并[3,4,b]吲哚]-4-胺盐酸盐的固体形式 2012-12-11 CN104168897B 用途 用于治疗纤维肌痛和慢性疲劳综合征的(1r,4r)-6'-氟-(n-甲基-或n,n-二甲基-)-4-苯基-4',9'-二氢-3'h-螺-[环己烷-1,1'-吡喃并[3,4,b]吲哚]-4-胺 2013-02-01 CN108524498A 制剂 药物组合物 2013-05-16 视为撤回 CN104302282A 制剂 包含(1r,4r)-6’-氟-N,N-二甲基-4-苯基-4’,9’-二氢-3’H-螺[环己烷-1,1’-吡喃并-[3,4,b]吲哚]-4-胺和对乙酰氨基酚或丙帕他莫的药物组合物 2013-05-16 驳回 CN118286209A 用途 西博帕多的滴定 2017-02-28 实质审查 CN109069483A 用途 西博帕多的滴定 2017-02-28 驳回 CN104271131A 制剂 包含(1r,4r)-6’-氟-N,N-二甲基-4-苯基-4’,9’-二氢-3’H-螺[环己烷-1,1’-吡喃并[3,4,b]吲哚]-4-胺和抗抑郁药的药物组合物 2013-05-16 驳回 CN107427493A 用途 用于治疗肝功能受损和/或肾功能受损的受试者的疼痛的cebranopadol 2016-01-22 视为撤回 CN106255680B 制备工艺 制备5-氟色醇的方法 2015-02-26 CN103260610A 用途 治疗伤害性疼痛的含6’-氟-(N-甲基-或N,N-二甲基-)-4-苯基-4’,9’-二氢-3’H-螺[环己烷-1,1’-吡喃并[3,4,b]吲哚]-4-胺的药物剂型 2011-08-04 驳回 CN104284658A 制剂 包含(1r,4r)-6’-氟-N,N-二甲基-4-苯基-4’,9’-二氢-3’H-螺[环己烷-1,1’-吡喃并[3,4,b]吲哚]-4-胺和加巴喷丁类的药物组合物 2013-05-16 驳回 CN104284661A 制剂 包含(1r,4r)-6’-氟-N,N-二甲基-4-苯基-4’,9’-二氢-3’H-螺[环己烷-1,1’-吡喃并-[3,4,b]吲哚]-4-胺和水杨酸组分的药物组合物 2013-05-16 驳回 CN108451956A 制剂 药物组合物 2013-05-16 视为撤回 CN104302288A 制剂 包含(1r,4r)-6’-氟-N,N-二甲基-4-苯基-4’,9’-二氢-3’H-螺[环己烷-1,1’-吡喃并-[3,4,b]吲哚]-4-胺和昔康类的药物组合物 2013-05-16 驳回 CN106432256B 晶型 盐酸盐的固体形式 2012-12-11 CN106939005A 晶型 晶态的（1r,4r）‑6’‑氟‑n,n‑二甲基‑4‑苯基‑4’,9’‑二氢‑3’h‑螺[环己烷‑1,1’‑吡喃并[3,4,b]吲哚]‑4‑胺 2012-07-06 视为放弃 CN103339102A 制备工艺 合成取代的氨基环己酮衍生物的方法 2011-12-07 驳回 CN103079548A 晶型 含有6’-氟-(N-甲基-或N,N-二甲基)-4-苯基-4’,9’-二氢-3’H-螺[环己烷-1,1’-吡喃并[3,4,b]吲哚]-4-胺的药物剂型 2011-08-04 实质审查 CN103153282B 制剂 含6’-氟-(N-甲基-或N,N-二甲基-)-4-苯基-4’,9’-二氢-3’H-螺[环己烷-1,1’-吡喃并[3,4,B]吲哚]-4-胺的药物剂型 2011-08-04 未缴年费 CN101693714B 化合物 螺环环己烷衍生物 2003-11-05 未缴年费 9、研究历程 2025年05月01日，由Tris Pharma Inc开展临床二期试验，用于治疗神经痛和腰痛。（https://www.trispharma.com/pipeline/） 2024年07月18日，由Tris Pharma Inc在美国开展临床三期试验，用于治疗急性疼痛。（NCT06423703; NCT06545097） 2022年07月29日，由Tris Pharma Inc在荷兰开展临床一期试验，用于治疗疼痛。（NCT05491785） 2022年03月28日，由Tris Pharma Inc在美国开展临床一期试验，用于治疗物质相关性障碍。（NCT06453265; NCT05256108） 2019年05月23日，治疗心脏病的研究暂无进展。（NCT03958123） 2018年12月04日，治疗物质相关性障碍的研究暂无进展。（NCT03757559） 2016年05月10日，治疗肿瘤、疼痛和慢性疼痛的研究终止。（NCT01964378; NCT02031432） 2015年11月05日，治疗肿瘤、疼痛和慢性疼痛的研究终止。（NCT01964378） 2015年01月30日，治疗糖尿病神经病变、糖尿病和慢性疼痛的研究暂无进展。（NCT01939366; NCT01347671; NCT00878293） 2014年07月03日，治疗膝关节炎的研究暂无进展。（NCT01709214） 2014年04月17日，治疗腰痛的研究暂无进展。（NCT01725087） 2013年10月29日，由Tris Pharma Inc在奥地利、比利时和保加利亚等国家和地区开展临床三期试验，用于治疗肿瘤、疼痛和慢性疼痛。（NCT01964378; NCT02031432） 2013年09月27日，由Tris Pharma Inc在奥地利、丹麦和法国等国家和地区开展临床二期试验，用于治疗糖尿病神经病变、糖尿病和慢性疼痛。（NCT01939366） 2013年07月10日，由Tris Pharma Inc在美国开展临床一期试验，用于治疗心脏病。（NCT03958123） 2013年04月15日，由Tris Pharma Inc在加拿大开展临床一期试验，用于治疗物质相关性障碍。（NCT03757559） 2012年12月04日，由Tris Pharma Inc在美国开展临床二期试验，用于治疗膝关节炎。