Identification

Name
Aminosalicylic Acid
Accession Number
DB00233  (APRD00749, EXPT00693, DB09367)
Type
Small Molecule
Groups
Approved
Description

An antitubercular agent often administered in association with isoniazid. The sodium salt of the drug is better tolerated than the free acid.

Structure
Thumb
Synonyms
  • 4-amino-2-hydroxybenzoic acid
  • 4-aminosalicylate
  • 4-aminosalicylic acid
  • p-aminosalicylic acid
  • para-amino salicylic acid
  • para-aminosalicylic acid
  • PAS
Product Ingredients
IngredientUNIICASInChI Key
Aminosalicylate calcium73I4QDW01W133-15-3XDWVNCOPMIEDJK-UHFFFAOYSA-L
Aminosalicylate sodiumT9ZKL3TNQF133-10-8FVVDKUPCWXUVNP-UHFFFAOYSA-M
Calcium aminosalicylate trihydrate9VF16M7FWU6059-16-1IPLQYSPEGHNJCQ-UHFFFAOYSA-L
Potassium aminosalicylate7N21461LKD133-09-5PRZJIMSXCLZGLT-UHFFFAOYSA-M
Sodium aminosalicylate dihydrateS38B9W6AXW6018-19-5GMUQJDAYXZXBOT-UHFFFAOYSA-M
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
GranupasGranule, delayed release4 gOralLucane Pharma2014-04-07Not applicableEu
Nemasol Sodium Tab 500mgTablet500 mgOralIcn Pharmaceuticals1966-12-312005-04-26Canada
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
PaserGranule, delayed release4 g/1OralJacobus Pharmaceutical1995-02-15Not applicableUs
International/Other Brands
Pamisyl (Parke-Davis) / Rexipas (Bristol-Myers Squibb) / Rezipas (Bristol-Myers Squibb)
Categories
UNII
5B2658E0N2
CAS number
65-49-6
Weight
Average: 153.1354
Monoisotopic: 153.042593095
Chemical Formula
C7H7NO3
InChI Key
WUBBRNOQWQTFEX-UHFFFAOYSA-N
InChI
InChI=1S/C7H7NO3/c8-4-1-2-5(7(10)11)6(9)3-4/h1-3,9H,8H2,(H,10,11)
IUPAC Name
4-amino-2-hydroxybenzoic acid
SMILES
NC1=CC(O)=C(C=C1)C(O)=O

Pharmacology

Indication

For the treatment of tuberculosis

Structured Indications
Pharmacodynamics

Aminosalicylic acid is an anti-mycobacterial agent used with other anti-tuberculosis drugs (most often isoniazid) for the treatment of all forms of active tuberculosis due to susceptible strains of tubercle bacilli. The two major considerations in the clinical pharmacology of aminosalicylic acid are the prompt production of a toxic inactive metabolite under acid conditions and the short serum half life of one hour for the free drug. Aminosalicylic acid is bacteriostatic against Mycobacterium tuberculosis (prevents the multiplying of bacteria without destroying them). It also inhibits the onset of bacterial resistance to streptomycin and isoniazid.

Mechanism of action

There are two mechanisms responsible for aminosalicylic acid's bacteriostatic action against Mycobacterium tuberculosis. Firstly, aminosalicylic acid inhibits folic acid synthesis (without potentiation with antifolic compounds). The binding of para-aminobenzoic acid to pteridine synthetase acts as the first step in folic acid synthesis. Aminosalicylic acid binds pteridine synthetase with greater affinity than para-aminobenzoic acid, effectively inhibiting the synthesis of folic acid. As bacteria are unable to use external sources of folic acid, cell growth and multiplication slows. Secondly, aminosalicylic acid may inhibit the synthesis of the cell wall component, mycobactin, thus reducing iron uptake by M. tuberculosis.

TargetActionsOrganism
UProstaglandin G/H synthase 2
inhibitor
Human
UInhibitor of nuclear factor kappa-B kinase subunit alpha
inhibitor
Human
UArachidonate 5-lipoxygenase
inhibitor
Human
UGroup IIE secretory phospholipase A2
unknown
Human
U2-amino-4-hydroxy-6-hydroxymethyldihydropteridine pyrophosphokinase
unknown
Mycobacterium tuberculosis
Absorption
Not Available
Volume of distribution
Not Available
Protein binding

50-60%

Metabolism

Hepatic.

Route of elimination
Not Available
Half life
Not Available
Clearance
Not Available
Toxicity

LD50=4 gm/kg (orally in mice); LD50=3650 mg/kg (orally in rabbits)

