多項監管突破與上億美元支持，多肽療法在第一季度迎來多項進展 | Bilingual

編者按：近年來，憑借代謝穩定性高、靶點親和力強以及生物特異性優異等優勢，多肽療法正迅速崛起為全球新藥研發的重要方向。從GLP-1類代謝疾病療法持續取得突破，到腫瘤、神經系統疾病及免疫疾病等領域不斷涌現的新型多肽分子，多肽藥物的研發版圖正在不斷拓展。為了更好地滿足全球合作伙伴的研發需求，藥明康德圍繞多肽及其相關化學偶聯藥物構建了一體化解決方案，覆蓋定制合成、共價連接、工藝開發以及CMC等關鍵環節，并提供藥代動力學分析和免疫原性檢測等整合生物分析解決方案，為發現和開發多肽及復雜多肽偶聯藥物提供有力支持。本文將盤點2026年第一季度全球多肽療法在監管審批、臨床研究以及產業合作等方面的重要進展，并結合相關技術挑戰，帶您了解這一快速發展領域的最新動態與趨勢。

監管進展

2026年第一季度，多肽療法在全球范圍內迎來多項重要監管進展。其中，GLP-1類療法繼續在肥胖及相關疾病領域取得突破。諾和諾德（Novo Nordisk）高劑量司美格魯肽Wegovy HD（7.2 mg）注射劑在本季度獲得美國FDA批準，用于已耐受2.4 mg劑量治療至少4周、且仍需進一步減重的肥胖患者。與此同時，司美格魯肽（商品名Kayshild）獲得歐洲藥品管理局（EMA）人用藥品委員會（CHMP）推薦有條件批準，用于治療伴有肝纖維化的非肝硬化性代謝功能障礙相關脂肪性肝炎（MASH），預計將在今年4月正式獲批。根據新聞稿介紹，Kayshild有望成為首個獲EMA批準用于MASH適應癥的GLP-1類藥物。

此外，加拿大衛生部（Health Canada）在今年1月批準司美格魯肽口服片劑（商品名Rybelsus），用于降低患有2型糖尿病且已確診心血管疾病或具有高心血管風險的成人患者發生主要不良心血管事件（MACE，包括心血管死亡、非致死性心肌梗死或非致死性卒中）的風險。

在非GLP-1類療法方面，多款多肽藥物也取得關鍵監管突破。Ascendis Pharma旗下Yuviwel（navepegritide；TransCon CNP）獲得美國FDA加速批準，用于治療2歲及以上且骨骺尚未閉合的軟骨發育不全兒童。根據公司新聞稿，該藥物為首個獲批用于該患者人群、且每周一次給藥的治療方案。

同樣在3月，強生（Johnson & Johnson）與Protagonist Therapeutics公司聯合開發的口服多肽療法Icotyde（icotrokinra）獲得FDA批準，用于一線治療中重度斑塊狀銀屑病（PsO）成人患者，以及12歲及以上、體重至少40 kg且適合接受全身治療或光療的兒童患者。根據新聞稿，Icotyde是首個能夠精準阻斷IL-23受體的靶向口服多肽藥物。

此外，Rhythm Pharmaceuticals旗下多肽藥物Imcivree（setmelanotide）的擴展適應癥也在本季度獲得FDA批準，用于治療成人及4歲及以上兒童獲得性下丘腦性肥胖（HO），以降低過多體重并長期維持減重效果。同樣值得關注的是，歐盟委員會（EC）批準Sobi與Apellis Pharmaceuticals聯合開發的Aspaveli（pegcetacoplan），用于與腎素-血管緊張素系統（RAS）抑制劑聯合治療12至17歲青少年及成人C3腎小球病（C3G）或原發性免疫復合物型膜增生性腎小球腎炎（IC-MPGN）。

