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GLP-1 수용체 작용제 및 인크레틴계 치료제 : 경쟁 구도(2026년)GLP-1 RAs & Incretin Based Therapies - Competitive landscape, 2026 |
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DelveInsight
GIP와 GLP-1은 혈당 항상성을 조절하는 두 가지 주요 인크레틴 호르몬입니다. 주로 십이지장과 공장에서 K세포에 의해 분비되는 GIP는 혈당 의존성 인슐린 분비를 촉진하는 반면, 주로 회장과 결장에서 L세포에 의해 생성되는 GLP-1은 강력한 인슐린 분비 촉진 작용을 발휘합니다. 이 호르몬들은 모두 혈당 조절 유지에 필수적인 역할을 하며, 포유류 종 간에 고도로 보존되어 있습니다.
GIP와 GLP-1은 중복되는 부분도 있지만 서로 다른 기전을 통해 혈당 및 지질 대사를 조절하는 상호 보완적인 인크레틴 호르몬입니다. GIP는 혈당 의존성 인슐린 분비, 저혈당 시 글루카곤 분비, 그리고 지방 조직으로의 지질 저장을 촉진하는 반면, GLP-1은 인슐린 분비를 촉진하고, 고혈당 시 글루카곤을 억제하며, 위 내용물의 배출을 지연시키고, 포만감을 높입니다. 두 호르몬 모두 클래스 B GPCR 및 cAMP 매개 신호 전달을 통해 작용하지만, DPP-4에 의한 급속한 분해로 인해 반감기가 짧습니다. 이러한 상호 보완적인 작용으로 인해 GLP-1 수용체 작용제 및 세마글루티드, 틸제파티드 등의 GIP/GLP-1 이중 작용제의 치료적 활용이 지지되고 있습니다.
GIP와 GLP-1은 2형 당뇨병(T2DM) 및 비만에 대한 중요한 치료 표적이며, 특히 GLP-1은 더 확립된 임상적 유효성을 가지고 있습니다. 2형 당뇨병에서는 GIP의 활성이 저하되어 있지만, GLP-1 신호 전달과 결합함으로써 그 활성화가 혈당 조절을 개선할 가능성이 있습니다. GLP-1은 포만감을 높이고, 식사 섭취량을 줄이며, 에너지 대사에 영향을 미침으로써 혈당 조절을 개선하고 체중 감소를 촉진합니다. 이러한 상호 보완적인 효과로 인해, GIP/GLP-1 수용체 작용제인 틸제파티드나 GIPR 길항제/GLP-1R 작용제인 마리데바트·카프라글루티드 등, 이중 및 다기능형 인크레틴 요법의 개발이 진행되고 있으며, 이들은 단일 인크레틴 요법보다 더 큰 대사적 이점을 가져다줄 가능성이 있습니다.
천연 GIP 및 GLP-1은 반감기가 짧기 때문에 안정성과 약동학이 개선된 지속형 인크레틴 아날로그의 개발이 진행되어 왔습니다. 엑세나티드, 릴라글루티드, 듀라글루티드, 세마글루티드 등의 GLP-1 작용제는 DPP-4에 의한 분해를 견디고 혈중 농도를 유지하도록 구조가 개량되어, 1일 1회, 주 1회, 나아가 경구 투여가 가능해졌습니다. 이러한 진보를 바탕으로, 틸제파티드 등의 GIP/GLP-1 이중 작용제는 상호 보완적인 인크레틴 경로를 결합함으로써 치료 효과를 높이고 있습니다. 이러한 혁신을 통해 인크레틴 요법의 적용 범위는 혈당 조절에서 체중 관리, 나아가 더 광범위한 심혈관 및 대사 측면의 이점으로 확대되었습니다.
2형 당뇨병(T2DM)의 관리는 혈당 조절에 그치지 않고, 비만 및 심혈관·대사 위험 요인의 통합 관리로 진화해 왔습니다. GLP-1 수용체 작용제(GLP-1RA) 및 틸제파티드는 HbA1c를 대폭 낮추며, 특히 틸제파티드는 매우 높은 유효성을 보이고 있습니다. 한편, 지속형 제제는 일반적으로 인슐린보다 우수한 전반적인 혈당 조절과 저혈당 위험 감소를 가져옵니다. 또한, 이러한 치료법은 임상적으로 의미 있는 체중 감소를 촉진하며, 티르제파티드가 일반적으로 가장 큰 체중 감소 효과를 나타냅니다. 릴라글루티드, 세마글루티드, 알비글루티드, 듀라글루티드를 포함한 일부 GLP-1RA는 MACE 감소를 포함한 심혈관계상의 이점이 입증되었으나, 틸제파티드의 심혈관계에 미치는 영향에 대해서는 현재도 평가가 진행 중입니다. 전반적으로, 인크레틴 계열 치료제는 현재 혈당 조절, 체중 관리, 심혈관 위험, 그리고 잠재적으로는 신장 보호에 이르기까지 폭넓은 이점을 제공하고 있습니다.
