Drug Database
LE

leuprolide acetate (Leupronax)

✓ Approved

Nanox · GNRH1 · Small Molecule

What is leuprolide acetate?

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

Drug Profile

Brand NamesLeupronax
CompanyNanox
Drug ClassSmall Molecule, Polypeptide
Molecular TargetGNRH1
RouteInjectable (Others), Intramuscular (IM) Injection
StatusApproved

Mechanism of Action

Molecular Targets

leuprolide acetate acts on 1 molecular target:

GNRH1gonadotropin releasing hormone 1 (GNRH, LHRH)
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Therapeutic Indications

leuprolide acetate is developed for 4 unique indications across 2 therapeutic areas.

Therapeutic AreaConditionPhase
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

Related Research Articles

PubMedInternational journal of mass spectrometry2026-05-25

Impact of Supercharging on Top-Down Characterization of Monoclonal Antibodies by Collision Induced Dissociation.

Amunugama Lasini L, Shaw Jared B JB

Native top-down characterization of monoclonal antibodies (mAbs) is an attractive approach due to the narrow charge state distribution of the intact mAb and the spectral decongestion afforded by relatively low charge product ions being spread over a broad m/z range. However, low precursor charge and extensive disulfide bonding together greatly limit characterization by collision induced dissociation (CID). This study evaluates solution phase supercharging in ammonium acetate electrospray solutions to produce charge state distributions with intermediate charge, i.e., somewhere between native and fully denatured. Sequence coverage and interchain disulfide bond cleavage were evaluated as a function of precursor charge and collision energy for denatured, native, and supercharged "native" mAb precursor ions. Native ESI produced low charge precursors (z~22-23) that required high collision energies (~200-225 eV/q) for interchain disulfide cleavages (i.e., light chain (LC) release) and yielded modest sequence coverage. Formic acid, 50:50 acetonitrile/water with formic acid, dimethyl sulfoxide, propylene carbonate, and sulfolane were compared as additives; many increased precursors charge states but produced broader envelopes and degraded spectral quality. In contrast 3% sulfolane in 100 mM ammonium acetate increased average charges to ~39 for Infliximab and ~42 for SigmaMAb and reduced the dissociation threshold to 125 eV/q as expected for higher charge precursor ions. Optimized conditions produced abundant [LC-S]/[LC]/[LC+S] triplets and extended b/y ions into CDR3 regions. Overall, adding 3% sulfolane in ammonium acetate provides a practical way to overcome key CID limitations for intact mAbs and enables more extensive sequence characterization.

PubMedChemSusChem2026-05-25

Green Synthesis of Alkyl Carbamates via Non-Phosgene Process From Reactions of NH3 and Dialkyl Carbonate Over Zn-Acetate-Triazolato Catalysts.

Wang Peixue P, Li Wenjing W, Liu Shimin S, Zhang Wei W et al.

A series of zinc-acetate-triazolato catalysts (Zn(OAc)ATZ, Zn(OAc)TZ, Zn(OAc)TRZ, ATZ = 3-amino-1,2,4-triazolate, TZ = 1,2,4-triazolate, TRZ = 5-aminotetrazole) were developed for the direct synthesis of alkyl carbamates and corresponding alcohols from ammonia and dialkyl carbonates. Among them, Zn(OAc)ATZ exhibited exceptional catalytic performance due to its high surface area (441.11 m2/g), hierarchical porosity, and appropriate coordination environment. Under optimized conditions, 89% conversion of diethyl carbonate (DEC) with 88% ethyl carbamate (EC) yield could be achieved over Zn(OAc)ATZ at 80°C for 16 h. For dimethyl carbonate (DMC), a remarkable 98% conversion and 97% methyl carbamate (MC) yield were obtained at 30°C within 6 h, while dibutyl carbonate (DBC) required 24 h at 90°C to reach 95% conversion and 93% butyl carbamate (BC) yield. Characterization of XPS and FT-IR revealed that the synergistic interaction between Zn-N bonds and carboxylate groups stabilized the active sites, enabling efficient substrate activation. The catalyst retained >87% activity after three cycles, demonstrating excellent stability in alkaline ammonia environments. This work provides a sustainable and industrially viable strategy for alkyl carbamate synthesis, aligning with green chemistry principles and the "dual-carbon" agenda.