臨床進展

在臨床研究方面，GLP-1相關療法仍是本季度多肽研發最活躍的領域之一，多家藥企在肥胖及代謝疾病治療方向持續取得進展。禮來（Eli Lilly and Company）宣布，其潛在“first-in-class”三重激素受體激動劑retatrutide在3期試驗中取得積極結果。該分子可同時靶向葡萄糖依賴性促胰島素多肽（GIP）、胰高血糖素樣肽-1（GLP-1）以及胰高血糖素受體。研究分析顯示，2型糖尿病患者在接受每周一次retatrutide治療40周后，糖化血紅蛋白（A1C）平均下降1.7–2.0個百分點，而最高劑量組患者的平均體重下降達到16.8%（36.6磅）。

與此同時，輝瑞（Pfizer）的長效GLP-1受體激動劑PF-08653944（PF'3944，曾用名MET-097i）也在2b期試驗中取得積極結果。研究顯示，所有四種劑量方案在主要終點——從隨機分組至第28周的體重降低——方面均顯著優于安慰劑（P<0.001）。值得關注的是，在切換至每月給藥后，減重效果依然強勁且持續，在第28周尚未出現平臺期，提示該療法具備每月一次給藥的潛力。目前，PF'3944的多項3期試驗正在推進中。

此外，Viking Therapeutics旗下GIP/GLP-1雙重受體激動劑VK2735的2期試驗結果發表于《肥胖》期刊，其3期試驗也在本季度完成患者招募。Altimmune旗下候選藥物pemvidutide則在今年年初獲得FDA突破性療法認定，用于治療MASH。公司已與FDA就3期注冊試驗關鍵設計達成一致，即將啟動針對中至重度肝纖維化MASH患者的3期研究。

與此同時，諾和諾德宣布其固定劑量聯合療法CagriSema在3期試驗中，在減重與改善A1C方面均優于司美格魯肽。CagriSema由長效胰淀素類似物cagrilintide（2.4 mg）與司美格魯肽（2.4 mg）組成。此外，Zealand Pharma與艾伯維（AbbVie）旗下的胰淀素靶向療法petrelintide與ABBV-295也在本季度分別公布了用于治療肥胖患者的2期與1期試驗積極結果。

值得注意的是，GLP-1療法的應用范圍正在逐步拓展至代謝疾病之外。禮來在本季度宣布，其GLP-1/GIP雙重受體激動劑Zepbound（tirzepatide）聯合IL-17A單抗Taltz（ixekizumab），在兩項分別針對中重度斑塊狀銀屑病及活動性銀屑病關節炎（PsA）肥胖或超重患者的3期試驗中均達到主要終點。這些結果顯示，GLP-1類療法有望與銀屑病生物制品形成新的聯合治療策略。

除GLP-1相關療法外，本季度多項多肽療法也在其他疾病領域取得進展。例如，Priavoid旗下靶向β-淀粉樣蛋白（Aβ）寡聚體的口服多肽療法PRI-002在2期試驗中顯示，其淀粉樣相關影像學異常（ARIA）發生率與既往3期研究中安慰劑組水平相當。此外，一項1/2期試驗結果顯示，一名同時患有家族性腺瘤性息肉病（FAP）及相關硬纖維瘤的患者在接受Parabilis Medicines潛在“first-in-class”多肽療法zolucatetide治療60周后，十二指腸息肉病變顯著改善。與治療前評估相比，該患者息肉數量和大小均明顯減少，疾病分期由Spigelman II期降至I期，同時硬纖維瘤直徑減少了52.2%。根據新聞稿，zolucatetide是首個直接抑制β-catenin與TCF相互作用的抑制劑。

研發合作與融資進展

在產業合作方面，本季度多家大型藥企圍繞多肽療法達成金額達數億美元甚至數十億美元的合作協議。今年1月，阿斯利康（AstraZeneca）與石藥集團達成最高可達35億美元的戰略合作，雙方將共同推進覆蓋肥胖癥與2型糖尿病的8項下一代療法研發。根據協議，雙方將首先推進其中4個項目，這些項目將結合石藥集團AI驅動的肽類藥物發現平臺以及其專有的LiquidGel每月一次給藥平臺技術。此外，諾華（Novartis）在2月與Unnatural Products（UNP）達成總金額超過17億美元的大環肽合作，進一步加碼這一新興分子領域。

