Synopsis
Synopsis
0
CEP/COS
0
JDMF
0
VMF
0
Europe
0
Australia
0
South Africa
DRUG PRODUCT COMPOSITIONS
0
EDQM
0
USP
0
JP
0
Others
0
Stock Recap #PipelineProspector
0
Weekly News Recap #Phispers
1. (2s)-2-(((2-(benzofuran-6-ylcarbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinolin-6- Yl)carbonyl)amino)-3-(3-(methylsulfonyl)phenyl)propanoic Acid
2. L-phenylalanine, N-((2-(6-benzofuranylcarbonyl)-5,7-dichloro-1,2,3,4-tetrahydro-6-isoquinolinyl)carbonyl)-3-(methylsulfonyl)-
3. Lifitegrast Ophthalmic Solution
4. Sar 1118
5. Sar-1118
6. Shp-606
7. Shp606
8. Xiidra
1. 1025967-78-5
2. Xiidra
3. Sar 1118
4. Sar-1118
5. Shp606
6. Shp-606
7. (s)-2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-(methylsulfonyl)phenyl)propanoic Acid
8. Chembl2048028
9. 038e5l962w
10. (2s)-2-(((2-(benzofuran-6-ylcarbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinolin-6- Yl)carbonyl)amino)-3-(3-(methylsulfonyl)phenyl)propanoic Acid
11. L-phenylalanine, N-((2-(6-benzofuranylcarbonyl)-5,7-dichloro-1,2,3,4-tetrahydro-6-isoquinolinyl)carbonyl)-3-(methylsulfonyl)-
12. L-phenylalanine, N-[[2-(6-benzofuranylcarbonyl)-5,7-dichloro-1,2,3,4-tetrahydro-6-isoquinolinyl]carbonyl]-3-(methylsulfonyl)-
13. Lifitegrast [usan:inn]
14. Unii-038e5l962w
15. Sar1118
16. Xiidra (tn)
17. Lifitegrast [mi]
18. Lifitegrast [inn]
19. Lifitegrast (usan/inn)
20. Lifitegrast [usan]
21. Lifitegrast; Sar 1118
22. Lifitegrast [who-dd]
23. Lifitegrast Ophthalmic Solution
24. Gtpl7533
25. Schembl2632068
26. Amy4450
27. Dtxsid60145345
28. Lifitegrast [orange Book]
29. Chebi:133023
30. Ex-a2582
31. Bdbm50386331
32. Mfcd28502439
33. S3714
34. Zinc84668739
35. Ccg-270245
36. Cs-6264
37. Db11611
38. Compound 1g [pmid: 24900456]
39. Ac-32534
40. Ds-20052
41. Hy-19344
42. D10374
43. A900838
44. Q23044263
45. (2s)-2-[[2-(1-benzofuran-6-carbonyl)-5,7-dichloro3,4-dihydro-1h-isoquinoline-6-carbonyl]amino]-3-(3-methylsulfonylphenyl)propanoic Acid
46. N-[[2-(6-benzofuranylcarbonyl)-5,7-dichloro-1,2,3,4-tetrahydro-6-isoquinolinyl]carbonyl]-3-(methylsulfonyl)-l-phenylalanine
47. N-[2-(1-benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carbonyl]-3-(methanesulfonyl)-l-phenylalanine
| Molecular Weight | 615.5 g/mol |
|---|---|
| Molecular Formula | C29H24Cl2N2O7S |
| XLogP3 | 4.7 |
| Hydrogen Bond Donor Count | 2 |
| Hydrogen Bond Acceptor Count | 7 |
| Rotatable Bond Count | 7 |
| Exact Mass | 614.0681277 g/mol |
| Monoisotopic Mass | 614.0681277 g/mol |
| Topological Polar Surface Area | 142 Ų |
| Heavy Atom Count | 41 |
| Formal Charge | 0 |
| Complexity | 1100 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 1 |
| Undefined Atom Stereocenter Count | 0 |
| Defined Bond Stereocenter Count | 0 |
| Undefined Bond Stereocenter Count | 0 |
| Covalently Bonded Unit Count | 1 |
For the treatment of signs and symptoms of keratoconjunctivitis sicca (dry eye syndrome).
