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leuprolide

✓ Approved

AimPharma · GNRHR · 小分子

什么是 leuprolide？

leuprolide 是一种小分子，由AimPharma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

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

作用机制

分子靶点

leuprolide 作用于 1 个分子靶点：

GNRHRgonadotropin releasing hormone receptor (HH7, GRHR)
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 针对 4 个适应症，涉及 3 个治疗领域。

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

相关研究文献

PubMedNature communications2026-09-10

Zinc displacement and metabolic interference: cobalt ion-mediated therapy for broad-spectrum CRKP-resistant pneumonia via inhalable microspheres.

Chu Zhaoyou Z, Liang Jun J, Wu Yayun Y, Fu Wanyue W et al.

Currently, broad-spectrum carbapenem-resistant Klebsiella pneumoniae (CRKP) infectious pneumonia remains clinically difficult to treat. This study develops inhalable microspheres (SCM) loaded with meropenem (MEM), fabricated via microfluidics by cross-linking sodium alginate with Co2+, for synergistic therapy against drug-resistant bacterial pneumonia. The core discovery lies in Co2+'s dual mechanism of action, which addresses both metallo- and serine-mediated carbapenem resistance. Co2+ irreversibly inhibits NDM-1 by displacing its active-site Zn2+ to restore MEM's bactericidal effect. For KPC-2-producing CRKP, Co2+ disrupts bacterial iron/sulfur metabolism, induces energy crisis and nutrient starvation, and reprograms bacterial metabolism toward inefficient fermentation. SCM shows potent in vitro activity against target strains and anti-biofilm capacity. In mouse models, treatment with inhaled SCM reduces bacterial levels in the lungs, improves survival rates, and lessens inflammatory damage. It also regulates the immune response in the lungs. Specifically, this therapy prevents the excessive migration of neutrophils to the lungs, inhibits excessive M1 polarization of macrophages and promotes their conversion to the M2 phenotype, while reverses T-cell exhaustion and maintains the homeostasis of NK cells. Transcriptome analysis confirms reversed infection-induced dysregulation and enhanced genes related to tissue repair. This work clarifies Co2+'s dual role (both an enzyme inhibitor and a metabolic disruptor) and provides an inhalable co-delivery strategy for CRKP.

PMID 42717206
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PubMedRSC advances2026-09-10

Fe2O3/Bi2WO6 hierarchical microspheres for visible-light-driven degradation of p-nitrophenol: performance, mechanism, and green metrics.

Kaur Manmeet M, Dhir Amit A, Verma Shilpi S

Bismuth tungstate (Bi2WO6), an Aurivillius-phase visible-light semiconductor, has a wide band gap and rapid charge-carrier recombination that significantly affects its photocatalytic efficiency. To overcome these intrinsic limitations, Fe2O3/Bi2WO6 composites were synthesised via a facile single-step hydrothermal technique with Fe2O3 loadings of 1, 3, and 5 wt%. XRD confirmed that the orthorhombic Bi2WO6 phase was retained without segregated Fe2O3, indicating that the incorporation of Fe into the lattice was successful. Raman spectroscopy proved that the WO6 octahedral framework was distorted by Fe, as evidenced by the broadening of the W-O stretching (∼800 cm-1) and O-W-O bending (∼308 cm-1) modes. FEG-SEM revealed morphological modifications in the hierarchical nanosheet assemblies, and UV-DRS showed a band-gap narrowing from 3.1 eV to 2.9 eV, leading to extended visible-light absorption. BET analysis confirmed comparable mesopores. PL spectroscopy, on the other hand, demonstrated the lowest charge-carrier recombination rate for the 1% Fe2O3/Bi2WO6 composite, consistent with its superior photocatalytic performance. XPS investigations further confirmed the slight distortion in the Bi-O coordination environment induced by the inclusion of Fe. Under optimized conditions (catalyst dose: 250 mg L-1, pH 7, and PNP: 20 mg L-1), the 1% Fe2O3/Bi2WO6 composite achieved 84.5% PNP removal under visible-light irradiation, following pseudo-first-order kinetics (k app = 0.0093 min-1). The photocatalyst exhibited good stability and reusability. In addition, the PNP degradation pathway was proposed based on HR-MS-identified intermediates and supported by TOC analysis and reactive-species detection. The process sustainability was further assessed based on green chemistry metrics, including water intensity, mass intensity, reaction mass intensity, E-factor, and energy consumption, demonstrating favorable environmental credentials relative to conventional remediation methods. These findings identify 1% Fe2O3/Bi2WO6 as an efficient and sustainable visible-light photocatalyst for the remediation of recalcitrant phenolic wastewater.

PMID 42719209
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PubMedFrontiers in pharmacology2026-09-09

Comparison of Beiyi® and its reference product Enantone® as agonists of luteinizing hormone-releasing hormone against prostate cancer: a multicenter, randomized single-dose study.

Yi Yuyao Y, Shen Pengfei P, Zheng Tongsen T, Hou Ruigang R et al.

