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urokinase

✓ Approved

Bharat Serums and Vaccines Limited · FSHR · Small Molecule

What is urokinase?

urokinase is a small molecule developed by Bharat Serums and Vaccines Limited. It is approved for therapeutic indications via injectable (others) or intravenous (iv).

Drug Profile

CompanyBharat Serums and Vaccines Limited
Drug ClassSmall Molecule, Polyclonal Antibodies, Recombinant Proteins, Polypeptide, Antibody
Molecular TargetFSHR, LHCGR, PLAU, PLG
RouteInjectable (Others), Intravenous (IV)
StatusApproved
Sources: ClinicalTrials.gov, Bharat Serums and Vaccines Limited

Mechanism of Action

Molecular Targets

urokinase acts on 4 molecular targets:

FSHRfollicle stimulating hormone receptor (FSHRO, ODG1)
LHCGRluteinizing hormone/choriogonadotropin receptor (ULG5, LH/CGR)
PLAUplasminogen activator, urokinase (URK, UPA)
PLGplasminogen (HAE4)
Want deeper analysis?Noah AI can explain complex mechanisms and compare to similar drugs.

Therapeutic Indications

urokinase is developed for 1 unique indication across 1 therapeutic area.

Therapeutic AreaConditionPhase
Vascular disordersThrombosis✓ Approved

Related Research Articles

PubMednpj biomedical innovations2026-05-23

A "turn-off" photoacoustic contrast for urokinase-type plasminogen activator activity.

Sharma Ananya A, Panda Suvam Kumar SK, Hasan Thuria T, Ravanan Sneha S et al.

The ability to distinguish cancerous lesions based on aggressiveness using noninvasive molecular imaging techniques enables more precise and accurate diagnosis. In colorectal cancer screening, current approaches such as blood or fecal tests and endoscopic examination are widely used. However, reliably differentiating malignant adenomatous lesions from benign lesions, particularly those ≤5 mm in size, remains a significant clinical challenge. We synthesized, optimized, and validated a small-molecule near-infrared (NIR) activated photoacoustic dye conjugated to a tripeptide substrate specific for urokinase plasminogen activator (uPA), a protease that is upregulated in colorectal cancer tissues. The probe was designed to produce an "ON-OFF" photoacoustic signal upon activation by uPA. Specificity of the probe towards aggressiveness was evaluated using two colorectal cancer cell lines with differential uPA and cathepsin B expression. The uPA-responsive photoacoustic probe demonstrated high sensitivity and a clear "ON-OFF" activation signal in response to uPA activity. It showed strong specificity between colorectal cancer cell lines with different levels of uPA expression, confirming its selective activation. Noninvasive monitoring of extracellular uPA activity using photoacoustic imaging shows promise as a predictive screening approach for distinguishing malignant and premalignant colorectal lesions, particularly those that are small and difficult to classify using current screening methods.

PMID 42174191
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PubMedMikrochimica acta2026-05-22

Self-enhanced electrochemiluminescence of gold nanoclusters via host-guest assembly for ultrasensitive protein biosensing.

Hu Shuang S, Li Keyu K, Xie Pan P, Zhu Xiaochun X et al.

Host-guest assembly-induced Au NCs (DMPDA@ ATT-Au NCs) with highly efficient self-enhanced electrochemiluminescence (ECL) were developed for sensitive detection of soluble urokinase-type plasminogen activator receptor (suPAR), a neotype biomarker in kidney diseases. Impressively, DMPDA@ ATT-Au NCs were assembled via host-guest recognition between the ligand 6-aza-2-thiothymine (ATT) protected Au NCs and the coreactant N, N-Dimethyl-1,3-propanediamine (DMPDA) through hydrogen-bond, which exhibited strong ECL signal due to the synergistic enhancement effect of the inhibition of non-radiative transitions by suppressing the rotation of the ligand ATT molecule and the reduction of energy loss by shortening the distance of electron transfer between the Au NCs and DMPDA. Furthermore, trace suPAR was transformed to enormous DNA network nanostructure with participation of high-efficiency dual-catalyst hairpin assembly (DCHA) system and DNA self-assembly, thereby significantly improving the detection sensitivity. Consequently, based on the DMPDA@ ATT-Au NCs as excellent ECL emitter and DCHA induced DNA network nanostructure as signal amplifier, the developed ECL biosensor realized the sensitive detection of suPAR with a detection limit (DL) of 1.48 fg/mL, which represents a sensitivity gain of about five orders of magnitude compared to a standard ELISA kit (DL: ng/mL). In three clinical samples, the biosensor showed excellent agreement with ELISA at high concentrations, and successfully quantified trace suPAR levels below the DL of ELISA kit. This strategy offers a novel ECL enhancement strategy of AuNCs to construct sensitive biosensing platform, which holds potential for extension to trace-level detection of other biomarkers toward clinical biomarker analysis, diagnostic evaluation, and treatment surveillance.