融資方面，多家創新公司也獲得資本市場支持。Parabilis Medicines在今年初完成超過3億美元的F輪融資，所獲資金將用于推進zolucatetide的開發。同時，峰肽藥業（Pinnacle Medicines）也于3月時完成8900萬美元的B輪融資，用于加速管線的臨床推進。

▲2026年第一季度多肽藥物領域部分投融資信息

一體化平臺助力多肽藥物創新

隨著多肽療法在肥胖、代謝疾病以及更多創新適應癥中的研發不斷推進，其分子設計也正變得愈發復雜。從脂肪酸修飾、PEG化，到蛋白融合與多肽偶聯等策略，越來越多的新一代多肽分子通過結構改造實現更長半衰期或更優藥效。然而，這些創新設計在帶來治療潛力提升的同時，也對藥物開發過程中的生物分析提出了更高要求。特別是在臨床研究階段，如何準確解析多肽藥物的體內暴露特征、免疫原性風險以及結構修飾帶來的影響，已成為推動相關療法順利進入后期開發的重要基礎。

在這一趨勢下，能夠同時支持藥代動力學（PK）與免疫原性評價的系統化生物分析能力，正成為創新多肽藥物研發的重要技術支撐。為幫助合作伙伴更好地應對這些挑戰，藥明康德生物分析部（BAS）依托高度成熟的生物分析技術平臺，構建了面向新一代多肽藥物開發需求的系統化分析解決方案，能夠有效應對多肽分子在臨床試驗中藥代動力學與免疫原性研究的復雜挑戰。

隨著多肽藥物分子量增加、結構修飾增多及偶聯形式日益復雜，其生物分析面臨一系列特有挑戰。例如，一方面，多肽在液相色譜串聯質譜（LC-MS/MS）分析中通常呈現多電荷態分布及電離效率不均一，導致信號分散與離子抑制，從而影響檢測靈敏度與方法穩健性；另一方面，多肽分子表位有限且與內源性肽序列高度同源，往往表現為免疫原性較低、特異性抗體制備困難，同時在配體結合分析（LBA）中易出現內源性干擾與交叉反應，增加免疫原性評價的復雜性。此外，脂肪酸修飾、PEG化或蛋白融合等結構改造在延長半衰期的同時，也可能引入新的免疫原性風險（如抗PEG抗體），對抗藥抗體（ADA）與中和抗體（NAb）檢測提出更高要求。

針對上述行業痛點，藥明康德生物分析部整合高靈敏度LC-MS/MS、免疫捕獲-質譜、ELISA/MSD平臺及細胞功能分析方法，實現PK分析、抗藥抗體（ADA）與中和抗體（NAb）評價的一體化支持。通過優化樣本前處理策略、建立免疫捕獲-質譜聯用技術及基于胰蛋白酶消化的bottom-up分析方法，可顯著提升檢測靈敏度并降低基質干擾，在復雜修飾多肽及長鏈多肽分析中表現出良好的方法特異性與穩健性。同時，針對多肽藥物免疫原性評價中的低免疫原性與高同源性帶來的檢測難點，團隊建立了分層（tiered）免疫原性評價體系，整合橋式（bridging）ADA檢測、確認實驗及滴度分析，并結合酸解離（ACE）、MRD優化等策略提升藥物耐受性與檢測靈敏度；通過優化標記試劑設計及方法學條件，有效降低內源性干擾與非特異性結合，并結合細胞功能性NAb分析方法，實現從ADA篩查到中和效應評價的全流程覆蓋，從而系統性支持復雜修飾多肽及偶聯多肽藥物的免疫原性風險評估。

藥明康德生物分析技術平臺已成功支持GLP-1類似物、胰島素類似物等新一代多肽藥物的臨床PK研究及免疫原性評估，形成覆蓋方法開發、驗證到樣本檢測的端到端能力。依托標準化流程與多技術協同優勢，藥明康德生物分析部能夠為合作伙伴提供高靈敏度、高可靠性的多肽藥物生物分析支持，加速創新多肽療法從研究階段邁向臨床開發。

