Germanin (suramin) / Optimum Therap - LARVOL DELTA

Ionic agarose derivatives as polyelectrolytic additives for drug release. (PubMed, Carbohydr Polym) - "Incorporating ionic agarose derivatives into these materials proved to effectively reduce the burst release and sustain the release of adenosine triphosphate (ATP), suramin, methylene blue, and A740003 over a time of 14 days. The release curves were evaluated using established models as well as two novel Langmuir-like models. Especially the latter two offered additional insight into the release and yielded higher scores in Akaike's Information Criterion rankings than commonly used models."

Journal

Mechanism-informed identification of FDA-approved topoisomerase inhibitors disrupting SARS-CoV-2 nucleocapsid-RNA interactions. (PubMed, BMC Chem) - "Inspired by adenosine triphosphate (ATP)'s competitive inhibition of NP-RNA binding, we screened 121 FDA-approved ATP-competitive kinase inhibitors, identifying mitoxantrone (IC₅₀ = 1.22 µM) as a potent inhibitor. Considering its known topoisomerase inhibitory activity, we further screened 23 additional topoisomerase inhibitors, uncovering four active compounds-pixantrone (IC₅₀ = 5.67 µM), doxorubicin (IC₅₀ = 20.19 µM), epirubicin (IC₅₀ = 7.23 µM), and suramin (IC₅₀ = 0.44 µM)...Our findings demonstrate the feasibility of a mechanism-informed repurposing strategy and identify FDA-approved topoisomerase inhibitors and suramin as valuable chemical starting points. Although these compounds are not directly suitable as antivirals due to toxicity concerns, they provide promising scaffolds for further optimization aimed at selective disruption of SARS-CoV-2 NP-RNA interactions."

FDA event • Journal • Infectious Disease • Novel Coronavirus Disease • Respiratory Diseases

Suramin protects against chronic stress-induced neurobehavioral deficits via cGAS-STING/NF-κB suppression. (PubMed, Sci Rep) - "The level of corticosterone and neurotransmitters (dopamine and serotonin); various parameters of oxidative stress and neuroinflammation; acetylcholinesterase (AChE) activity and histological changes in hippocampus and cortex were also assessed. The results highlighted that administration of suramin (5, 10 and 20 mg/kg, i.p.) dose dependently improves neurobehavioral parameters, decreases corticosterone; elevates the level of neurotransmitters, and reduces the deleterious effects of CUS on oxidative stress and neuroinflammation; along with the histological improvement by inhibiting the cGAS-STING pathway and modulating NF-κB signaling as observed from decrease NF-κB levels in our study This study provides insights into suramin as a new treatment approach for mitigating the effects of chronic stress on restoring neurobehavioral changes."

Journal • Alzheimer's Disease • CNS Disorders • Cognitive Disorders • Depression • Inflammation • Mood Disorders • Pain • Psychiatry • STING

Role of S1P- and Rho-kinase signalling in age-related myogenic tone deficiency in murine resistance arteries. (PubMed, Exp Physiol) - "The P2Y-receptor blocker suramin inhibited MT, whereas PPADS and apyrase did not...High-resolution microangiography confirmed that infusion of JTE-013 or KD025 (a Rho-kinase 2 inhibitor) preferentially dilated small (distal) CAs, and infusion of nifedipine (an L-type channel inhibitor) dilated all CAs in all mice, independent of age. SK and S1P2-R are crucially involved in pressure sensing in MT. RhoA/Rho-kinase signalling might be involved in age-related MT deficiency."

Journal • Preclinical • Alzheimer's Disease • Cardiovascular • CNS Disorders • RHOA

YopP modulates bacterial virulence and systemic dissemination in Peyer´s patches during murine Yersinia enterocolitica infection. (PubMed, Med Microbiol Immunol) - "Additionally, inhibition of cytotoxicity by suramin treatment in mice promoted wild-type Ye (Ye WT) dissemination to levels comparable to Ye ΔyopP...Blocking DC migration by FTY720 treatment in Ye ΔyopP-infected mice significantly reduced the MLN bacterial burden, indicating that YopP regulates Ye-transporting DCs from PP to MLN. Overall, our findings provide insights into how YopP participates in host-pathogen interactions, seemingly benefiting the host while simultaneously facilitating bacterial evasion from early immune clearance. These findings contribute to understanding the impact of YopP on the clinical outcome of Ye infection."

