pentosan sulfuric polyester


Summary: A sulfated pentosyl polysaccharide with heparin-like properties.

Top Publications

  1. Shen B, Shimmon S, Smith M, Ghosh P. Biosensor analysis of the molecular interactions of pentosan polysulfate and of sulfated glycosaminoglycans with immobilized elastase, hyaluronidase and lysozyme using surface plasmon resonance (SPR) technology. J Pharm Biomed Anal. 2003;31:83-93 pubmed
    ..The SPR technology therefore offers not only a sensitive and reproducible method for ranking noncompetitive enzyme inhibitors for drug discovery but a rapid and quantitative bioassay for monitoring batch consistency of manufacture. ..
  2. Dell J, Butrick C. Multimodal therapy for painful bladder syndrome/interstitial cystitis. J Reprod Med. 2006;51:253-60 pubmed
    ..Patient education and support are critical in managing this complex but treatable disorder. ..
  3. Kwan C, Bell R, Koenig T, Bischofberger A, Horadagoda N, Perkins N, et al. Effects of intra-articular sodium pentosan polysulfate and glucosamine on the cytology, total protein concentration and viscosity of synovial fluid in horses. Aust Vet J. 2012;90:315-20 pubmed publisher
    ..Evaluate synovial fluid cytology, total protein concentration and viscosity after intra-articular administration of combined pentosan polysulfate and glucosamine in horses...
  4. Budsberg S, Bergh M, Reynolds L, Streppa H. Evaluation of pentosan polysulfate sodium in the postoperative recovery from cranial cruciate injury in dogs: a randomized, placebo-controlled clinical trial. Vet Surg. 2007;36:234-44 pubmed
    ..PPS administered after stabilization of the cruciate deficient stifle may prove to be a useful adjunctive treatment option, although further studies are necessary to substantiate this claim. ..
  5. Honda H, Sasaki K, Minaki H, Masui K, Suzuki S, Doh ura K, et al. Protease-resistant PrP and PrP oligomers in the brain in human prion diseases after intraventricular pentosan polysulfate infusion. Neuropathology. 2012;32:124-32 pubmed publisher
    ..Although intraventricular PPS infusion might modify the accumulation of PrP oligomers in the brains of patients with prion diseases, the therapeutic effects are still uncertain. ..
  6. Dimitrakov J, Kroenke K, Steers W, Berde C, Zurakowski D, Freeman M, et al. Pharmacologic management of painful bladder syndrome/interstitial cystitis: a systematic review. Arch Intern Med. 2007;167:1922-9 pubmed
    ..Pentosan polysulfate may be modestly beneficial for symptoms of PBS/IC. There is insufficient evidence for other pharmacologic treatments. A consensus on standardized outcome measures is urgently needed. ..
  7. Takizawa M, Yatabe T, Okada A, Chijiiwa M, Mochizuki S, Ghosh P, et al. Calcium pentosan polysulfate directly inhibits enzymatic activity of ADAMTS4 (aggrecanase-1) in osteoarthritic chondrocytes. FEBS Lett. 2008;582:2945-9 pubmed publisher
    ..These data suggest that CaPPS could function as chondroprotective agent for the treatment of osteoarthritis by inhibition of ADAMTS4 through interaction with the C-terminal ancillary domain. ..
  8. Deli M, Veszelka S, Csiszár B, Tóth A, Kittel A, Csete M, et al. Protection of the blood-brain barrier by pentosan against amyloid-?-induced toxicity. J Alzheimers Dis. 2010;22:777-94 pubmed publisher
    ..The present data further support the toxic effects of amyloid peptides on brain endothelial cells, and can contribute to the development of molecules protecting the blood-brain barrier in Alzheimer's disease. ..
  9. Lupia E, Zheng F, Grosjean F, Tack I, Doublier S, Elliot S, et al. Pentosan polysulfate inhibits atherosclerosis in Watanabe heritable hyperlipidemic rabbits: differential modulation of metalloproteinase-2 and -9. Lab Invest. 2012;92:236-45 pubmed publisher
    ..Thus, PPS may be a useful agent in inhibiting the progression of atherosclerosis. ..