DelveInsight's, "GLP-1 RAs & Incretin Based Therapies - Competitive landscape, 2026," report provides comprehensive insights about 180+ companies and 200+ drugs in GLP-1 RAs & Incretin Based Therapies Competitive landscape. It covers the therapeutics assessment by product type, stage, route of administration, and molecule type. It further highlights the inactive pipeline products in this space.
GLP-1 RAs & Incretin Based Therapies: Understanding
GLP-1 RAs & Incretin Based Therapies: Overview
GIP and GLP-1 are the two primary incretin hormones that regulate glucose homeostasis. GIP, secreted mainly by K cells in the duodenum and jejunum, enhances glucose-dependent insulin secretion, while GLP-1, produced predominantly by L cells in the ileum and colon, exerts potent insulinotropic effects. Both hormones play essential roles in maintaining glucose control and are highly conserved across mammalian species.
GIP and GLP-1 are complementary incretin hormones that regulate glucose and lipid metabolism through overlapping yet distinct mechanisms. GIP enhances glucose-dependent insulin secretion, glucagon release during hypoglycemia, and adipose lipid storage, whereas GLP-1 promotes insulin secretion, suppresses glucagon during hyperglycemia, delays gastric emptying, and increases satiety. Both act through class B GPCRs and cAMP-mediated signaling but have short half-lives due to rapid DPP-4 degradation. Their complementary effects support the therapeutic use of GLP-1 receptor agonists and dual GIP/GLP-1 agonists such as semaglutide and tirzepatide.
GIP and GLP-1 are important therapeutic targets for T2DM and obesity, with GLP-1 having more established clinical benefits. While GIP activity is impaired in T2DM, its activation may enhance glucose control when combined with GLP-1 signaling. GLP-1 improves glycemic control and promotes weight loss by enhancing satiety, reducing food intake, and influencing energy metabolism. These complementary effects have driven the development of dual- and multifunctional incretin therapies, including the GIP/GLP-1 receptor agonist tirzepatide and the GIPR antagonist/GLP-1R agonist maridebart cafraglutide, which may offer greater metabolic benefits than single-incretin therapies.
Native GIP and GLP-1 have short half-lives, prompting the development of longer-acting incretin analogues with improved stability and pharmacokinetics. GLP-1 agonists such as exenatide, liraglutide, dulaglutide, and semaglutide incorporate structural modifications to resist DPP-4 degradation and prolong circulation, enabling daily, weekly, and oral dosing. Building on these advances, dual GIP/GLP-1 agonists such as tirzepatide combine complementary incretin pathways to enhance therapeutic efficacy. These innovations have expanded incretin therapies from glycemic control to weight management and broader cardiometabolic benefits.
T2DM management has evolved beyond glycemic control toward integrated management of obesity and cardiometabolic risk. GLP-1RAs and tirzepatide provide substantial HbA1c reductions, with tirzepatide showing particularly strong efficacy, while long-acting agents generally offer better overall glycemic control and lower hypoglycemia risk than insulin. These therapies also promote clinically meaningful weight loss, with tirzepatide generally producing the greatest reductions. Several GLP-1RAs, including liraglutide, semaglutide, albiglutide, and dulaglutide, have demonstrated cardiovascular benefits, including reduced MACE, whereas tirzepatide's cardiovascular effects remain under evaluation. Overall, incretin-based therapies now offer broader benefits across glycemic control, weight management, cardiovascular risk, and potentially renal protection.
GLP-1 RAs & Incretin Based Therapies: Company and Product Profiles (Marketed Therapies)
Eli Lilly and Company is a global pharmaceutical company focused on transforming scientific discoveries into innovative medicines that improve health and quality of life. With nearly 150 years of research and development experience, Lilly leverages biotechnology, chemistry, and genetic medicine to address major healthcare challenges, including diabetes, obesity, Alzheimer's disease, immune disorders, and difficult-to-treat cancers. The company also emphasizes diverse clinical trials and efforts to improve the accessibility and affordability of its medicines worldwide.
