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leuprolide acetate (Leupronax)

✓ Approved

Nanox · GNRH1 · 小分子

什么是 leuprolide acetate？

leuprolide acetate 是一种小分子，由Nanox研发。该药已获批，用于治疗相关适应症，给药途径：Injectable (Others)、Intramuscular (IM) Injection。

药物档案

商品名Leupronax
公司Nanox
药物类别小分子, 多肽类
分子靶点GNRH1
给药途径Injectable (Others), Intramuscular (IM) Injection
状态Approved
来源： ClinicalTrials.gov, Nanox

作用机制

分子靶点

leuprolide acetate 作用于 1 个分子靶点：

GNRH1gonadotropin releasing hormone 1 (GNRH, LHRH)
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

leuprolide acetate 针对 4 个适应症，涉及 2 个治疗领域。

治疗领域疾病/病症分期
Neoplasms benign, malignant and unspecified (incl cysts and polyps)Breast cancer✓ Approved
Reproductive system and breast disordersEndometriosis✓ Approved
Neoplasms benign, malignant and unspecified (incl cysts and polyps)Prostate cancer✓ Approved
Reproductive system and breast disordersUterine fibrosis✓ Approved

相关研究文献

PubMedScience China. Life sciences2026-08-04

The maternal gut microbiota influences myocardial maturation and diastolic function of offspring in mice.

Li Shanshan S, Zhang Yiqiong Y, Li Yang Y, Lei Yuyang Y et al.

Although the maternal microbiome is recognized as a critical regulator of offspring physiology, its role in heart development and the pathogenesis of heart failure remains largely unclear. Using a germ-free (GF) mouse model, we demonstrated that maternal microbiota depletion leads to spontaneous heart failure with preserved ejection fraction (HFpEF) in adult female offspring, recapitulating the phenotypes of human diastolic dysfunction. Integrated transcriptomic and proteomic profiling of fetal hearts revealed impaired structural cardiomyocyte maturation in GF offspring, characterized by suppressed sarcomere assembly. Metabolomic analysis revealed that acetate was concurrently downregulated in maternal serum and fetal cardiomyocytes. Importantly, prenatal acetate supplementation and fecal microbiota transplantation rescued fetal cardiomyocyte maturation defects and prevented the onset of HFpEF in adult female offspring. Mechanistically, maternal microbe-derived acetate regulates fetal cardiomyocyte maturation by enhancing the levels of H3K9ac and H3K27ac in the MYL2 promoter region, thereby promoting the transcriptional enhancement of MYL2. This developmental reprogramming provides lifelong protection against diastolic dysfunction. In addition, the concentration of acetate in pregnant women's serum was positively correlated with myocardial thickness in the left ventricle of the fetus. Our findings establish maternal microbial metabolites as determinants of cardiac maturation and suggest prenatal acetate supplementation as a novel preventive intervention for developmental diastolic dysfunction.

PMID 42550453
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PubMedClinical pharmacology in drug development2026-08-04

Open-Label, Balanced, Randomized, Single-Dose, Three-Treatment, Three-Sequence, Three-Period, Three-Way Crossover Oral Bioequivalence Study of Desmopressin Acetate Oral Solution.

Christensen Adam A, Parth Axay A, Kotak Mansi M, Radosavjevic Danka D et al.

Desmopressin is first-line therapy for central diabetes insipidus, also known as arginine vasopressin deficiency, but presents dosing challenges due to its narrow therapeutic index. This open-label, randomized, three-way crossover study evaluated the bioequivalence of a new desmopressin acetate oral solution (50 mcg/mL) compared to desmopressin acetate tablets (200 mcg) in 75 healthy adults. In a balanced, three-sequence, three-period design with 14-day washout periods, participants received a single 600-mcg dose of test product and reference product under fasted conditions. Plasma desmopressin concentrations were measured using a validated liquid chromatography-electrospray ionization tandem mass spectrometry method, and primary pharmacokinetic parameters (maximum plasma concentration [Cmax], area under the plasma concentration-time curve from time 0 to the last measurable concentration [AUC0-t], AUC from time 0 extrapolated to infinity [AUC0-∞]) were derived from resulting concentration-time profiles. Bioequivalence was assessed using analysis of variance on log-transformed parameters, with 90% confidence intervals (CIs) for geometric mean ratios 80%-125%. Results demonstrated bioequivalence between formulations, with geometric mean ratios of 101.9% (93.9%-110.5%) for Cmax, 103.7% (94.8%-113.5%) for AUC0-t, and 103.7% (94.9%-113.3%) for AUC0-∞. Both formulations exhibited similar pharmacokinetic profiles with 1.0 h median time to maximum concentration, ∼3.6 h mean elimination half-life, and 30%-33% intrasubject variability. Five adverse events were reported by five participants (6.7%), including two cases of hyponatremia (reference group) and one case of vomiting (test group); all were mild to moderate and resolved completely. This study establishes bioequivalence between desmopressin acetate oral solution and tablets, supporting regulatory approval of the oral solution formulation.