Affected organisms
  • Mycobacteria
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
16-BromoepiandrosteroneThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with 16-Bromoepiandrosterone.Investigational
19-norandrostenedioneThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with 19-norandrostenedione.Experimental, Illicit
5-androstenedioneThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with 5-androstenedione.Experimental, Illicit
AbciximabThe risk or severity of adverse effects can be increased when Abciximab is combined with Aminosalicylic Acid.Approved
AcarboseAminosalicylic Acid may increase the hypoglycemic activities of Acarbose.Approved, Investigational
AcenocoumarolAminosalicylic Acid may increase the anticoagulant activities of Acenocoumarol.Approved
AcetazolamideThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Acetazolamide.Approved, Vet Approved
Acetylsalicylic acidThe risk or severity of adverse effects can be increased when Acetylsalicylic acid is combined with Aminosalicylic Acid.Approved, Vet Approved
AlbiglutideAminosalicylic Acid may increase the hypoglycemic activities of Albiglutide.Approved
AlclometasoneThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Alclometasone.Approved
AldosteroneThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Aldosterone.Experimental, Investigational
AlogliptinAminosalicylic Acid may increase the hypoglycemic activities of Alogliptin.Approved
AloxiprinThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Aloxiprin.Experimental
AlprostadilThe risk or severity of adverse effects can be increased when Alprostadil is combined with Aminosalicylic Acid.Approved, Investigational
AlteplaseThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Alteplase.Approved
ALX-0081The risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with ALX-0081.Investigational
AmcinonideThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Amcinonide.Approved
Ammonium chlorideThe serum concentration of Aminosalicylic Acid can be increased when it is combined with Ammonium chloride.Approved, Vet Approved
AnagrelideThe risk or severity of adverse effects can be increased when Anagrelide is combined with Aminosalicylic Acid.Approved
AncrodAminosalicylic Acid may increase the anticoagulant activities of Ancrod.Investigational
AndrographolideThe risk or severity of adverse effects can be increased when Andrographolide is combined with Aminosalicylic Acid.Investigational
AndrostenedioneThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Androstenedione.Experimental, Illicit
AnecortaveThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Anecortave.Investigational
anecortave acetateThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with anecortave acetate.Investigational
AnistreplaseThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Anistreplase.Approved
Antithrombin III humanAminosalicylic Acid may increase the anticoagulant activities of Antithrombin III human.Approved
ApixabanAminosalicylic Acid may increase the anticoagulant activities of Apixaban.Approved
ArdeparinAminosalicylic Acid may increase the anticoagulant activities of Ardeparin.Approved, Investigational, Withdrawn
ArgatrobanThe risk or severity of adverse effects can be increased when Argatroban is combined with Aminosalicylic Acid.Approved, Investigational
AstaxanthinThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Astaxanthin.Investigational
AtamestaneThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Atamestane.Investigational
AzelastineThe risk or severity of adverse effects can be increased when Azelastine is combined with Aminosalicylic Acid.Approved
BalsalazideAminosalicylic Acid may increase the anticoagulant activities of Balsalazide.Approved, Investigational
BatroxobinThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Batroxobin.Experimental
BCG vaccineThe therapeutic efficacy of BCG vaccine can be decreased when used in combination with Aminosalicylic Acid.Investigational
BecaplerminAminosalicylic Acid may increase the anticoagulant activities of Becaplermin.Approved, Investigational
Beclomethasone dipropionateThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Beclomethasone dipropionate.Approved, Investigational
BemiparinThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Bemiparin.Approved, Investigational
BenazeprilAminosalicylic Acid may decrease the antihypertensive activities of Benazepril.Approved, Investigational
BeraprostThe risk or severity of adverse effects can be increased when Beraprost is combined with Aminosalicylic Acid.Investigational
BetamethasoneThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Betamethasone.Approved, Vet Approved
BivalirudinAminosalicylic Acid may increase the anticoagulant activities of Bivalirudin.Approved, Investigational
BrinaseThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Brinase.Experimental
BrinzolamideThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Brinzolamide.Approved
BromocriptineAminosalicylic Acid may increase the hypoglycemic activities of Bromocriptine.Approved, Investigational
BudesonideThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Budesonide.Approved
BuflomedilThe risk or severity of adverse effects can be increased when Buflomedil is combined with Aminosalicylic Acid.Experimental
BumetanideAminosalicylic Acid may decrease the diuretic activities of Bumetanide.Approved
ButylphthalideThe risk or severity of adverse effects can be increased when Butylphthalide is combined with Aminosalicylic Acid.Investigational
CanagliflozinAminosalicylic Acid may increase the hypoglycemic activities of Canagliflozin.Approved
CandoxatrilAminosalicylic Acid may decrease the antihypertensive activities of Candoxatril.Experimental
CangrelorThe risk or severity of adverse effects can be increased when Cangrelor is combined with Aminosalicylic Acid.Approved
CaptoprilAminosalicylic Acid may decrease the antihypertensive activities of Captopril.Approved
CertoparinAminosalicylic Acid may increase the anticoagulant activities of Certoparin.Approved, Investigational
ChlorpropamideAminosalicylic Acid may increase the hypoglycemic activities of Chlorpropamide.Approved
CiclesonideThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Ciclesonide.Approved, Investigational
CilazaprilAminosalicylic Acid may decrease the antihypertensive activities of Cilazapril.Approved
