probenecid / Generic mfg. - LARVOL DELTA

p-Cresyl sulfate promotes smooth muscle cell proliferation and endothelial dysfunction, leading to development of neointimal hyperplasia. (PubMed, Kidney Res Clin Pract) - "In co-culture, p-CS-stimulated HUVECs enhanced SMC proliferation; this effect was attenuated by NAC, probenecid, or neutralizing antibodies against MCP-1 and ICAM-1...These findings suggest that p-CS may promote SMC proliferation both directly and indirectly through endothelial dysfunction, ultimately contributing to neointimal hyperplasia. Further studies are needed to clarify the clinical implications of p-CS in vascular access dysfunction."

Journal • Renal Disease • ICAM1 • NOS3

PROB2: Probenecid Administration for Alcohol Craving and Consumption (clinicaltrials.gov) - P2 | N=120 | Recruiting | Sponsor: Brown University | Not yet recruiting ➔ Recruiting | Initiation date: Nov 2025 ➔ Mar 2026

Enrollment open • Trial initiation date • Addiction (Opioid and Alcohol)

EVALUATION OF RENAL FUNCTION AND HYPERTENSION STATUS IN PAEDIATRIC PATIENTS WHO UNDERWENT BONE MARROW TRANSPLANTATION (EBMT 2026) - "BK virus infection in 43.4% (n=148) of the patients and hemorrhagic cystitis developed in 17.4% (n=59), most commonly treated with cidofovir + probenecid (n=30, 50.8%). Renal dysfunction after pediatric HSCT is multifactorial and significantly impairs long-term survival. Close monitoring of hypertension and infections—both major contributors to renal injury—is essential, along with timely preventive measures."

Clinical • Acute Graft versus Host Disease • Acute Kidney Injury • Bone Marrow Transplantation • Cardiovascular • Chronic Graft versus Host Disease • Chronic Kidney Disease • Graft versus Host Disease • Hypertension • Immunology • Infectious Disease • Nephrology • Pediatrics • Renal Disease • Transplantation

EVALUATION OF RENAL FUNCTION AND HYPERTENSION STATUS IN PAEDIATRIC PATIENTS WHO UNDERWENT BONE MARROW TRANSPLANTATION (EBMT 2026) - "BK virus infection in 43.4% (n=148) of the patients and hemorrhagic cystitis developed in 17.4% (n=59), most commonly treated with cidofovir + probenecid (n=30, 50.8%). Renal dysfunction after pediatric HSCT is multifactorial and significantly impairs long-term survival. Close monitoring of hypertension and infections—both major contributors to renal injury—is essential, along with timely preventive measures."

Clinical • Acute Graft versus Host Disease • Acute Kidney Injury • Bone Marrow Transplantation • Cardiovascular • Chronic Graft versus Host Disease • Chronic Kidney Disease • Graft versus Host Disease • Hypertension • Immunology • Infectious Disease • Nephrology • Pediatrics • Renal Disease • Transplantation

18β-Glycyrrhetinic acid attenuates endoplasmic reticulum stress and neuroinflammation via the PI3K/AKT-dependent pathway in MPTP/p-induced Parkinson's disease mouse model. (PubMed, 3 Biotech) - "This study investigates the neuroprotective potential of 18β-Glycyrrhetinic acid (18βGA) in a chronic MPTP/probenecid (MPTP/p)-induced mouse model of PD...Collectively, these findings demonstrate that 18βGA exerts robust neuroprotective effects by attenuating mitochondrial dysfunction, oxidative stress, ER stress, inflammation, and apoptosis, highlighting its potential as a promising therapeutic candidate for Parkinson's disease. The online version contains supplementary material available at 10.1007/s13205-026-04757-4."

