probenecid / Generic mfg. - LARVOL DELTA

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

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

Treadmill exercise improves constipation in mice with chronic Parkinson's disease through activating autophagy (PubMed, Sheng Li Xue Bao) - "A chronic PD mouse model was prepared using 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) combined with probenecid (MPTP/p)...After treadmill exercise intervention, all the above changes in the PD group were significantly improved, and autophagy inhibitor 3MA could counteract these improving effects of treadmill exercise intervention. These results suggest that 8-week treadmill exercise can improve constipation symptoms in MPTP/p-induced chronic PD mice, and its protective effect may be achieved by activating autophagy."

Journal • Preclinical • CNS Disorders • Constipation • Gastroenterology • Gastrointestinal Disorder • Movement Disorders • Parkinson's Disease • BECN1 • CHAT

Phase 1 Study of the Pharmacokinetics of Amoxicillin in Pregnancy (clinicaltrials.gov) - P1 | N=13 | Completed | Sponsor: University of Alabama at Birmingham | Recruiting ➔ Completed | N=20 ➔ 13 | Trial completion date: Dec 2025 ➔ Jun 2025

Enrollment change • Trial completion • Trial completion date • Infectious Disease

TRPV2 in muscle satellite cells is crucial for skeletal muscle remodelling. (PubMed, Cell Death Dis) - "In cultured myofibre, MuSCs express TRPV2 and exhibit Ca2+ responses to the TRPV2 agonists 2-aminoethoxydiphenyl borate and probenecid, which are abolished upon TRPV2 deletion...Muscle-administered cardiotoxin promoted muscle regeneration and resulted in the appearance of numerous Pax7-positive MuSCs between myofibres...Additionally, MuSCs exhibit Ca2+ responses to hypo-osmotic stimuli, which are suppressed by TRPV2 inhibitors and TRPV2 deletion, suggesting that MuSCs exhibit TRPV2-dependent mechanical responses. These results establish TRPV2 as a critical regulator of MuSC-mediated muscle remodelling, an important finding that may lead to therapeutic strategies for muscle repair and adaptation."

Journal • IGF1 • PAX7 • TRPV2

Evaluative Review of Sulopenem Etzadroxil/Probenecid for Urinary Tract Infections: Clinical Evidence, Efficacy, and Safety Outcomes (ASHP 2025) - No abstract available

Clinical • Review • Infectious Disease • Nephrology

Biodistribution and Pathophysiology Study of 11C-para-aminobenzoic Acid (clinicaltrials.gov) - P=N/A | N=13 | Completed | Sponsor: Johns Hopkins University | Recruiting ➔ Completed | N=30 ➔ 13 | Trial completion date: Nov 2027 ➔ Nov 2025 | Trial primary completion date: Nov 2026 ➔ Nov 2025

Enrollment change • Trial completion • Trial completion date • Trial primary completion date • Infectious Disease • Inflammation

Lysophosphatidylcholine sensitizes TRPV2 by indirect mechanisms. (PubMed, Pflugers Arch) - "However, 3 µM LPC induced a reversible potentiation of membrane currents induced by 2-APB, cannabidiol (CBD), probenecid (PBC) and weak acids, but not to heat...A disruption of the actin cytoskeleton with cytochalasin D, but also the depletion of cholesterol or sphingomyelin from the cell membrane diminished the potentiating effects of LPC on TRPV2. In conclusion, we present novel data describing that the PLA2 downstream signaling lipid LPC amplifies TRPV2-mediated responses via indirect mechanisms that seem to involve a destabilization of lipid rafts and the actin cytoskeleton."

Journal • Cardiovascular • Oncology • Pain • TRPV2

Pharmacokinetics of Sulopenem Etzadroxil Plus Probenecid in Adolescents (clinicaltrials.gov) - P1 | N=12 | Recruiting | Sponsor: Iterum Therapeutics, International Limited | Initiation date: Sep 2025 ➔ Jan 2026 | Not yet recruiting ➔ Recruiting

Enrollment open • Trial initiation date • Infectious Disease

Effect of ibuprofen on the pharmacokinetics of intravenous flucloxacillin in healthy adults. (PubMed, Int J Antimicrob Agents) - "Orally administered ibuprofen had no measurable effect on plasma flucloxacillin PK in healthy adults. Given the lack of drug-drug interaction, there is no benefit to prescribe ibuprofen alongside flucloxacillin to increase flucloxacillin exposure."

Journal • PK/PD data • Infectious Disease • Pain

A Study to Learn About How the Study Medicines Called Itraconazole and Probenecid Change How the Body Processes PF-07220060 (clinicaltrials.gov) - P1 | N=28 | Recruiting | Sponsor: Pfizer | Not yet recruiting ➔ Recruiting

Enrollment open

Probenecid Treatment Inhibits Replication of the Edmonston Measles Virus Strain in Vero Cells. (PubMed, Viruses) - "MeV treatments may include vitamin A, ribavirin, the MeV vaccine, or human immunoglobulin for pregnant patients exposed to MeV but lacking immunity. This study indicates that pre-treatment with probenecid (prophylaxis) can inhibit the replication of the Edmonston MeV strain in VeroE6 cells (1.12 μM) and Vero-SLAM cells (1.03 μM), while treatment (1 h post-infection, hpi) inhibits replication in VeroE6 cells (1.32 μM) and Vero-SLAM cells (8.66 μM). These results suggest that probenecid is an effective, host-directed antiviral drug against MeV replication in vitro."

Journal • Infectious Disease • Measles • Mumps • Rubella

Colon-Specific Delivery of Probenecid Enhances Therapeutic Activity of the Uricosuric Agent Against Rat Colitis. (PubMed, Pharmaceutics) - "Moreover, PBN-GA therapeutically surpassed sulfasalazine, a currently used anti-IBD drug, in rat colitis. These results suggest that amide conjugation with GA can be used to design a colon-targeting prodrug for PBN. Colon-targeted PBN may not only enhance therapeutic effectiveness but also improve the safety of PBN repositioned for the treatment of IBD and may be a pharmacological alternative for current small-molecule anti-IBD drugs with low efficacy or serious adverse effects with long-term use."

Journal • Preclinical • Gastroenterology • Gastrointestinal Disorder • Gout • Immunology • Inflammation • Inflammatory Arthritis • Inflammatory Bowel Disease • Rheumatology