Drug Database
LE

leuprolide

✓ Approved

AimPharma · GNRHR · Small Molecule

What is leuprolide?

leuprolide is a small molecule developed by AimPharma. It is approved for therapeutic indications via injectable (others) or intramuscular (im) injection.

Drug Profile

CompanyAimPharma
Drug ClassSmall Molecule, Polypeptide
Molecular TargetGNRHR
RouteInjectable (Others), Intramuscular (IM) Injection
StatusApproved

Mechanism of Action

Molecular Targets

leuprolide acts on 1 molecular target:

GNRHRgonadotropin releasing hormone receptor (HH7, GRHR)
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Therapeutic Indications

leuprolide is developed for 4 unique indications across 3 therapeutic areas.

Therapeutic AreaConditionPhase
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

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Commentary on "Transarterial Embolization Alone Versus Drug-Eluting Microspheres Chemoembolization for Hepatocellular Carcinoma (RAD-18-TACE): A Multicenter Randomized Clinical Trial" Mosconi C, et al. CVIR 2026.

Sato Yozo Y, Tsuchiya Satoshi S, Takaki Haruyuki H, Matsueda Kiyoshi K

PubMedActa biomaterialia2026-07-17

Accurate Control of Microspheres by Surface Acoustic Waves for Quantitative Force Characterization and Cell Mechanics Measurement.

Qu Hengchao H, Shi Jialin J, Wang Hongyu H, Zhang Zijian Z et al.

The mechanical properties of cells are critical indicators of cellular physiological state and function. However, existing technologies still face challenges in achieving non-contact, force-calibrated, and precisely controlled single-probe measurements of single-cell mechanical properties. A phase-programmable surface acoustic wave (SAW) platform is presented, in which orthogonally arranged interdigitated transducers (IDTs) generate controllable acoustic fields for deterministic two-dimensional manipulation of microspheres. Dynamic phase modulation of the SAW fields enables high-precision microsphere steering while producing tunable acoustic radiation forces in the piconewton-nanonewton range. To enable direct quantitative characterization of acoustic forces, a calibrated microneedle-microsphere force probe is integrated into the platform. This configuration establishes an experimental phase-force relationship, enabling in situ calibration of acoustic radiation forces without relying on theoretical models or indirect calculation. Based on this experimentally calibrated acoustic force framework, SAW-driven 5 μm microspheres are employed as localized single probes to perform controlled acoustic indentation of adherent C2C12 myoblasts. The apparent Young's modulus is determined to be 1.63 ± 0.21 kPa using Hertzian contact mechanics and shows agreement with AFM-based measurements under comparable experimental conditions. c Overall, this work establishes a calibrated acoustic radiation force measurement and single-cell apparent Young's modulus characterization approach. This approach may have potential significance for non-contact mechanophenotyping and lab-on-chip based cell mechanics studies. STATEMENT OF SIGNIFICANCE: R2: Accurate single-cell mechanical characterization is limited by the lack of direct force calibration and controllable acoustic loading in SAW-based techniques. In this work, we implemented a phase-programmable SAW platform that enables deterministic microsphere manipulation and controllable acoustic force generation. By integrating a calibrated microneedle-microsphere probe, we established a direct phase-force relationship, enabling in situ and direct measurement of acoustic radiation forces and overcoming reliance on theoretical or indirect force estimation. This calibrated acoustic manipulation framework further enables controlled probe-based indentation of adherent cells and quantitative determination of their apparent Young's modulus. The proposed work may advance acoustic force-based mechanophenotyping and provide a promising pathway toward scalable, chip-integrated single-cell mechanical analysis.

PubMedJournal of vascular and interventional radiology : JVIR2026-07-17

Phase I Dose-Escalation Study Combining Irinotecan-Loaded Drug-Eluting Bead Chemoembolization with Yttrium-90 Glass Microspheres Radioembolization in Colorectal Liver Metastases (DEBIR90Y).

Ho Li Shen LS, Alsultan Ahmed A, Smits Maarten L J MLJ, Koopman Miriam M et al.

