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exenatide (exenatide LAR / AC 2993 LAR / Bydureon Pen)

✓ Approved

3SBio · GLP1R · 小分子

什么是 exenatide？

exenatide 是一种小分子，由3SBio研发。该药已获批，用于治疗相关适应症，给药途径：Injectable (Others)、Intradermal Injection、Subcutaneous Injection。

药物档案

商品名exenatide LAR, AC 2993 LAR, Bydureon Pen
公司3SBio
药物类别小分子, 多肽类
分子靶点GLP1R
给药途径Injectable (Others), Intradermal Injection, Subcutaneous Injection
状态Approved
来源： ClinicalTrials.gov, 3SBio

作用机制

分子靶点

exenatide 作用于 1 个分子靶点：

GLP1Rglucagon like peptide 1 receptor (GLP-1R, GLP-1-R)
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

exenatide 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 disordersType 2 diabetes mellitus✓ Approved

相关研究文献

PubMedThe Journal of clinical endocrinology and metabolism2026-10-26

Efficacy and Safety of Lonapegsomatropin in Children With Turner Syndrome: 52-Week Results From the New InsiGHTS Trial.

Davis Shanlee M SM, Abuzzahab M Jennifer MJ, Tryggestad Jeanie B JB, Fechner Patricia Y PY et al.

Treatment with growth hormone is effective in improving height outcomes in children with Turner syndrome. However, poor adherence-often influenced by daily injection burden-may compromise treatment outcomes. Lonapegsomatropin is a prodrug, administered once weekly, that provides sustained release of somatropin. To evaluate the efficacy and safety of lonapegsomatropin in children with Turner syndrome. New InsiGHTS is a phase 2 dose-ranging trial (ClinicalTrials.gov: NCT05690386). This trial was conducted across 19 centers in the United States. This trial enrolled and dosed 49 prepubertal children with Turner syndrome. Randomization was 1:1:1:1 to receive once-weekly lonapegsomatropin (0.24, 0.30, or 0.36 mg hGH/kg/week) or daily somatropin (0.35 mg/kg/week). The primary efficacy endpoint was annualized height velocity (AHV) at week 26. Secondary efficacy endpoints included AHV at week 52 and change from baseline in height standard deviation score (SDS) at weeks 26 and 52. At week 26, AHV was comparable between lonapegsomatropin starting dose cohorts (range: 9.23 to 10.36 cm/year) and the somatropin cohort (10.86 cm/year). At week 52, AHV was comparable between pooled lonapegsomatropin cohorts (9.05 cm/year) and the somatropin cohort (9.04 cm/year), with mean gains in height SDS of 0.60 and 0.67, respectively. Lonapegsomatropin was well tolerated with a safety profile similar to somatropin. Across evaluated doses, lonapegsomatropin treatment demonstrated comparable efficacy, safety, and tolerability to somatropin after 1 year, supporting development of lonapegsomatropin as a once-weekly treatment option for short stature in children with Turner syndrome.

PMID 42929032
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PubMedHepatology (Baltimore, Md.)2026-10-26

Phase 1b study of miricorilant in patients with presumed metabolic dysfunction-associated steatohepatitis (MASH).

Alkhouri Naim N, Rudraraju Madhavi M, Leibowitz Mark M, Jenders Robert A RA et al.

Miricorilant, an oral nonsteroidal selective glucocorticoid receptor modulator, is being investigated as a therapy that modulates hepatic cortisol activity in patients with metabolic dysfunction-associated steatohepatitis (MASH). This phase 1b study evaluated miricorilant's efficacy and safety. Seventy patients with presumed MASH received oral miricorilant daily (30-150 mg) or intermittent (100-200 mg once, twice, or thrice weekly) dosing regimens for 12 or 24 weeks. Across dosing regimens, reductions in relative liver fat content (LFC) ranged from 10.1% to 76.6%. Improvements in MASH liver function markers and the enhanced liver fibrosis (ELF) score were observed across regimens. Treatment-emergent adverse events (TEAE) leading to drug interruption/discontinuation occurred in 12.9% of patients (n=9) each; most were due to aminotransferase elevations during an excessively rapid drop in LFC (up to 70.2% at week 6) and in patients receiving daily dosing. Intermittent dosing enabled more patients to complete 12 weeks of treatment without discontinuation due to TEAEs. Intermittent dosing with miricorilant 100 mg twice weekly had the best benefit-risk profile; this cohort demonstrated a mean LFC reduction of 28.2% at week 12, with a corresponding decline in liver enzymes (ALT, -3.8 U/L; AST, -6.0 U/L). Patients in this cohort also had numerical improvement in lipid profiles, glycemic markers, and fibrosis biomarkers. Intermittent miricorilant dosing of 100 mg twice weekly achieved meaningful reductions in LFC and improved liver health markers with a favorable safety profile. This regimen is being evaluated in the phase 2b MONARCH study (NCT06108219).