（NCT01709214） 2012年11月01日，由Tris Pharma Inc在奥地利、比利时和丹麦等国家和地区开展临床二期试验，用于治疗腰痛。（NCT01725087） 2012年04月03日，治疗糖尿病神经病变的研究暂无进展。（NCT01347671） 2011年12月22日，治疗膝关节炎的研究暂无进展。（NCT01357837） 2011年05月01日，由Tris Pharma Inc在奥地利、保加利亚和德国等国家和地区开展临床二期试验，用于治疗膝关节炎、糖尿病神经病变和疼痛。（NCT01357837; NCT01347671） 2010年08月19日，治疗糖尿病神经病变的研究暂无进展。（NCT00878293） 2009年12月07日，治疗术后疼痛的研究暂无进展。（NCT00872885） 2009年04月01日，由Tris Pharma Inc在德国和英国开展临床二期试验，用于治疗糖尿病神经病变。（NCT01939366; NCT01347671; NCT00878293） 2009年03月01日，由Tris Pharma Inc在美国开展临床二期试验，用于治疗术后疼痛。（NCT00872885） 10、临床试验 登记号 试验标题 试验药 对照药 适应症 原始适应症 申办/合作机构 试验分期 开始日期 完成日期 国家/地区 NCT06545097 A Multicenter, Randomized, Double-Blind, Placebo-Controlled Study to Evaluate the Efficacy and Safety of Cebranopadol for the Treatment of Moderate to Severe Acute Pain After Full Abdominoplasty Cebranopadol hemicitrate - 急性疼痛 Acute Pain Tris Pharma, Inc. 临床3期 2024-09-03 2024-12-30 美国 NCT06453265 A Double-Blind, Randomized, Crossover Study to Assess the Abuse Potential of Intranasal Cebranopadol Compared to Oxycodone and Placebo in Healthy, Nondependent Recreational Opioid Users Cebranopadol hemicitrate (鼻腔给药) - 药物滥用 Abuse, Drug Tris Pharma, Inc. | National Institutes of Health 临床1期 2024-06-28 2024-11-06 美国 NCT06423703 A Multicenter, Randomized, Double-Blind, Placebo- and Active-Controlled Study to Evaluate the Efficacy and Safety of Cebranopadol for the Treatment of Moderate to Severe Acute Pain After Primary Unilateral Bunionectomy Cebranopadol hemicitrate 盐酸羟考酮 急性疼痛 Acute Pain Tris Pharma, Inc. 临床3期 2024-07-18 2025-01-31 美国 NCT05491785 Randomized, Double-blind, Four Period, Six-treatment, Double-dummy, Placebo Controlled, Partial-crossover Study to Explore and Compare the Ventilatory Response to Hypercapnia (VRH) of Cebranopadol, Oxycodone, and Placebo in Healthy Subjects Cebranopadol hemicitrate (片剂) 盐酸羟考酮 疼痛 | 高碳酸血症 Pain Tris Pharma, Inc. 临床1期 2022-07-29 2024-01-02 荷兰 NCT05256108 A Single-dose, Randomized, Double-blind, Placebo- and Active-controlled Crossover Trial to Evaluate the Abuse Potential of Two Doses of Cebranopadol in Adult Nondependent Recreational Opioid Users Cebranopadol hemicitrate (胶囊剂, 口服) 盐酸曲马多 | 盐酸羟考酮 - Human Abuse Potential Tris Pharma, Inc. 临床1期 2022-03-28 2022-07-12 美国 NCT03958123 Evaluation of the Effects of Multiple Therapeutic and Supratherapeutic Doses of Cebranopadol on Cardiac Repolarization in Healthy Subjects 盐酸莫西沙星 | Cebranopadol hemicitrate - - Prolonged QTc Interval | Pharmacokinetic Tris Pharma, Inc. | Forest Laboratories, Inc. 