Product Description: Mounjaro
Mounjaro(R) (tirzepatide) is a once-weekly, injectable dual GIP/GLP-1 receptor agonist developed by Eli Lilly and Company for the treatment of type 2 diabetes (T2D). It enhances glucose-dependent insulin secretion, suppresses glucagon release, slows gastric emptying, and promotes satiety, resulting in improved glycemic control and weight reduction. Tirzepatide has demonstrated substantial reductions in HbA1c and body weight compared with several established diabetes therapies. Its dual incretin mechanism represents an advancement over selective GLP-1 receptor agonists by simultaneously activating GIP and GLP-1 pathways. In May 2022, the U.S. Food and Drug Administration (FDA) approved Mounjaro(TM) (tirzepatide) injection, Eli Lilly and Company's new once-weekly GIP (glucose-dependent insulinotropic polypeptide) and GLP-1 (glucagon-like peptide-1) receptor agonist indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes.
Novo Nordisk is a leading global healthcare company with more than a century of experience developing innovative medicines for diabetes and other serious chronic diseases, including obesity and rare blood and endocrine disorders. The company focuses on long-term, sustainable growth through scientific innovation and financially, socially, and environmentally responsible business practices. In the US, Novo Nordisk has operated for approximately 40 years, with its headquarters in New Jersey and around 10,000 employees across more than 10 manufacturing, R&D, and corporate locations in seven states and Washington, DC.
Product Description: Ozempic
Ozempic(R) (semaglutide) is a prescription medicine used alongside diet and exercise to improve blood glucose control in adults with type 2 diabetes. Ozempic injection is additionally indicated to reduce the risk of major cardiovascular events (heart attack, stroke, or cardiovascular death) in adults with T2D and established heart disease, and to reduce the risk of kidney disease progression, kidney failure, and cardiovascular death in adults with T2D and chronic kidney disease. Ozempic tablets are also indicated for cardiovascular risk reduction in adults with T2D who are at high risk of major cardiovascular events. The safety and efficacy of Ozempic injection and tablets in children have not been established.
GLP-1 RAs & Incretin Based Therapies: Company and Product Profiles (Pipeline Therapies)
Regeneron is a leading biotechnology company focused on discovering, developing, and commercializing transformative medicines for serious diseases. Founded and led by physician-scientists, the company leverages its in-house scientific expertise and proprietary technologies, including VelociSuite(R) and the Regeneron Genetics Center(R), to accelerate drug discovery and development. Its diverse pipeline addresses major therapeutic areas such as eye diseases, allergic and inflammatory disorders, cancer, cardiovascular and metabolic diseases, neurological and hematologic conditions, infectious diseases, and rare disorders, while its advanced antibody and genetic medicine platforms support the identification of novel therapeutic targets and innovative treatment approaches.
Hansoh Pharma is a leading innovation-driven pharmaceutical company in China, focused on major therapeutic areas including oncology, anti-infectives, central nervous system (CNS) disorders, metabolism, and immunology. Guided by its mission of "continuous innovation for better life," the company has launched seven innovative medicines in China, with innovative and collaborative products contributing more than 80% of revenue and supporting a broad development pipeline. Hansoh Pharma consistently ranks among the top 100 global pharmaceutical companies and top three pharmaceutical R&D enterprises in China, and is recognized as a National Key High-Tech Enterprise and National Technology Innovation Demonstration Enterprise. The company has been listed on the Hong Kong Stock Exchange since June 2019.
Product Description: Olatorepatide
Olatorepatide is a proprietary dual GLP-1/GIP receptor agonist discovered and developed in-house by Hansoh Pharma. By selectively activating GLP-1 and GIP receptors, the drug modulates metabolic pathways governing appetite suppression, glucose homeostasis, and energy balance to deliver glycemic control and weight reduction benefits. It is administered once weekly via subcutaneous injection. Currently, the drug is in Phase III stage of its development for the treatment of indications for cardio metabolic health. The New Drug Application was accepted by NMPA for for chronic weight management in adults with obesity or overweight. Currently, the therapy is in Registration stage of its development for the treatment of indications for cardio metabolic health.