More Information


  1. Moldwin R, Sant G. Interstitial cystitis: a pathophysiology and treatment update. Clin Obstet Gynecol. 2002;45:259-72 pubmed
  2. Ghosh P. The pathobiology of osteoarthritis and the rationale for the use of pentosan polysulfate for its treatment. Semin Arthritis Rheum. 1999;28:211-67 pubmed
    ..However, additional long-term clinical studies employing methods of assessing joint structural changes will be needed to confirm this view. ..
  3. Troeberg L, Mulloy B, Ghosh P, Lee M, Murphy G, Nagase H. Pentosan polysulfate increases affinity between ADAMTS-5 and TIMP-3 through formation of an electrostatically driven trimolecular complex. Biochem J. 2012;443:307-15 pubmed publisher
    ..4 M NaCl. These results suggest that PPS enhances the affinity between ADAMTS-5 and TIMP-3 by forming electrostatically driven trimolecular complexes under physiological conditions. ..
  4. Ghosh P, Cheras P. Vascular mechanisms in osteoarthritis. Best Pract Res Clin Rheumatol. 2001;15:693-709 pubmed
    ..Experimental studies are described which support this proposal. ..
  5. Troeberg L, Fushimi K, Khokha R, Emonard H, Ghosh P, Nagase H. Calcium pentosan polysulfate is a multifaceted exosite inhibitor of aggrecanases. FASEB J. 2008;22:3515-24 pubmed publisher
    ..Studies with TIMP-3-null mouse cartilage indicated that CaPPS inhibition of aggrecan degradation is TIMP-3 dependent. These unique properties make CaPPS a prototypic disease-modifying agent for osteoarthritis. ..
  6. Miyata N, Kumagai K, Osaki M, Murata M, Tomita M, Hozumi A, et al. Pentosan reduces osteonecrosis of femoral head in SHRSP. Clin Exp Hypertens. 2010;32:511-6 pubmed publisher
    ..Pentosan seems to reduce the incidence of ONFH in SHRSP by improving lipid metabolism and decreasing oxidative stress. ..
  7. McIlwraith C, Frisbie D, Kawcak C. Evaluation of intramuscularly administered sodium pentosan polysulfate for treatment of experimentally induced osteoarthritis in horses. Am J Vet Res. 2012;73:628-33 pubmed publisher
    ..To assess clinical, radiographic, histologic, and biochemical effects of sodium pentosan polysulfate (NaPPS) administered IM for treatment of experimentally induced osteoarthritis in horses...
  8. Sant G, Propert K, Hanno P, Burks D, Culkin D, Diokno A, et al. A pilot clinical trial of oral pentosan polysulfate and oral hydroxyzine in patients with interstitial cystitis. J Urol. 2003;170:810-5 pubmed
    ..This trial demonstrated the feasibility of conducting a multicenter randomized clinical trial in IC using uniform procedures and outcomes. However, slow recruitment underscored the difficulties of evaluating commonly available IC drugs. ..
  9. Anger J, Zabihi N, Clemens J, Payne C, Saigal C, Rodriguez L. Treatment choice, duration, and cost in patients with interstitial cystitis and painful bladder syndrome. Int Urogynecol J. 2011;22:395-400 pubmed publisher
    ..Hydrodistension and intravesical instillations were utilized in less than 25% of patients. Hydrodistension was used more frequently among subjects with a new diagnosis; this may reflect its utilization as part of a diagnostic algorithm. ..
  10. Mayor S. Small improvement seen in teenager with vCJD. BMJ. 2003;327:765 pubmed
  11. Pazin C, de Souza Mitidieri A, Silva A, Gurian M, Poli Neto O, Rosa e Silva J. Treatment of bladder pain syndrome and interstitial cystitis: a systematic review. Int Urogynecol J. 2016;27:697-708 pubmed publisher
    ..The lack of standardized treatment may be related to the diversity of interventions used; therefore, further studies with better methodological quality are needed. ..
