Details of the Drug

General Information of Drug (ID: DMOL5IU)

Drug Name
Mesalazine
Synonyms
Apriso; Asacol; Asacolitin; Asacolon; Asalit; Ascolitin; Canasa; Claversal; Fisalamine; Fivasa; Iialda; Ipocol; Lialda; Lixacol; Mesacol; Mesalamine; Mesalazina; Mesalazinum; Mesasal; Mesavance; Mesavancol; Mezavant; Pentacol; Pentasa; Rowasa; Salofalk; Salozinal; SfRowasa; Allphar Brand of Mesalamine; Antigen Brand of Mesalamine; Asacol HD; Axcan Brand of Mesalamine; Byk Brand of Mesalamine; Celltech Brand of Mesalamine; Falk Brand of Mesalamine; Farmasa Brand of Mesalamine; Ferring Brand of Mesalamine; GlaxoSmithKline Brand of Mesalamine; Henning Berlin Brand of Mesalamine; M Aminosalicylic Acid; Merckle Brand of Mesalamine; Mesalamine Hydrochloride; Mesalamine Monosodium Salt; Mesalamine [USAN]; Mesalazina[Spanish]; Mesalazine MMX; Mesalazinum [Latin]; Meta Aminosalicylic Acid; Mezavant XL; Minosalicylic acid; Norgine Brand of Mesalamine; Novopharm Brand of Mesalamine; Provalis Brand of Mesalamine; Sanofi Synthelabo Brand of Mesalamine; Schering Plough Brand of Mesalamine; SmithKline Brand of Mesalamine; Solvay Brand of Mesalamine; Yamanouchi Brand of Mesalamine; Novo 5 ASA; Novo5 ASA; AJG-501; Apriso (TN); Asacol (TN); Canasa (TN); Hydrochloride, Mesalamine; Iialda (TN); Ipocal (TN); Lialda (TN); M-A; M-Aminosalicylic acid; MAX-002; MD-0901; Masacol (TN); Mesalamine (USP); Meta-AminosalicylicAcid; Monosodium Salt, Mesalamine; Novo-5 ASA; P-Aminosalicylsaeure; P-Aminosalicylsaeure [German]; Pentasa (TN); Procter & Gamble Brand of Mesalamine; Rowasa (TN); SPD-476; SPD-480; Salofalk (TN); Salofalk Granu-Stix; Schering-Plough Brand of Mesalamine; Z-206; Mesalazine (JAN/INN); Salicylic acid, 5-amino-(8CI); 2-Hydroxy-5-aminobenzoic acid; 3-carboxy-4-hydroxyaniline; 5 Aminosalicylate; 5 Aminosalicylic Acid; 5-AS; 5-ASA; 5-Amino-2-hydroxybenzoic acid; 5-Aminosalicylate; 5-Aminosalicylic acid; 5-amino-2-hydroxy-benzoic acid; 5-aminosalicylic acid, Mesalazine, Asacol, Pentasa, Canasa, Mesalamine
Indication
Disease Entry ICD 11 Status REF
Ulcerative colitis DD71 Approved [1], [2]
Therapeutic Class
Antiinflammatory Agents
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 0 Molecular Weight (mw) 153.14
Topological Polar Surface Area (xlogp) 1.3
Rotatable Bond Count (rotbonds) 1
Hydrogen Bond Donor Count (hbonddonor) 3
Hydrogen Bond Acceptor Count (hbondacc) 4
ADMET Property
BDDCS Class
Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 2: low solubility and high permeability [3]
Clearance
The drug present in the plasma can be removed from the body at the rate of 9.3 mL/min/kg [4]
Elimination
7% of drug is excreted from urine in the unchanged form [3]
Half-life
The concentration or amount of drug in body reduced by one-half in 0.61 hours [4]
MRTD
The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 447.7695 micromolar/kg/day [5]
Unbound Fraction
The unbound fraction of drug in plasma is 0.39% [4]
Vd
Fluid volume that would be required to contain the amount of drug present in the body at the same concentration as in the plasma 0.33 L/kg [4]
Water Solubility
The ability of drug to dissolve in water is measured as 1 mg/mL [3]
Chemical Identifiers
Formula
C7H7NO3
IUPAC Name
5-amino-2-hydroxybenzoic acid
Canonical SMILES
C1=CC(=C(C=C1N)C(=O)O)O
InChI
InChI=1S/C7H7NO3/c8-4-1-2-6(9)5(3-4)7(10)11/h1-3,9H,8H2,(H,10,11)
InChIKey
KBOPZPXVLCULAV-UHFFFAOYSA-N
Cross-matching ID
PubChem CID
4075
ChEBI ID
CHEBI:6775
CAS Number
89-57-6