CilostazolThe risk or severity of adverse effects can be increased when Cilostazol is combined with Aminosalicylic Acid.Approved
Citric AcidAminosalicylic Acid may increase the anticoagulant activities of Citric Acid.Approved, Nutraceutical, Vet Approved
ClobetasolThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Clobetasol.Investigational
Clobetasol propionateThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Clobetasol propionate.Approved
ClobetasoneThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Clobetasone.Approved
ClocortoloneThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Clocortolone.Approved
ClopidogrelThe risk or severity of adverse effects can be increased when Clopidogrel is combined with Aminosalicylic Acid.Approved, Nutraceutical
CloricromenThe risk or severity of adverse effects can be increased when Cloricromen is combined with Aminosalicylic Acid.Experimental
ClorindioneAminosalicylic Acid may increase the anticoagulant activities of Clorindione.Experimental
Cortexolone 17α-propionateThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Cortexolone 17α-propionate.Investigational
CorticosteroneThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Corticosterone.Experimental
Cortisone acetateThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Cortisone acetate.Approved
Dabigatran etexilateAminosalicylic Acid may increase the anticoagulant activities of Dabigatran etexilate.Approved
DalteparinAminosalicylic Acid may increase the anticoagulant activities of Dalteparin.Approved
DanaparoidAminosalicylic Acid may increase the anticoagulant activities of Danaparoid.Approved, Withdrawn
DapagliflozinAminosalicylic Acid may increase the hypoglycemic activities of Dapagliflozin.Approved
DarexabanAminosalicylic Acid may increase the anticoagulant activities of Darexaban.Investigational
DefibrotideThe risk or severity of adverse effects can be increased when Defibrotide is combined with Aminosalicylic Acid.Approved, Investigational
DeflazacortThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Deflazacort.Approved
DelaprilAminosalicylic Acid may decrease the antihypertensive activities of Delapril.Experimental
dersalazineAminosalicylic Acid may increase the anticoagulant activities of dersalazine.Investigational
DesirudinAminosalicylic Acid may increase the anticoagulant activities of Desirudin.Approved
DesmoteplaseThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Desmoteplase.Investigational
DesonideThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Desonide.Approved, Investigational
DesoximetasoneThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Desoximetasone.Approved
Desoxycorticosterone acetateThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Desoxycorticosterone acetate.Approved
Desoxycorticosterone PivalateThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Desoxycorticosterone Pivalate.Experimental, Vet Approved
DexamethasoneThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Dexamethasone.Approved, Investigational, Vet Approved
Dexamethasone isonicotinateThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Dexamethasone isonicotinate.Vet Approved
DexketoprofenThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Dexketoprofen.Approved, Investigational
DextranAminosalicylic Acid may increase the anticoagulant activities of Dextran.Approved, Vet Approved
Dextran 40Aminosalicylic Acid may increase the anticoagulant activities of Dextran 40.Approved
Dextran 70Aminosalicylic Acid may increase the anticoagulant activities of Dextran 70.Approved
Dextran 75Aminosalicylic Acid may increase the anticoagulant activities of Dextran 75.Approved
DiclofenamideThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Diclofenamide.Approved
DicoumarolAminosalicylic Acid may increase the anticoagulant activities of Dicoumarol.Approved
DiflorasoneThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Diflorasone.Approved
DiflunisalAminosalicylic Acid may increase the anticoagulant activities of Diflunisal.Approved
DifluocortoloneThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Difluocortolone.Approved, Investigational
DifluprednateThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Difluprednate.Approved
DiltiazemDiltiazem may increase the anticoagulant activities of Aminosalicylic Acid.Approved
DiphenadioneAminosalicylic Acid may increase the anticoagulant activities of Diphenadione.Experimental
DipyridamoleThe risk or severity of adverse effects can be increased when Dipyridamole is combined with Aminosalicylic Acid.Approved
DisopyramideAminosalicylic Acid may increase the hypoglycemic activities of Disopyramide.Approved
DitazoleThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Ditazole.Approved, Withdrawn
DorzolamideThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Dorzolamide.Approved
Drotrecogin alfaThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Drotrecogin alfa.Approved, Investigational, Withdrawn
DulaglutideAminosalicylic Acid may increase the hypoglycemic activities of Dulaglutide.Approved
Edetic AcidAminosalicylic Acid may increase the anticoagulant activities of Edetic Acid.Approved, Vet Approved
EdoxabanAminosalicylic Acid may increase the anticoagulant activities of Edoxaban.Approved
EmpagliflozinAminosalicylic Acid may increase the hypoglycemic activities of Empagliflozin.Approved
EnalaprilAminosalicylic Acid may decrease the antihypertensive activities of Enalapril.Approved, Vet Approved
EnalaprilatAminosalicylic Acid may decrease the antihypertensive activities of Enalaprilat.Approved
EnoxaparinAminosalicylic Acid may increase the anticoagulant activities of Enoxaparin.Approved
EpinastineThe risk or severity of adverse effects can be increased when Epinastine is combined with Aminosalicylic Acid.Approved, Investigational
EplivanserinThe risk or severity of adverse effects can be increased when Eplivanserin is combined with Aminosalicylic Acid.Investigational
eplivanserineThe risk or severity of adverse effects can be increased when eplivanserine is combined with Aminosalicylic Acid.Investigational
EpoprostenolThe risk or severity of adverse effects can be increased when Epoprostenol is combined with Aminosalicylic Acid.Approved
EptifibatideThe risk or severity of adverse effects can be increased when Eptifibatide is combined with Aminosalicylic Acid.Approved, Investigational
EquileninThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Equilenin.Experimental
EquilinThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Equilin.Approved
EstroneThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Estrone.Approved
Estrone sulfateThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Estrone sulfate.Approved
Etacrynic acidAminosalicylic Acid may decrease the diuretic activities of Etacrynic acid.Approved
EthoxzolamideThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Ethoxzolamide.Withdrawn
Ethyl biscoumacetateAminosalicylic Acid may increase the anticoagulant activities of Ethyl biscoumacetate.Withdrawn
ExenatideAminosalicylic Acid may increase the hypoglycemic activities of Exenatide.Approved, Investigational
Ferulic acidAminosalicylic Acid may increase the anticoagulant activities of Ferulic acid.Experimental
FibrinolysinThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Fibrinolysin.Investigational
fluasteroneThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with fluasterone.Investigational
FludrocortisoneThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Fludrocortisone.Approved
FluindioneAminosalicylic Acid may increase the anticoagulant activities of Fluindione.Investigational
FlumethasoneThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Flumethasone.Approved, Vet Approved
FlunisolideThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Flunisolide.Approved, Investigational
Fluocinolone AcetonideThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Fluocinolone Acetonide.Approved, Investigational, Vet Approved
FluocinonideThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Fluocinonide.Approved, Investigational
FluocortoloneThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Fluocortolone.Approved, Withdrawn
FluorometholoneThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Fluorometholone.Approved
FluprednideneThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Fluprednidene.Approved, Withdrawn
FluprednisoloneThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Fluprednisolone.Approved
FlurandrenolideThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Flurandrenolide.Approved
Fluticasone furoateThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Fluticasone furoate.Approved
Fluticasone propionateThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Fluticasone propionate.Approved
FondaparinuxAminosalicylic Acid may increase the anticoagulant activities of Fondaparinux.Investigational
Fondaparinux sodiumAminosalicylic Acid may increase the anticoagulant activities of Fondaparinux sodium.Approved, Investigational
FormestaneThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Formestane.Approved, Investigational, Withdrawn
FosinoprilAminosalicylic Acid may decrease the antihypertensive activities of Fosinopril.Approved
FurosemideAminosalicylic Acid may decrease the diuretic activities of Furosemide.Approved, Vet Approved
GabexateAminosalicylic Acid may increase the anticoagulant activities of Gabexate.Investigational
Ginkgo bilobaGinkgo biloba may increase the anticoagulant activities of Aminosalicylic Acid.Approved, Investigational, Nutraceutical
GliclazideAminosalicylic Acid may increase the hypoglycemic activities of Gliclazide.Approved
GlimepirideAminosalicylic Acid may increase the hypoglycemic activities of Glimepiride.Approved
GlipizideAminosalicylic Acid may increase the hypoglycemic activities of Glipizide.Approved
GlyburideAminosalicylic Acid may increase the hypoglycemic activities of Glyburide.Approved
GuacetisalAminosalicylic Acid may increase the anticoagulant activities of Guacetisal.Experimental
HalcinonideThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Halcinonide.Approved, Investigational, Withdrawn
HE3286The risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with HE3286.Investigational
Hemoglobin crosfumarilAminosalicylic Acid may increase the anticoagulant activities of Hemoglobin crosfumaril.Experimental
HeparinAminosalicylic Acid may increase the anticoagulant activities of Heparin.Approved, Investigational
HigenamineThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Higenamine.Investigational
HyaluronidaseThe therapeutic efficacy of Hyaluronidase can be decreased when used in combination with Aminosalicylic Acid.Approved, Investigational
HydrocortisoneThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Hydrocortisone.Approved, Vet Approved
HydroxytyrosolThe risk or severity of adverse effects can be increased when Hydroxytyrosol is combined with Aminosalicylic Acid.Investigational
IbudilastThe risk or severity of adverse effects can be increased when Ibudilast is combined with Aminosalicylic Acid.Approved, Investigational
Icosapent ethylThe risk or severity of adverse effects can be increased when Icosapent ethyl is combined with Aminosalicylic Acid.Approved, Nutraceutical
IdraparinuxAminosalicylic Acid may increase the anticoagulant activities of Idraparinux.Investigational
IfenprodilThe risk or severity of adverse effects can be increased when Ifenprodil is combined with Aminosalicylic Acid.Approved, Investigational, Withdrawn
IfetrobanThe risk or severity of adverse effects can be increased when Ifetroban is combined with Aminosalicylic Acid.Investigational
IloprostThe risk or severity of adverse effects can be increased when Iloprost is combined with Aminosalicylic Acid.Approved, Investigational
ImidaprilAminosalicylic Acid may decrease the antihypertensive activities of Imidapril.Investigational
IndobufenThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Indobufen.Investigational
Insulin AspartAminosalicylic Acid may increase the hypoglycemic activities of Insulin Aspart.Approved
Insulin DetemirAminosalicylic Acid may increase the hypoglycemic activities of Insulin Detemir.Approved
Insulin GlargineAminosalicylic Acid may increase the hypoglycemic activities of Insulin Glargine.Approved
Insulin GlulisineAminosalicylic Acid may increase the hypoglycemic activities of Insulin Glulisine.Approved
Insulin HumanAminosalicylic Acid may increase the hypoglycemic activities of Insulin Human.Approved, Investigational
Insulin LisproAminosalicylic Acid may increase the hypoglycemic activities of Insulin Lispro.Approved
IstaroximeThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Istaroxime.Investigational
KetanserinThe risk or severity of adverse effects can be increased when Ketanserin is combined with Aminosalicylic Acid.Investigational