  12. El Khoudary S, Talbott E, Bromberger J, Chang C, Songer T, Davis E. Severity of interstitial cystitis symptoms and quality of life in female patients. J Womens Health (Larchmt). 2009;18:1361-8 pubmed publisher
  13. Meyer D, Gregorin J, Schmid H. [Diagnosis and treatment of interstitial cystitis]. Praxis (Bern 1994). 2011;100:221-7 pubmed publisher
  14. Duthie G, Whyte L, Chandran H, Lawson S, Velangi M, McCarthy L. Introduction of sodium pentosan polysulfate and avoidance of urethral catheterisation: improved outcomes in children with haemorrhagic cystitis post stem cell transplant/chemotherapy. J Pediatr Surg. 2012;47:375-9 pubmed publisher
    ..05). Early identification, avoidance of urethral catheterisation, and use of SPP significantly reduces blood transfusion requirements and mortality from HC. ..
  15. Stengel A, Bach C, Vorberg I, Frank O, Gilch S, Lutzny G, et al. Prion infection influences murine endogenous retrovirus expression in neuronal cells. Biochem Biophys Res Commun. 2006;343:825-31 pubmed
    ..The results suggest that prion infection influences ERV expression in neuronal cell lines, that this influence is cell line-specific, ERV-specific, and responsive to anti-prion compound treatment. ..
  16. Fallgren C, Andersson A, Ljungh A. The role of glycosaminoglycan binding of staphylococci in attachment to eukaryotic host cells. Curr Microbiol. 2001;43:57-63 pubmed
    ..These observations may suggest that at least one mode of staphylococcal attachment utilizes GAG chains present on the surface of virtually all adherent cells. ..
  17. Persu C, Cauni V, Gutue S, Blaj I, Jinga V, Geavlete P. From interstitial cystitis to chronic pelvic pain. J Med Life. 2010;3:167-74 pubmed
    ..This condition is best managed by using a multidisciplinary approach. Management requires a good integration and knowledge of all pelvic organ systems and other systems including musculoskeletal, neurologic, and psychiatric systems. ..
  18. Binder I, Rossbach G, van Ophoven A. [The complexity of chronic pelvic pain exemplified by the condition currently called interstitial cystitis. Part 2: Treatment]. Aktuelle Urol. 2008;39:289-97 pubmed publisher
    ..There are hardly any controlled studies on alternative curative procedures although rather good results have been obtained in chronic pelvic pain syndrome with acupuncture as an additional therapeutic modality. ..
  19. Parry A, Baker I, Stacey R, Wimalaratna S. Long term survival in a patient with variant Creutzfeldt-Jakob disease treated with intraventricular pentosan polysulphate. J Neurol Neurosurg Psychiatry. 2007;78:733-4 pubmed
    ..Treatment with PPS appeared to be safe and well tolerated and was associated with prolonged survival (51 months) when compared to natural history studies. However, PPS treatment did not appear to arrest the progression of the disease. ..
  20. Sakaguchi S. [Systematic review of the therapeutics for prion diseases]. Brain Nerve. 2009;61:929-38 pubmed
    ..In this communication, we systematically list these anti-prion compounds and summarize their effectiveness and possible mechanisms of action. ..
  21. Davis E, El Khoudary S, Talbott E, Davis J, Regan L. Safety and efficacy of the use of intravesical and oral pentosan polysulfate sodium for interstitial cystitis: a randomized double-blind clinical trial. J Urol. 2008;179:177-85 pubmed
    ..We examined the safety and the efficacy of a combination of intravesical and oral pentosan polysulfate sodium in comparison to only oral pentosan polysulfate sodium in treating interstitial cystitis...