PMID 42171817
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PubMedFrontiers in cell and developmental biology2026-05-22

Novel mouse line with D277N mutation in the Plau gene displays autism spectrum disorder-like traits.

Karagyaur Maxim M, Averina Olga O, Bozov Kirill K, Dzhauari Stalik S et al.

Genetic technologies provide an opportunity to study the molecular basis of a wide range of hereditary pathologies, including mental disorders. Reproducing of potentially pathogenic genomic variants in cellular and animal models allows establishing their functional significance and possible mechanisms of involvement in the pathogenesis of certain disorders. In this study, a genetic variant of urokinase type plasminogen activator (uPA, gene Plau) was modeled in mice using CRISPR/Cas genome editing tool, enabling a better understanding of the role of this molecule and its associated pathways in brain development. The protease uPA plays an important role in the directed migration of neural progenitors, glial, endothelial and immune cells, it participates in axon guidance and maturation of synaptic connections, activation of growth factors and degradation of the extracellular matrix. To study the contribution of the catalytic function of uPA to brain development, we have created for the first time a mouse line carrying the D277N (rs1243306395) mutation. We assessed social activity, anxiety, memory, problem-solving ability and stress resistance of these mice, as well as histological features of their brains. Timely and correct functioning of the Plau gene ensures adequate positioning of crucial cellular components in the developing nervous system. According to bioinformatic calculations, the D277N (corresponds to the human single nucleotide variant rs1243306395) substitution that happens due to C-to-T mutation in the murine Plau gene may impair the catalytic activity of the uPA protein. While retaining their ability to find solutions in the escape test, this mouse line is characterized by high levels of anxiety, impaired social behavior, slowed learning dynamics (spatial memory), and impaired adaptation to stressors. This behavioral pattern can potentially be interpreted as autism spectrum disorder Histological analysis of the brain and cerebral cortex in Plau-D277N mice revealed brain volume enlargement and cortical thickening of approximately 10-15% compared to wild-type mice. In this study, we draw attention for the first time to the genomic variant rs1243306395 in the Plau gene as a potential cause of autism spectrum disorder and propose the genetically modified Plau-D277N mouse line as a model object for studying the pathogenesis of this disorder. These models can also be used for the development and testing of promising therapeutic approaches and pharmacological agents.

PMID 42170179
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PubMedBritish journal of cancer2026-05-21

Differentiating borderline HER2-expressing and HER2-positive cancers from other subtypes using serum urokinase plasminogen activator.

López Mujica Michael E J MEJ, Boonkaew Suchanat S, Christensen Nana L NL, Abildgaard Pedersen Mette M et al.

HER2-positive (HER2+) cancers are associated with aggressive tumour development but also high response rates to targeted blockade treatments of the HER-2/neu signalling pathway leading to improved clinical outcome for the patient. Current clinical analysis of the HER2 status primarily relies on solid tumour biopsies low-suitable for continuous real-time monitoring needed for possible adjustment of the treatment, while serum tests targeting blood-circulating HER-2/neu fragments often show conflicting tumour-serum relations. A cellulase-linked aptamer sandwich assay was used for detection of total urokinase plasminogen activator (uPA) and its different forms in serum of cancer patients and healthy individuals. Serum uPA levels were correlated with solid biopsy results and relevant clinical data extracted from electronic patient records, and FDG-PET/CT scanning. We show that serum uPA precisely stratifies patients with HER-2/neu overexpressing (HER2+) and borderline-expressing cancers. Serum levels of total uPA 96.8% accurately informed about HER-2/neu tumour status in a cohort of 100 patients, with a HER2+/borderline expression cut-off value of 0.973 ng mL-1. The established liquid biopsy test for serum uPA has potential for accurate diagnosis and staging of patients with HER2+ and borderline-expressing cancers requiring further confirmatory (or rejection) testing.