Multiple FDA Approvals and Hundreds of Millions in Investments: Peptide Therapeutics See Significant Progress in Q1

In recent years, peptide therapeutics have rapidly emerged as a major direction in global drug discovery, driven by their high metabolic stability, strong target affinity, and excellent biological specificity. From continued breakthroughs in glucagon-like peptide-1 (GLP-1)–based therapies for metabolic diseases to the emergence of novel peptide molecules targeting oncology, neurological disorders, and immune diseases, the landscape of peptide drug development continues to expand.

To better meet the evolving needs of global partners, WuXi AppTec has established an integrated solution for peptides and related chemical conjugates, covering key stages including custom synthesis, covalent conjugation, process development, and CMC, while also providing integrated bioanalytical solutions such as pharmacokinetic analysis and immunogenicity assessment. Together, these capabilities provide strong support for the discovery and development of peptides and complex peptide conjugate therapeutics.

This article reviews major developments in peptide therapeutics worldwide during the first quarter of 2026, including regulatory approvals, clinical progress, and industry collaborations, while highlighting key technical challenges and emerging trends shaping this rapidly evolving field.

Regulatory Developments

In the first quarter of 2026, peptide therapeutics achieved several important regulatory milestones globally. Among them, GLP-1 therapies continued to make breakthroughs in obesity and related disease areas.Novo Nordisk’s high-dose semaglutideWegovy HD (7.2 mg)injection received U.S. FDA approval this quarter for obesity patients who have tolerated the 2.4 mg dose for at least four weeks but still require additional weight reduction.

Meanwhile,semaglutide (brand name Kayshild)received a recommendation for conditional approval from the Committee for Medicinal Products for Human Use (CHMP) of the European Medicines Agency (EMA) for the treatment of metabolic dysfunction-associated steatohepatitis (MASH) with liver fibrosis in patients without cirrhosis. The therapy is expected to receive formal approval in April this year. According to the company,Kayshild could become the first GLP-1 therapy approved by the EMA for a MASH indication.

In addition, Health Canada approved the oral semaglutide tabletRybelsusin January for reducing the risk of major adverse cardiovascular events (MACE)—including cardiovascular death, non-fatal myocardial infarction, and non-fatal stroke—in adults with type 2 diabetes who have established cardiovascular disease or are at high cardiovascular risk.

Beyond GLP-1 therapies, several peptide drugs also achieved key regulatory breakthroughs. Yuviwel (navepegritide; TransCon CNP)from Ascendis Pharma received accelerated approval from the U.S. FDA for the treatment of children aged two years and older with achondroplasia whose growth plates have not yet closed. According to the company,the drug is the first once-weekly treatment approved for this patient population.

Also in March, oral peptide therapyIcotyde (icotrokinra)developed by Johnson & Johnson in collaboration with Protagonist Therapeutics received FDA approval as a first-line treatment for adults with moderate-to-severe plaque psoriasis (PsO), as well as pediatric patients aged 12 years and older weighing at least 40 kg who are eligible for systemic therapy or phototherapy. According to the press release,Icotyde is the first targeted oral peptide drug designed to selectively block the IL-23 receptor.

Additionally, Rhythm Pharmaceuticals’ peptide drugImcivree (setmelanotide)received FDA approval this quarter for an expanded indication to treat acquired hypothalamic obesity (HO) in adults and children aged four years and older, helping reduce excess body weight and maintain long-term weight loss.

Meanwhile, the European Commission (EC) approvedAspaveli (pegcetacoplan)developed by Sobi and Apellis Pharmaceuticals for use in combination with renin-angiotensin system (RAS) inhibitors to treat adolescents aged 12–17 and adults with C3 glomerulopathy (C3G) or primary immune complex membranoproliferative glomerulonephritis (IC-MPGN).