  22. Moldwin R, Evans R, Stanford E, Rosenberg M. Rational approaches to the treatment of patients with interstitial cystitis. Urology. 2007;69:73-81 pubmed
    ..Other forms of care ranging from intravesical therapy to endoscopic, percutaneous, or open surgery are options that may be used singly or in combination to optimize symptom reduction...
  23. Parsons C, Greene R, Chung M, Stanford E, Singh G. Abnormal urinary potassium metabolism in patients with interstitial cystitis. J Urol. 2005;173:1182-5 pubmed
    ..Higher urinary K in successfully treated vs untreated patients may reflect decreasing urinary K absorption due to mucosal repair and a resulting decrease in epithelial permeability. K/mg Cr appears accurate for normalizing urinary K. ..
  24. Dupiereux I, Falisse Poirrier N, Zorzi W, Watt N, Thellin O, Zorzi D, et al. Protective effect of prion protein via the N-terminal region in mediating a protective effect on paraquat-induced oxidative injury in neuronal cells. J Neurosci Res. 2008;86:653-9 pubmed
  25. Lee E, Pavy M, Young N, Freeman C, Lobigs M. Antiviral effect of the heparan sulfate mimetic, PI-88, against dengue and encephalitic flaviviruses. Antiviral Res. 2006;69:31-8 pubmed
    ..In mouse models for DEN and flaviviral encephalitis, only PI-88 demonstrated a significant beneficial effect in disease outcome...
  26. Kutlar A, Ataga K, McMahon L, Howard J, Galacteros F, Hagar W, et al. A potent oral P-selectin blocking agent improves microcirculatory blood flow and a marker of endothelial cell injury in patients with sickle cell disease. Am J Hematol. 2012;87:536-9 pubmed publisher
    ..They also demonstrate that oral PPS is beneficial to microvascular sickle cell blood flow and has potential as an efficacious agent for long-term prophylactic therapy of SCD. ..
  27. Lubeck D, Whitmore K, Sant G, Alvarez Horine S, Lai C. Psychometric validation of the O'leary-Sant interstitial cystitis symptom index in a clinical trial of pentosan polysulfate sodium. Urology. 2001;57:62-6 pubmed
    ..The ICSI is a valid, reliable, and responsive measure of change in IC symptoms. This outcome measure should be utilized in future treatment outcomes studies in IC. ..
  28. Yokoyama T, Takeuchi A, Yamamoto M, Kitamoto T, Ironside J, Morita M. Heparin enhances the cell-protein misfolding cyclic amplification efficiency of variant Creutzfeldt-Jakob disease. Neurosci Lett. 2011;498:119-23 pubmed publisher
    ..Heparin-assisted cell-PMCA of vCJD represents a significant step toward detecting very minute amounts of PrP(Sc) in the body fluids of asymptomatic vCJD patients...
  29. Nickel J, Payne C, Forrest J, Parsons C, Wan G, Xiao X. The relationship among symptoms, sleep disturbances and quality of life in patients with interstitial cystitis. J Urol. 2009;181:2555-61 pubmed publisher
    ..We conducted a retrospective analysis to determine associations among symptoms, sleep disturbances and quality of life in responder and nonresponder groups of patients with interstitial cystitis...
  30. Vana K, Zuber C, Pflanz H, Kolodziejczak D, Zemora G, Bergmann A, et al. LRP/LR as an alternative promising target in therapy of prion diseases, Alzheimer's disease and cancer. Infect Disord Drug Targets. 2009;9:69-80 pubmed
  31. Terada T, Tsuboi Y, Obi T, Doh ura K, Murayama S, Kitamoto T, et al. Less protease-resistant PrP in a patient with sporadic CJD treated with intraventricular pentosan polysulphate. Acta Neurol Scand. 2010;121:127-30 pubmed publisher
    ..These findings suggest that intraventricular PPS infusion might modify the accumulation of abnormal prion proteins in the brains of patients with sporadic Creutzfeldt-Jakob disease. ..