Eli Lilly and Company is a global pharmaceutical company focused on transforming scientific discoveries into innovative medicines that improve health and quality of life. With nearly 150 years of research and development experience, Lilly leverages biotechnology, chemistry, and genetic medicine to address major healthcare challenges, including diabetes, obesity, Alzheimer's disease, immune disorders, and difficult-to-treat cancers. The company also emphasizes diverse clinical trials and efforts to improve the accessibility and affordability of its medicines worldwide.
Product Description: Retatrutide
Retatrutide is an investigational once-weekly triple agonist targeting the GIP, GLP-1, and glucagon receptors. Lilly is evaluating its efficacy and safety across multiple Phase III trials in obesity and overweight-related conditions, type 2 diabetes, knee osteoarthritis pain, moderate-to-severe obstructive sleep apnea, chronic low back pain, cardiovascular and renal outcomes, and metabolic dysfunction-associated steatotic liver disease (MASLD). Retatrutide remains investigational and is currently available only to participants enrolled in Lilly-sponsored clinical trials. Currently, the drug is in Phase III stage of its development for the treatment of indications for cardio metabolic health.
Pfizer is a global biopharmaceutical company that leverages science and worldwide resources to develop innovative medicines and vaccines that extend and improve patients' lives. The company focuses on maintaining high standards of quality, safety, and value across the discovery, development, and manufacturing of healthcare products, while advancing treatments and preventive solutions for serious diseases. With operations across developed and emerging markets, Pfizer collaborates with healthcare providers, governments, and communities to expand access to reliable and affordable healthcare and has pursued this mission for more than 175 years.
Product Description: PF-08653944
PF-08653944 is an ultra-long-acting, fully biased GLP-1 receptor agonist being investigated as a next-generation incretin-based therapy. The candidate is being developed for once-weekly and potentially once-monthly administration, with the aim of providing sustained GLP-1 receptor activation and improving dosing convenience. In addition to monotherapy, PF-08653944 is being evaluated in combination with other metabolic peptides, including the amylin analogue PF-08653945 (PF'3945; MET-233i) and the GIP receptor agonist PF-08654696 (MET-034i), supporting its potential application in combination-based approaches for metabolic disorders such as obesity and type 2 diabetes. Currently, the drug is in Phase III stage of its development for the treatment of obesity.
Founded in 1896 in Basel, Switzerland, Roche has evolved from an early manufacturer of branded medicines into a global leader in biotechnology and in-vitro diagnostics, focused on developing innovative medicines and diagnostic solutions that improve and save lives. The company is a pioneer in personalized healthcare, integrating pharmaceutical and diagnostic capabilities with real-world clinical data to advance patient-centered care. Sustainability has remained an integral part of Roche's operations for more than 125 years, with the company targeting net-zero emissions by 2045 through initiatives such as the Science Based Targets initiative and Sustainable Markets Initiative. In the United States, Genentech operates as a wholly owned member of the Roche Group, while Roche is the majority shareholder of Chugai Pharmaceutical in Japan.
Product Description: CT-388
CT-388 is an investigational once-weekly subcutaneous dual GLP-1/GIP receptor agonist being developed for obesity, type 2 diabetes, and related metabolic comorbidities. It is designed to reduce appetite and improve glycemic control through potent activation of both GLP-1 and GIP receptors while minimizing B-arrestin recruitment, thereby limiting receptor internalization and desensitization. This biased signaling profile is intended to support prolonged receptor activity and sustained therapeutic effects. Currently, the drug is in Phase III stage of its development for the treatment of obesity and type 2 diabetes.
vTv Therapeutics is a clinical-stage biopharmaceutical company focused on discovering and developing innovative oral, small-molecule therapies for diseases with significant unmet medical needs, particularly in the areas of metabolic, inflammatory, and chronic disorders. The company leverages its proprietary drug-discovery capabilities and expertise in small-molecule biology to develop differentiated treatment approaches designed to improve efficacy, safety, convenience, and patient outcomes. Its research activities span multiple therapeutic pathways, with a broader focus on advancing novel medicines from early discovery through clinical development.
Product Description: TTP273
TTP273 is an investigational oral small-molecule glucagon-like peptide-1 (GLP-1) receptor agonist being developed for the treatment of type 2 diabetes mellitus (T2DM). In preclinical and clinical studies, TTP273 has demonstrated the ability to reduce postprandial glucose excursions following oral glucose or mixed-meal tolerance tests. GLP-1 is a naturally occurring hormone that activates the GLP-1 receptor and plays an important role in metabolic regulation, with effects including improved glycemic control, reduced inflammation, and potential cardiovascular and neuroprotective benefits. GLP-1 receptor agonists are well-established therapies for lowering HbA1c, supporting weight reduction, and reducing cardiovascular risk in appropriate patient populations. Currently, the drug is in Phase II stage of its development for the treatment of diabetes.