LepirudinAminosalicylic Acid may increase the anticoagulant activities of Lepirudin.Approved
LetaxabanAminosalicylic Acid may increase the anticoagulant activities of Letaxaban.Investigational
LinsidomineThe risk or severity of adverse effects can be increased when Linsidomine is combined with Aminosalicylic Acid.Experimental
LiraglutideAminosalicylic Acid may increase the hypoglycemic activities of Liraglutide.Approved
LisinoprilAminosalicylic Acid may decrease the antihypertensive activities of Lisinopril.Approved, Investigational
LoteprednolThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Loteprednol.Approved
ME-609The risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with ME-609.Investigational
MecaserminAminosalicylic Acid may increase the hypoglycemic activities of Mecasermin.Approved, Investigational
MedrysoneThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Medrysone.Approved
MelagatranAminosalicylic Acid may increase the anticoagulant activities of Melagatran.Experimental
MelengestrolThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Melengestrol.Vet Approved
MesalazineAminosalicylic Acid may increase the anticoagulant activities of Mesalazine.Approved
MetforminAminosalicylic Acid may increase the hypoglycemic activities of Metformin.Approved
MethazolamideThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Methazolamide.Approved
MethotrexateThe serum concentration of Methotrexate can be increased when it is combined with Aminosalicylic Acid.Approved
Methyl salicylateAminosalicylic Acid may increase the anticoagulant activities of Methyl salicylate.Approved, Vet Approved
MethylprednisoloneThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Methylprednisolone.Approved, Vet Approved
MifepristoneAminosalicylic Acid may increase the hypoglycemic activities of Mifepristone.Approved, Investigational
MiglitolAminosalicylic Acid may increase the hypoglycemic activities of Miglitol.Approved
MilrinoneThe risk or severity of adverse effects can be increased when Milrinone is combined with Aminosalicylic Acid.Approved
MoexiprilAminosalicylic Acid may decrease the antihypertensive activities of Moexipril.Approved
MometasoneThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Mometasone.Approved, Vet Approved
NadroparinAminosalicylic Acid may increase the anticoagulant activities of Nadroparin.Approved
NafamostatAminosalicylic Acid may increase the anticoagulant activities of Nafamostat.Approved, Investigational
NaftopidilThe risk or severity of adverse effects can be increased when Naftopidil is combined with Aminosalicylic Acid.Investigational
NateglinideAminosalicylic Acid may increase the hypoglycemic activities of Nateglinide.Approved, Investigational
NCX 1022The risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with NCX 1022.Investigational
NimesulideThe risk or severity of adverse effects can be increased when Nimesulide is combined with Aminosalicylic Acid.Approved, Investigational, Withdrawn
NitroaspirinThe risk or severity of adverse effects can be increased when Nitroaspirin is combined with Aminosalicylic Acid.Investigational
Oleoyl-estroneThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Oleoyl-estrone.Investigational
OlsalazineAminosalicylic Acid may increase the anticoagulant activities of Olsalazine.Approved
OmapatrilatAminosalicylic Acid may decrease the antihypertensive activities of Omapatrilat.Investigational
OtamixabanAminosalicylic Acid may increase the anticoagulant activities of Otamixaban.Investigational
OzagrelThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Ozagrel.Investigational
ParamethasoneThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Paramethasone.Approved
ParnaparinThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Parnaparin.Approved, Investigational
Pentaerythritol TetranitrateAminosalicylic Acid may increase the anticoagulant activities of Pentaerythritol Tetranitrate.Approved
PentamidineAminosalicylic Acid may increase the hypoglycemic activities of Pentamidine.Approved
Pentosan PolysulfateAminosalicylic Acid may increase the anticoagulant activities of Pentosan Polysulfate.Approved
PentoxifyllineThe risk or severity of adverse effects can be increased when Pentoxifylline is combined with Aminosalicylic Acid.Approved, Investigational
PerindoprilAminosalicylic Acid may decrease the antihypertensive activities of Perindopril.Approved
PhenindioneAminosalicylic Acid may increase the anticoagulant activities of Phenindione.Approved, Investigational
PhenprocoumonAminosalicylic Acid may increase the anticoagulant activities of Phenprocoumon.Approved, Investigational
Picosulfuric acidThe therapeutic efficacy of Picosulfuric acid can be decreased when used in combination with Aminosalicylic Acid.Approved
PicotamideThe risk or severity of adverse effects can be increased when Picotamide is combined with Aminosalicylic Acid.Experimental
PioglitazoneAminosalicylic Acid may increase the hypoglycemic activities of Pioglitazone.Approved, Investigational
PiretanideAminosalicylic Acid may decrease the diuretic activities of Piretanide.Experimental
PralatrexateThe serum concentration of Pralatrexate can be increased when it is combined with Aminosalicylic Acid.Approved
PramlintideAminosalicylic Acid may increase the hypoglycemic activities of Pramlintide.Approved, Investigational
PrasteroneThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Prasterone.Approved, Nutraceutical
Prasterone sulfateThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Prasterone sulfate.Investigational
PrasugrelThe risk or severity of adverse effects can be increased when Prasugrel is combined with Aminosalicylic Acid.Approved
PrednicarbateThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Prednicarbate.Approved
PrednisoloneThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Prednisolone.Approved, Vet Approved
PrednisoneThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Prednisone.Approved, Vet Approved
PregnenoloneThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Pregnenolone.Experimental, Investigational
ProbenecidThe therapeutic efficacy of Probenecid can be decreased when used in combination with Aminosalicylic Acid.Approved
Protein CAminosalicylic Acid may increase the anticoagulant activities of Protein C.Approved
Protein S humanAminosalicylic Acid may increase the anticoagulant activities of Protein S human.Approved
