Sanofi S.A · KCNJ11 · 小分子
glimepiride + metformin 是一种小分子，由Sanofi S.A研发。该药已获批，用于治疗相关适应症，给药途径：Oral (PO)。
| 商品名 | HOE490 O, HOE4900, Amaryl M IR |
| 公司 | Sanofi S.A |
| 药物类别 | 小分子 |
| 分子靶点 | KCNJ11, ABCC8 |
| 给药途径 | Oral (PO) |
| 状态 | Approved |
glimepiride + metformin 作用于 2 个分子靶点：
| KCNJ11 | potassium inwardly rectifying channel subfamily J member 11 (BIR, HHF2) |
| ABCC8 | ATP binding cassette subfamily C member 8 (MRP8, SUR1delta2) |
glimepiride + metformin 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 disorders | Type 2 diabetes mellitus | ✓ Approved |
Bujdei-Tebeică Ioana I, Pantea-Stoian Anca Mihaela AM, Mihai Doina Andrada DA, Ștefan Simona Diana SD et al.
In the original publication [...].
Zhao Yutong Y, Wang Sheng S, Zhou Luoling L, Xu Yuanyuan Y et al.
Pharmaceuticals and personal care products (PPCPs) are widespread environmental contaminants, but their associations with kidney function and lipid metabolism remain incompletely understood. This study included 2758 adults aged ≥ 60 years in Anhui Province, China, during 2022-2023 and used a cross sectional design. Urinary concentrations of 48 PPCPs and two metabolites were measured using high-performance liquid chromatography-tandem mass spectrometry. Estimated glomerular filtration rate (eGFR) was calculated using the Chronic Kidney Disease Epidemiology Collaboration equation. Individual associations were assessed using logistic and linear regression, and mixture associations using weighted quantile sum (WQS) regression and Bayesian kernel machine regression. Restricted cubic splines examined nonlinear associations, and exploratory mediation analyses assessed the statistical contribution of high-density lipoprotein cholesterol (HDL-C). Among nine PPCPs with detection frequencies > 50%, doxycycline, enrofloxacin, acetaminophen, metformin, and cotinine were associated with lower eGFR after full adjustment and Benjamini-Hochberg correction. Coefficients ranged from - 3.00 to - 0.93 mL/min/1.73 m2 per tenfold increase in urinary concentration. Tylosin and caffeine were positively associated with eGFR. The WQS index was inversely associated with eGFR, with metformin receiving the largest weight. HDL-C showed a positive nonlinear association with eGFR. Under the mediation model assumptions, HDL-C statistically accounted for 12.21-29.30% of the associations involving enrofloxacin, metformin, and acetaminophen, and 13.78% of the mixture association. The indirect association for cotinine was nonsignificant. These findings remain exploratory. Prospective studies are needed to clarify temporal relationships and address possible reverse causation.
Zhang Yilin Y, Cao Jie J, Yan Yong Y, Li Zhaoyang Z et al.
Bacterial-infected skin wounds, especially those caused by drug-resistant pathogens accompanied by persistent inflammation, remain a major clinical therapeutic challenge. Rising antimicrobial resistance compromises the therapeutic effect of conventional single-agent antibiotics, creating an urgent demand for novel wound therapeutics that integrate bactericidal potency, immunomodulation and tissue regeneration capacity. In this work, an injectable multifunctional chitosan-based hydrogel (C@MC) was developed, which simultaneously incorporates metformin hydrochloride (as a potential antibiotic adjuvant) and cefazolin sodium (as a β-lactam class antibacterial drug). The optimized C@MC possesses interconnected three-dimensional pores with an initial storage modulus of ~0.83 kPa (C@MC360), featuring desirable mechanical strength, injectability, tissue adhesion and dual pH/glucose-responsive sustained drug release. In vitro evaluations revealed the dose-dependent bactericidal activity of C@MC against Staphylococcus aureus (S. aureus), Escherichia coli (E. coli) and New Delhi metallo-β-lactamase-1-producing E. coli (NDM-1 E. coli, resistant bacteria). The highest drug-laden group nearly eliminated all wound bacteria in vitro. It scavenged reactive oxygen species (ROS) to lower cellular MDA levels and suppress pro-inflammatory TNF-α and IL-6 in LPS-stimulated RAW 264.7 macrophages. In full-thickness mouse wounds infected with NDM-1 E. coli, C@MC360 achieved nearly complete wound closure, with only a 4.2% residual wound area on day 14, accompanied by suppressed inflammatory infiltration and accelerated wound regeneration. This dual-drug hydrogel integrates antibiotic potentiation, anti-inflammation and antioxidation, providing an intervention regimen for skin wounds infected with drug-resistant bacteria.
Lizbelt Mugivhisa Liziwe ML, Faith Baloyi Khanyi BK, Oladeji Oluwaseun Mary OM, Olatunji Olatunde Stephen OS et al.