Clinical Progress

In clinical development,GLP-1–related therapies remained one of the most active areas of peptide drug research this quarter, with several pharmaceutical companies reporting progress in obesity and metabolic disease treatments.Eli Lilly and Company announced positive Phase 3 results for its potential first-in-class triple hormone receptor agonistretatrutide, which simultaneously targets GLP-1, glucose-dependent insulinotropic polypeptide (GIP), and glucagon receptors. Analysis showed that after 40 weeks of once-weekly treatment, patients with type 2 diabetes experienced an average HbA1c reduction of 1.7%–2.0%, while patients in the highest-dose group achieved an average body-weight reduction of 16.8% (36.6 lbs).

At the same time, Pfizer’s long-acting GLP-1 receptor agonistPF-08653944 (PF'3944, formerly MET-097i)demonstrated positive results in a Phase 2b trial. All four dosing regimens achieved significantly greater weight reduction from randomization to Week 28 compared with placebo (P<0.001). Notably, after transitioning to monthly dosing, weight-loss effects remained strong and sustained, with no plateau observed by Week 28, suggesting the therapy may support a once-monthly dosing regimen. Multiple Phase 3 trials of PF'3944 are currently underway.

Additionally, Viking Therapeutics’ dual GIP/GLP-1 receptor agonistVK2735reported Phase 2 results published in Obesity, while enrollment for its Phase 3 trial was completed this quarter. Altimmune’s candidatepemvidutidereceived FDA Breakthrough Therapy designation earlier this year for the treatment of MASH, and the company has reached agreement with the FDA on the key design of its Phase 3 registrational trial targeting patients with moderate-to-severe liver fibrosis.

Meanwhile, Novo Nordisk reported that its fixed-dose combination therapyCagriSemaoutperformed semaglutide in Phase 3 trials in both weight reduction and HbA1c improvement. CagriSema combines the long-acting amylin analog cagrilintide (2.4 mg) with semaglutide (2.4 mg). Zealand Pharma and AbbVie also reported encouraging results this quarter for amylin-targeting therapiespetrelintideandABBV-295, with positive Phase 2 and Phase 1 results, respectively, for the treatment of obesity.

Importantly, the application of GLP-1 therapies is expanding beyond metabolic diseases.This quarter, Eli Lilly reported that its GLP-1/GIP dual receptor agonistZepbound (tirzepatide)combined with the IL-17A monoclonal antibody Taltz (ixekizumab) met primary endpoints in two Phase 3 trials targeting overweight or obese patients with moderate-to-severe plaque psoriasis and active psoriatic arthritis (PsA).These findings suggest that GLP-1 therapies may form new combination treatment strategies alongside psoriasis biologics.

Beyond GLP-1–related therapies,several peptide drugs also advanced in other disease areas.For example,PRI-002, an oral peptide therapy from Priavoid targeting β-amyloid (Aβ) oligomers, demonstrated amyloid-related imaging abnormality (ARIA) rates comparable to the placebo group in previous Phase 3 studies.

In addition, results from a Phase 1/2 study showed that a patient with both familial adenomatous polyposis (FAP) and associated desmoid tumors experienced significant improvement after 60 weeks of treatment withzolucatetide, a potential first-in-class peptide therapy developed by Parabilis Medicines. Compared with baseline, both the number and size of duodenal polyps were significantly reduced, with disease stage improving from Spigelman stage II to stage I, while the desmoid tumor diameter decreased by 52.2%. According to the company,zolucatetide is the first inhibitor designed to directly block the interaction between β-catenin and TCF.

Partnerships and Financing

On the industry collaboration front,several large pharmaceutical companies announced peptide-focused partnerships this quarter.In January, AstraZeneca and CSPC Pharmaceutical Group announced a strategic collaboration worth up to $3.5 billion to advance eight next-generation therapies targeting obesity and type 2 diabetes. The partners will initially advance four programs combining CSPC’s AI-driven peptide discovery platform with its proprietary LiquidGel once-monthly delivery technology. In February, Novartis entered into a collaboration with Unnatural Products (UNP) worth more than $1.7 billion to develop macrocyclic peptide therapeutics.