Neurocrine Biosciences is a leading biopharmaceutical company focused on discovering, developing, and commercializing innovative treatments for neurological, psychiatric, endocrine, and immunological disorders with significant unmet medical needs. Its portfolio includes FDA-approved therapies for tardive dyskinesia, Huntington's disease-associated chorea, congenital adrenal hyperplasia, hyperphagia associated with Prader-Willi syndrome, endometriosis, and uterine fibroids, alongside a robust pipeline of mid- to late-stage clinical programs. With more than three decades of expertise in neuroscience and brain-body interactions, Neurocrine continues to advance therapies aimed at reducing the burden of complex and debilitating diseases.
Product Description: NBIP-'1968
NBIP-'1968 is an investigational long-acting, once-weekly triple agonist targeting the GLP-1, GIP, and glucagon receptors to modulate pathways involved in appetite, energy balance, and glycemic control. It is designed with balanced glucagon receptor activity to maximize potential metabolic benefits while maintaining tolerability. Neurocrine is developing NBIP-'1968 within its broader obesity portfolio alongside NBIP-'2118, an investigational corticotropin-releasing factor type 2 receptor agonist currently in Phase I development, with NBIP-'1968 intended for potential use in a fixed-dose combination with NBIP-'2118.
MetaVia Inc. is a clinical-stage biotechnology company focused on developing innovative therapies for cardiometabolic diseases, particularly obesity and metabolic dysfunction-associated steatohepatitis (MASH). Its lead obesity candidate, DA-1726, is a once-weekly GLP-1/glucagon receptor (GLP-1R/GCGR) dual agonist designed to reduce appetite through GLP-1R activation while increasing energy expenditure through glucagon receptor activation. The company is also developing vanoglipel (DA-1241), an oral GPR119 agonist being investigated for MASH and type 2 diabetes. As of 2026, DA-1726 is in Phase I development, with higher-dose studies evaluating dose titration, efficacy, and tolerability.
Product Description: DA-1726
DA-1726 is a novel oxyntomodulin (OXM) analogue and dual GLP-1/glucagon receptor agonist being developed as a once-weekly subcutaneous therapy for obesity and metabolic dysfunction-associated steatohepatitis (MASH). By activating GLP-1 and glucagon receptors, DA-1726 is designed to promote weight loss through appetite suppression and increased energy expenditure. Preclinical studies demonstrated greater weight loss than semaglutide and comparable weight reduction to tirzepatide and survodutide despite higher food intake, while also showing potential benefits in lean-mass preservation and lipid reduction. In a Phase I multiple-ascending-dose study, the 32 mg dose demonstrated promising effects on body weight, glycemic control, and waist circumference, supporting its potential as a next-generation metabolic therapy.
Sciwind Biosciences is a near-commercial-stage biopharmaceutical company focused on addressing unmet needs in weight management and metabolic diseases. Its pipeline is led by ecnoglutide (XW003) and is supported by proprietary technology platforms for biased agonist discovery, long-acting peptide delivery, and oral peptide delivery. Leveraging these platforms, Sciwind is developing a broad portfolio of injectable and oral therapies targeting GLP-1 and complementary metabolic pathways, with the goal of providing effective and durable treatment options for patients with metabolic disorders.
Product Description: XW014
XW014 is a Phase I oral small-molecule, cAMP-biased GLP-1 receptor agonist being developed as a potentially convenient and scalable alternative to peptide-based therapies. Designed for once-daily dosing, it aims to provide stable pharmacokinetics and a favorable safety profile while offering manufacturing and formulation advantages. Its small-molecule nature may enable greater production scalability, cost efficiency, and flexibility for combination with other oral therapies, potentially supporting synergistic treatment approaches.
GLP-1 RAs & Incretin Based Therapies Analytical Perspective by DelveInsight
The Report provides in-depth commercial assessment of drugs that have been included, which comprises collaboration, agreement, licensing and acquisition - deals values trends. The sub-segmentation is described in the report which provide company-company collaboration (licensing/partnering), company academic collaboration and acquisition analysis in tabulated form.
The report comprises of comparative assessment of Companies (by therapy, development stage, and technology).
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