IO biomarker • Journal • Preclinical • CNS Disorders • Inflammation • Metabolic Disorders • Movement Disorders • Parkinson's Disease • BCL2 • CASP3 • HSPA5 • IL1B • TNFA

Consensus Molecules Associated with Parkinson's Disease. (PubMed, Neurol Int) - "Drugs include L-dopa (49%), carbidopa (63%), benserazide (50%), entacapone (74%), tolcapone (56%), rasagiline (76%), selegiline (46%), pargyline (4%), ropinirole (61%), pramipexole (56%), lisuride (27%), cabergoline (16%), bromocriptine (12%), and zonisamide (9%). Adjunctive therapies include droxidopa (33%), trihexyphenidyl (28%), biperiden (17%), amantadine (24%), memantine (7%), rivastigmine (13%), donepezil (6%), galantamine (4%), domperidone (6%), clonazepam (4%), tetrabenazine (16%), mazindol (13%), quetiapine (6%), and clozapine (4%). Contraindicated drugs include haloperidol (4%), sulpiride (3%), and methyldopa (6%)...Chemical inducers of PD include 6-hydroxydopamine (40%), N-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP, 78%), tetrahydropyridine (77%), probenecid (4%), quinolinic acid (4%), 1,2,3,4-tetrahydroisoquinoline (TIQ, 16%), salsolinol (32%), rotenone (25%), and β-Methylamino-L-alanine (BMAA, 29%). Notably, our study highlights conditional essential..."

Journal • Review • CNS Disorders • Movement Disorders • Parkinson's Disease

GHD_2024_12: Efficacy of probenecid on cluster seizures during dosage reduction of Anti Seizure Medication (ASM) in presurgical focal epilepsy video-EEG monitoring (clinicaltrialsregister.eu) - P1/2 | N=192 | Not yet recruiting | Sponsor: Fondation A De Rothschild

New P1/2 trial • CNS Disorders • Epilepsy

Data Analysis for Drug Repurposing for Effective Alzheimer's Medicines - (DREAM) Probenecid vs Allopurinol (clinicaltrials.gov) - P=N/A | N=294878 | Completed | Sponsor: Brigham and Women's Hospital | Active, not recruiting ➔ Completed

Trial completion • Alzheimer's Disease • CNS Disorders • Gout • Inflammatory Arthritis • Rheumatology

Mechanisms and Targeted Therapeutic Strategies for Inflammation and Renal Fibrosis in Hyperuricemic Nephropathy. (PubMed, Cell Biochem Funct) - "Current treatments primarily consist of urate-lowering drugs such as allopurinol, febuxostat, benzbromarone, and probenecid, but their use is constrained by adverse effects including hepatotoxicity, nephrotoxicity, and Stevens-Johnson syndrome. Therefore, targeting inflammatory and fibrotic mechanisms presents a promising therapeutic approach. This review outlines key molecular pathways in HN, discusses contemporary research challenges, and suggests future directions for improved therapeutic strategies."

Journal • Review • Fibrosis • Immunology • Inflammation • Nephrology • Renal Disease • Steven-Johnson Syndrome • NQO1

Calcinosis Cutis Universalis: A Review of Therapeutic Strategies and Surgical Management. (PubMed, J Clin Med) - " Pharmacological treatments-including bisphosphonates, calcium-channel blockers, tetracyclines, phosphate binders, probenecid, immunomodulatory agents, biologics, colchicine, sodium thiosulfate and JAK inhibitors-show heterogeneous and often partial efficacy, with more favorable responses in early or localized disease. Surgical interventions such as excision, curettage, CO2 laser ablation, and reconstructive procedures provide meaningful symptomatic relief in selected patients but are associated."

Journal • Review • Dermatomyositis • Immunology • Infectious Disease • Inflammatory Arthritis • Lupus • Metabolic Disorders • Myositis • Pain • Rheumatology • Scleroderma • Systemic Lupus Erythematosus • Systemic Sclerosis

A Large Deletion With a Large Impact: Homozygous 5,600 bp Deletion of the GALNT3 Gene Causing Hyperphosphatemic Tumoral Calcinosis. (PubMed, Kidney Med) - "Treatment options to reduce blood phosphate levels have only been studied in case reports and small cohorts, with positive effects from phosphate binders, acetazolamide, anti-inflammatory drugs, probenecid, nicotinamide, and sodium thiosulfate. In this report, we present the case of a 50-year-old woman with a large (at least 5,600 base pair) deletion in the gene encoding for GalNAc-T3 (GALNT3) who experienced bone pain during childhood and calcifications of her lower limbs at least since her mid-thirties. Intragenic GALNT3 copy number variants have, to our knowledge, not yet been described as a cause of HTC."