Journal • Preclinical • Gastroenterology • Gastrointestinal Disorder • Infectious Disease • Inflammation • IL10 • ITGAM

Epithelial cell signaling modulates responses of intrinsic primary afferent neurons of the mouse ileum to mechanical stimulation (Neuroscience 2025) - "To test the role of enterochromaffin cells, the same set of experiments were repeated with the addition of ondansetron (1 µM), GR 113808 (30nM), and suramin (500 µM)...Hex increased and Neo decreased immediate responses in submucosal neurons (Basal: Avil 19%/64%/17%, Hex: 29%/41%30%, Neo: 0%,25%,75%; p=0.006, Chi-square). Collectively, these results demonstrate mucosal mechanical receptive fields of IPANs that are modulated rather than mediated by neuroepithelial signaling of 5-HT, ATP, and acetylcholine."

Preclinical • CNS Disorders

Retraction: In vivo experiments demonstrate the potent antileishmanial efficacy of repurposed suramin in visceral leishmaniasis. (PubMed, PLoS Negl Trop Dis) - No abstract available

Journal • Preclinical • Infectious Disease

Extending Thioflavin T Fluorescence Probe to 2-Ethenyl-benzothiazole Derivatives: Drug-like Quadruplex Ligands with Potent Antitrypanosomatid Activity. (PubMed, ACS Infect Dis) - "In fact, compound 2b demonstrated superior efficacy and selectivity in comparison to the clinically used drugs suramin, fexinidazole, miltefosine, and amphotericin B. Biophysical studies revealed that all tested derivatives exhibited significant G4 stabilization, surpassing ThT. Location of compound 2b inside the nucleus and the kinetoplast, as well as partially in the mitochondria, opens up the possibility of 2b acting against the parasite through binding to G4."

Journal • Infectious Disease

Mechanism and therapeutic potential of purinergic receptor antagonism for treatment of cerebral malaria (ASTMH 2025) - "We have also found that suramin protects endothelial cells independently of calcium and cAMP, the canonical second messengers involved in purinergic receptor signaling, further pointing to alternative pathways of endothelial barrier enhancement. We will also perform RNA-sequencing to identify the cell signaling pathways that are modulated by suramin and further clarify how it protects brain endothelial cells from iRBC-mediated disruption."

CNS Disorders • Infectious Disease • Malaria • P2RY13

Rapamycin and Suramin Effects on TNF-⍺-Mediated Mast Cell and Brain Microvascular Endothelial Cell Dysfunction. (PubMed, Biotechnol Bioeng) - "However, suramin also increased intracellular BMEC levels of multiple pro-inflammatory cytokines. Neither rapamycin nor suramin improved the intracellular inflammatory profile of cocultured MCs, indicating that MC activation had not been resolved by either treatment."

Journal • Alzheimer's Disease • CNS Disorders • Inflammation • CCL2 • CCL3 • CSF2 • RPS6 • TNFA

Structural basis for suramin binding to the C-terminal domain of the SARS-CoV-2 nucleocapsid protein. (PubMed, Acta Biochim Biophys Sin (Shanghai)) - "Furthermore, ITC and EMSA experiments demonstrate that suramin can bind to the full-length N protein at multiple sites and dissociate RNA from the N protein. Taken together, these findings provide structural and biophysical insights into the mechanism of action of suramin and establish a rational basis for the development of targeted antiviral therapies against SARS-CoV-2."

Journal • Infectious Disease • Novel Coronavirus Disease • Respiratory Diseases

Discovery of therapeutic AGC2 modulators by combining docking, binding, and vesicle-based transport assays. (PubMed, J Transl Med) - "This study establishes a reproducible, and scalable workflow that bridges high-throughput ligand identification with high-resolution kinetic characterization for targeting mitochondrial carriers."

Journal • Genetic Disorders • Oncology

Human African Trypanosomiasis (HAT): Epidemiology, Biological Diagnosis and Treatment: A Review. (PubMed, Acta Parasitol) - "All these difficulties raised raise questions about the need to develop new diagnostic tools that are more specific, more sensitive and better suited to field screening. They also call out the urgency of finding new drugs that are less toxic, easy to administer and more effective."

