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glucagon (LY 900018 / glucagon, Eli Lilly / Baqsimi)

✓ Approved

Amphastar Pharmaceuticals, Inc. · GCGR · 多肽类

什么是 glucagon？

glucagon 是一种多肽类，由Amphastar Pharmaceuticals, Inc.研发。该药已获批，用于治疗相关适应症，给药途径：Inhaled、Intramuscular (IM) Injection、Intranasal。

药物档案

商品名LY 900018, glucagon, Eli Lilly, Baqsimi
公司Amphastar Pharmaceuticals, Inc.
药物类别多肽类
分子靶点GCGR
给药途径Inhaled, Intramuscular (IM) Injection, Intranasal
状态Approved
来源： ClinicalTrials.gov, Amphastar Pharmaceuticals, Inc.

作用机制

分子靶点

glucagon 作用于 1 个分子靶点：

GCGRglucagon receptor (GL-R, GGR)
需要更深入的分析？Noah AI 可解释复杂机制并与同类药物比较。

治疗适应症

glucagon 针对 1 个适应症，涉及 1 个治疗领域。

治疗领域疾病/病症分期
Metabolism and nutrition disordersHypoglycaemia✓ Approved

相关研究文献

PubMedFrontiers in endocrinology2026-09-10

Sex-specific differences in pancreatic α-cell function.

Ampofo Emmanuel E, Wrublewsky Selina S, Laschke Matthias W MW

Although sex is a critical biological variable determining physiology, disease risk and therapeutic responses, it remains underrepresented in biomedical research. While sex-dependent differences are well established in cardiovascular and metabolic diseases, their impact on glucagon biology is less understood. Glucagon is the key counter-regulatory hormone to insulin and plays a central role in glucose homeostasis by regulating hepatic glucose production. To date, only a limited number of studies have addressed sex-specific differences in glucagon plasma levels, secretion and α-cell function, indicating that females tend to exhibit a higher glucagon secretion. For the first time, this review summarizes the current literature on glucagon biology suggesting a sex-biased regulation of α-cell activity.

PMID 42719565
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PubMedFrontiers in physiology2026-09-10

Aberrant hepatic glycogenolysis and elevated insulin clearance can lead to major glucose irregularities in type 2 diabetes: insights from system identification.

Wang Chengcheng C, Kanaley Jill A JA, Chen Junqing J, Tan Jinglu J

Complex interactions obscure the behavior of the glucose regulation processes as a system, hampering advances in diabetes care. We synthesized the current understandings of pancreatic hormones, glucose transporters, and glycogen metabolism into a model structure of biochemical reactions and mass transport. The model structure was then used as a soft sensor or filter to computationally extract system characteristics (model coefficients) from experimental measurements. Changes in coefficient values were analyzed to observe system differences among non-obese (n=18), obese (n=18), and type 2 diabetic (n=16) individuals under three conditions: none, morning, and post-dinner exercise. The model structure captures the major kinetics in blood glucose, insulin, and glucagon and the extracted coefficient values revealed metabolic differences and impairments. Relative to the non-obese group, the obese group showed impaired glucagon clearance (47% reduction) and reduced insulin sensitivity for glycogenesis, while the diabetic group exhibited elevated glucagon sensitivity (2.4-fold increase) and an aberrant effect of glycogen on glycogenolysis, which was associated with dysregulated hepatic glucose production and rising glucose during fasting. Parameter sensitivity analysis identified insulin clearance as a dominant factor in endogenous glucose production and fasting glucose level. Exercise effects varied: post-dinner exercise enhanced hepatic glycogen synthesis and hepatic sensitivity to glucose in non-obese individuals, while morning exercise improved muscle glucose uptake in the groups with obesity and type 2 diabetes. Derivation of the model structure and its application as a soft sensor elucidate the complex metabolic interactions underlying diabetes and provide a method to generate hypothesis for future research.

PMID 42719083
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PubMedIntestinal research2026-09-10

Comparative outcomes for tirzepatide versus glucagon-like peptide-1 receptor agonists in patients with inflammatory bowel disease: a national propensity matched study.

Patel Krishan S KS, Fakhoury Butros B, Parmar Kavin K, Jahagirdar Vinay V et al.