Journal • Chronic Kidney Disease • Metabolic Disorders • Musculoskeletal Pain • Nephrology • Oncology • Pain • Rare Diseases • Renal Disease • FGF23

N,N-dimethyltryptamine (DMT) is neither formed nor retained in serotonin terminals in the rat brain. (PubMed, Neuropharmacology) - "We tested the joint hypotheses that endogenous DMT would accumulate in rat brain after inhibiting monoamine oxidase with pargyline, whereas its acidic metabolite 3-indoleacetic acid (3-IAA) would accumulate after pretreatment with the inhibitor of acidic metabolic transport, probenecid. We also tested the hypothesis that pretreatment with inhibitors of plasma membrane 5-HT uptake (escitalopram, ESC) or the vesicular monoamine transporter 2 (dihydrotetrabenazine, DTBZ) would reduce the retention in brain of exogenous DMT after administration of DMT+harmine (1 mg/kg each)...ESC did not alter the disposition of exogenous DMT or its metabolite 3-IAA, whereas DTBZ slightly increased 3-IAA formation in some brain regions. In summary, we could not detect an endogenous DMT pool in rat brain, and saw scant evidence of retention of exogenous DMT in 5-HT terminals."

Journal • Preclinical

Pannexin-1 Inhibits Pathologic Neovascularization in Oxygen-Induced Retinopathy by Targeting the HIF-1α/VEGF Pathway in Vitro. (PubMed, Curr Eye Res) - "Probenecid (PBC) treatment inhibited the hypoxia-driven upregulation of Panx1, HIF-1α, and VEGF at both mRNA and protein levels. CCK-8 assays showed that hypoxia significantly impaired HRMEC proliferation (24h: p < 0.05; 48h: p < 0.001), and PBC further suppressed this effect (p < 0.0001). Panx1 inhibition (via PBC) suppresses the HIF-1α/VEGF signaling pathway and reduces hypoxia-induced endothelial cell proliferation, providing a novel preventive strategy for ROP."

Journal • Preclinical • Age-related Macular Degeneration • Ophthalmology • Retinal Disorders • Retinopathy of Prematurity • HIF1A

TENS alleviates CP/CPPS-related inflammation and pain by modulating Kir2.1-dependent macrophage polarization. (PubMed, Front Immunol) - "In cell experiments, RAW264.7 macrophages were grouped into control, LPS-stimulated, electrical stimulation (ES)-treated (0.1-0.5 V/cm), and ES + pharmacological intervention (zacopride/probenecid) groups to study repolarization mechanisms...Agonists of Kir2.1 TRPV2 reversed these effects. TENS alleviates CP/CPPS by promoting M1-to-M2 macrophage repolarization, representing a promising therapeutic strategy."

Journal • Benign Prostatic Hyperplasia • Gynecology • Immunology • Inflammation • Musculoskeletal Pain • Pain • STAT1 • STAT6 • TRPV2

Calcitriol-Mediated Modulation of Organic Anion Transporters: Insights from Endogenous Biomarkers and Methotrexate Pharmacokinetics. (PubMed, Eur J Pharm Sci) - "Additional probenecid inhibition studies supported the Oat1-mediated modulation. Taurine induced more significant changes than PDA, indicating its greater sensitivity as an endogenous biomarker for Oat1 activity. These findings highlight the modulatory effects of calcitriol on Oat-mediated transport and demonstrate the utility of taurine and PDA as translational biomarkers for investigating transporter-mediated drug-drug interactions in drug development."

Biomarker • Journal • PK/PD data

Evaluation of Probenecid Against Filovirus Replication in Vero E6 Cells. (PubMed, Viruses) - "It also reduced plaque size in infected Vero cell lawns, suggesting reduced virus spread. These studies show that probenecid is an effective, broad-spectrum, host-directed antiviral drug."

Journal • Ebola Virus Disease • Hematological Disorders • Infectious Disease • Influenza • Novel Coronavirus Disease • Respiratory Diseases • Respiratory Syncytial Virus Infections

SerendipityPB1: Probenecid (PB) to Treat Hereditary Nephrogenic Diabetes Insipidus (NDI), ADPKD Treated With Tolvaptan, and Severely Polyuric Patients With Previous Lithium Administration (clinicaltrials.gov) - P2 | N=36 | Completed | Sponsor: Mayo Clinic | Recruiting ➔ Completed

Trial completion • Autosomal Dominant Polycystic Kidney Disease • Genetic Disorders • Metabolic Disorders • Nephrology • Polycystic Kidney Disease • Renal Disease