DrugBank ID
DB00244
TTD ID
D0C4YC
VARIDT ID
DR00856
INTEDE ID
DR1032
ACDINA ID
D00401

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Prostaglandin G/H synthase 1 (COX-1) TT8NGED PGH1_HUMAN Inhibitor [6]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
Multidrug resistance-associated protein 2 (ABCC2) DTFI42L MRP2_HUMAN Substrate [7]
Organic anion transporting polypeptide 2B1 (SLCO2B1) DTPFTEQ SO2B1_HUMAN Substrate [8]
Organic anion transporting polypeptide 1B1 (SLCO1B1) DT3D8F0 SO1B1_HUMAN Substrate [8]
Organic anion transporting polypeptide 1B3 (SLCO1B3) DT9C1TS SO1B3_HUMAN Substrate [8]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
RNA cytidine acetyltransferase (hALP)
Main DME 		DEZV4AP NAT10_HUMAN Substrate [9]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Molecular Expression Atlas of This Drug

The Studied Disease Ulcerative colitis
ICD Disease Classification DD71
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Prostaglandin G/H synthase 1 (COX-1) DTT PTGS1 3.97E-03 0.16 0.43
Organic anion transporting polypeptide 2B1 (SLCO2B1) DTP OATP2B1 6.30E-05 2.52E-01 5.88E-01
Multidrug resistance-associated protein 2 (ABCC2) DTP MRP2 7.16E-01 -1.28E-02 -6.06E-02
Organic anion transporting polypeptide 1B3 (SLCO1B3) DTP OATP1B3 9.69E-01 1.16E-03 3.56E-03
Organic anion transporting polypeptide 1B1 (SLCO1B1) DTP OATP1B1 8.15E-01 6.20E-03 5.61E-02
RNA cytidine acetyltransferase (hALP) DME NAT10 8.46E-03 -4.02E-02 -2.28E-01
Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from Mesalazine (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Remdesivir DMBFZ6L Moderate Decreased renal excretion of Mesalazine caused by Remdesivir mediated nephrotoxicity. 1D6YCoronavirus Disease 2019 [1D6YCoronavirus Disease 2019] [61]
Repaglinide DM5SXUV Moderate Increased risk of hypoglycemia by the combination of Mesalazine and Repaglinide. Acute diabete complication [5A2Y] [62]
Glibenclamide DM8JXPZ Moderate Increased risk of hypoglycemia by the combination of Mesalazine and Glibenclamide. Acute diabete complication [5A2Y] [62]
Nateglinide DMLK2QH Moderate Increased risk of hypoglycemia by the combination of Mesalazine and Nateglinide. Acute diabete complication [5A2Y] [62]
Acetohexamide DMR6N7H Moderate Increased risk of hypoglycemia by the combination of Mesalazine and Acetohexamide. Acute diabete complication [5A2Y] [62]
Glipizide DMZA5PQ Moderate Increased risk of hypoglycemia by the combination of Mesalazine and Glipizide. Acute diabete complication [5A2Y] [62]
Thioguanine DM7NKEV Moderate Decreased metabolism of Mesalazine caused by Thioguanine mediated inhibition of non-CYP450 enzyme. Acute myeloid leukaemia [2A60] [63]
Framycetin DMF8DNE Moderate Increased risk of nephrotoxicity by the combination of Mesalazine and Framycetin. Alcoholic liver disease [DB94] [64]
Inotersen DMJ93CT Major Increased risk of nephrotoxicity by the combination of Mesalazine and Inotersen. Amyloidosis [5D00] [61]
Kanamycin DM2DMPO Moderate Increased risk of nephrotoxicity by the combination of Mesalazine and Kanamycin. Bacterial infection [1A00-1C4Z] [64]
Amikacin DM5PDRB Moderate Increased risk of nephrotoxicity by the combination of Mesalazine and Amikacin. Bacterial infection [1A00-1C4Z] [64]
Streptomycin DME1LQN Moderate Increased risk of nephrotoxicity by the combination of Mesalazine and Streptomycin. Bacterial infection [1A00-1C4Z] [64]
Gentamicin DMKINJO Moderate Increased risk of nephrotoxicity by the combination of Mesalazine and Gentamicin. Bacterial infection [1A00-1C4Z] [64]
