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sitagliptin phosphate + ipragliflozin L-proline (Sujanu / MK0431J)

✓ Approved

Kotobuki Pharmaceutical Co., Ltd. · DPP4 · 小分子

什么是 sitagliptin phosphate + ipragliflozin L-proline？

sitagliptin phosphate + ipragliflozin L-proline 是一种小分子，由Kotobuki Pharmaceutical Co., Ltd.研发。该药已获批，用于治疗相关适应症，给药途径：Oral (PO)。

药物档案

商品名Sujanu, MK0431J
公司Kotobuki Pharmaceutical Co., Ltd.
药物类别小分子
分子靶点DPP4, SLC5A2
给药途径Oral (PO)
状态Approved
来源： ClinicalTrials.gov, Kotobuki Pharmaceutical Co., Ltd.

作用机制

分子靶点

sitagliptin phosphate + ipragliflozin L-proline 作用于 2 个分子靶点：

DPP4dipeptidyl peptidase 4 (CD26, DPPIV)
SLC5A2solute carrier family 5 member 2 (SGLT2)
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

sitagliptin phosphate + ipragliflozin L-proline 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

PubMedPharmaceuticals (Basel, Switzerland)2026-10-27

Bioequivalence Assessment of Sitagliptin/Metformin Extended-Release Fixed-Dose Combinations in Healthy Mexican Subjects Under Fasting and Fed Conditions.

Hernández Piña Omar Emmanuel OE, de la Cruz Cruz Porfirio P, Guido Ávila Erika Gabriela EG, Martínez Muñoz Alberto A et al.

Background/Objectives: Management of Type 2 Diabetes (T2D) frequently requires combination therapy. Fixed-dose combinations (FDCs) of sitagliptin and extended-release (ER) metformin improve therapeutic adherence but pose biopharmaceutical challenges related to matrix robustness and food-drug interactions. This study evaluated the pharmacokinetics and bioequivalence of two generic sitagliptin/metformin ER FDCs (50/1000 mg and 100/1000 mg) versus reference products under fasting and fed conditions in healthy Mexican subjects. Methods: Four independent, randomized, open-label, two-period, single-dose crossover studies were conducted. We enrolled 184 healthy subjects (46 per study) with a 7-day washout period. Plasma concentrations of sitagliptin and metformin were quantified using a validated LC-MS/MS method. Results: The 90% confidence intervals for the geometric mean ratios (Test/Reference) of Cmax, AUC0-t, and AUC0-∞ for both analytes fell entirely within the 80.00-125.00% bioequivalence acceptance range across all studies. Under fed conditions, prolonged tmax and the absence of concentration spikes confirmed ER matrix preservation, with no evidence of food-induced dose dumping. The safety profile was highly favorable; all adverse events were mild or moderate and completely resolved without sequelae. Conclusions: The evaluated generic sitagliptin/metformin ER FDCs demonstrated pharmacokinetic bioequivalence to the reference products under fasting and fed conditions. These findings meet stringent regulatory requirements (NOM-177-SSA1-2013), support pharmacokinetic bioequivalence as the regulatory basis for safe therapeutic interchangeability, and provide robust, region-specific clinical data for the Latin American population. ClinicalTrials.gov identifiers: NCT07763899, NCT07763912, NCT07763951, and NCT07763964.

PMID 42943229
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PubMedDiabetes, obesity, and cardiometabolic CARE2026-10-27

Comparative Effectiveness of Individual DPP-4 Inhibitors on Kidney Outcomes in Type 2 Diabetes With Moderate Cardiovascular Risk: A Target Trial Emulation.

Sklepinski Stacey M SM, Herrin Jeph J, Neumiller Joshua J JJ, Polley Eric C EC et al.