Australian Gonococcal Surveillance Program, 1 April to 30 June 2025. (PubMed, Commun Dis Intell (2018)) - "The antibiotics reported represent current or potential agents used for the treatment of gonorrhoea, and include ceftriaxone, azithromycin, ciprofloxacin and penicillin. More recently, gentamicin and tetracycline are included in the AGSP Annual Report...In these regions, an oral treatment regimen comprising amoxycillin, probenecid, and azithromycin was recommended. However, since January 2023, increasing reports of penicillin-resistant N. gonorrhoeae in the Northern Territory have changed treatment recommendations to align with the majority of Australia.1 Additional data on other antibiotics are reported in the AGSP Annual Report. The AGSP has a programme-specific quality assurance process."

Journal • Infectious Disease

A comparative in vitro analysis of pannexin1-targeting agents. (PubMed, Biochem Pharmacol) - "Thus, carbenoxolone, probenecid, 10Panx1 and pannexin1-targeting nanobodies achieved blocking effects by reducing both ATP release and YO-PRO1 uptake. Collectively, the nanobodies show inhibitory effects by using smaller concentrations than traditional pannexin1 channel inhibitors. Therefore, nanobodies offer unique features for the development of pannexin1 channel inhibitors as novel anti-inflammatory therapeutics."

Journal • Preclinical • Inflammation

Gepotidacin (Blujepa) - a new antibiotic for uncomplicated UTI. (PubMed, Med Lett Drugs Ther) - No abstract available

Journal • Infectious Disease • Nephrology

The Re-Prosper HF Study (clinicaltrials.gov) - P2/3 | N=99 | Completed | Sponsor: VA Office of Research and Development | Active, not recruiting ➔ Completed

Trial completion • Cardiovascular • Congestive Heart Failure • Heart Failure

PROBCLUSTER: Efficacy of Probenecid on Cluster Seizures During Anti Seizure Medication Withdrawal in Presurgical Focal Epilepsy Video-EEG Monitoring (clinicaltrials.gov) - P2 | N=600 | Not yet recruiting | Sponsor: Fondation Ophtalmologique Adolphe de Rothschild

New P2 trial • CNS Disorders • Epilepsy

Use of cimetidine to enhance systemic acyclovir concentrations in patients with ineffective suppressive therapy for recurring herpes simplex virus infections: A novel purpose for an old drug. (PubMed, Br J Clin Pharmacol) - "We report a series of patients nonresponsive to suppressive valacyclovir therapy, explained by subtherapeutic acyclovir plasma levels. After a dose increase, or in some patients only after concomitant prescription of cimetidine, adequate levels were reached associated with significant clinical improvement."

Journal • Herpes Simplex • Infectious Disease

Probenecid Suppresses Migration, invasion and angiogenesis in hepatocellular carcinoma by modulating purinergic signaling and p38 MAPK pathway. (PubMed, Biochem Pharmacol) - "Altogether, these findings indicate that PBN may represent a promising candidate for drug repurposing in hepatocellular carcinoma. By modulating purinergic signaling and selectively inhibiting p38 MAPK, PBN appears to limit tumor invasiveness and angiogenesis, supporting its potential relevance for further preclinical and clinical investigation."

Journal • Gout • Hepatocellular Cancer • Inflammatory Arthritis • Oncology • Rheumatology • Solid Tumor

Drug Development. (PubMed, Alzheimers Dement) - "The inclusion criteria include mild cognitive impairment or mild dementia due to AD, AD medications are planned to remain stable throughout, willingness and ability to complete all aspects of the study including assessments, neuropsychological testing, and MRI. Exclusion criteria includes clinically significant abnormalities in screening laboratory tests, chronic liver disease, renal insufficiency, poorly managed hypertension and participants taking the following concomitant medications, based on the current Prescribing Information for bumetanide: lithium, drugs with ototoxic potential, drugs with nephrotoxic potential, probenecid, and indomethacin We present the clinical trial protocol and design for a phase II trial evaluating the effect of bumetanide in AD."

Clinical • Journal • Alzheimer's Disease • Cardiovascular • CNS Disorders • Cognitive Disorders • Dementia • Hepatology • Hypertension • Nephrology • Renal Disease • APOE