临床1期 2013-07-10 2013-11-27 美国 NCT03882762 A Non-randomized, Single-dose, Open-Label, Pharmacokinetic Study of Cebranopadol in Patients With Impaired Renal Function and Subjects With Normal Renal Function Cebranopadol hemicitrate - 肾功能不全 Pharmacokinetic Tris Pharma, Inc. | Forest Laboratories LLC 临床1期 2013-06-20 2014-09-17 美国 NCT03757559 A Single-dose, Nested-randomized, Double-blind, Double-dummy, Placebo- and Active-controlled Crossover Trial to Evaluate the Abuse Potential of 3 Doses of GRT6005 in Adult Non-dependent Recreational Opioid Users Cebranopadol hemicitrate 盐酸氢吗啡酮 药物滥用 Abuse, Drug Tris Pharma, Inc. 临床1期 2013-04-15 2014-03-08 加拿大 PER-003-14 AN OPEN-LABEL, MULTI-SITE TRIAL TO DESCRIBE THE SAFETY AND TOLERABILITY OF ORAL CEBRANOPADOL ADMINISTERED FOR 26 WEEKS IN SUBJECTS WITH CANCER-RELATED PAIN WHO HAVE COMPLETED TREATMENT IN THE KF6005/07 TRIAL. Cebranopadol hemicitrate - - -D48  Neoplasm of uncertain or unknown behaviour of other and unspecified sites Neoplasm of uncertain or unknown behaviour of other and unspecified sites | D48 | Neoplasm of uncertain or unknown behaviour of other and unspecified sites Grünenthal GmbH 临床3期 2014-01-31 - 德国 | 奥地利 | 比利时 | 保加利亚 | 克罗地亚 | 丹麦 | 斯洛伐克 | 西班牙 | 法国 | 匈牙利 | 波兰 | United Kindgdom | 罗马尼亚 | 瑞典 | 新西兰 | 塞尔维亚共和国 | 阿根廷 | 巴西 | 智利 | 墨西哥 | 秘鲁 NCT02031432 An Open-label, Multi-site Trial to Describe the Safety and Tolerability of Oral Cebranopadol Administered for 26 Weeks in Subjects With Cancer-related Pain Who Have Completed Treatment in the KF6005/07 Trial Cebranopadol hemicitrate - 癌症疼痛 | 肿瘤 | 慢性疼痛 Pain | Neoplasms | Chronic Pain Tris Pharma, Inc. 临床3期 2013-12-18 2016-05-03 奥地利 | 罗马尼亚 | 匈牙利 | 比利时 | 波兰 | 丹麦 | 斯洛伐克 | 塞尔维亚共和国 | 保加利亚 | 德国 PER-041-13 EFFICACY, SAFETY, AND TOLERABILITY OF ORAL CEBRANOPADOL VERSUS MORPHINE SULFATE PR IN SUBJECTS WITH CHRONIC MODERATE TO SEVERE PAIN RELATED TO CANCER. Cebranopadol hemicitrate - - -D48  Neoplasm of uncertain or unknown behaviour of other and unspecified sites Neoplasm of uncertain or unknown behaviour of other and unspecified sites | D48 | Neoplasm of uncertain or unknown behaviour of other and unspecified sites Grünenthal GmbH 临床3期 2013-12-02 - 德国 | 奥地利 | 比利时 | 保加利亚 | 克罗地亚 | 丹麦 | 斯洛伐克 | 西班牙 | 法国 | 荷兰 | 匈牙利 | 波兰 | United Kindgdom | 罗马尼亚 | 瑞典 | Yugoslavia | 阿根廷 | 巴西 | 智利 | 墨西哥 | 秘鲁 NCT01964378 Efficacy, Safety, and Tolerability of Oral Cebranopadol Versus Morphine Sulfate PR in Subjects With Chronic Moderate to Severe Pain Related to Cancer. Cebranopadol hemicitrate 硫酸吗啡 肿瘤 | 慢性疼痛 Pain | Neoplasms | Chronic Pain Tris Pharma, Inc. 