FDA Label
Treatment of dry eye disease
Lifitegrast addresses both the symptoms and the resulting ocular surface damage by interfering with ocular inflammatory cycle. Lifitegrast is a lymphocyte functionassociated antigen-1 antagonist through direct competitive antagonism and sequentially inhibits the T-cell recruitment, activation, and proinflammatory cytokine release associated with dry eye syndrome.
Ophthalmic Solutions
Sterile solutions that are intended for instillation into the eye. It does not include solutions for cleaning eyeglasses or CONTACT LENS SOLUTIONS. (See all compounds classified as Ophthalmic Solutions.)
S - Sensory organs
S01 - Ophthalmologicals
S01X - Other ophthalmologicals
S01XA - Other ophthalmologicals
S01XA25 - Lifitegrast
Absorption
The mean peak plasma concentration (Cmax) of 1.70ng/mL was reached within 15 minutes of application. Quantifiable trough plasma concentrations ranged from 0.55 ng/mL to 3.74 ng/mL. Observations show limited systemic exposure that produces significant clinical outcomes.
Route of Elimination
Not possible to perform mass balance study to determine the main route of elimination.
Clearance
Not possible to calculate clearance rate based on plasma concentrations of lifitegrast, but reported to be relatively fast in rat I.V. pharmacokinetics study. It is predicted that lifitegrast is cleared via nasal and subsequently gastrointestinal tract.
Based on the findings of an in vitro metabolism study using fresh human hepatocytes, lifitegrast does not appear to undergo significant metabolism.
Not possible to calculate plasma elimination half-life based on plasma concentrations of lifitegrast, but reported to be relatively short in rat I.V. pharmacokinetics study.
Lifitegrast binds to the integrin lymphocyte function-associated antigen-1 (LFA-1), a cell surface protein found on leukocytes and blocks the interaction of LFA-1 with its cognate ligand intercellular adhesion molecule-1 (ICAM-1). ICAM-1 may be overexpressed in corneal and conjunctival tissues in dry eye disease. LFA-1/ICAM-1 interaction can contribute to the formation of an immunological synapse resulting in T-cell proliferation/activation and migration to target tissues. In vitro studies demonstrated that lifitegrast may inhibit T-cell adhesion to ICAM-1 in a human T-cell line and may inhibit secretion of inflammatory cytokines, inflammatory mediators, chemokines, TNF-, and IL-1 in human peripheral blood mononuclear cells.
API SUPPLIERS
FULL SCREEN VIEW Click here to open all results in a new tab [this preview display 10 results]
USDMF
FULL SCREEN VIEW Click here to open all results in a new tab [this preview display 10 results]EU WC
FULL SCREEN VIEW Click here to open all results in a new tab [this preview display 10 results]Drugs in Development
Details:
Novartis will focus on other therapeutic areas, like retinal diseases via platforms including gene therapy and optogenetics through divestment of Xiidra (lifitegrast), the first approved treatment for dry eye disease, and SAF312 (libvatrep), for chronic ocular surface pain.
Lead Product(s): Lifitegrast
Therapeutic Area: Ophthalmology Brand Name: Xiidra
Study Phase: ApprovedProduct Type: Small molecule
Sponsor: Bausch & Lomb Incorporated
Deal Size: $2,500.0 million Upfront Cash: $1,750.0 million
Deal Type: Divestment September 29, 2023
Lead Product(s) : Lifitegrast
Therapeutic Area : Ophthalmology
Highest Development Status : Approved
Partner/Sponsor/Collaborator : Bausch & Lomb Incorporated
Deal Size : $2,500.0 million
Deal Type : Divestment
Novartis Completes Divestment of ‘Front of Eye’ Ophthalmology Assets
Details : Novartis will focus on other therapeutic areas, like retinal diseases via platforms including gene therapy and optogenetics through divestment of Xiidra (lifitegrast), the first approved treatment for dry eye disease, and SAF312 (libvatrep), for chronic ...
Brand Name : Xiidra
Molecule Type : Small molecule
Upfront Cash : $1,750.0 million
September 29, 2023
Details:
The financing will fund the acquisition Xiidra (lifitegrast ophthalmic solution), a non-steroid eye drop specifically approved to treat the signs and symptoms of dry eye disease focusing on inflammation associated with dry eye, and certain other ophthalmology assets.