PMID 42548160
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PubMedMaterials advances2026-08-04

Laser-induced carbonization of cellulose acetate for controlled carbon structure evolution.

Bisceglie Angelica A, Zaccagnini Pietro P, Baudino Luisa L, Fontana Marco M et al.

Biomass offers a low-cost and sustainable carbon source. Yet, conventional pyrolytic routes remain energy intensive and require harsh processing conditions. Laser-induced carbonization provides a rapid, efficient and green alternative for the conversion of biomass into carbon structures. Building on the growing demand for sustainable alternatives to petroleum-derived polymers in laser writing, we investigate laser-induced carbon (LIC) produced from cellulose acetate (CA) membranes, a widely available biopolymer, via CO2 laser irradiation. The flame-retardant bis[2-(methacryloyloxy)ethyl] phosphate (BMEP) enables localized carbonization, overcoming CA's poor thermal stability. By tuning laser parameters, namely the defocus distance and the number of passes, we selectively obtain amorphous carbon, activated carbon (AC), graphene oxide (GO), and laser-induced graphene (LIG). Among these, AC fabricated through a double-pass process at a defocus distance of 7.5 mm achieves outstanding electrochemical performance as a microsupercapacitor (μSC) electrode, delivering an areal capacitance of up to 63 mF cm-2, an energy density of 3.3 µWh cm-2, and a power density of 0.42 mW cm-2. These results outperform those of petroleum-based polymer-derived LIG while utilizing a potentially upcycled precursor. This work expands the scope of LIG precursors and offers a versatile platform for engineering sustainable carbon-based electrodes.

PMID 42549133
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PubMedInternational journal of pharmaceutics2026-08-04

A comparative study of the oxidative degradation of poloxamer 188, polysorbate 20 and polysorbate 80 in various buffered solutions.

Bollenbach Lukas L, Weber Johanna J, Schultz-Fademrecht Torsten T, Mäder Karsten K et al.

The importance of biologics has increased over the last few decades. Since proteins in liquid formulations tend to form protein particles in response to external stress factors, surfactants are added to prevent this. Currently, polysorbates (PSs) 20 and 80 are mainly used for this purpose. However, alternatives are being investigated, as PSs have stability issues, primarily due to oxidative or enzymatic degradation. The alternative that is discussed most frequently and already used in commercial biologics is poloxamer 188 (P188). However, this triblock copolymer, which consists of a polyoxypropylene block flanked by polyoxyethylene units, may also degrade through oxidative processes. Surprisingly, there are no direct comparative stability studies for PSs and P188. Therefore, the present study compared the oxidative degradation profiles of PS20 and PS80 with those of P188 in various relevant buffer systems. To this end, the formulations were subjected to stress in the form of 50 ppb (approximately 0.9 µM) of Fe2+ and light in the visible range, in line with their exposure during pharmaceutical production. Samples that received neither an iron spike nor light served as controls. The solutions contained 0.4 mg∙mL-1 PS20, PS80, or P188, respectively. The surfactants were formulated in either a 25 mM acetate, citrate, or histidine buffer solution (all pH 5.5) or in pure water. Significant differences were observed between these buffers, with greater effects at higher temperatures. The stability of the surfactant depended greatly on the buffer and the applied stress. All surfactants exhibited high rates of oxidative degradation when formulated in acetate buffer or pure water. PSs demonstrated the highest overall stability in citrate buffer, while P188 remained most stable in histidine, as well as in citrate buffer. However, both PSs exhibited instability in the presence of iron and light in histidine buffer, a phenomenon not observed in P188.

