Drug General Information
Drug ID
D04ISS
Former ID
DIB002444
Drug Name
SAR-1118
Synonyms
Dual LFA-1/ICAM-1 inhibitors, Sunesis; Dual LFA-1/ICAM-1 inhibitors (inflammatory diseases), SARcode; Dual leukocytefunction-associated antigen-1/intracellular adhesion molecule-1 inhibitors (inflammatory diseases), SARcode
Drug Type
Small molecular drug
Indication Allergic conjunctivitis [ICD9: 204.0, 372.0, 372.14, 995.3; ICD10:C91.0, H10, H10.45, T78.4] Phase 3 [523596], [542538]
Company
Sunesis Pharmaceuticals Inc
Formula
C29H24Cl2N2O7S
InChI
InChI=1S/C29H24Cl2N2O7S/c1-41(38,39)20-4-2-3-16(11-20)12-23(29(36)37)32-27(34)25-22(30)13-19-15-33(9-7-21(19)26(25)31)28(35)18-6-5-17-8-10-40-24(17)14-18/h2-6,8,10-11,13-14,23H,7,9,12,15H2,1H3,(H,32,34)(H,36,37)/t23-/m0/s1
InChIKey
JFOZKMSJYSPYLN-QHCPKHFHSA-N
PubChem Compound ID
PubChem Substance ID
Target and Pathway
Target(s) Lymphocyte function-associated antigen 1 Target Info Inhibitor [532142]
ICAM-1 Target Info Inhibitor [532815]
KEGG Pathway Rap1 signaling pathway
Cell adhesion molecules (CAMs)
Natural killer cell mediated cytotoxicity
Leukocyte transendothelial migration
Regulation of actin cytoskeleton
Malaria
Staphylococcus aureus infection
HTLV-I infection
Epstein-Barr virus infection
Rheumatoid arthritis
Viral myocarditishsa04064:NF-kappa B signaling pathway
TNF signaling pathway
African trypanosomiasis
Influenza A
Viral myocarditis
NetPath Pathway TCR Signaling Pathway
RANKL Signaling PathwayNetPath_17:IL5 Signaling Pathway
IL1 Signaling Pathway
TSH Signaling Pathway
IL6 Signaling Pathway
IL2 Signaling Pathway
ID Signaling Pathway
TWEAK Signaling Pathway
RANKL Signaling Pathway
TNFalpha Signaling Pathway
PANTHER Pathway Inflammation mediated by chemokine and cytokine signaling pathway
Integrin signalling pathway
Pathway Interaction Database Integrin family cell surface interactions
Beta2 integrin cell surface interactions
CXCR3-mediated signaling eventstxa2pathway:Thromboxane A2 receptor signaling
Glucocorticoid receptor regulatory network
amb2 Integrin signaling
Reactome Immunoregulatory interactions between a Lymphoid and a non-Lymphoid cell
Cell surface interactions at the vascular wall
Integrin cell surface interactionsR-HSA-198933:Immunoregulatory interactions between a Lymphoid and a non-Lymphoid cell
Integrin cell surface interactions
Interferon gamma signaling
WikiPathways Focal Adhesion
Integrin-mediated Cell Adhesion
Integrin cell surface interactions
Immunoregulatory interactions between a Lymphoid and a non-Lymphoid cell
Cell surface interactions at the vascular wallWP619:Type II interferon signaling (IFNG)
IL1 and megakaryotyces in obesity
Human Complement System
Spinal Cord Injury
Interleukin-11 Signaling Pathway
RANKL/RANK Signaling Pathway
Folate Metabolism
Vitamin B12 Metabolism
Selenium Micronutrient Network
References
Ref 523596ClinicalTrials.gov (NCT01421498) Safety and Efficacy Study of SAR 1118 to Treat Dry Eye. U.S. National Institutes of Health.
Ref 542538(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7533).
Ref 532142Corneal inflammation is inhibited by the LFA-1 antagonist, lifitegrast (SAR 1118). J Ocul Pharmacol Ther. 2013 May;29(4):395-402.
Ref 532815Discovery and Development of Potent LFA-1/ICAM-1 Antagonist SAR 1118 as an Ophthalmic Solution for Treating Dry Eye. ACS Med Chem Lett. 2012 Jan 31;3(3):203-6.

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