Capreomycin DMNZBRY Moderate Increased risk of nephrotoxicity by the combination of Mesalazine and Capreomycin. Bacterial infection [1A00-1C4Z] [64]
Netilmicin DMRD1QK Moderate Increased risk of nephrotoxicity by the combination of Mesalazine and Netilmicin. Bacterial infection [1A00-1C4Z] [64]
Tobramycin DMUI0CH Moderate Increased risk of nephrotoxicity by the combination of Mesalazine and Tobramycin. Bacterial infection [1A00-1C4Z] [64]
Etidronic acid DM1XHYJ Moderate Increased risk of nephrotoxicity by the combination of Mesalazine and Etidronic acid. Bone paget disease [FB85] [65]
Iodipamide DMXIQYS Major Increased risk of nephrotoxicity by the combination of Mesalazine and Iodipamide. Cholelithiasis [DC11] [66]
Phenylbutazone DMAYL0T Moderate Increased risk of nephrotoxicity by the combination of Mesalazine and Phenylbutazone. Chronic pain [MG30] [64]
Ketoprofen DMRKXPT Moderate Increased risk of nephrotoxicity by the combination of Mesalazine and Ketoprofen. Chronic pain [MG30] [64]
Oxaliplatin DMQNWRD Moderate Decreased renal excretion of Mesalazine caused by Oxaliplatin mediated nephrotoxicity. Colorectal cancer [2B91] [67]
Methoxyflurane DML0RAE Moderate Increased risk of nephrotoxicity by the combination of Mesalazine and Methoxyflurane. Corneal disease [9A76-9A78] [64]
Cidofovir DMA13GD Major Increased risk of nephrotoxicity by the combination of Mesalazine and Cidofovir. Cytomegaloviral disease [1D82] [68]
Mefenamic acid DMK7HFI Moderate Increased risk of nephrotoxicity by the combination of Mesalazine and Mefenamic acid. Female pelvic pain [GA34] [64]
Pentamidine DMHZJCG Moderate Increased risk of nephrotoxicity by the combination of Mesalazine and Pentamidine. Fungal infection [1F29-1F2F] [64]
Amphotericin B DMTAJQE Moderate Increased risk of nephrotoxicity by the combination of Mesalazine and Amphotericin B. Fungal infection [1F29-1F2F] [64]
177Lu-DOTATATE DMT8GVU Moderate Increased risk of nephrotoxicity by the combination of Mesalazine and 177Lu-DOTATATE. Hepatitis virus infection [1E50-1E51] [64]
Givosiran DM5PFIJ Moderate Increased risk of nephrotoxicity by the combination of Mesalazine and Givosiran. Inborn porphyrin/heme metabolism error [5C58] [64]
Meclofenamic acid DM05FXR Moderate Increased risk of nephrotoxicity by the combination of Mesalazine and Meclofenamic acid. Inflammatory spondyloarthritis [FA92] [64]
Moxetumomab pasudotox DMN63DZ Moderate Increased risk of nephrotoxicity by the combination of Mesalazine and Moxetumomab pasudotox. Mature B-cell leukaemia [2A82] [64]
Clofarabine DMCVJ86 Moderate Increased risk of nephrotoxicity by the combination of Mesalazine and Clofarabine. Mature B-cell lymphoma [2A85] [69]
Exjade DMHPRWG Major Increased risk of nephrotoxicity by the combination of Mesalazine and Exjade. Mineral absorption/transport disorder [5C64] [70]
Pamidronate DMB4AVP Moderate Increased risk of nephrotoxicity by the combination of Mesalazine and Pamidronate. Mineral excesses [5B91] [65]
Gallium nitrate DMF9O6B Moderate Increased risk of nephrotoxicity by the combination of Mesalazine and Gallium nitrate. Mineral excesses [5B91] [64]
Zoledronate DMIXC7G Moderate Increased risk of nephrotoxicity by the combination of Mesalazine and Zoledronate. Mineral excesses [5B91] [65]
Rofecoxib DM3P5DA Moderate Increased risk of nephrotoxicity by the combination of Mesalazine and Rofecoxib. Osteoarthritis [FA00-FA05] [64]