PMID 42546993
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PubMedRSC advances2026-08-04

Cu(ii) complex of a furoic acid-derived amide-imine conjugate for fluorescence detection of Th4+ with anticancer and molecular docking studies.

Changdar Sutapa S, Mitra Pritish P, Chatterjee Sabyasachi S, Suryakanta Uday U et al.

A furoic acid derived amide based imine derivative has been employed to prepare a copper complex (C2) which is characterized by different analytical as well as spectroscopic techniques and, structurally authenticated by SC-XRD analysis. The C2 is explored for selective detection of Th4+ in ethyl acetate medium via 'turn-on' fluorescence, following the metal ion displacement protocol. The associated binding constant and detection limit for Th4+ are 3.03 × 105 M-1 and 7.58 nM respectively. ESI-MS spectrum and Job's plot confirm 1 : 1 (mole ratio) stoichiometric interaction. The C2 shows cytotoxicity against human colon cancer cell lines such as HCT 116 and a breast cancer cell line, MCF 7 having IC50 values of 2.07 µM and 1.72 µM, respectively. Moreover, molecular docking studies unveil drug-like behavior, along with the mode of action of C2 towards retrieved proteins.

PMID 42549108
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PubMedJournal of dairy science2026-08-04

Integrated multi-omics analysis reveals the co-adaptive mechanisms between ruminal microbiota and host epithelium in water buffaloes under chronic heat stress.

Wu Yan-Zhi YZ, Yu Jin-Chi JC, Li Jian J, Yang Cheng-Jian CJ et al.

Chronic heat stress is a major environmental challenge constraining water buffalo (Bubalus bubalis) production, yet its mechanistic impacts on the ruminal ecosystem remain unclear. This study aims to systematically elucidate the coordinated changes in ruminal microbial structure and function, metabolome, and epithelial transcriptional responses in water buffaloes under chronic heat stress. Ten cannulated buffaloes (Nili-Ravi × Murrah) were used as experimental subjects and randomly assigned to 2 groups: one receiving fan and sprinkler cooling (NHS) and the other exposed to the natural environment (HS). This study aimed to analyze their apparent digestibility, ruminal fermentation parameters, and ruminal microbial community structure and function along with their metabolic characteristics, as well as to dissect the transcriptional responses of the rumen epithelium to chronic heat stress. Results showed that chronic heat stress did not significantly affect feed intake or apparent nutrient digestibility, but markedly altered ruminal fermentation and nitrogen metabolism, manifested as a reduced ammonia nitrogen (NH3-N) concentration (HS vs. NHS, 4.44 vs. 7.86 mg/dL), an increased proportion of acetate (HS vs. NHS, 68.86 vs. 66.74%), and a decreased proportion of propionate(HS vs. NHS, 20.40 vs. 22.14%). Chronic heat stress imposed selective pressure on the ruminal microbial community, driving functional changes at the microbial level. The overall abundance of multiple CAZyme families increased, enhancing the potential for structural carbohydrate degradation; concurrently, the abundance of genes encoding key enzymes for pyruvate-to-acetyl-CoA conversion rose, consistent with elevated acetate synthesis potential; enrichment of nitrogen metabolism-related genes suggested enhanced microbial ammonia assimilation capacity. At the metabolic level, chronic heat stress induced specific metabolite dynamics, including decreased phosphatidylcholine PC(16:0/18:1(9Z)) content and accumulation of the flavonoid metabolite naringenin, indicating co-activation of phospholipid hydrolysis and flavonoid metabolic pathways. At the host level, transcriptional changes in rumen epithelium were primarily reflected in reduced ion transport capacity and enhanced cellular stress protection. In summary, the adaptive response of water buffaloes to chronic heat stress is primarily driven by the functional plasticity of the ruminal microbiome, which maintains energy supply and metabolic homeostasis to some extent by altering carbon and nitrogen metabolic fluxes; meanwhile, transcriptional regulation in the host rumen epithelium contributes to co-adaptation, though certain absorption-related functions may be compromised due to stress. These findings provide a biological basis for maintaining ruminal functional homeostasis and health in water buffaloes under high-temperature conditions through nutritional interventions.

PMID 42547019
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