Background/Objectives: Pharmaceutical residues in human urine have raised serious concerns about the safe reuse of urine in agriculture. The current study investigates and compares the concentrations of pharmaceuticals in urine samples collected from male patients undergoing active antiretroviral regimens and self-reported "healthy individuals" at a government hospital in Pretoria, South Africa, and determines how the residues changed during three months of ambient storage, which is the usual recommendation before use in agriculture. Methods: The urine samples were collected in a plastic bottle to prevent fecal contamination, and 15 targeted compounds were analyzed using solid-phase extraction and liquid chromatography-mass spectrometry. The linearity ranged from 0.9910 to 0.9999, 75.5% to 99.1% for recovery, and intra-day and inter-day precision were below 6%. The urine from each group was collected into one pooled sample and then analyzed both pre- and post-storage. Results: Thirteen pharmaceuticals were detected in urine from patients on regular medication before storage; in "healthy individuals", detections rose from eight to twelve after storage. Concentrations in the composite samples after storage were higher for some of the compounds but lower for others, including caffeine, nevirapine, prednisolone and 17α-ethinylestradiol. Metformin was highest overall at 1186.25 µg/L and remained at 806.68 µg/L after storage. The highest concentration for all the pharmaceuticals was reported for metformin, with a value of 1186.25 µg/L, occurring in the group of patients on a regular regimen. There could be a possibility that the rise can be attributed to the hydrolysis of conjugated metabolites during storage; however, no analysis of conjugates was carried out. Conclusions: This study shows the need for appropriate treatment of human urine prior to its reuse as fertilizer and echoes the importance of further research into human exposure pathways and effective pharmaceutical removal strategies.
Broulikova Hana M HM, van der Wel Anne W T AWT, Rademaker Doortje D, de Wit Leon L et al.
To assess the cost-effectiveness of treatment with sequential oral antihyperglycemic agents (OHA; metformin and glibenclamide) versus insulin for gestational diabetes (GDM). Cost-effectiveness analysis from a societal and healthcare perspective alongside a randomized controlled trial (SUGAR-DIP). Twenty-five hospitals in the Netherlands. Women with GDM and a singleton pregnancy, randomized to OHA (n = 409) or insulin (n = 411) between 16 to 34 weeks' gestation. Missing data were handled using multiple imputation. Differences in costs and effects were estimated using bivariate regression with bootstrapping to derive incremental cost-effectiveness ratios. Cost-effectiveness acceptability curves were constructed across a range of willingness-to-pay (WTP) thresholds. Large for gestational age (LGA), quality-adjusted life-years (QALYs), costs and cost-effectiveness. OHA slightly increased QALYs (0.009; 95% CI 0.004 to 0.014), corresponding to approximately 3 days in perfect health. There were no statistically significant differences in LGA avoided (-0.039; 95% CI-0.097 to 0.018) or societal costs (mean difference-€1004; 95% CI-€3503 to €1495). OHA were less costly and less effective than insulin for LGA, whereas for QALYs they were less costly and more effective. The probability of OHA being cost-effective at a WTP threshold of €0 was 79% for both outcomes. OHA have a high probability of being cost-effective compared with insulin for QALYs, although the QALY gain is small and of limited clinical relevance. For LGA, OHA were less costly but less effective, and cost-effectiveness depends on acceptable trade-offs between costs and neonatal outcomes.
Devane Declan D, Fitzgerald Mary M, O'Donnell Martin M, Alvarez-Iglesias Alberto A et al.
To assess whether initiating metformin at 25 weeks' gestation influences exclusive breastfeeding at 12 weeks postpartum in gestational diabetes mellitus (GDM). We performed a prespecified secondary analysis of the Effectiveness of Metformin in Addition to Usual Care in the Reduction of Gestational Diabetes Effects (EMERGE) trial, a multicenter, double-blind, placebo-controlled randomized study. A total of 535 pregnant women (510 with newly diagnosed GDM) were allocated 1:1 to metformin (titrated to 2.5 g/day) or placebo alongside usual care. Infant feeding was prospectively documented at birth and at 4 and 12 weeks postpartum. The primary outcome was exclusive breastfeeding at 12 weeks (intention to treat). Multivariable logistic regression adjusted for race, education, smoking, booking BMI, health care access markers, and diagnostic oral glucose tolerance test (OGTT) glucose levels. Twelve-week feeding data were available for 476 pregnancies (236 in the metformin group and 240 in the placebo group). Exclusive breastfeeding at 12 weeks was 27% with metformin and 26% with placebo (absolute difference +1.3%; 95% CI -6.3 to 8.7; P = 0.75). The adjusted odds ratio (OR) for metformin versus placebo was 1.24 (95% CI 0.79-1.96; P = 0.36). Feeding patterns shifted from breastfeeding to formula temporally in both groups (P < 0.001), with no treatment-by-time interaction (P = 0.61). Non-Caucasian ethnicity independently predicted exclusive breastfeeding (adjusted OR 2.37; 95% CI 1.27-4.42). Starting metformin treatment at 25 weeks in the GDM group was not associated with differences in exclusive breastfeeding at 12 weeks postpartum. Where metformin was discontinued at delivery, the results support compatibility of antenatal metformin with breastfeeding objectives. Breastfeeding outcomes were more linked to sociodemographic factors than metabolic ones, highlighting the need for culturally appropriate postpartum support.
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