临床3期 2013-10-29 2015-10-16 罗马尼亚 | 匈牙利 | 英国 | 西班牙 | 奥地利 | 比利时 | 波兰 | 丹麦 | 斯洛伐克 | 塞尔维亚共和国 | 智利 | 保加利亚 | 德国 | 克罗地亚 NCT01939366 Efficacy, Safety and Tolerability of Multiple Doses of Oral Cebranopadol in Subjects With Moderate to Severe Chronic Pain Due to Diabetic Peripheral Neuropathy. Cebranopadol hemicitrate 普瑞巴林 慢性疼痛 | 神经变性 | 糖尿病周围神经性疼痛 | 糖尿病周围神经病变 Chronic Pain | Diabetic Neuropathies | Diabetes Mellitus Tris Pharma, Inc. 临床2期 2013-09-27 2015-01-28 荷兰 | 奥地利 | 美国 | 丹麦 | 意大利 | 法国 | 德国 | 西班牙 NCT01725087 Efficacy, Safety, and Tolerability of GRT6005 in Subjects With Moderate to Severe Chronic Low Back Pain. Cebranopadol hemicitrate 盐酸他喷他多 腰痛 Low Back Pain Tris Pharma, Inc. | Forest Laboratories, Inc. 临床2期 2012-11-01 2014-07-01 瑞典 | 荷兰 | 奥地利 | 匈牙利 | 比利时 | 芬兰 | 波兰 | 丹麦 | 英国 | 德国 | 西班牙 NCT01709214 A Randomized, Double-Blind, Placebo- and Active Controlled Study to Evaluate the Safety and Efficacy of GRT6005 in Patients With Moderate to Severe Chronic Pain Due to Osteoarthritis of the Knee Cebranopadol hemicitrate 盐酸羟考酮 慢性疼痛 | 膝关节炎 Moderate to Severe Chronic Pain Due to Osteoarthritis of the Knee Tris Pharma, Inc. | Forest Laboratories, Inc. 临床2期 2012-12-04 2014-04-04 美国 NCT01357837 A Randomized 4 Week Phase IIa Trial Evaluating the Efficacy, Safety, and Tolerability of GRT6005, a New Centrally Acting Analgesic, in Subjects With Moderate to Severe Pain Due to Osteoarthritis (OA) of the Knee Cebranopadol hemicitrate - 疼痛 | 膝关节炎 Osteoarthritis of the Knee Tris Pharma, Inc. | Forest Laboratories, Inc. 临床2期 2011-05-01 2011-12-01 奥地利 | 波兰 | 西班牙 NCT01347671 A Randomized 4-week Phase IIa Trial Evaluating the Efficacy, Safety, and Tolerability of GRT6005, a New Centrally Acting Analgesic, in Subjects With Pain Due to Diabetic Polyneuropathy. Cebranopadol hemicitrate - 疼痛 | 糖尿病性神经病变 Pain | Diabetic Neuropathies Tris Pharma, Inc. | Forest Laboratories, Inc. 临床2期 2011-05-01 2012-01-01 罗马尼亚 | 保加利亚 | 德国 NL-OMON32792 A randomized, single center, 2-way crossover, comparator controlled Phase I trial to evaluate the effect of a new analgesic on ventilation in healthy subjects - A study to investigate the effect of GRT6005 on ventilation. Cebranopadol hemicitrate - 伤害性疼痛 pijn nociceptive pain pain Grünenthal GmbH N/A 2010-03-04 - 荷兰 NCT00878293 A Randomized Phase IIa Trial Evaluating the Safety and Efficacy of a New Centrally Acting Analgesic in Subjects With Pain Due to Diabetic Polyneuropathy Cebranopadol hemicitrate - 糖尿病周围神经性疼痛 Diabetic Polyneuropathy Tris Pharma, Inc. 临床2期 2009-04-01 2010-05-01 英国 | 德国 NCT00872885 A Randomized, Phase IIa Trial Evaluating the Safety and Efficacy of a New Centrally Acting Analgesic in Subjects With Moderate to Severe Pain Following Bunionectomy. Cebranopadol hemicitrate 硫酸吗啡 术后疼痛 Post Operative Pain Tris Pharma, Inc. 