PI-88

Identification

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Name
PI-88
Accession Number
DB05808
Type
Small Molecule
Groups
Investigational
Description

PI-88 is a mixture of highly sulfated, monophosphorylated mannose oligosaccharides, derived from the extracellular phosphomannan of the yeast Pichia (Hansenula) holstii, with potential antiangiogenic activity.

Synonyms
Not Available
Categories
UNII
Not Available
CAS number
Not Available
Weight
Not Available
Chemical Formula
Not Available
InChI Key
Not Available
InChI
Not Available
IUPAC Name
Not Available
SMILES
Not Available

Pharmacology

Indication

Investigated for use/treatment in hepatocellular carcinoma, liver cancer, melanoma, and multiple myeloma.

Pharmacodynamics
Not Available
Mechanism of action

PI-88 retards the growth of primary tumours by inhibiting new blood vessel growth (angiogenesis) in two ways: Heparan sulfate mimicry causes inhibition of heparanase, which prevents the release of angiogenic growth factors from the extracellular matrix (ECM). Interaction with angiogenic growth factors VEGF (Vascular Endothelial Growth Factor), FGF-1 (Fibroblast Growth Factor -1) and FGF-2, reduces their functional activity. PI-88 binds with high (nanomolar) affinity to these growth factors.

Absorption
Not Available
Volume of distribution
Not Available
Protein binding
Not Available
Metabolism
Not Available
Route of elimination
Not Available
Half life
Not Available
Clearance
Not Available
Toxicity
Not Available
Affected organisms
Not Available
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
Not Available
Food Interactions
Not Available

References

General References
  1. Fairweather JK, Hammond E, Johnstone KD, Ferro V: Synthesis and heparanase inhibitory activity of sulfated mannooligosaccharides related to the antiangiogenic agent PI-88. Bioorg Med Chem. 2008 Jan 15;16(2):699-709. Epub 2007 Oct 18. [PubMed:17967543]
  2. Basche M, Gustafson DL, Holden SN, O'Bryant CL, Gore L, Witta S, Schultz MK, Morrow M, Levin A, Creese BR, Kangas M, Roberts K, Nguyen T, Davis K, Addison RS, Moore JC, Eckhardt SG: A phase I biological and pharmacologic study of the heparanase inhibitor PI-88 in patients with advanced solid tumors. Clin Cancer Res. 2006 Sep 15;12(18):5471-80. [PubMed:17000682]
External Links
PubChem Substance
347910242

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1, 2CompletedTreatmentMelanoma1
1, 2CompletedTreatmentMelanoma (Skin) / Unspecified Adult Solid Tumor, Protocol Specific1
2CompletedTreatmentHepatocellular,Carcinoma1
2CompletedTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
2CompletedTreatmentLung Cancers1
2CompletedTreatmentMelanoma1
2CompletedTreatmentProstate Cancer1
3TerminatedTreatmentHepatocellular,Carcinoma / Liver Cancer / Malignancies1
3TerminatedTreatmentHepatocellular,Carcinoma / Liver Cancer / Malignancies / Primary Liver Cancers1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
Not Available
Predicted ADMET features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Taxonomy

Classification
Not classified

Drug created on November 18, 2007 11:27 / Updated on June 04, 2019 06:19