Valdecoxib DMAY7H4 Moderate Increased risk of nephrotoxicity by the combination of Mesalazine and Valdecoxib. Osteoarthritis [FA00-FA05] [64]
Diclofenac DMPIHLS Moderate Increased risk of nephrotoxicity by the combination of Mesalazine and Diclofenac. Osteoarthritis [FA00-FA05] [64]
Naproxen DMZ5RGV Moderate Increased risk of nephrotoxicity by the combination of Mesalazine and Naproxen. Osteoarthritis [FA00-FA05] [64]
Etodolac DM6WJO9 Moderate Increased risk of nephrotoxicity by the combination of Mesalazine and Etodolac. Pain [MG30-MG3Z] [64]
Diflunisal DM7EN8I Moderate Increased risk of nephrotoxicity by the combination of Mesalazine and Diflunisal. Pain [MG30-MG3Z] [64]
Ibuprofen DM8VCBE Moderate Increased risk of nephrotoxicity by the combination of Mesalazine and Ibuprofen. Pain [MG30-MG3Z] [64]
Nabumetone DMAT2XH Moderate Increased risk of nephrotoxicity by the combination of Mesalazine and Nabumetone. Pain [MG30-MG3Z] [64]
Piroxicam DMTK234 Moderate Increased risk of nephrotoxicity by the combination of Mesalazine and Piroxicam. Pain [MG30-MG3Z] [64]
Pemetrexed DMMX2E6 Moderate Decreased renal excretion of Mesalazine caused by Pemetrexed mediated nephrotoxicity. Pleural mesothelioma [2C26] [71]
Ketorolac DMI4EL5 Moderate Increased risk of nephrotoxicity by the combination of Mesalazine and Ketorolac. Postoperative inflammation [1A00-CA43] [64]
Bromfenac DMKB79O Moderate Increased risk of nephrotoxicity by the combination of Mesalazine and Bromfenac. Postoperative inflammation [1A00-CA43] [64]
Temsirolimus DMS104F Moderate Increased risk of nephrotoxicity by the combination of Mesalazine and Temsirolimus. Renal cell carcinoma [2C90] [64]
Colistimethate DMZ9BMU Moderate Increased risk of nephrotoxicity by the combination of Mesalazine and Colistimethate. Respiratory infection [CA07-CA4Z] [64]
Salsalate DM13P4C Moderate Increased risk of nephrotoxicity by the combination of Mesalazine and Salsalate. Rheumatoid arthritis [FA20] [64]
Meloxicam DM2AR7L Moderate Increased risk of nephrotoxicity by the combination of Mesalazine and Meloxicam. Rheumatoid arthritis [FA20] [64]
Sulindac DM2QHZU Moderate Increased risk of nephrotoxicity by the combination of Mesalazine and Sulindac. Rheumatoid arthritis [FA20] [64]
Celecoxib DM6LOQU Moderate Increased risk of nephrotoxicity by the combination of Mesalazine and Celecoxib. Rheumatoid arthritis [FA20] [64]
Oxaprozin DM9UB0P Moderate Increased risk of nephrotoxicity by the combination of Mesalazine and Oxaprozin. Rheumatoid arthritis [FA20] [64]
Flurbiprofen DMGN4BY Moderate Increased risk of nephrotoxicity by the combination of Mesalazine and Flurbiprofen. Rheumatoid arthritis [FA20] [64]
Fenoprofen DML5VQ0 Moderate Increased risk of nephrotoxicity by the combination of Mesalazine and Fenoprofen. Rheumatoid arthritis [FA20] [64]
Indomethacin DMSC4A7 Moderate Increased risk of nephrotoxicity by the combination of Mesalazine and Indomethacin. Rheumatoid arthritis [FA20] [64]
Tolmetin DMWUIJE Moderate Increased risk of nephrotoxicity by the combination of Mesalazine and Tolmetin. Rheumatoid arthritis [FA20] [64]
Bacitracin DM5OHYE Moderate Increased risk of nephrotoxicity by the combination of Mesalazine and Bacitracin. Skin and skin-structure infection [1F28-1G0Z] [64]
Cisplatin DMRHGI9 Moderate Increased risk of nephrotoxicity by the combination of Mesalazine and Cisplatin. Solid tumour/cancer [2A00-2F9Z] [64]
Telavancin DM58VQX Moderate Increased risk of nephrotoxicity by the combination of Mesalazine and Telavancin. Staphylococcal/streptococcal disease [1B5Y] [64]