PMID 42929711
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PubMedCureus2026-10-26

IcoSema in Weight Management and Glycaemic Control: A Systematic Review and Meta-Analysis.

Nouh Mahmoud Ismail MI, Karrar Hani Raka HR, AlButi Hala H, Alhendi Rehab Salah Aldin RSA et al.

IcoSema is a once-weekly, fixed-ratio injection that combines insulin icodec, a weekly basal insulin, with semaglutide, a glucagon-like peptide-1 (GLP-1) receptor agonist. It is intended to control fasting and post-meal glucose in a single weekly injection whilst limiting the weight gain and hypoglycaemia that accompany insulin therapy. Its pivotal trials each used a different comparison treatment, and the only previous pairwise synthesis pooled them into single estimates carrying extreme statistical heterogeneity. We therefore re-synthesised the randomised evidence using a comparator-specific approach. Eight sources (PubMed/MEDLINE, Embase, Scopus, Web of Science, Cochrane Central Register of Controlled Trials (CENTRAL), Cochrane Database of Systematic Reviews (CDSR), ClinicalTrials.gov, and citation searching) were searched from inception to September 5, 2026, for randomised controlled trials of IcoSema in adults with type 2 diabetes. Two reviewers independently screened records, extracted data, and applied Cochrane Risk of Bias 2. Covariate-adjusted treatment differences were combined by random-effects inverse-variance meta-analysis, stratified by comparator class, with an exploratory all-comparator pool retained for comparison only and certainty rated with GRADE. Four phase 3 trials (3,138 participants) were eligible: COMBINE 1, 2, 3 and 4. Against basal insulin alone (COMBINE 1 and 4; two trials, 1,776 participants), IcoSema lowered HbA1c by 0.74 percentage points (95% confidence interval (CI) -0.95 to -0.53; I² = 63%), reduced body weight by 5.15 kg (95% CI -6.10 to -4.19; I² = 70%), and reduced clinically significant or severe hypoglycaemia (rate ratio 0.35, 95% CI 0.14 to 0.87; I² = 84%). Against semaglutide alone (COMBINE 2; single trial), IcoSema lowered HbA1c by a further 0.44 percentage points (95% CI -0.56 to -0.33), but body weight was 4.54 kg higher (95% CI 3.84 to 5.23), with no significant difference in hypoglycaemia. Against daily basal-bolus insulin (COMBINE 3; single trial), IcoSema met non-inferiority for HbA1c (-0.06 percentage points, 95% CI -0.22 to 0.09), reduced body weight by 6.72 kg (95% CI -7.58 to -5.86), and reduced hypoglycaemia (rate ratio 0.12, 95% CI 0.08 to 0.17). Exploratory pooling across all comparators produced estimates with I² of 92%-99.5% that should not be read as an overall treatment effect. The effects of IcoSema on glycaemia, weight, and hypoglycaemia differ in size, and for body weight in direction, according to the regimen it is compared with; comparator-specific estimates, not a single pooled figure, should inform interpretation.

PMID 42928846
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PubMedCurrent oncology (Toronto, Ont.)2026-10-26

Cisplatin-Induced Ototoxicity in Head and Neck Cancer: A Systematic Review of Current Evidence, Clinical Implications, and the Need for Standardized Monitoring.

Mirabile Aurora A, Vukatana Alert A, Guizzardi Mathilda M, Vaccarello Giorgia G et al.

Background: Cisplatin-based chemoradiotherapy remains a standard treatment for locally advanced head and neck squamous cell carcinoma (HNSCC), but cisplatin-induced ototoxicity is common, usually irreversible and inconsistently monitored. Methods: MEDLINE, EMBASE and the Cochrane Library were searched for English-language clinical studies in adults published between January 2016 and January 2026. Primary full-text clinical studies reporting at least one hearing, tinnitus, vestibular or ototoxicity outcome were eligible; conference-only abstracts, duplicate reports, reviews and consensus papers were not. Twenty-four studies were retained from the original database route. A targeted supplementary PubMed verification performed on 16 September 2026 with broader auditory and vestibular terminology identified six additional eligible full-text studies, which were included through the PRISMA 2020 'other methods' pathway, for a total of 30 studies. Risk of bias was appraised for all 30 studies with RoB 2, ROBINS-I and Joanna Briggs Institute (JBI) tools by a single review author; duplicate independent appraisal was not performed and is reported as a limitation. Meta-analysis had been planned but was not undertaken because audiometric frequencies, grading systems, follow-up intervals and effect measures were not comparable; this is reported as a protocol deviation. Results: The 30 studies comprised approximately 10,500 participants, although two reports used overlapping Hungarian patient samples and several studies included non-HNSCC populations. Reported ototoxicity ranged from 13% (severe, irreversible loss after weekly cisplatin with cochlear-sparing radiotherapy) to 72% (screen-detected loss in a survivorship clinic), reflecting different definitions rather than a single underlying rate. Comparative HNSCC cohorts consistently reported more hearing loss with 100 mg/m2 every three weeks than with weekly 40 mg/m2. Ten of the 30 studies were at high, serious or critical risk of bias, with one additional comparative study at moderate-to-serious risk; the long-term randomized comparison reported inferior locoregional control with weekly 30 mg/m2. Baseline hearing, cochlear radiation exposure, monitoring adherence and pharmacogenetic susceptibility were further determinants. Objective vestibular dysfunction was documented in the absence of dizziness. No pharmacological otoprotective strategy is established in adults. Conclusions: Cisplatin ototoxicity is a core survivorship endpoint. Weekly dosing may reduce hearing toxicity in selected settings but must not be read as universal oncological equivalence. Standardized definitions, baseline and longitudinal testing, cochlear-dose reporting and prospective evaluation of vestibular outcomes and otoprotective agents are the priorities.