Evidence suggests glucagon-like peptide-1 receptor agonists (GLP-1RAs) may improve disease-specific outcomes for inflammatory bowel disease (IBD). Tirzepatide, a dual GLP-1 and glucose-dependent insulinotropic polypeptide receptor agonist, may offer additional benefits. We compared clinical and safety outcomes among patients with IBD treated with tirzepatide versus GLP-1RAs. Patients aged ≥ 18 years with IBD were identified within a retrospective multiinstitutional U.S. database who were prescribed tirzepatide or GLP-1RA between May 2022 and January 2025. Propensity score matching (1:1) was performed for demographics, comorbidities, and IBD medications. Outcomes were assessed over 18 months and included intravenous (IV) steroid use, intestinal surgery, emergency department visits, hospitalization, and a composite of IV steroids and surgery. Adverse outcomes were assessed. After matching, 3,042 patients (mean age, 54.6 years; 71.3% female) were analyzed in each cohort. Median follow-up was 540 days (interquartile range, 478-540 days) for tirzepatide versus 540 days (interquartile range, 540-540 days) for GLP-1RA. Patients taking tirzepatide had a significantly reduced risk of IV steroid use (adjusted hazard ratio [aHR], 0.81; 95% confidence interval [CI], 0.68-0.94) and composite IBD outcomes (aHR, 0.86; 95% CI, 0.73-0.97) with similar risk of hospitalization, emergency department visit and receipt of intestinal surgery. In patients with ulcerative colitis specifically, tirzepatide was similarly associated with a reduced risk of IV steroid use (aHR, 0.82; 95% CI, 0.69-0.97). Adverse outcome risks were similar. Patients with IBD prescribed tirzepatide may have lower risk of IV steroid use compared to those taking GLP-1RAs. Prospective studies are warranted to validate these results and explore underlying mechanisms.

PMID 42717572
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PubMedJournal of medicinal chemistry2026-09-10

Mechanistic Basis and Therapeutic Potential of a Novel TXNIP Inhibitor in Diabetes Treatment.

Luo Zhikuan Z, Han Jun J, Zhong Tao T, Tian Qiong Q et al.

Recently, inhibiting thioredoxin-interacting protein (TXNIP), a protein that plays critical roles in glucose metabolism, has emerged as a promising therapeutic strategy for diabetes. Through screening a compound library using a TXNIP reporter system, we identified an orally bioavailable small molecule (SKL-1223) that exhibits an excellent safety profile and potent glucose-lowering effects in streptozotocin-induced and db/db murine models. Notably, SKL-1223 promotes beta-cell formation and loss of alpha-cells in these disease models. Mechanistic studies indicate that SKL-1223 ameliorates hyperglycemia by directly modulating TXNIP transcription through attenuation of transcription factor binding. Compared with current therapies, SKL-1223 demonstrates improved efficacy in suppressing glucagon-mediated hepatic gluconeogenesis in diabetes treatment. Together, our findings not only identify a novel TXNIP inhibitor for controlling glucose production but also position SKL-1223 as a first-in-class therapeutic candidate addressing an unmet need in diabetes management.

PMID 42720460
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PubMedThe British journal of cardiology2026-09-10

GLP-1 receptor agonists in cardiovascular disease: a guide for cardiologists.

Ayton Sarah L SL, Papamargaritis Dimitris D, Davies Melanie J MJ, McCann Gerry P GP et al.

Obesity is a global epidemic, which, directly and indirectly, contributes to almost all cardiovascular diseases, including atherosclerotic cardiovascular disease, heart failure and atrial fibrillation. Reduction of weight is associated with substantial improvements in cardiometabolic risk factors, including blood pressure and glycaemic control, with over 10% weight loss required to see improvement in rates of major adverse cardiovascular events. Glucagon-like peptide-1 (GLP-1) receptor agonists have changed the landscape of type 2 diabetes and obesity management, showing significant benefit in glycaemic control and weight loss. Their potential for cardiovascular benefits means that they will likely have a central role in the management of patients with obesity-related cardiovascular diseases. This review summarises currently available GLP-1-based pharmacotherapies and highlights recent trials demonstrating cardiovascular benefits, and also provides practical guidance for patient selection, available agents, their initiation and patient monitoring. This will serve as an aid for cardiovascular clinicians, who will inevitably encounter patients suitable for, or already using, these drugs in their daily practice.

PMID 42719822
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PubMedJCEM case reports2026-09-10

Metastatic proinsulin-secreting tumor: a rare cause of persistent hypoglycemia.

Heins Robert J RJ, Yazji John J, Eber Philip P, Furlan Stefanie S

Proinsulin-secreting neuroendocrine tumors (NETs) are a rare cause of severe hypoglycemia, characterized by normal or low insulin levels and disproportionate elevations of proinsulin. Clinical features and optimal management of unresectable cases remain poorly defined, in part due to such few cases described in the literature. We describe a 47-year-old female with metastatic large-cell neuroendocrine carcinoma who presented with obstructive jaundice and was incidentally found to have profound, asymptomatic fasting hypoglycemia. Initial insulin and C-peptide levels were within reference ranges, but proinsulin concentrations were markedly elevated. The patient developed recurrent, refractory hypoglycemia requiring high-dose corticosteroids, glucagon, diazoxide, octreotide, and ultimately central-line infusion of 70% concentrated dextrose via total parenteral nutrition. Glycemic control could not be achieved despite maximal medical therapy, and the patient experienced rapid clinical deterioration leading to comfort-focused hospice management. This case highlights the diagnostic challenges of proinsulin-driven hypoglycemia and underscores the need for earlier recognition and improved treatment pathways for patients with proinsulin-secreting NETs.

PMID 42719453
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