  32. Abdel Haq H, Bossù E. Capillary electrophoresis as a tool for the characterization of pentosan nanoparticles. J Chromatogr A. 2012;1257:125-30 pubmed publisher
    ..Moreover, it allowed the evaluation of the size and charge of the NPs. This protocol might be suitable for the characterization of other kinds of NPs also. ..
  33. Wu E, Birnbaum H, Mareva M, Parece A, Huang Z, Mallett D, et al. Interstitial Cystitis: Cost, treatment and co-morbidities in an employed population. Pharmacoeconomics. 2006;24:55-65 pubmed
  34. Nickel J, Parsons C, Forrest J, Kaufman D, Evans R, Chen A, et al. Improvement in sexual functioning in patients with interstitial cystitis/painful bladder syndrome. J Sex Med. 2008;5:394-9 pubmed
    ..Sexual functioning is one of the strongest predictors of poorer quality of life (QOL) in patients diagnosed with interstitial cystitis/painful bladder syndrome (IC/PBS)...
  35. Shah H, Conkie J, Tait R, Johnson J, Wilson C. A novel, biodegradable and reversible polyelectrolyte platform for topical-colonic delivery of pentosan polysulphate. Int J Pharm. 2011;404:124-32 pubmed publisher
    ..The digestion of the reversible polyelectrolyte complexes was measured using a dinitro salicylic acid assay and an increased release of drug was also confirmed in the presence of bacterial enzymes. ..
  36. Todd N, Morrow J, Doh ura K, Dealler S, O Hare S, Farling P, et al. Cerebroventricular infusion of pentosan polysulphate in human variant Creutzfeldt-Jakob disease. J Infect. 2005;50:394-6 pubmed
    ..Follow-up CT scans demonstrated progressive brain atrophy during PPS administration. Further basic and clinical research is needed in order to address the issue of efficacy of PPS in vCJD and in other prion diseases. ..
  37. Vij M, Srikrishna S, Cardozo L. Interstitial cystitis: diagnosis and management. Eur J Obstet Gynecol Reprod Biol. 2012;161:1-7 pubmed publisher
    ..This condition usually warrants a multidisciplinary approach for optimum outcome. This article gives an overview of the changes in definition, aetiopathogenesis and available treatments. ..
  38. Lynch G, Low L, Li S, Sloane A, Adams S, Parish C, et al. Sulfated polyanions prevent HIV infection of lymphocytes by disruption of the CD4-gp120 interaction, but do not inhibit monocyte infection. J Leukoc Biol. 1994;56:266-72 pubmed
    ..However, HIV infection and gp120 binding to monocytes was unaffected by SPs, probably because SPs were unable to block the CD4-gp 120 interaction in monocytes. ..
  39. Jerebtsova M, Wong E, Przygodzki R, Tang P, Ray P. A novel role of fibroblast growth factor-2 and pentosan polysulfate in the pathogenesis of intestinal bleeding in mice. Am J Physiol Heart Circ Physiol. 2007;292:H743-50 pubmed
    ..These findings might have wider clinical implications for the systemic use of PPS and other heparinoids in the treatment of patients with angiogenic diseases associated with high levels of circulating FGF-2. ..
  40. Lamb G, Posterino G, Stephenson D. Effects of heparin on excitation-contraction coupling in skeletal muscle toad and rat. J Physiol. 1994;474:319-29 pubmed
    ..7. These results indicate that heparin blocks E-C coupling in toad muscle if, and only if, it is present when the voltage sensors are activated by depolarization.(ABSTRACT TRUNCATED AT 400 WORDS) ..
  41. Daha L, Riedl C, Lazar D, Simak R, Pfluger H. Effect of intravesical glycosaminoglycan substitution therapy on bladder pain syndrome/interstitial cystitis, bladder capacity and potassium sensitivity. Scand J Urol Nephrol. 2008;42:369-72 pubmed publisher
    ..2 M KCl solution. These data demonstrate that in patients who respond symptomatically to intravesical GAG substitution therapy, cystometric bladder capacity is increased, whereas non-responders experience a decrease in bladder capacity. ..