Lead Product(s): Lifitegrast
Therapeutic Area: Ophthalmology Brand Name: Xiidra
Study Phase: ApprovedProduct Type: Small molecule
Sponsor: Undisclosed
Deal Size: Undisclosed Upfront Cash: Undisclosed
Deal Type: Financing September 11, 2023
Lead Product(s) : Lifitegrast
Therapeutic Area : Ophthalmology
Highest Development Status : Approved
Partner/Sponsor/Collaborator : Undisclosed
Deal Size : Undisclosed
Deal Type : Financing
Bausch + Lomb Announces Launch of Proposed Financing for Acquisition of XIIDRA®
Details : The financing will fund the acquisition Xiidra (lifitegrast ophthalmic solution), a non-steroid eye drop specifically approved to treat the signs and symptoms of dry eye disease focusing on inflammation associated with dry eye, and certain other ophthalm...
Brand Name : Xiidra
Molecule Type : Small molecule
Upfront Cash : Undisclosed
September 11, 2023
Details:
Novartis will focus on other therapeutic areas, like retinal diseases via platforms including gene therapy and optogenetics through divestment of Xiidra (lifitegrast), the first approved treatment for dry eye disease, and SAF312 (libvatrep), for chronic ocular surface pain.
Lead Product(s): Lifitegrast
Therapeutic Area: Ophthalmology Brand Name: Xiidra
Study Phase: ApprovedProduct Type: Small molecule
Sponsor: Bausch & Lomb Incorporated
Deal Size: $2,500.0 million Upfront Cash: $1,750.0 million
Deal Type: Divestment June 30, 2023
Lead Product(s) : Lifitegrast
Therapeutic Area : Ophthalmology
Highest Development Status : Approved
Partner/Sponsor/Collaborator : Bausch & Lomb Incorporated
Deal Size : $2,500.0 million
Deal Type : Divestment
Novartis Signs Agreement to Divest Front of Eye Ophthalmology Assets in Line with Focused Strategy
Details : Novartis will focus on other therapeutic areas, like retinal diseases via platforms including gene therapy and optogenetics through divestment of Xiidra (lifitegrast), the first approved treatment for dry eye disease, and SAF312 (libvatrep), for chronic ...
Brand Name : Xiidra
Molecule Type : Small molecule
Upfront Cash : $1,750.0 million
June 30, 2023
Details:
Novartis intends to develop the AcuStream technology for potential use with its existing and future front-of-eye therapies, which could include Xiidra® (lifitegrast ophthalmic solution) 5%, a first-in-class prescription LFA 1 antagonist for the treatment of dry eye disease.
Lead Product(s): Lifitegrast
Therapeutic Area: Ophthalmology Brand Name: Xiidra
Study Phase: ApprovedProduct Type: Small molecule
Sponsor: Novartis Pharmaceuticals Corporation
Deal Size: Undisclosed Upfront Cash: Undisclosed
Deal Type: Acquisition June 30, 2022
Lead Product(s) : Lifitegrast
Therapeutic Area : Ophthalmology
Highest Development Status : Approved
Partner/Sponsor/Collaborator : Novartis Pharmaceuticals Corporation
Deal Size : Undisclosed
Deal Type : Acquisition
Details : Novartis intends to develop the AcuStream technology for potential use with its existing and future front-of-eye therapies, which could include Xiidra® (lifitegrast ophthalmic solution) 5%, a first-in-class prescription LFA 1 antagonist for the treatmen...
Brand Name : Xiidra
Molecule Type : Small molecule
Upfront Cash : Undisclosed
June 30, 2022
FULL SCREEN VIEW Click here to open all results in a new tab [this preview display 10 results]INTERMEDIATES SUPPLIERS
FULL SCREEN VIEW Click here to open all results in a new tab [this preview display 10 results]FDF Dossiers
FULL SCREEN VIEW Click here to open all results in a new tab [this preview display 10 results]FDA Orange Book
FULL SCREEN VIEW Click here to open all results in a new tab [this preview display 10 results]Related Excipient Companies
Digital Content
DATA COMPILATION #PharmaFlow
NEWS #PharmaBuzz
Global Sales Information
US Medicaid Prescriptions
FULL SCREEN VIEW Click here to open all results in a new tab [this preview display 10 results]Market Place
Patents & EXCLUSIVITIES
ABOUT THIS PAGE
LOOKING FOR A SUPPLIER?