ProtocatechualdehydeAminosalicylic Acid may increase the anticoagulant activities of Protocatechualdehyde.Approved
QuinaprilAminosalicylic Acid may decrease the antihypertensive activities of Quinapril.Approved, Investigational
QuinineAminosalicylic Acid may increase the hypoglycemic activities of Quinine.Approved
RamatrobanThe risk or severity of adverse effects can be increased when Ramatroban is combined with Aminosalicylic Acid.Investigational
RamiprilAminosalicylic Acid may decrease the antihypertensive activities of Ramipril.Approved
RepaglinideAminosalicylic Acid may increase the hypoglycemic activities of Repaglinide.Approved, Investigational
RescinnamineAminosalicylic Acid may decrease the antihypertensive activities of Rescinnamine.Approved
ResveratrolThe risk or severity of adverse effects can be increased when Resveratrol is combined with Aminosalicylic Acid.Approved, Experimental, Investigational
ReteplaseThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Reteplase.Approved
ReviparinAminosalicylic Acid may increase the anticoagulant activities of Reviparin.Approved, Investigational
RidogrelThe risk or severity of adverse effects can be increased when Ridogrel is combined with Aminosalicylic Acid.Approved
RimexoloneThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Rimexolone.Approved
RivaroxabanAminosalicylic Acid may increase the anticoagulant activities of Rivaroxaban.Approved
RosiglitazoneThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Rosiglitazone.Approved, Investigational
Salicylic acidSalicylic acid may increase the anticoagulant activities of Aminosalicylic Acid.Approved, Vet Approved
SarpogrelateThe risk or severity of adverse effects can be increased when Sarpogrelate is combined with Aminosalicylic Acid.Investigational
SaruplaseThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Saruplase.Experimental
SaxagliptinAminosalicylic Acid may increase the hypoglycemic activities of Saxagliptin.Approved
SelexipagThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Selexipag.Approved
SevofluraneThe risk or severity of adverse effects can be increased when Sevoflurane is combined with Aminosalicylic Acid.Approved, Vet Approved
SitagliptinAminosalicylic Acid may increase the hypoglycemic activities of Sitagliptin.Approved, Investigational
SpiraprilAminosalicylic Acid may decrease the antihypertensive activities of Spirapril.Approved
SRT501The risk or severity of adverse effects can be increased when SRT501 is combined with Aminosalicylic Acid.Investigational
StreptokinaseThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Streptokinase.Approved, Investigational
SulfadiazineAminosalicylic Acid may increase the hypoglycemic activities of Sulfadiazine.Approved, Vet Approved
SulfamethoxazoleAminosalicylic Acid may increase the hypoglycemic activities of Sulfamethoxazole.Approved
SulfisoxazoleAminosalicylic Acid may increase the hypoglycemic activities of Sulfisoxazole.Approved, Vet Approved
SulodexideAminosalicylic Acid may increase the anticoagulant activities of Sulodexide.Approved, Investigational
SunitinibAminosalicylic Acid may increase the hypoglycemic activities of Sunitinib.Approved, Investigational
TemocaprilAminosalicylic Acid may decrease the antihypertensive activities of Temocapril.Experimental, Investigational
TenecteplaseThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Tenecteplase.Approved
TesmilifeneThe risk or severity of adverse effects can be increased when Tesmilifene is combined with Aminosalicylic Acid.Investigational
TicagrelorThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Ticagrelor.Approved
TiclopidineThe risk or severity of adverse effects can be increased when Ticlopidine is combined with Aminosalicylic Acid.Approved
TinzaparinThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Tinzaparin.Approved
TioclomarolAminosalicylic Acid may increase the anticoagulant activities of Tioclomarol.Experimental
TirofibanThe risk or severity of adverse effects can be increased when Tirofiban is combined with Aminosalicylic Acid.Approved
TixocortolThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Tixocortol.Approved
TolazamideAminosalicylic Acid may increase the hypoglycemic activities of Tolazamide.Approved
TolbutamideAminosalicylic Acid may increase the hypoglycemic activities of Tolbutamide.Approved
TorasemideAminosalicylic Acid may decrease the diuretic activities of Torasemide.Approved
TrandolaprilAminosalicylic Acid may decrease the antihypertensive activities of Trandolapril.Approved
TranilastThe risk or severity of adverse effects can be increased when Tranilast is combined with Aminosalicylic Acid.Approved, Investigational
TrapidilThe risk or severity of adverse effects can be increased when Trapidil is combined with Aminosalicylic Acid.Approved
TreprostinilThe risk or severity of adverse effects can be increased when Treprostinil is combined with Aminosalicylic Acid.Approved, Investigational
TriamcinoloneThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Triamcinolone.Approved, Vet Approved
TriflusalThe risk or severity of adverse effects can be increased when Triflusal is combined with Aminosalicylic Acid.Approved, Investigational
Trolamine salicylateAminosalicylic Acid may increase the anticoagulant activities of Trolamine salicylate.Approved
TroxerutinAminosalicylic Acid may increase the anticoagulant activities of Troxerutin.Investigational
UlobetasolThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Ulobetasol.Approved
UrokinaseThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Urokinase.Approved, Investigational, Withdrawn
Valproic AcidThe serum concentration of Valproic Acid can be increased when it is combined with Aminosalicylic Acid.Approved, Investigational
VerapamilVerapamil may increase the anticoagulant activities of Aminosalicylic Acid.Approved
VorapaxarThe risk or severity of adverse effects can be increased when Vorapaxar is combined with Aminosalicylic Acid.Approved
WarfarinAminosalicylic Acid may increase the anticoagulant activities of Warfarin.Approved
XimelagatranAminosalicylic Acid may increase the anticoagulant activities of Ximelagatran.Approved, Investigational, Withdrawn
ZofenoprilAminosalicylic Acid may decrease the antihypertensive activities of Zofenopril.Experimental
Food Interactions
  • Take without regard to meals.