临床2期 2009-03-01 2009-10-01 美国 EUCTR2008-004794-18-DE A randomized Phase IIa trial evaluating the safety and efficacy of a new centrally acting analgesic in subjects with pain due to diabetic polyneuropathy Cebranopadol hemicitrate (口服溶液剂, 口服) 硫酸吗啡 糖尿病周围神经性疼痛 painful diabetic polyneuropathy | Diabetic polyneuropathy Grünenthal GmbH 临床2期 2009-03-30 2010-05-25 德国 11、临床结果 标题 登记号 来源 分期 适应症 评价人数 用药方案 结果 评价 发布日期 申办/合作机构 来源链接 Synapse链接 Tris touts second Phase III success for dual NMR agonist in acute pain NCT06423703 NEWS 临床3期 急性疼痛 240 CebranopadolCebranopadolCebranopadol 400 µg NRS = 223.4 Point (SE, 9.58) 达到 积极 2025-03-06 Tris Pharma, Inc. https://firstwordpharma.com/story/5940248 | https://www.trispharma.com/tris-pharma-announces-positive-results-from-alleviate-2-phase-3-pivotal-trial-for-cebranopadol-an-investigational-first-in-class-oral-dual-nmr-agonist-for-the-treatment-of-moderate-to-severe-acute-p/ https://synapse.zhihuiya.com/clinical-result-detail/a4a599ae825aa2d282dd322deea3d9e3 Tris touts second Phase III success for dual NMR agonist in acute pain NCT06423703 NEWS 临床3期 急性疼痛 240 oxycodone 10 mgoxycodone 10 mgoxycodone 10 mg NRS = 250.4 Point (SE, 9.53) 达到 积极 2025-03-06 Tris Pharma, Inc. https://firstwordpharma.com/story/5940248 | https://www.trispharma.com/tris-pharma-announces-positive-results-from-alleviate-2-phase-3-pivotal-trial-for-cebranopadol-an-investigational-first-in-class-oral-dual-nmr-agonist-for-the-treatment-of-moderate-to-severe-acute-p/ https://synapse.zhihuiya.com/clinical-result-detail/a4a599ae825aa2d282dd322deea3d9e3 Tris Pharma Announces Positive Results from ALLEVIATE-1 Phase 3 Clinical Trial of Cebranopadol, an Investigational First-in-Class Oral Dual-NMR Agonist, for the Treatment of Moderate-to-Severe Acute Pain NCT06545097 BusinessWire 临床3期 急性疼痛 - Cebranopadol 400 µg NRS: Difference (LS Mean) = -59.2, P-Value = <0.001 达到 积极 2025-01-22 Tris Pharma, Inc. https://www.businesswire.com/news/home/20250122472082/en https://synapse.zhihuiya.com/clinical-result-detail/d38a93a925e2890a2a55e8aa32283a3e Tris Pharma Announces Positive Results from ALLEVIATE-1 Phase 3 Clinical Trial of Cebranopadol, an Investigational First-in-Class Oral Dual-NMR Agonist, for the Treatment of Moderate-to-Severe Acute Pain NCT06545097 BusinessWire 临床3期 急性疼痛 - Placebo NRS: Difference (LS Mean) = -59.2, P-Value = <0.001 达到 积极 2025-01-22 Tris Pharma, Inc. https://www.businesswire.com/news/home/20250122472082/en https://synapse.zhihuiya.com/clinical-result-detail/d38a93a925e2890a2a55e8aa32283a3e