ISIS 113715

Identification

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Name
ISIS 113715
Accession Number
DB05506
Type
Small Molecule
Groups
Investigational
Description

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.

Synonyms
Not Available
Categories
Not Available
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 diabetes mellitus type 2.

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
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
Not Available
External Links
PubChem Substance
347910178

Clinical Trials

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

Taxonomy

Classification
Not classified

Targets

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 on November 18, 2007 11:25 / Updated on June 04, 2019 06:17