References

Synthesis Reference

Thomas M. Parkinson, Joseph P. Brown, Robert E. Wingard, Jr., "Pharmaceutical preparations containing a polymeric agent for releasing 5-aminosalicylic acid or its salts into the gastrointestinal tract." U.S. Patent US4298595, issued January, 1975.

US4298595
General References
Not Available
External Links
Human Metabolome Database
HMDB14378
KEGG Drug
D00162
KEGG Compound
C02518
PubChem Compound
4649
PubChem Substance
46505572
ChemSpider
4488
BindingDB
48319
ChEBI
27565
ChEMBL
CHEMBL1169
PharmGKB
PA448382
HET
BHA
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
4-Aminosalicylic_acid
ATC Codes
J04AA01 — 4-aminosalicylic acidJ04AA02 — Sodium aminosalicylateJ04AA03 — Calcium aminosalicylate
PDB Entries
1pbc / 1pbf / 1sxk / 5x7z
MSDS
Download (73.6 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedTreatmentHealthy Volunteers1
2CompletedTreatmentColorectal Cancers1
2CompletedTreatmentJaundice / Malignant Neoplasm of Pancreas1
2CompletedTreatmentMalignant Neoplasm of Stomach3
2TerminatedTreatmentCrohn's Disease (CD)2
4RecruitingTreatmentHuman Immunodeficiency Virus (HIV) Infections1
Not AvailableCompletedTreatmentHuman Immunodeficiency Virus (HIV) Infections / Tuberculosis1

Pharmacoeconomics

Manufacturers
  • Century pharmaceuticals inc
  • Hexcel chemical products
  • Panray corp sub ormont drug and chemical co inc
  • Lannett co inc
  • Consolidated midland corp
  • Jacobus pharmaceutical co
  • Bristol myers squibb co
Packagers
Dosage forms
FormRouteStrength
Granule, delayed releaseOral4 g
TabletOral500 mg
Granule, delayed releaseOral4 g/1
Prices
Unit descriptionCostUnit
Paser granules 4 gm packet3.59USD packet
Aminosalicylic acid powder2.4USD g
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)150.5 dec °CPhysProp
water solubility1690 mg/L (at 23 °C)YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP0.89SANGSTER (1994)
pKa2.05 (at 25 °C)KORTUM,G ET AL (1961)
Predicted Properties
PropertyValueSource
Water Solubility11.8 mg/mLALOGPS
logP0.62ALOGPS
logP0.83ChemAxon
logS-1.1ALOGPS
pKa (Strongest Acidic)3.68ChemAxon
pKa (Strongest Basic)2.19ChemAxon
Physiological Charge-1ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count3ChemAxon
Polar Surface Area83.55 Å2ChemAxon
Rotatable Bond Count1ChemAxon
Refractivity40 m3·mol-1ChemAxon
Polarizability14.29 Å3ChemAxon
Number of Rings1ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9356
Blood Brain Barrier-0.7101
Caco-2 permeable-0.852
P-glycoprotein substrateNon-substrate0.8405
P-glycoprotein inhibitor INon-inhibitor0.9777
P-glycoprotein inhibitor IINon-inhibitor0.9905
Renal organic cation transporterNon-inhibitor0.9337
CYP450 2C9 substrateNon-substrate0.8174
CYP450 2D6 substrateNon-substrate0.8358
CYP450 3A4 substrateNon-substrate0.7782
CYP450 1A2 substrateNon-inhibitor0.8645
CYP450 2C9 inhibitorNon-inhibitor0.8281
CYP450 2D6 inhibitorNon-inhibitor0.9627
CYP450 2C19 inhibitorInhibitor0.5778
CYP450 3A4 inhibitorNon-inhibitor0.7324
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9157
Ames testNon AMES toxic0.9388
CarcinogenicityNon-carcinogens0.8045
BiodegradationReady biodegradable0.6246
Rat acute toxicity1.5761 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9689
hERG inhibition (predictor II)Non-inhibitor0.9676
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Download (9.18 KB)
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-QQ , negativeLC-MS/MSsplash10-0udi-0900000000-9edb9b6028f854f76708
LC-MS/MS Spectrum - LC-ESI-QQ , negativeLC-MS/MSsplash10-0a4i-1900000000-e893f1439cefbeef271a
LC-MS/MS Spectrum - LC-ESI-QQ , negativeLC-MS/MSsplash10-0a4i-5900000000-09273d1390d26a8def2d
LC-MS/MS Spectrum - LC-ESI-QQ , negativeLC-MS/MSsplash10-066r-9200000000-e029b385a8c32e95b6b7
LC-MS/MS Spectrum - LC-ESI-QQ , negativeLC-MS/MSsplash10-00ku-9000000000-58cccd83d40f8fade4dc
MS/MS Spectrum - , positiveLC-MS/MSsplash10-06dr-2900200000-832b5b02326d8b11bac4