Journal • Review • Narcolepsy • Sleep Disorder

The immunoregulator β-glucan produces antidepressant effects through microglia-mobilized astrocytic P2Y1R-BDNF signaling in the dentate gyrus. (PubMed, Int Immunopharmacol) - "Degradation of endogenous ATP by apyrase, non-specific antagonism of purinergic receptors by suramin, specific antagonism of P2Y1Rs in the hippocampus or selective deletion of P2Y1R in astrocytes was able to abolish the antidepressant effect of β-glucan...Further analysis showed that antagonism of BDNF signaling in the hippocampus abolished the antidepressant effect of β-glucan. These results suggest that ATP-triggered astrocytic P2Y1R signaling may mediate the antidepressant effect of β-glucan by promoting BDNF production in the hippocampus."

Journal • CNS Disorders • Depression • Inflammation • Psychiatry

3-benzylaminomethyl lithocholic acid derivatives as selective and uncompetitive inhibitors of protein tyrosine phosphatase 1B (PTP1B) (ACS-Fall 2025) - "Additionally, these compounds demonstrated enhanced potency in comparison to the reference compounds (suramin, chlorogenic acid, ursolic acid and TCS401). The docking studies revealed hydrogen bond interactions with amino acid residues in the unstructured C-terminal region, while MDS showed that these interactions were maintained throughout the 200 ns simulation. This finding underscores the crucial role of the C-terminal region in the biological activity and inhibition of PTP1B."

Diabetes • Genetic Disorders • Metabolic Disorders • Obesity • Type 2 Diabetes Mellitus • LEP • PTPN1 • PTPN2

Anti-angiogenic effects of Moringa oleifera silver nanoparticles on endothelial cells: in vitro and ex vivo studies. (PubMed, Explor Target Antitumor Ther) - "Comparisons were made with known inhibitors: quercetin (15.11 μg/mL) and suramin (100 μg/mL)...MO-AgNPs exhibit strong anti-angiogenic and anti-invasive effects across various tumor-relevant models, highlighting their potential as a therapeutic agent against tumor progression and angiogenesis-related diseases. These results support further investigation of MO-AgNPs as a novel nanotherapeutic for cancer treatment."

Journal • Preclinical • Oncology

Impairment of P2 Receptor-Mediated Modulation of Skeletal Muscle Contractions in Transgenic Mice with Modeled Amyotrophic Lateral Sclerosis. (PubMed, Bull Exp Biol Med) - "Application of a non-selective P2 receptor antagonist suramine and application of ATP against the background of suramine did not change the amplitude of contractions of the studied skeletal muscles in FUS-transgenic mice. Thus, FUS model of ALS is based on the impairment of purinergic regulation of skeletal muscle contractile activity, which can play a role in the pathogenesis of ALS."

Journal • Preclinical • Amyotrophic Lateral Sclerosis • CNS Disorders • FUS

SKF-38393 regulates the expression of glutamic acid decarboxylase 67 via heparanase-1 in 6-hydroxydopamine-induced neurodegeneration. (PubMed, Sci Rep) - "In contrast, treatment with the heparanase inhibitor suramin led to a reduction in the GAD67 expression. Therefore, the DA D1-like receptor agonist SKF38393 can modulate GAD67 expression under DA degenerative conditions by interacting with heparanase-1."

Journal • CNS Disorders

Screening of Protein Tyrosine Phosphatase 1B Inhibitors from Actinomycete Extracts Using Recombinant Saccharomyces cerevisiae. (PubMed, J Microbiol Biotechnol) - "In a protein-chip assay, actinomycete extract 4585DW showed PTP1B inhibitory activity comparable to the positive controls, suramin and vanadate. The extract was non-cytotoxic in mammalian and yeast cells and inhibited PTP1B with Km and Vmax values of 10.91 ± 0.50 mM and 0.02 ± 0.00 μmol/min, respectively. In conclusion, 4585DW is a promising candidate for further investigation as a PTP1B inhibitor."

Journal • Preclinical • Diabetes • Genetic Disorders • Metabolic Disorders • Obesity • Oncology • Sarcoma • Solid Tumor • Type 2 Diabetes Mellitus • LEP • PTPN1

An Updated Insight on Phyto-therapeutics and Their Novel Approaches in the Management of Brain Cancer. (PubMed, Curr Top Med Chem) - "Recent developments in the treatment of brain cancer include the use of paclitaxel, temozolomide, and irinotecan. New medications, including thalidomide, suramin, and marimastat, can be used to treat brain tumour invasion and neoplastic angiogenesis...Phytochemicals themselves may be functionalized into a portion of the micron-sized particles to help them pass across the bloodbrain barrier and, once released into the brain microenvironment, use their therapeutic properties for therapy. Additionally, liposomes are useful to encapsulate chemotherapy medications and enable focused distribution via the blood-brain barrier."