Tris Pharma Presents New Clinical Data Demonstrating Robust Safety and Efficacy of Investigational, First-in-Class Therapy Cebranopadol for Treatment of Pain NCT05491785 BusinessWire 临床2期 疼痛 30 Cebranopadol respiratory depression: Difference (%) = -25 积极 2024-08-06 Tris Pharma, Inc. https://www.businesswire.com/news/home/20240805194778/en https://synapse.zhihuiya.com/clinical-result-detail/52d92ae802832ee22ea082e3e884224e Tris Pharma Presents New Clinical Data Demonstrating Robust Safety and Efficacy of Investigational, First-in-Class Therapy Cebranopadol for Treatment of Pain NCT05491785 BusinessWire 临床2期 疼痛 30 Oxycodone respiratory depression: Difference (%) = -25 积极 2024-08-06 Tris Pharma, Inc. https://www.businesswire.com/news/home/20240805194778/en https://synapse.zhihuiya.com/clinical-result-detail/52d92ae802832ee22ea082e3e884224e An Open-label, Multi-site Trial to Describe the Safety and Tolerability of Oral Cebranopadol Administered for 26 Weeks in Subjects With Cancer-related Pain Who Have Completed Treatment in the KF6005/07 Trial NCT02031432 CTgov 临床3期 癌症疼痛 | 肿瘤 | 慢性疼痛 76 Cebranopadol Number of Participants With Treatment Emergent Adverse Event (TEAEs) = 64 Pts  - 2020-01-18 Tris Pharma, Inc. https://clinicaltrials.gov/ct2/show/results/NCT02031432 https://synapse.zhihuiya.com/clinical-result-detail/9d4200a822ae095a3aee9aa0aee5d3a4 Efficacy, Safety, and Tolerability of Oral Cebranopadol Versus Morphine Sulfate PR in Subjects With Chronic Moderate to Severe Pain Related to Cancer. NCT01964378 CTgov 临床3期 肿瘤 | 慢性疼痛 200 Cebranopadol(Cebranopadol) Average Amount of Daily Rescue Medication at the End of the Maintenance Period (Per Protocol Set)(LS Mean) = 4.25 milligram(s)/24 hours  - 2019-12-30 Tris Pharma, Inc. https://clinicaltrials.gov/ct2/show/results/NCT01964378 https://synapse.zhihuiya.com/clinical-result-detail/85ae3e502e2d0eae8ee9dda5585a5e23 Efficacy, Safety, and Tolerability of Oral Cebranopadol Versus Morphine Sulfate PR in Subjects With Chronic Moderate to Severe Pain Related to Cancer. NCT01964378 CTgov 临床3期 肿瘤 | 慢性疼痛 200 Morphine Prolonged Release(Morphine Prolonged Release) Average Amount of Daily Rescue Medication at the End of the Maintenance Period (Per Protocol Set)(LS Mean) = 8.92 milligram(s)/24 hours  - 2019-12-30 Tris Pharma, Inc. https://clinicaltrials.gov/ct2/show/results/NCT01964378 https://synapse.zhihuiya.com/clinical-result-detail/85ae3e502e2d0eae8ee9dda5585a5e23 Efficacy, Safety and Tolerability of Multiple Doses of Oral Cebranopadol in Subjects With Moderate to Severe Chronic Pain Due to Diabetic Peripheral Neuropathy. NCT01939366 CTgov 临床2期 慢性疼痛 | 神经变性 | 糖尿病周围神经性疼痛 | 糖尿病周围神经病变 699 Cebranopadol 100 µg(Cebranopadol 100 µg) Change in Average Pain Intensity.