PubMedJournal of clinical biochemistry and nutrition2026-05-25

Non-thermal plasma-activated methionine-containing Ringer's solution enhances cytotoxicity by increasing oxidative stress.

Fujisawa Kosei K, Tanahashi Sakura S, Katagiri Kyoka K, Takasu Soo S et al.

Non-thermal plasma (NTP) is an ionized gas composed of electrons, ions, radicals, and UV. NTP-irradiated solutions induce reactive oxygen species (ROS)-dependent cell death. NTP irradiation of solutions containing methionine (Met) has been reported to enhance the cytotoxic effects of NTP; however, the exact mechanism by which NTP-irradiated Met solutions exhibit cytotoxicity is not fully understood. In this study, we aimed to elucidate the mechanism using the human breast cancer cell line MDA-MB-231 cells. NTP-irradiated Met-containing acetate Ringer's solution (Met/PAA) potently induced cytotoxicity compared with NTP-irradiated acetate Ringer's solution (PAA). Catalase-treated Met/PAA induced cytotoxicity to the same extent, suggesting that NTP irradiation might generate a novel cytotoxic substance distinct from ROS. Catalase-treated Met/PAA decreased intracellular glutathione (GSH) levels, increased ROS production, and caused mitochondrial dysfunction. When catalase-treated Met/PAA was pretreated with antioxidants, GSH and N-acetylcysteine, its cytotoxicity was suppressed. These phenomena indicate that oxidative stress is involved in cell death induced by catalase-treated Met/PAA. Dehydromethionine and methionine sulfoxide were identified as oxidation products of Met in the Met/PAA solution, but neither of the products exhibited cytotoxicity. Taken together, the irradiation of Met-containing solutions likely generates unidentified Met oxidation products other than ROS, resulting in cell death through oxidative stress-induced energy production failure.

PubMedScientific reports2026-05-25

NMR-based metabolomics analysis in breast cancer patients from Saudi Arabia: a pilot study.

Ullah Muhammad Ikram MI, Rashid Shazia S, Tahir Aisha A, Alameen Ayman Ali Mohammed AAM et al.

In breast cancer (BC), metabolomic profiles have largely focused on Western and East Asian groups, with limited data from the Middle East. Population-specific studies are required to better understand metabolite alterations due to regional, environmental and genetic heterogeneity. This exploratory pilot study aimed to evaluate serum metabolic alterations in breast cancer patients and their associations with disease stage using NMR-based metabolomics in the Saudi Arabian cohort. A total of 30 female breast cancer patients and 30 healthy controls were included. Patient samples showed higher levels of ketoglutarate, glutamine, lipids, and branched-chain amino acids, while acetate, creatine, and glucose were lower in the patient group (all FDR q < 0.05). Ketoglutarate (AUC = 0.85), glutamine (AUC = 0.84), and lipids (AUC = 0.82) demonstrated discriminatory ability. A combined model incorporating acetate and ketoglutarate achieved an AUC of 0.91. With advancing disease stage, lactate (p-trend = 0.005), leucine (p-trend = 0.044), and glutamate (p-trend = 0.033) showed decreasing trends. Lactate, choline, and glucose were each independently associated with more advanced disease in multivariable models. Unsupervised principal component analysis (PCA), supervised partial least squares-discriminant analysis (PLS-DA), and orthogonal PLS-DA (OPLS-DA) showed metabolic separation between patients and controls. Permutation testing indicated that class separation exceeded random classification; however, overfitting remains possible due to reliance on internal validation. The negative Q² value (- 0.577) indicates poor predictive generalizability. In conclusion, this study identifies candidate metabolite signatures associated with breast cancer in a Saudi cohort. These findings require validation in independent cohorts before clinical application.

PubMedACS omega2026-05-25

Synthesis, Structural Insights, and In Vitro Evaluation of Novel Silver Complexes Supported by Amantadine-Functionalized Bis(pyrazolyl)acetate Ligands as Anticancer Agents.