Journal • Brain Cancer • Glioblastoma • Oncology • Solid Tumor

NTPDase8 Protects Against Liver Ischemia-Reperfusion Injury in Mice. (PubMed, FASEB J) - "The P2 receptor antagonist suramin decreased liver injury in Entpd8-/- mice indicating P2 signaling contributes to liver injury in these mice. Finally, Entpd8-/- mice had increased liver injury compared to WT mice also after hemorrhagic shock and resuscitation. These findings highlight the differential roles of NTPDase family members in the liver, with parenchymal/hepatocyte expression of NTPDase8 emerging as a critical suppressor of the inflammatory and metabolic responses to hepatic I/R insult, even in the presence of vascular NTPDase1 expression."

Journal • Preclinical • Cardiovascular • Hematological Disorders • Hepatology • Liver Failure • Reperfusion Injury • ENTPD1

Autoradiographic Investigation of P2Y12R, Synaptic Density, and Tau Expression in Alzheimer’s Disease (SNMMI 2025) - "Radiotracer binding was quantified using digital ARG in regions of interest (ROI), and non-specific binding was determined through homologous blockage with 10 µM of Suramin, Levetiracetam, and cold MK-6240, known ligands for P2Y12R, SV2A, and tau, respectively. [3H]PSB-0413 autoradiography had significantly decreased binding in sub-hippocampal regions including in the subiculum (SUB) (AD: 1.29 ± 0.61 µCi/g, n = 4 vs. NC: 2.56 ± 1.0 µCi/g, n = 3) and entorhinal cortex (EC) (AD: 1.41 ± 0.6 µCi/g, n = 5 vs. NC: 3.02 ± 0.86 µCi/g, n = 3)."

Alzheimer's Disease • CNS Disorders • Cognitive Disorders • Dementia • LPAR6

Differential regulation of MMP activity by TGFβ1 in fast- and slow- twitch muscle repair: insights from EDL and soleus muscle-derived myoblasts. (PubMed, Front Cell Dev Biol) - "Using siRNA to silence TβR1 expression, suramin as a competitive inhibitor of the TβR1 receptor, and inhibitors of both the canonical and non-canonical TGFβ signaling pathways, we characterized the role of TGFβ1 in regulating MMP-9 and MMP-2 during differentiation of myoblasts derived from slow-twitch Soleus and fast-twitch EDL muscles in vitro. Our results demonstrated that blocking TGFβ1 signaling pathway significantly improved regeneration in slow-twitch Soleus muscle, altered the activity of MMP-9 and MMP-2 in in vitro differentiating myoblasts, and Soleus and EDL-derived myoblasts differ in their response to inhibition of TGFβ-dependent signaling pathways."

Journal • Fibrosis • Immunology • MMP2 • MMP9 • TGFB1

Single-Molecule Assay Reveals Binding Dynamics of SARS-CoV-2 Polymerase Components and Provides a New Tool to Distinguish Polymerase Inhibitors. (PubMed, ACS Infect Dis) - "The SM-PIFE assay distinguishes inhibitors that impact protein binding from those that prevent replication, as demonstrated with suramin and remdesivir, respectively. The data reveals a correlation between binding lifetime/affinity and protein activity and underscores differences between coexpressed vs reconstituted mixtures, suggesting the existence of trapped conformations that may not evolve to productive binding."

Journal • Infectious Disease • Novel Coronavirus Disease • Respiratory Diseases

Suramin blocked hCAP18/LL-37-induced macrophage recruitment and M2 polarization to enhance the therapeutic efficacy of 1,25(OH)2D3 against hepatocellular carcinoma in vitro and in vivo mouse model. (PubMed, Front Nutr) - "While suramin potently disrupts this axis, blocking LL-37-mediated TAMs recruitment and M2 polarization, while promoting antitumor M1 phenotype responses. These findings highlight suramin as a promising adjunct to 1,25(OH)2D3-based immunotherapy for HCC."

IO biomarker • Journal • Preclinical • Hepatocellular Cancer • Oncology • Solid Tumor