In terms of financing, several emerging companies also secured strong investor support. Parabilis Medicines completed a Series F financing exceeding $300 million earlier this year to advance the development of zolucatetide. Meanwhile, Pinnacle Medicines completed $89 million Series B financing in March to accelerate the clinical development of its pipelines.

WuXi AppTec Supports Innovation in Peptide Therapeutics

As peptide therapeutics continue to expand into obesity, metabolic diseases, and a growing range of innovative indications, molecular designs are becoming increasingly sophisticated. From fatty-acid modification and PEGylation to protein fusion and peptide conjugation, many next-generation peptide drugs are engineered to achieve longer half-lives and improved therapeutic performance. However,these innovations also introduce new analytical challenges in drug development.Particularly during clinical studies, accurately characterizing the in vivo exposure profile and immunogenicity risks of peptide drugs, and understanding how structural modifications may influence these parameters, has become critical for advancing therapies into later-stage development.

Against this backdrop, integrated bioanalytical capabilities supporting both pharmacokinetics (PK) and immunogenicity assessment are becoming increasingly essential. To help partners address these challenges,WuXi AppTec Bioanalytical Services (BAS), supported by a highly mature bioanalytical technology platform, has established a systematic analytical solution tailored to the development needs of next-generation peptide therapeutics.This integrated platform effectively addresses the complex challenges associated with pharmacokinetics (PK) and immunogenicity studies in clinical trials. As peptide drugs continue to increase in molecular weight, incorporate more structural modifications, and adopt increasingly complex conjugation formats, their bioanalysis presents a series of unique challenges.

In LC–MS/MS analysis, peptides often exhibit broad charge state distributions and heterogeneous ionization efficiency, leading to signal dispersion and ion suppression that can compromise sensitivity and method robustness. Meanwhile, peptides typically possess limited epitopes and high homology to endogenous counterparts, resulting in low immunogenicity and challenges in generating highly specific antibodies, as well as increased susceptibility to endogenous interference and cross-reactivity in ligand-binding assays (LBA). In addition, structural modifications such as fatty acid conjugation, PEGylation, or protein fusion—while extending half-life—may introduce additional immunogenicity risks (e.g., anti-PEG antibodies), further complicating anti-drug antibody (ADA) and neutralizing antibody (NAb) assessments.

To address these challenges,WuXi AppTec BAS integrates high-sensitivity LC–MS/MS, immunocapture–mass spectrometry, ELISA/MSD platforms, and cell-based functional assays to enable seamless support from PK analysis to comprehensive immunogenicity evaluation.Through optimized sample preparation strategies, implementation of immunocapture techniques, and adoption of bottom-up approaches such as trypsin digestion, the platform significantly enhances detection sensitivity and reduces matrix interference, ensuring robust and specific analysis of structurally complex and long-chain peptides. For immunogenicity assessment, a tiered evaluation framework is established, incorporating bridging ADA assays, confirmatory testing, and titer determination, alongside advanced strategies such as acid dissociation (ACE) and minimum required dilution (MRD) optimization to improve drug tolerance and assay sensitivity. In parallel, careful optimization of labeled reagents and assay conditions minimizes endogenous interference and non-specific binding, while cell-based NAb assays provide functional evaluation of neutralizing responses—enabling an end-to-end immunogenicity assessment workflow for complex peptide and peptide-conjugated therapeutics.

WuXi AppTec BAS has successfully supported clinical PK and immunogenicity studies for a wide range of peptide therapeutics, including GLP-1 analogs and insulin analogs, delivering end-to-end capabilities from method development and validation to sample analysis.Enabled by standardized workflows and integrated multi-technology expertise, WuXi AppTec provides high-sensitivity, high-reliability bioanalytical support for peptide therapeutics, accelerating the advancement of innovative peptide drugs from research into clinical development.

參考資料：

[1] 各公司官網

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