Pellei Maura M, De Franco Michele M, Santini Carlo C, Caviglia Miriam M et al.

Bis-(pyrazol-1-yl)-acetic acid (HC-(pz)2COOH) and bis-(3,5-dimethyl-pyrazol-1-yl)-acetic acid (HC-(pzMe2)2COOH) were conjugated with amantadine to yield the ligands LAd and L2Ad, respectively. These chelating ligands were used for the synthesis of silver complexes 1-5, whose electronic and molecular structures were investigated by X-ray Photoelectron Spectroscopy (XPS) and Near Edge X-ray Absorption Fine Structure (NEXAFS) spectroscopy. The coordination geometry of the noble metal ion was assessed by combining X-ray Absorption Spectroscopy (XAS) data analysis with Density Functional Theory (DFT) modeling. The structures of the ligand LAd and of the complex [Ag-(L2Ad)-(PPh3)]-NO3·0.5CH3CN (3a) were determined by single-crystal X-ray diffraction analysis. The bis-(pyrazolyl)-acetamide ligand crystallizes in the I2/a space group and is similar to the 3,5-dimethyl analogue. The complex crystallizes in the P-1 space group and is the first reported example of a tetra-coordinated silver-(I) complex incorporating a tridentate bis-(pyrazolyl)-acetate ligand. The cytotoxicity potential of the new phosphane Ag-(I) complexes was tested on various human cancer cell lines, together with that of the two unfunctionalized analogs [Ag-(L2OiPr)-(PPh3)]-NO3 (6) and [Ag-(L2OiPr)-(PTA)]-NO3 (7), synthesized and studied for useful comparison. Notably, the novel complexes exhibited pronounced cytotoxic effects against the human-derived pancreatic cancer BxPC-3 cell line, both in 2D monolayers and in 3D spheroid models. Mechanistic studies revealed efficient intracellular accumulation of the complexes, likely favored by increased lipophilicity, and inhibition of thioredoxin reductase (TrxR), ultimately disrupting redox homeostasis and promoting oxidative stress, which are key contributors to their antiproliferative effects.

PubMedJournal of electroanalytical chemistry (Lausanne, Switzerland)2026-05-25

Understanding Baseline Drift in Laser-Induced Graphene Electrodes and Its Impact on Heavy Metal Detection by Anodic Stripping Voltammetry: Comparison with Glassy Carbon Electrode.

Chen Kuo-Hao KH, Arora Kamal K, Earwood John J, Deng Baolin B et al.

The planar Laser-Induced Graphene (LIG) patterned electrochemical sensor device was fabricated with a CO2 infrared laser on a commercial polyimide film. We investigated the dynamic surface and baseline current changes in LIG versus Glassy carbon (GC) electrodes after multiple square wave voltammetry (SWV) scans in 0.1 M acetate buffer (pH 4.5), using OCP and EIS techniques. Additionally, bismuth-film coated on LIG (Bi/LIG) and GC (Bi/GC) electrode were characterized and compared for detection of heavy metal ions using anodic stripping voltammetry (ASV). The electrochemical deposition and stripping processes of Pb, Cu, Zn and Cd on these Bi/LIG were studied to obtain mechanistic insights. Results show that the nature and condition of the LIG substrates have a profound effect upon the nucleation and growth of the bismuth deposit. A simple baseline correction strategy was used on LIG device for detection of multiple heavy metal ions (i.e. Pb2+, Cd2+, Cu2+ and Zn2+) in 0.1 M acetate buffer (pH 4.5) with square wave anodic stripping voltammetry (SWASV) and the corresponding limit of detections (LOD) are found to be 14.82 ppb (Zn2+), 12.11 ppb (Cd2+), 11.55 ppb (Pb2+), and 14.64 ppb (Cu2+) respectively. The Bi/LIG sensor device was further tested for metal analysis in a real-world sample. Results show that baseline correction provides accurate Pb2+ detection despite limitations towards other metal ions. LIG electrodes also provide better detection for Zn2+ and Cu2+ than GC electrode. This study provides the methods and mechanistic understandings for the use of porous and heterogeneous LIG materials in the analytical detection of multiple heavy metals.

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