PMID 42930151
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PubMedCurrent oncology (Toronto, Ont.)2026-10-26

A New Era of Treatment Sequencing in Platinum-Resistant Ovarian Cancer: Integrating Immunotherapy, Antibody-Drug Conjugates, and Targeted Therapies.

Mabuchi Seiji S, Kusakabe Ai A, Takimoto Yumi Y

Platinum-resistant ovarian cancer (PROC) has historically been treated with sequential non-platinum chemotherapy, with bevacizumab added when appropriate. The therapeutic landscape has expanded with positive randomized phase III data for pembrolizumab plus weekly paclitaxel with or without bevacizumab (KEYNOTE-B96), mirvetuximab soravtansine (MIRV) in FRα-high disease (MIRASOL), and relacorilant plus nab-paclitaxel (ROSELLA). Trastuzumab deruxtecan (T-DXd) has also shown substantial activity in previously treated HER2-expressing ovarian cancer, although its ovarian cohort was small, nonrandomized, and not restricted to PROC. These trials enrolled different populations and do not establish a cross-trial efficacy hierarchy. We therefore review the development of immunotherapy leading to KEYNOTE-B96, compare newer strategies with established PROC treatments, distinguish phase III evidence from regulatory approval and routine availability, and propose an evidence-informed framework for treatment selection and sequencing. The framework prioritizes current treatment opportunity while accounting for biomarker eligibility, prior treatment, residual toxicity, treatment and financial burden, patient priorities, and the feasibility of later-line therapy.

PMID 42930189
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PubMedThe New England journal of medicine2026-10-26

Divarasib as Compared with Sotorasib or Adagrasib in KRAS G12C-Mutated NSCLC.

Skoulidis Ferdinandos F, Ahn Myung-Ju MJ, Gadgeel Shirish S, Popat Sanjay S et al.

Divarasib, a next-generation, oral KRAS G12C inhibitor, is more potent and selective in vitro than the first-generation KRAS G12C inhibitors sotorasib and adagrasib. In this phase 3, international, open-label trial, patients with previously treated KRAS G12C-mutated advanced or metastatic non-small-cell lung cancer (NSCLC) were randomly assigned to receive divarasib orally at a dose of 400 mg once daily or control treatment (sotorasib orally at a dose of 960 mg once daily or adagrasib orally at a dose of 600 mg twice daily) until the occurrence of disease progression, unacceptable adverse events, loss of clinical benefit, withdrawal of consent, death, or trial termination. The primary end point was progression-free survival as assessed by blinded independent central review. Secondary end points included overall survival, confirmed overall response, duration of response, patient-reported outcomes, and safety. A total of 338 patients received divarasib (167 patients) or control treatment (171 patients; 156 received sotorasib and 15 received adagrasib). The median follow-up was 14.3 months. The median progression-free survival was 9.8 months with divarasib and 5.7 months with control treatment (hazard ratio for disease progression or death, 0.58; 95% confidence interval [CI], 0.44 to 0.76; P<0.001). The median overall survival was 17.7 months with divarasib and 12.0 months with control treatment (hazard ratio for death, 0.56; 95% CI, 0.41 to 0.78; P<0.001). Of the 328 patients who could be evaluated for response, a confirmed response occurred in 58.4% in the divarasib group and in 32.3% in the control group. The median duration of response was 11.9 months with divarasib and 6.9 months with control treatment. Fewer grade 3 or 4 treatment-related adverse events were noted with divarasib (24.6%) than with control treatment (34.5%). Among patients with previously treated KRAS G12C-mutated advanced or metastatic NSCLC, divarasib led to significantly longer progression-free and overall survival than control treatment. (Supported by F. Hoffmann-La Roche; Krascendo 1 ClinicalTrials.gov number, NCT06497556.).

PMID 42929675
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