General Information of Drug (ID: DMICA9H)

Drug Name
Sulfasalazine Drug Info
Synonyms
sulfasalazine; 599-79-1; Salicylazosulfapyridine; Salazosulfapyridine; Azulfidine; Asulfidine; Salazopyridin; Sulcolon; Azopyrin; Accucol; Colo-Pleon; Salazopiridazin; Salisulf; Reupirin; Benzosulfa; Azopyrine; Salazosulfapyridin; Sulfasalazina; w-t Sasp oral; Sulfasalazinum; Sulfasalazin; Azulfidine EN; Sulfazalazine; Azulfidine EN-tabs; Salazosulfapiridina; Sas-500; Salazosulfapyridinum; Azosulfidin; SASP; Salazo-sulfapyridinum; 5-(p-(2-Pyridylsulfamyl)phenylazo)salicylic acid; SAS-500; Sulfasalizine
Indication
Disease Entry ICD 11 Status REF
Irritable bowel syndrome DD91.0 Approved [1]
Rheumatoid arthritis FA20 Approved [2]
Ulcerative colitis DD71 Approved [3]
Therapeutic Class
Antiinflammatory Agents
Cross-matching ID
PubChem CID
5339
ChEBI ID
CHEBI:9334
CAS Number
CAS 599-79-1
TTD Drug ID
DMICA9H
VARIDT Drug ID
DR00201
INTEDE Drug ID
DR1513
ACDINA Drug ID
D00643

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
ATP-binding cassette transporter G2 (ABCG2) TTIMJ02 ABCG2_HUMAN Inhibitor [4]
Nuclear factor NF-kappa-B (NFKB) TTSXVID NFKB1_HUMAN; NFKB2_HUMAN; TF65_HUMAN; RELB_HUMAN; REL_HUMAN Activator [5]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID Highest Status REF
Peptide transporter 1 (SLC15A1) DT9G7XN S15A1_HUMAN Approved [6]
Multidrug resistance-associated protein 2 (ABCC2) DTFI42L MRP2_HUMAN Approved [7]
Organic anion transporting polypeptide 2B1 (SLCO2B1) DTPFTEQ SO2B1_HUMAN Approved [8]
Breast cancer resistance protein (ABCG2) DTI7UX6 ABCG2_HUMAN Approved [9]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID Highest Status REF
Cytochrome P450 3A5 (CYP3A5) DEIBDNY CP3A5_HUMAN Approved [10]
Azoreductase (azoR) DEEISQ2 AZOR_ENTFA Approved [11] , [12]
Azoreductase (azoR) DEM1BHT A0A132Z973_ENTFC Approved [11] , [12]
Azoreductase (azoR) DE5CAX1 A0A074IU04_STRSL Approved [11]
Azoreductase (azoR) DEGTKHL T0VG26_9ENTE Approved [13]
Azoreductase (azoR) DEI2PC5 AZOR_CLOP1 Approved [11] , [12]
Azoreductase (azoR) DEIHK8V A0A349MYB4_9LACO Approved [11] , [12]
Azoreductase (azoR) DE3UF6Z A0A0P0ETC6_BACT4 Approved [13]
Azoreductase (azoR) DE6GHJ5 A0A0P0ETC6_BACT4 Approved [13]
Azoreductase (azoR) DETEMAH A0A349MYB4_9LACO Approved [13]
Azoreductase (azoR) DEIKZOU A0A0P0ETC6_BACT4 Approved [14]
Azoreductase (azoR) DENLBG3 A0A0P0ETC6_BACT4 Approved [11] , [12]

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

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
Nuclear factor NF-kappa-B (NFKB) DTT NFKB1 5.38 4.436 4.89 5.698
ATP-binding cassette transporter G2 (ABCG2) DTT ABCG2 7.802 7.781 7.934 7.821
Organic anion transporting polypeptide 2B1 (SLCO2B1) DTP OATP2B1 8.165 6.597 6.591 6.397
Breast cancer resistance protein (ABCG2) DTP BCRP 6.732 7.513 6.326 9.277
Multidrug resistance-associated protein 2 (ABCC2) DTP MRP2 7.751 4.17 6.425 6.282
Peptide transporter 1 (SLC15A1) DTP PEPT1 3.807 4.52 5.285 7.133
Cytochrome P450 3A5 (CYP3A5) DME CYP3A5 10.08 7.207 5.403 9.211
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 Irritable bowel syndrome
ICD Disease Classification DD91.0
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Nuclear factor NF-kappa-B (NFKB) DTT NFKB1; NFKB2; RELA; RELB; REL 5.39E-01 0.16 0.27
Organic anion transporting polypeptide 2B1 (SLCO2B1) DTP OATP2B1 1.87E-02 -1.32E-01 -2.75E-01
Breast cancer resistance protein (ABCG2) DTP BCRP 1.20E-13 -1.20E+00 -1.06E+00
Multidrug resistance-associated protein 2 (ABCC2) DTP MRP2 1.29E-14 -3.25E-01 -7.49E-01
Peptide transporter 1 (SLC15A1) DTP PEPT1 7.54E-01 -1.25E-02 -8.78E-02
Cytochrome P450 3A5 (CYP3A5) DME CYP3A5 1.69E-01 2.37E-02 2.14E-01
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
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: 4840).
3 Sulfasalazine FDA Label
4 The anti-inflammatory mechanism of sulfasalazine is related to adenosine release at inflamed sites. J Immunol. 1996 Mar 1;156(5):1937-41.
5 Emerging drugs for rheumatoid arthritis. Expert Opin Emerg Drugs. 2008 Mar;13(1):175-96.
6 Peptide transporter substrate identification during permeability screening in drug discovery: comparison of transfected MDCK-hPepT1 cells to Caco-2 cells. Arch Pharm Res. 2007 Apr;30(4):507-18.
7 Small intestinal efflux mediated by MRP2 and BCRP shifts sulfasalazine intestinal permeability from high to low, enabling its colonic targeting. Am J Physiol Gastrointest Liver Physiol. 2009 Aug;297(2):G371-7.
8 Small-Dosing Clinical Study: Pharmacokinetic, Pharmacogenomic (SLCO2B1 and ABCG2), and Interaction (Atorvastatin and Grapefruit Juice) Profiles of 5 Probes for OATP2B1 and BCRP. J Pharm Sci. 2017 Sep;106(9):2688-2694.
9 Curcumin inhibits the activity of ABCG2/BCRP1, a multidrug resistance-linked ABC drug transporter in mice. Pharm Res. 2009 Feb;26(2):480-7.
10 Urinary 6 beta-hydroxycortisol excretion in rheumatoid arthritis. Br J Rheumatol. 1997 Jan;36(1):54-8.
11 The influence of probiotic treatment on sulfasalazine metabolism in rat. Xenobiotica. 2012 Aug;42(8):791-7.
12 Developing a metagenomic view of xenobiotic metabolism. Pharmacol Res. 2013 Mar;69(1):21-31.
13 The role of intestinal bacteria in the metabolism of salicylazosulfapyridine. J Pharmacol Exp Ther. 1972 Jun;181(3):555-62.
14 Mapping human microbiome drug metabolism by gut bacteria and their genes. Nature. 2019 Jun;570(7762):462-467.