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
- External Links
- PubChem Substance
- 347909854
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 3 Terminated Prevention Cornea Transplant / Corneal Diseases 1 3 Terminated Prevention Corneal Graft Rejection / Corneal Transplant 1
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
- Chromatographic Properties
Collision Cross Sections (CCS)
Not Available
Drug created at October 21, 2007 22:23 / Updated at June 12, 2020 16:52