Leuprolide acetate is a potent agonist of luteinizing hormone-releasing hormone that has been licensed to treat prostate cancer. The microsphere formulation of leuprolide acetate called Beiyi®, developed in China, has shown favorable pharmacokinetics, pharmacodynamics and safety similar to those of the reference drug Enantone® in healthy individuals. The present study examined whether the two formulations are bioequivalent in men with prostate cancer. This multicenter, open-label study randomized 120 Chinese men with prostate cancer 1:1 to receive a single subcutaneous injection of Beiyi® or Enantone® (3.75 mg). The two groups were compared in terms of pharmacokinetics and safety. The ratio of the geometric means of the maximum serum concentration (Cmax) of Beiyi® and Enantone® was 98.34% (91.88%-105.25%); the ratio of the geometric means of the concentration-time curve from 7 to 28 days (AUC7-28) was 100.52% (88.17%-114.60%); and the ratio of the geometric means of the concentration-time curve from 0 to 28 days (AUC0-28) was 109.07% (98.54%-120.73%). The three 90% confidence intervals fell within the range of 80.00%-125.00%, indicating similar pharmacokinetics. The two drugs showed similar safety profiles, with no treatment-emergent adverse events leading to withdrawal or death. The two formulations of leuprolide acetate microspheres Beiyi® and Enantone® show similar pharmacokinetics and safety in Chinese men with prostate cancer. These results support the further clinical development of Beiyi® as a generic formulation of Enantone®. CTR20222654 on http://www.chinadrugtrials.org.cn/index.html.

PMID 42713047
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PubMedMacromolecular rapid communications2026-09-09

Synthesis and Characterization of Monodisperse Sulfonic Acid-Functionalized Hollow Polymer Microspheres Using Precipitation Polymerization as Recyclable Solid Acid Catalysts.

Alam Md Rabiul MR, Hashimoto Yuri Y, Ikke Tomoya T, Haraguchi Naoki N

Monodisperse crosslinked sulfonic acid-functionalized hollow polymer microspheres were prepared via the chemical cleavage of core-shell polymer microspheres containing a cleavable core. First, the core-shell polymer microspheres were synthesized through the precipitation polymerization of styrene and a styrene dimer bearing two phenylsulfonate groups, followed by seed polymerization of N,N'-1,3-phenylenedimaleimide. The effects of polymerization parameters on the yield, particle size, size distribution, and shell thickness were investigated. Smaller microspheres with thicker shells were obtained at lower monomer concentrations. The resulting core-shell polymer microspheres were then treated with an aqueous KOH solution, followed by solvent washing to remove the core polymer. Subsequent acid treatment regenerated the sulfonic acid groups, yielding sulfonic acid-functionalized hollow polymer microspheres. The sulfonic acid-functionalized hollow polymer microspheres were evaluated as solid acid catalysts for the esterification reaction of 2-phenylethanol with acetic acid. Compared with uniform-type polymer microspheres and commercially available solid acid resin, the hollow polymer microspheres exhibited higher reactivity. In addition, they could be readily recovered from the reaction mixture by simple centrifugation. The recovered catalysts were reused for five consecutive cycles without any significant loss of activity.

PMID 42712132
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PubMedACS applied bio materials2026-09-09

Fabrication of Polyglycidyl Methacrylate Multilayer Carboxylated Magnetic Microspheres Immobilized with Affinity Ligands for Diagnostic Allergen Testing.

Zhang Yadong Y, Wang Guangyu G, Li Yunli Y, Li Yaxuan Y et al.

Magnetic microspheres immobilized with affinity ligands are highly efficient tools for immunoassays. Low non-specific adsorption and high affinity ligand loading capacity are crucial for the sensitivity of immunoassays, especially diagnostic allergen testing. This paper reports a carboxylated magnetic microsphere (PNFC@AA) via a multilayer cross-linked strategy. Monodisperse aminated polyglycidyl methacrylate (PGMA) microspheres were synthesized, followed by the incorporation of Fe3O4 nanoparticles through in situ coprecipitation. Polyacrylic acid (PAA) segments were then grafted onto the microsphere surface via surface radical polymerization using different crosslinkers, ultimately yielding magnetic PNFC@AA microspheres with high carboxyl loading. The prepared PNFC@AA microspheres exhibit uniform particle size, good monodispersity, and typical superparamagnetic properties. It was found that compared to divinylbenzene (DVB) and ethylene glycol dimethacrylate (EGDMA) crosslinkers, the hydrophilic crosslinker polyethylene glycol diacrylate (PEGDA) microspheres exhibited a larger specific surface area (19.17 m2/g), a higher carboxyl loading (655 μmol/g), and a stronger streptavidin (SA)-immobilized biotin binding capacity (2328 pmol/mg). In AMPPD chemiluminescent immunoassay (CLIA), these microspheres effectively suppressed non-specific adsorption, reduced background luminescence, and substantially improved the signal-to-noise ratio. Furthermore, the SA-coupling microspheres were successfully applied to the detection of specific IgE against four common allergens (house dust mite (Dermatophagoides farinae), German cockroach (Blatella germanica), milk, and egg), respectively, which effectively distinguished the sensitization levels of different allergens. This study provides a simple and efficient strategy for the design of high-performance immunodiagnostic carriers.

PMID 42715526
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PubMediScience2026-09-09

Functional switching from circularly polarized luminescence to whispering gallery modes in a chiral Schiff base.

Li Jinhui J, Luo Yue Y, Chen Cong C, Tong Liang L et al.

This work demonstrates a design concept for dual-mode optical materials, embodied by an axially chiral fluorescent Schiff base, (R/S)-BN-2HGCA. The compound exhibits two competing optical functions that are toggled by its physical aggregation state. In a dilute solution, the molecule's chirality is expressed, resulting in clear circularly polarized luminescence (CPL). In contrast, upon self-assembly into morphologically pristine microspheres, the chiroptical property is suppressed. This structural transition represents a functional transition where intense optical confinement within the microcavity is accompanied by suppression of the observable CPL, while enabling the emergence of whispering gallery mode (WGM) resonance. These spheres function as active optical resonators supporting distinct WGM resonance, with an average Q-factor of approximately 190, demonstrating effective light confinement within the self-assembled organic microcavities. Controlling dissolution and self-assembly to switch between chiroptical and photonic modalities provides a promising design concept that may be developed toward smart materials.

PMID 42713080
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