(LS Mean) = -2.24 Unit (95%CI, -2.78 ~ -1.70) - 2019-12-26 Tris Pharma, Inc. https://clinicaltrials.gov/ct2/show/results/NCT01939366 https://synapse.zhihuiya.com/clinical-result-detail/ae5e40a22a2ad8ad3340254e8d32a0dd Efficacy, Safety and Tolerability of Multiple Doses of Oral Cebranopadol in Subjects With Moderate to Severe Chronic Pain Due to Diabetic Peripheral Neuropathy. NCT01939366 CTgov 临床2期 慢性疼痛 | 神经变性 | 糖尿病周围神经性疼痛 | 糖尿病周围神经病变 699 Cebranopadol 300 µg(Cebranopadol 300 µg) Change in Average Pain Intensity.(LS Mean) = -2.28 Unit (95%CI, -2.86 ~ -1.71) - 2019-12-26 Tris Pharma, Inc. https://clinicaltrials.gov/ct2/show/results/NCT01939366 https://synapse.zhihuiya.com/clinical-result-detail/ae5e40a22a2ad8ad3340254e8d32a0dd 12、转化医学 研究 亮点 主题 期刊/会议 出版日期 适应症 机构 Cebranopadol, a novel long-acting opioid agonist with low abuse liability, to treat opioid use disorder: Preclinical evidence of efficacy - 药物发现/临床前 Neuropharmacology 2024-10-01 opoid use disorder School of Pharmacy, Center for Neuroscience, Pharmacology Unit, University of Camerino, Italy. Cebranopadol, a Novel First-in-Class Analgesic Drug Candidate: First Experience With Cancer-Related Pain for up to 26 Weeks 研究发现，Cebranopadol是一种新型一类镇痛药物候选药，结合了痛觉素/孤儿肽和阿片肽受体激动作用。针对患有慢性中至重度癌症相关疼痛的患者进行的长期治疗显示，Cebranopadol在测试剂量范围内（200-1000 μg每日一次）是安全耐受的。该药具有一次日服用、小药片易于吞咽以及灵活调整有效剂量的特点，对于患有多种疾病且接受多药治疗的癌症患者而言易于应对。研究结果显示，Cebranopadol在治疗期间疼痛水平维持在轻度疼痛范围内。因此，Cebranopadol在先前接受Cebranopadol或吗啡缓释剂治疗的患者中长达26周的安全性和耐受性得到了验证。 药物发现/临床前 Pubmed 2019-09-01 癌症疼痛 Innovation Unit Pain, Clinical Science, Grünenthal GmbH, Aachen, Germany. Electronic address: dietlind.koch@grunenthal.com. Cebranopadol, a dual opioid and NOP receptor agonist, inhibits escalation of cocaine self-administration and conditioned reinstatement of cocaine seeking Cebranopadol是一种双重阿片和NOP受体激动剂，能够抑制可卡因自我使用的升级和条件性可卡因寻求的复发。该药物目前正在进行临床二期和三期试验，用于慢性和急性疼痛的治疗。最近的证据表明，阿片和NOP受体激动的组合可能是治疗可卡因成瘾的新方法。研究发现，Cebranopadol在大鼠中能够抑制可卡因自我使用的升级，阻断条件性可卡因寻求，并且预防成瘾行为的出现。然而，Cebranopadol也具有奖赏性质，有可能引起滥用行为。因此，需要未来的研究来进一步评估其奖赏性和潜在的滥用风险。Cebranopadol可能是治疗可卡因使用障碍的新型药物，但仍需要更多研究来证实其作用机制和安全性。 药物发现/临床前 SFN 2017 2017-11-15 - The Dept. of Neurosci., The Scripps Res. Inst., La Jolla, CA Discovery of a Potent Analgesic NOP and Opioid Receptor Agonist: Cebranopadol 本研究报道了一种强效镇痛剂NOP和阿片受体激动剂Cebranopadol的发现。Cebranopadol目前正在临床开发，用于治疗严重的慢性伤害性和神经病性疼痛。该化合物具有良好的体外和体内药理特性，是一种潜在的镇痛药物。 药物发现/临床前 ACS Med Chem Lett 2014-06-24 神经痛 Grünenthal GmbH