To examine kidney disease outcomes associated with dipeptidyl peptidase 4 inhibitors (DPP-4i). In this target trial emulation, claims data from enrollees in commercial, Medicare Advantage, and traditional Medicare health plans were used to identify adults ≥21 years old with type 2 diabetes, with moderate cardiovascular risk, and without stage 3 or worse chronic kidney disease (CKD) initiating alogliptin, linagliptin, saxagliptin, or sitagliptin between 2014 and 2021. The primary outcome was a composite of incident CKD stages 3-5, kidney failure, or kidney replacement therapy. Random treatment assignment was emulated using propensity scores, estimated using the super learner ensemble method and incorporated as inverse probability of treatment weights into proportional hazards models. The weighted study cohort included 3,026 individuals starting alogliptin, 38,213 starting linagliptin, 14,934 starting saxagliptin, and 115,091 starting sitagliptin. One year after treatment initiation, the primary outcome occurred in 1.4%, 2.7%, 2.2%, and 2.4% of patients initiating alogliptin, linagliptin, saxagliptin, and sitagliptin, respectively, increasing to 3.2%, 6.2%, 5.0%, and 5.4%, respectively, at 3 years. Alogliptin was associated with lower risk of stage 3 or worse CKD than linagliptin (hazard ratio [HR] 0.50; 95% CI 0.37-0.69), saxagliptin (HR 0.63; 95% CI 0.45-0.86), and sitagliptin (HR 0.58; 95% CI 0.42-0.79), while saxagliptin was associated with lower risk than linagliptin (HR 0.80; 95% CI 0.73-0.87). Conversely, linagliptin was associated with higher risk than sitagliptin (HR 1.15, 95% CI 1.10-1.21). Alogliptin was associated with lower risk of moderate-to-severe kidney disease than other DPP-4i, while linagliptin was associated with higher risk. Limitations include lack of laboratory data and potential unmeasured confounding.

PMID 42935587
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PubMedPlants (Basel, Switzerland)2026-10-27

SAMDC Activity Is Involved in the Melatonin-Mediated Tolerance of Barley (Hordeum vulgare L.) Seedlings to Osmotic Stress.

Chang Yunxia Y, Yu Jinming J, Hua Congmin C, Liu Huaipan H

Exogenous melatonin can elevate the tolerance of plants to drought stress. The mechanism of melatonin-mediated tolerance has been extensively studied. Numerous studies have shown that melatonin treatment can increase contents of osmotic adjustment substances, alleviate oxidative damage, and maintain photosynthetic characteristics of plants under drought stress. However, a research gap remains, i.e., whether melatonin plays the above-mentioned functions by regulating polyamine metabolism. In the present study, S-adenosylmethionine decarboxylase (SAMDC) activity and the levels of spermine and spermidine were detected in melatonin-treated barley (Hordeum vulgare L.) seedlings under polyethylene glycol-6000, which was used to simulate drought stress. The aim was to probe whether polyamine metabolism was involved in the process of melatonin-mediated osmotic stress tolerance. The results indicated that exogenous melatonin improved the tolerance of barley seedlings to osmotic stress, coupled with increasing content of proline, alleviating oxidative damage and maintaining the photosynthetic characteristics of barley seedlings. More importantly, melatonin elevated the activity of SAMDC, and thereby the contents of spermine and spermidine. Thus, it was speculated that melatonin functioned by regulating polyamine metabolism. The hypothesis was further reinforced by the results of inhibitor experiments. Inhibitor methylglyoxal-bis (guanylhydrazone), which can inhibit SAMDC activity strongly and specifically, not only inhibited the melatonin-induced increases in the activity of SAMDC and the levels of spermine and spermidine, but also inhibited melatonin-induced increases in antioxidant ability, proline content, and photosynthetic capacity. The relationship between SAMDC activity and the effects of melatonin on proline content, antioxidant ability, and leaf photosynthetic characteristics was further explored and is discussed below. Therefore, it could be concluded that SAMDC might be involved in the melatonin-mediated tolerance of barley (Hordeum vulgare L.) seedlings to osmotic stress.

PMID 42943068
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PubMedPhysical chemistry chemical physics : PCCP2026-10-27

Probing chiral chromatography systems in vacuo: cryogenic ion trap laser spectroscopy of diastereomeric copper(II)-proline-tyrosine complexes.

Vo Kien X KX, Izu Tomonori T, Hirata Keisuke K, Fujii Masaaki M et al.

The copper(II)-proline-L-tyrosine and copper(II)-proline-D-tyrosine complex ions, denoted as LL and LD, play an important role in chiral ligand-exchange chromatography (CLEC). These singly charged complexes, containing one neutral and one anionic amino acid ligand, have been isolated in a cryogenic ion trap and characterised by laser spectroscopy in the 3 µm and fingerprint regions. The two diastereomers can be clearly differentiated by their vibrational spectra. Two different isomers for LL and three for LD are deduced from IR-IR hole burning spectra. Quantum chemical calculations show that LL and LD both exist in two square planar structures involving deprotonation of Tyr for one of them or Pro for the other. Although similar in nature, the corresponding LL and LD structures differ by the relative position of the Tyr aromatic ring and the Pro ring, which are on the same side of the N/O⋯Cu⋯N/O plane for LL and on opposite sides for LD. They also differ by the puckering state, endo or exo, of the proline ring. In addition, the LD complex stands out by the presence of a kinetically trapped structure that contains Pro in its zwitterion form, with a very characteristic spectroscopic signature. This finding confirms the role of zwitterionic structures in the chemistry of copper clusters of amino acids.

