NAV

ISIS 113715

Identification

Generic Name
ISIS 113715
DrugBank Accession Number
DB05506
Background

ISIS 113715 is our second-generation antisense inhibitor of protein tyrosine phosphatase 1b, or PTP‑1b, for the treatment of type 2 diabetes. In early trials, ISIS 113715 induced statistically significant improvements in multiple measures of glucose control along with statistically significant reductions in LDL-cholesterol.

Type
Small Molecule
Groups
Investigational
Synonyms
Not Available

Pharmacology

Indication

Investigated for use/treatment in diabetes mellitus type 2.

Reduce drug development failure rates
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Contraindications & Blackbox Warnings
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Pharmacodynamics

Because ISIS 113715 is an insulin sensitizer that acts by increasing the activity of the insulin receptor in response to insulin, the most logical place for this drug in the diabetes treatment regimen is as an adjunct to insulin therapy. ISIS 113715 has a novel mechanism of PTP-1b inhibiting action, and acts as an insulin signal enhancer with anti-obesity and lipid lowering potential. PTP‑1b has long been recognized as an attractive target for treatment of diabetes, but due to structural similarities among closely related proteins, it has been difficult to identify small molecule drugs with sufficient specificity to be safe. Antisense technology allowed for the design of very specific drugs that inhibit PTP‑1b and that do not inhibit other family members, making it possible to reduce PTP‑1b activity without having other effects on closely related proteins that would likely lead to unwanted side effects.

Mechanism of action

ISIS 113715 is our second-generation antisense inhibitor of protein tyrosine phosphatase 1b, or PTP‑1b, for the treatment of type 2 diabetes. PTP‑1b is responsible for turning off the activated insulin receptor, so by reducing levels of PTP‑1b, ISIS 113715 enhances the activity of insulin. Antisense technology allows us to design very specific drugs that inhibit PTP‑1b and that do not inhibit other family members, making it possible to reduce PTP‑1b activity without having other effects on closely related proteins that would likely lead to unwanted side effects.

TargetActionsOrganism
UTyrosine-protein phosphatase non-receptor type 1Not AvailableHumans
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
Not Available
Classification
Not classified
Affected organisms
Not Available

Chemical Identifiers

UNII
Not Available
CAS number
Not Available
InChI Key
Not Available
InChI
Not Available
IUPAC Name
Not Available
SMILES
Not Available

References

General References
Not Available
PubChem Substance
347910178

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
2CompletedTreatmentType 2 Diabetes Mellitus2
2TerminatedTreatmentType 2 Diabetes Mellitus1
2WithdrawnTreatmentType 2 Diabetes Mellitus1
1CompletedTreatmentType 2 Diabetes Mellitus1

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

Targets

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Details1. Tyrosine-protein phosphatase non-receptor type 1
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Zinc ion binding
Specific Function
Tyrosine-protein phosphatase which acts as a regulator of endoplasmic reticulum unfolded protein response. Mediates dephosphorylation of EIF2AK3/PERK; inactivating the protein kinase activity of EI...
Gene Name
PTPN1
Uniprot ID
P18031
Uniprot Name
Tyrosine-protein phosphatase non-receptor type 1
Molecular Weight
49966.44 Da

Drug created at November 18, 2007 18:25 / Updated at June 12, 2020 16:52