LX201

Identification

Generic Name
LX201
DrugBank Accession Number
DB04943
Background

LX201 is a silicone matrix ocular implant that provides sustained release of cyclosporine A (CsA) locally to the eye over the course of one year. LX201 is implanted subconjunctivally (beneath the transparent membrane covering the white of the eye) in a minimally invasive procedure. The implant is being developed clinically for the prevention of rejection in corneal transplantation. It is being developed by Lux Biosciences, Inc.

Type
Small Molecule
Groups
Investigational
Synonyms
Not Available

Pharmacology

Indication

Investigated for use/treatment in eye disorders/infections and transplant (rejection).

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Pharmacodynamics

LX201 is a sustained release silicone implant containing 30% cyclosporine A (CsA) by weight. The LX201 implant releases the cyclosporine at steady doses over the course of a year. Local delivery of CsA through LX201 potentially offers significant benefits in the treatment of corneal transplantation due to: (i) increased safety resulting from the absence of systemic toxicity of CsA, in particular of renal toxicity as, based on animal studies, LX201 does not produce measurable systemic levels; (ii) increased efficacy as, based on animal studies, LX201 can establish continuous and relatively high therapeutic levels of CsA – higher than could be established by tolerable oral doses - at or near the transplanted cornea; and (iii) increased patient compliance as the implant is hardly perceptible by the patient and dosing cannot be missed throughout the first year after transplantation.

Mechanism of action

LX201 provides a delivery mechanism for cyclosporine. Cyclosporine binds to cyclophillin. The complex then inhibits calcineurin which is normally responsible for activating transcription of interleukin 2. Cyclosporine also inhibits lymphokine production and interleukin release.

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
  • Humans and other mammals

Chemical Identifiers

UNII
10EHY3D8GY
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
347909854

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
3TerminatedPreventionCornea Transplant / Corneal Diseases1
3TerminatedPreventionCorneal Graft Rejection / Corneal Transplant1

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 October 21, 2007 22:23 / Updated at June 12, 2020 16:52