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Description

Pentosan polysulfate sodium (brand name ELMIRON) is a low molecular weight heparin-like compound. It has anticoagulant and fibrinolytic effects and is indicated for the relief of bladder pain or discomfort associated with interstitial cystitis. The mechanism of action of pentosan polysulfate sodium in interstitial cystitis is not known but was discovered, that it t binds Fibroblast growth factors (FGFs) as well as other heparin-binding growth factors.

Approval Year

Targets

Primary TargetPharmacologyConditionPotency

Conditions

ConditionModalityTargetsHighest PhaseProduct
Palliative
ELMIRON

Cmax

ValueDoseCo-administeredAnalytePopulation
68.7 ng/mL
400 mg/m² 3 times / day multiple, oral
PENTOSAN POLYSULFATE plasma
Homo sapiens
462 ng/mL
400 mg/m² 3 times / day multiple, oral
PENTOSAN POLYSULFATE plasma
Homo sapiens
250 ng × eq/mL
300 mg single, oral
PENTOSAN POLYSULFATE plasma
Homo sapiens
358 ng × eq/mL
450 mg single, oral
PENTOSAN POLYSULFATE plasma
Homo sapiens

AUC

ValueDoseCo-administeredAnalytePopulation
987.5 ng × h/mL
400 mg/m² 3 times / day multiple, oral
PENTOSAN POLYSULFATE plasma
Homo sapiens
6660 ng × h/mL
400 mg/m² 3 times / day multiple, oral
PENTOSAN POLYSULFATE plasma
Homo sapiens
21 ng × eq × h/mL
300 mg single, oral
PENTOSAN POLYSULFATE plasma
Homo sapiens
33.8 ng × eq × h/mL
450 mg single, oral
PENTOSAN POLYSULFATE plasma
Homo sapiens

T1/2

ValueDoseCo-administeredAnalytePopulation
26.5 h
300 mg single, oral
PENTOSAN POLYSULFATE plasma
Homo sapiens
19.5 h
450 mg single, oral
PENTOSAN POLYSULFATE plasma
Homo sapiens

Doses

AEs

PubMed

Sample Use Guides

In Vivo Use Guide
The recommended dose of ELMIRON® (pentosan polysulfate sodium, capsules) is 300 mg/day taken as one 100 mg capsule orally three times daily. The capsules should be taken with water at least 1 hour before meals or 2 hours after meals. Patients receiving ELMIRON® should be reassessed after 3 months. If improvement has not occurred and if limiting adverse events are not present, ELMIRON® may be continued for another 3 months.
Route of Administration: Oral
In Vitro Use Guide
Effect of pentosan polysulfate (PPS) on p38, ERK1/2 and JNK MAPK activation was studied. Canine chondrocytes were plated onto 6-well culture plates in serum free DMEM for 24 hr. Cells were pre-treated with 100 µg/ml of PPS for 1 hr and then incubated with 10 ng/ml of recombinant human (rh) IL-1β for 5, 15, 30, 60 or 240 min. It was shown, that phosphorylation of p38 and ERK were inhibited by 100 mg/ml of PPS, while JNK remained constant despite PPS pretreatment prior to rhIL-1β stimulation. Effect of PPS on NF-κB translocation induced by rhIL- 1β: Under control conditions, a diffuse cytoplasmic staining was seen and the average percentage of NF-κB positive nuclei cells was 9.5%. On the other hand, 78.2% of chondrocytes incubated with rhIL- 1β had a nuclear staining pattern, indicating NF-κB nuclear translocation. Preincubation with 10 and 100 µg/ml PPS reduced NF-κB translocation rate.