PMID 42162363
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PubMedScientific reports2026-05-20

Select novel small-molecule uPA potential inhibitors as anti-cancer agents against breast cancer.

Almosnid Nadin N, Islam Imadul I, Ali Rizwan R, Algheribi Shatha S et al.

Cancer metastasis is a significant contributor to global morbidity and mortality rates. The urokinase type plasminogen activator (uPA) and its receptor (uPAR) play an essential role in facilitating abnormal cell metastasis and tumor progression. This research examines novel uPA/uPAR compounds as potential anticancer targets in various types of tumors. Several compounds were screened for their bioactivity and inhibitory effects on uPA and its receptor interactions, demonstrating the significant potential of a compound previously recognized as a promising uPA inhibitor, initially developed for the treatment of multiple sclerosis. The compounds exhibited notably low IC₅₀ values, as low as 1.4 μM, against the aggressive triple negative breast cancer cell line MDA-MB-231 compared to the chemotherapeutic drug Mitoxantrone. MDA-MB-231 cells treated with KCO241 and KCO246 exhibited selective anticancer activity, inducing apoptotic pathways and demonstrating selective anticancer efficacy. This study showed that these novel uPA inhibitors have potential therapeutic applications for the treatment of metastatic cancers and the modulation of disease progression. Subsequent preclinical in vivo investigations will further evaluate the safety as well as pharmacological characteristics and potential for translation.

PMID 42156439
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PubMedRSC advances2026-05-18

Adjunctive therapeutic strategy for in-stent thrombosis: in vitro pharmacodynamic evaluation of COX-1 inhibitor 3d combined with catheter-directed thrombolysis.

Ma Bo B, Liang Zenghui Z, Fu Liping L, Ma Yanbiao Y et al.

Twelve benzohydrazide Schiff base derivatives (3a-3l) with systematic variations in the aromatic aldehyde moiety were designed and synthesized to evaluate their anti-inflammatory, antiplatelet, and in vitro antithrombotic activities. Among them, compound 3d (the condensation product of 4-chlorobenzohydrazide and furan-2-carbaldehyde) was identified as the most promising lead, displaying moderately selective COX-1 inhibition (IC50 = 1.63 µM, selectivity index = 8.87) together with moderate 5-LOX inhibition (IC50 = 10.63 µM). In LPS-stimulated macrophages, 3d concentration-dependently suppressed the release of TNF-α, IL-6, IL-1β, and PGE2. It inhibited ADP- and collagen-induced platelet aggregation (IC50 = 5.48 µM and 4.52 µM, respectively), reduced the expression of platelet activation markers CD62P and PAC-1, and prolonged clotting time while decreasing clot strength in thromboelastography. Under arterial shear conditions in a parallel-plate flow chamber, 3d significantly attenuated thrombus formation in a concentration-dependent manner. Importantly, in an in vitro clot lysis model, 3d (50 µM) enhanced the thrombolytic rate of low-dose urokinase (100 IU per mL) from 35.0% to 45.2%, highlighting its potential to augment thrombolysis. Preliminary ADME profiling revealed moderate plasma protein binding (89.3%) and a metabolic half-life of 0.75 h in liver microsomes. This study provides the first systematic structure-activity relationship analysis of aromatic aldehyde substituents on benzohydrazide Schiff bases and identifies 3d as a lead compound possessing combined anti-inflammatory, antiplatelet, and thrombolysis-enhancing activities. These findings support the potential of 3d as an adjunctive agent for catheter-directed thrombolysis in in-stent thrombosis, pending further in vivo efficacy and safety investigations.

PMID 42148270
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