  42. Frith J, Menzies D, Cameron A, Ghosh P, Whitehead D, Gronthos S, et al. Effects of bound versus soluble pentosan polysulphate in PEG/HA-based hydrogels tailored for intervertebral disc regeneration. Biomaterials. 2014;35:1150-62 pubmed publisher
  43. Waters M, Suleskey J, Finkelstein L, Van Overbeke M, Zizza V, Stommel M. Interstitial cystitis: a retrospective analysis of treatment with pentosan polysulfate and follow-up patient survey. J Am Osteopath Assoc. 2000;100:S13-8 pubmed
    ..001) over the treatment interval. The most common side effect attributable to PPS was diarrhea in 15% of subjects. Pentosan proved to be an efficacious option for reducing the debilitating symptoms of interstitial cystitis. ..
  44. Jolobe O. Hyperkalaemic paralysis. Age Ageing. 2003;32:556-7 pubmed
  45. Horiuchi M. [Prion diseases as zoonosis]. Uirusu. 2005;55:45-53 pubmed
    ..Furthermore, it is also important to establish therapeutics of human prion diseases. ..
  46. Erickson D, Sheykhnazari M, Bhavanandan V. Molecular size affects urine excretion of pentosan polysulfate. J Urol. 2006;175:1143-7 pubmed
    ..In patients with IC who are on oral PPS the PPS recovered in the urine is all of LMW. In rabbits the HMW fraction of PPS is recovered in small amounts from urine after intravenous administration and not at all after oral administration. ..
  47. Doh ura K. [Innovation of therapeutics and prophylaxis for prion diseases]. Rinsho Shinkeigaku. 2009;49:946-8 pubmed
    ..Exploitation of these items should be tough but will be deserved for overcoming the fatal diseases. ..
  48. Doh ura K. [Prion diseases: disease diversity and therapeutics]. Rinsho Shinkeigaku. 2004;44:855-6 pubmed
  49. Weberschock T, Meister A, Bohrt K, Schmitt J, Boehncke W, Ludwig R. The risk for cross-reactions after a cutaneous delayed-type hypersensitivity reaction to heparin preparations is independent of their molecular weight: a systematic review. Contact Dermatitis. 2011;65:187-94 pubmed publisher
    ..4%) and fondaparinux (10.4%). In the clinical context, fondaparinux is recommended as the current best alternative when a DTH reaction occurs. ..
  50. Sakurai Yamashita Y, Kinugawa H, Niwa M. Neuroprotective effect of pentosan polysulphate on ischemia-related neuronal death of the hippocampus. Neurosci Lett. 2006;409:30-4 pubmed
    ..These results demonstrated that both PPS and dalteparin could thus protect brain neurons against ischemia/reperfusion-induced damage thus suggesting that they may be potentially useful therapeutic agents for acute ischemic stroke. ..
  51. Baba M, Snoeck R, Pauwels R, De Clercq E. Sulfated polysaccharides are potent and selective inhibitors of various enveloped viruses, including herpes simplex virus, cytomegalovirus, vesicular stomatitis virus, and human immunodeficiency virus. Antimicrob Agents Chemother. 1988;32:1742-5 pubmed
    ..These results indicate that, with the exception of parainfluenza virus, enveloped viruses are specifically susceptible to the inhibitory activity of sulfated polysaccharides. ..
  52. Anderson V, Perry C. Pentosan polysulfate: a review of its use in the relief of bladder pain or discomfort in interstitial cystitis. Drugs. 2006;66:821-35 pubmed
    ..It is the only US FDA-approved oral treatment for the relief of bladder pain or discomfort associated with IC, and data support its role as an important option in the treatment of patients with IC. ..
  53. Dimitrakov J, Kaplan S, Kroenke K, Jackson J, Freeman M. Management of chronic prostatitis/chronic pelvic pain syndrome: an evidence-based approach. Urology. 2006;67:881-8 pubmed