PMID 42936903
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PubMedEnvironmental science and pollution research international2026-10-27

Phosphate-solubilizing bacteria enhance lead extraction efficiency by Artemisia annua L.: insights into detoxification, tolerance and mechanisms.

Zhang Yewen Y, Yuan Junjun J, Cheng Yuxin Y, Liu Xiang X et al.

Phosphate-solubilizing bacteria (PSB) combined with plants for heavy metal phytoextraction is a promising remediation strategy for lead (Pb)-contaminated soils, yet the intrinsic mechanisms remain not fully elucidated. Thus, this study inoculated the PSB strain Leclercia adecarboxylata L1-5 into the rhizosphere of Artemisia annua L. to investigate its regulatory effects on soil Pb extraction. The results showed that PSB inoculation significantly enhanced the Pb extraction efficiency of A. annua L., with a 96.72% increase compared to the control group. Additionally, the above-ground biomass and root biomass of A. annua L. increased by 51.39% and 155.22%, respectively. Chlorophyll a and chlorophyll b contents increased from 0.30 mg · g⁻1 FW and 0.44 mg · g⁻1 FW to 1.55 mg · g⁻1 FW and 1.50 mg · g⁻1 FW, respectively, with a 51.56% increase of the Ca/Cb ratio, suggesting that PSB improved plant growth and chlorophyll synthesis. Transmission electron microscopy revealed that PSB inoculation reduced ultrastructural damage of the plant leaves. Furthermore, the activities of key antioxidant enzymes-superoxide dismutase, catalase, and peroxidase-increased by 155.95%, 271.23%, and 192.55%, respectively, suggesting that PSB reduced Pb-induced oxidative stress in the plants. These findings provide new insights into the proof of the combined effect of PSB and A. annua L. and underscore their promising translational potential for the sustainable remediation of heavy metal-contaminated soils.

PMID 42934474
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PubMedPlants (Basel, Switzerland)2026-10-27

Concentration-Dependent Effects of Foliar Zinc Oxide Nanoparticles on Growth, Photosynthesis, Antioxidant Defence and Yield in Brassica juncea L.

Kouser Rizwana R, Shiraz Mohammad M, Zaidi Sameen S, Hayat Shamsul S et al.

Nanotechnology offers approaches to improve crop productivity through nutrient delivery. This study investigated the concentration-dependent effects of foliar-applied zinc oxide nanoparticles (ZnO-NPs) on growth, photosynthesis, antioxidant defense, redox homeostasis, and yield of mustard (Brassica juncea L.) ZnO-NPs were characterized by X-ray diffraction, Fourier transform infrared spectroscopy, and scanning electron microscopy, confirming a crystalline hexagonal wurtzite structure with a crystallite size of 29.3 nm and an aggregated morphology. Plants were treated with 25, 50, 75, or 100 mg/L ZnO-NPs and evaluated at 30 and 45 days after sowing, with yield assessed at harvest. Responses were concentration-dependent, with 50 mg/L producing the greatest benefits. This treatment enhanced growth, biomass, SPAD index, leaf area, gas exchange, PSII efficiency, carbohydrate and protein accumulation, antioxidant enzyme activities, leaf elemental composition, and yield traits. It also reduced reactive oxygen species, malondialdehyde, and electrolyte leakage while increasing proline and glutathione, indicating improved redox balance and membrane stability. Among the concentrations tested, 50 mg/L ZnO-NPs produced the most consistent beneficial response under the present experimental conditions, whereas the magnitude of these effects declined at 75 and 100 mg/L. These findings highlight the significance of concentration optimization while considering the use of ZnO-NPs as foliar treatment in B. juncea for Zn fertilization. Nevertheless, further comparative studies using conventional Zn fertilizers are necessary to determine whether the observed responses are specifically associated with the nanoscale properties of ZnO-NPs or are primarily attributable to Zn nutrition.

PMID 42943130
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