Identification

Generic Name
PI-88
DrugBank Accession Number
DB05808
Background

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.

Type
Small Molecule
Groups
Investigational
Synonyms
Not Available

Pharmacology

Indication

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

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Contraindications & Blackbox Warnings
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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

Adverse Effects
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Toxicity

Not Available

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Not Available
Food Interactions
Not Available

Categories

Drug Categories
Classification
Not classified
Affected organisms
Not Available

Chemical Identifiers

UNII
4ROB1M2DHD
CAS number
Not Available
InChI Key
Not Available
InChI
Not Available
IUPAC Name
Not Available
SMILES
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. [Article]
  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. [Article]
PubChem Substance
347910242

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
3TerminatedTreatmentCancer / Hepatocellular Carcinoma / Liver Cancer1
3TerminatedTreatmentCancer / Hepatocellular Carcinoma / Liver Cancer / Primary Liver Cancers1
2CompletedTreatmentHepatocellular Carcinoma1
2CompletedTreatmentLung Cancers1
2CompletedTreatmentMelanoma1
2CompletedTreatmentNon-Small Cell Lung Carcinoma (NSCLC)1
2CompletedTreatmentProstate Cancer1
1, 2CompletedTreatmentMelanoma1
1, 2CompletedTreatmentMelanoma / Unspecified Adult Solid Tumor, Protocol Specific1

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

Drug created at November 18, 2007 18:27 / Updated at June 12, 2020 16:52