To find the maximum tolerated dose (MTD) of yttrium-90 (90Y) glass microspheres, with irinotecan-loaded drug-eluting beads (DEBIRI) in patients with colorectal liver metastases (CRLM). In this prospective study, participants with bilobar, unresectable, liver-dominant CRLM progressing after first-line systemic therapy received sequential bilobar 90Y glass microsphere radioembolization at increasing dose levels (60 Gy, 80 Gy, 100 Gy perfused normal liver absorbed dose), followed by DEBIRI, using a 3+3 dose-escalation design. The primary endpoint was MTD determination. Secondary endpoints included objective response rate (ORR) by RECIST 1.1 and PERCIST, (serious) adverse events ((S)AEs), carcinoembryonic antigen response (CEA), conversion to resection, and overall survival. Descriptive statistics and independent t-tests were applied. Twelve participants were enrolled. One dose-limiting toxicity (DLT; possible treatment-related fatal liver failure) occurred in the 80 Gy cohort, with no additional DLTs after cohort expansion (n=6). At 100 Gy, two additional DLTs (probable and possible treatment-related fatal liver failure) occurred, establishing 80 Gy as the MTD when combined with full-dose DEBIRI. Eighty treatment-related (S)AEs occurred, most commonly increased gamma-glutamyl transferase (12/12, grade 1-3) and abdominal pain (10/12, grade 1-2). ORR was 9% (RECIST) and 18% (PERCIST). Index lesion response rates were 20% (RECIST) and 35% (PERCIST). CEA response occurred in 42%. In this phase I study in patients with liver-dominant colorectal metastases, receiving a combination of yttrium-90 radioembolization with DEBIRI combined with DEBIRI, the maximum tolerated dose was 80 Gy. Considerable treatment-related toxicity was observed and objective response rates were limited.

PubMedJournal of agricultural and food chemistry2026-07-17

Size-Tailored Nanospaces in Hierarchical Magnetic Core-Shell Microspheres for Lipase Immobilization and Phytosterol Ester Synthesis.

Fan Yuqi Y, He Zhonglin Z, Mao Jin J, Deng Qianchun Q et al.

A size-matched magnetic core-shell platform (Fe3O4@MnO2@mSiO2) was constructed for immobilizing Candida rugosa lipase (CRL). The flower-like MnO2 interlayer provides chemical shielding, while mesoporous channels were expanded to 6.45 nm to geometrically match CRL (approximately 5 nm). Driven by interfacial activation, the support exhibited a selective purification effect, achieving a high activity-based immobilization yield (85.2%) and protein loading (143.1 mg g-1). The immobilized specific activity reached 31.4 U mg-1 (1.57-fold higher than the free enzyme) with 88.2% recovered activity. Crucially, in the sterically demanding esterification of phytosterols, the biocatalyst achieved 84.33% maximum conversion at 50 °C within 40 h. Furthermore, the rigid silica walls exerted a spatial "cage effect" that locked the enzyme active conformation, conferring exceptional thermal stability and reusability. This hierarchical support design offers a robust solution for macromolecular industrial biocatalysis.

PubMedColloids and surfaces. B, Biointerfaces2026-07-17

A near-infrared light-triggered platform for on-demand drug release in bone repair.

Shi Yue Y, Jiao Junjun J, Hu Yue Y, Zheng Yi Y et al.

Three-dimensional (3D) of multifunctional bone scaffolds is currently a major research hotspot in the field of bone repair. Nevertheless, achieving on-demand modulation of scaffold performance remains a significant and unresolved challenge. In this study, the photothermal agent indocyanine green (ICG) was loaded into ZIF-8 and co-encapsulated with the osteogenic drug total flavonoids of Drynaria (TF) in thermosensitive PLGA microspheres to construct a NIR-triggered on-demand release module TF/ICG/ZIF-8@PLGA (TZP). This module was further integrated into a PLGA/β-TCP scaffold to develop a multifunctional biomimetic scaffold (TZP/PT).The system exhibited a dual-mode release behavior, showing sustained release over 28 days under non-NIR conditions and significantly accelerated release upon NIR irradiation, demonstrating an "on-off" switchable drug delivery profile. Biological evaluation demonstrated good biocompatibility, high antibacterial activity with a bacterial inhibition rate of 99%, and the formation of mineralized hydroxyapatite layers within 7 days, which can be attributed to combined osteogenic drug delivery and NIR-triggered photothermal (PTT) and photodynamic (PDT)-related effects.

PubMedUltrastructural pathology2026-07-17

Progressive podocyte infolding glomerulopathy in a patient with systemic lupus erythematosus revealed by serial renal biopsies: a case report and literature review.

Nagayama Yoshikuni Y, Otani Masako M, Ono Kyoko K, Hayashi Hiroyuki H

Podocyte infolding glomerulopathy (PIG) is a rare pathological diagnosis based on characteristic electron microscopic findings of microspheres and/or microtubular structures associated with podocyte infoldings into the glomerular basement membrane (GBM) and was proposed as a new entity from Japan in 2008. PIG has been increasingly reported not only in Japan but also worldwide; however, the precise cause and mechanisms of PIG are unknown. PIG cases investigated by repeated renal biopsies are even rarer. We herein report a patient with systemic lupus erythematosus (SLE) who showed progressive podocyte infoldings into GBM by serial renal biopsies and review previous reports of PIG comparing the findings of serial renal biopsies. PIG may progress in association with the activity of the underlying disease, particularly in patients with autoimmune diseases. In the present case, proteinuria persisted, and PIG progressed independently of the activity of SLE. Although PIG appears to follow a progressive course accompanied by proteinuria, further accumulation of data on PIG cases with serial renal biopsies will contribute to elucidating its pathophysiology.

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