Sirolimus DMGW1ID Major Increased risk of nephrotoxicity by the combination of Mesalazine and Sirolimus. Transplant rejection [NE84] [72]
Azathioprine DMMZSXQ Moderate Decreased metabolism of Mesalazine caused by Azathioprine mediated inhibition of non-CYP450 enzyme. Transplant rejection [NE84] [63]
Tacrolimus DMZ7XNQ Major Increased risk of nephrotoxicity by the combination of Mesalazine and Tacrolimus. Transplant rejection [NE84] [72]
Chlorpropamide DMPHZQE Moderate Increased risk of hypoglycemia by the combination of Mesalazine and Chlorpropamide. Type 2 diabetes mellitus [5A11] [62]
Plazomicin DMKMBES Moderate Increased risk of nephrotoxicity by the combination of Mesalazine and Plazomicin. Urinary tract infection [GC08] [64]
Valaciclovir DMHKS94 Moderate Increased risk of nephrotoxicity by the combination of Mesalazine and Valaciclovir. Virus infection [1A24-1D9Z] [64]
Aciclovir DMYLOVR Moderate Increased risk of nephrotoxicity by the combination of Mesalazine and Aciclovir. Virus infection [1A24-1D9Z] [64]
⏷ Show the Full List of 68 DDI Information of This Drug

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG
DIG Name DIG ID PubChem CID Functional Classification
Aspartame E00402 134601 Flavoring agent
Dibutyl phthalate E00064 3026 Plasticizing agent; Solvent
FD&C blue no. 1 E00263 19700 Colorant
Kyselina citronova E00014 311 Acidulant; Antioxidant; Buffering agent; Complexing agent; Flavoring agent
Quinoline yellow WS E00309 24671 Colorant
Stearic acid E00079 5281 Emulsifying agent; Solubilizing agent; Viscosity-controlling agent; lubricant
Carboxymethylcellulose sodium E00621 Not Available Adsorbent; Binding agent; Disintegrant; Emulsifying agent; Suspending agent; Viscosity-controlling agent
Dibutyl sebacate E00160 7986 Plasticizing agent
Eisenoxyd E00585 56841934 Colorant
Ferric hydroxide oxide yellow E00539 23320441 Colorant
Lactose monohydrate E00393 104938 Binding agent; Diluent; Dry powder inhaler carrier; Lyophilization aid
Magnesium stearate E00208 11177 lubricant
Polyethylene glycol 6000 E00655 Not Available Coating agent; Diluent; Ointment base; Plasticizing agent; Solvent; Suppository base; lubricant
Povidone E00667 Not Available Binding agent; Coating agent; Disintegrant; Film/membrane-forming agent; Solubilizing agent; Suspending agent
Silicon dioxide E00670 Not Available Anticaking agent; Opacifying agent; Viscosity-controlling agent
Talc E00520 16211421 Anticaking agent; Diluent; Glidant; lubricant
Titanium dioxide E00322 26042 Coating agent; Colorant; Opacifying agent
Triethyl citrate E00128 6506 Plasticizing agent; Solvent
⏷ Show the Full List of 18 Pharmaceutical Excipients of This Drug
Pharmaceutical Formulation
Formulation Name Drug Dosage Dosage Form Route
Mesalamine 1200 mg tablet 1200 mg Delayed Release Oral Tablet Oral
Mesalamine 375 mg capsule 375 mg 24 HR Extended Release Oral Capsule Oral
Mesalamine 400 mg tablet 400 mg Delayed Release Oral Tablet Oral
Mesalamine 800 mg tablet 800 mg Delayed Release Oral Tablet Oral
Mesalamine 250 mg capsule 250 mg Extended Release Oral Capsule Oral
Mesalamine 500 mg capsule 500 mg Extended Release Oral Capsule Oral
Mesalamine 500 mg capsule 500 mg Extended Release Capsule Oral
Mesalamine 400 mg capsule 400 mg Delayed Release Oral Capsule Oral
Jump to Detail Pharmaceutical Formulation Page of This Drug

References

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