Details of the Drug-Related molecule(s) Expression Atlas

General Information of Drug (ID: DM4WVC5)

Drug Name
lifitegrast Drug Info
Synonyms
Lifitegrast; Xiidra; 1025967-78-5; SAR-1118; SAR 1118; UNII-038E5L962W; CHEMBL2048028; 038E5L962W; (S)-2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-(methylsulfonyl)phenyl)propanoic acid; (S)-2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-(methylsulfonyl)phenyl)propanoic acid;(S)-2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-(methylsulfonyl)phenyl)propanoic acid; SAR-1118; SAR-1119; SHP606; SPD606
Indication
Disease Entry ICD 11 Status REF
Dry eye disease 9E1Z Approved [1]
Allergic conjunctivitis 9A60.02 Phase 3 [2]
Cross-matching ID
PubChem CID
11965427
ChEBI ID
CHEBI:133023
CAS Number
CAS 1025967-78-5
TTD Drug ID
DM4WVC5
VARIDT Drug ID
DR00072
ACDINA Drug ID
D01208

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Integrin alpha-L (ITGAL) TT48WR6 ITAL_HUMAN Modulator [3]
Intercellular adhesion molecule ICAM-1 (ICAM1) TTCT6F7 ICAM1_HUMAN Inhibitor [4]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID Highest Status REF
Organic anion transporting polypeptide 2B1 (SLCO2B1) DTPFTEQ SO2B1_HUMAN Approved [5]
Organic anion transporting polypeptide 1A2 (SLCO1A2) DTE2B1D SO1A2_HUMAN Approved [5]

The Expression Level of Molecule(s) in Normal Tissue of Major ADME-Related Organs

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
Intercellular adhesion molecule ICAM-1 (ICAM1) DTT ICAM1 7.993 5.81 6.662 5.926
Integrin alpha-L (ITGAL) DTT ITGAL 3.459 4.858 3.406 3.365
Organic anion transporting polypeptide 2B1 (SLCO2B1) DTP OATP2B1 8.165 6.597 6.591 6.397
Organic anion transporting polypeptide 1A2 (SLCO1A2) DTP OATP1A2 4.365 4.466 3.248 2.632
Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

The Expression Level of Molecule(s) between Disease Section and Healthy Individual Tissue

The Studied Disease Dry eye disease
ICD Disease Classification 9E1Z
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Intercellular adhesion molecule ICAM-1 (ICAM1) DTT ICAM1 5.21E-01 0.38 0.32
Organic anion transporting polypeptide 2B1 (SLCO2B1) DTP OATP2B1 2.89E-11 -1.11E+00 -2.81E+00
Organic anion transporting polypeptide 1A2 (SLCO1A2) DTP OATP1A2 5.20E-01 -2.26E-01 -4.65E-01
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1 2016 FDA drug approvals. Nat Rev Drug Discov. 2017 Feb 2;16(2):73-76.
2 URL: 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).
3 Corneal inflammation is inhibited by the LFA-1 antagonist, lifitegrast (SAR 1118). J Ocul Pharmacol Ther. 2013 May;29(4):395-402.
4 Discovery 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.
5 Clinical Pharmacology and Biopharmaceutics review(s)