Taxonomy

Description
This compound belongs to the class of organic compounds known as aminosalicylic acids. These are salicylic acids carrying an amino group on the benzene ring.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Benzene and substituted derivatives
Sub Class
Benzoic acids and derivatives
Direct Parent
Aminosalicylic acids
Alternative Parents
4-aminosalicylic acids / Salicylic acids / Aminobenzoic acids / Benzoic acids / m-Aminophenols / Benzoyl derivatives / Aniline and substituted anilines / 1-hydroxy-2-unsubstituted benzenoids / 1-hydroxy-4-unsubstituted benzenoids / Vinylogous acids
show 8 more
Substituents
4-aminosalicylic acid / Aminosalicylic acid / Salicylic acid / Aminobenzoic acid or derivatives / Aminobenzoic acid / Benzoic acid / Aniline or substituted anilines / M-aminophenol / Aminophenol / Benzoyl
show 19 more
Molecular Framework
Aromatic homomonocyclic compounds
External Descriptors
phenols, aminobenzoic acid (CHEBI:27565)

Targets

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Prostaglandin-endoperoxide synthase activity
Specific Function
Converts arachidonate to prostaglandin H2 (PGH2), a committed step in prostanoid synthesis. Constitutively expressed in some tissues in physiological conditions, such as the endothelium, kidney and...
Gene Name
PTGS2
Uniprot ID
P35354
Uniprot Name
Prostaglandin G/H synthase 2
Molecular Weight
68995.625 Da
References
  1. Mifflin RC, Saada JI, Di Mari JF, Valentich JD, Adegboyega PA, Powell DW: Aspirin-mediated COX-2 transcript stabilization via sustained p38 activation in human intestinal myofibroblasts. Mol Pharmacol. 2004 Feb;65(2):470-8. [PubMed:14742690]
  2. Generini S, Fiori G, Matucci Cerinic M: Therapy of spondylarthropathy in inflammatory bowel disease. Clin Exp Rheumatol. 2002 Nov-Dec;20(6 Suppl 28):S88-94. [PubMed:12463455]
  3. Distrutti E, Sediari L, Mencarelli A, Renga B, Orlandi S, Russo G, Caliendo G, Santagada V, Cirino G, Wallace JL, Fiorucci S: 5-Amino-2-hydroxybenzoic acid 4-(5-thioxo-5H-[1,2]dithiol-3yl)-phenyl ester (ATB-429), a hydrogen sulfide-releasing derivative of mesalamine, exerts antinociceptive effects in a model of postinflammatory hypersensitivity. J Pharmacol Exp Ther. 2006 Oct;319(1):447-58. Epub 2006 Jul 19. [PubMed:16855178]
  4. Cipolla G, Crema F, Sacco S, Moro E, de Ponti F, Frigo G: Nonsteroidal anti-inflammatory drugs and inflammatory bowel disease: current perspectives. Pharmacol Res. 2002 Jul;46(1):1-6. [PubMed:12208114]
  5. Pruzanski W, Stefanski E, Vadas P, Ramamurthy NS: Inhibition of extracellular release of proinflammatory secretory phospholipase A2 (sPLA2) by sulfasalazine: a novel mechanism of anti-inflammatory activity. Biochem Pharmacol. 1997 Jun 15;53(12):1901-7. [PubMed:9256165]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Scaffold protein binding
Specific Function
Serine kinase that plays an essential role in the NF-kappa-B signaling pathway which is activated by multiple stimuli such as inflammatory cytokines, bacterial or viral products, DNA damages or oth...
Gene Name
CHUK
Uniprot ID
O15111
Uniprot Name
Inhibitor of nuclear factor kappa-B kinase subunit alpha
Molecular Weight
84638.88 Da
References
  1. Bantel H, Berg C, Vieth M, Stolte M, Kruis W, Schulze-Osthoff K: Mesalazine inhibits activation of transcription factor NF-kappaB in inflamed mucosa of patients with ulcerative colitis. Am J Gastroenterol. 2000 Dec;95(12):3452-7. [PubMed:11151876]
  2. Allgayer H: Review article: mechanisms of action of mesalazine in preventing colorectal carcinoma in inflammatory bowel disease. Aliment Pharmacol Ther. 2003 Sep;18 Suppl 2:10-4. [PubMed:12950415]
  3. Weber CK, Liptay S, Wirth T, Adler G, Schmid RM: Suppression of NF-kappaB activity by sulfasalazine is mediated by direct inhibition of IkappaB kinases alpha and beta. Gastroenterology. 2000 Nov;119(5):1209-18. [PubMed:11054378]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Iron ion binding
Specific Function
Catalyzes the first step in leukotriene biosynthesis, and thereby plays a role in inflammatory processes.
Gene Name
ALOX5
Uniprot ID
P09917
Uniprot Name
Arachidonate 5-lipoxygenase
Molecular Weight
77982.595 Da
References
  1. Nielsen OH, Bukhave K, Elmgreen J, Ahnfelt-Ronne I: Inhibition of 5-lipoxygenase pathway of arachidonic acid metabolism in human neutrophils by sulfasalazine and 5-aminosalicylic acid. Dig Dis Sci. 1987 Jun;32(6):577-82. [PubMed:2882965]
  2. Allgayer H, Eisenburg J, Paumgartner G: Soybean lipoxygenase inhibition: studies with the sulphasalazine metabolites N-acetylaminosalicylic acid, 5-aminosalicylic acid and sulphapyridine. Eur J Clin Pharmacol. 1984;26(4):449-51. [PubMed:6428914]
  3. Sircar JC, Schwender CF, Carethers ME: Inhibition of soybean lipoxygenase by sulfasalazine and 5-aminosalicylic acid: a possible mode of action in ulcerative colitis. Biochem Pharmacol. 1983 Jan 1;32(1):170-2. [PubMed:6131674]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Unknown
General Function
Phospholipase a2 activity
Specific Function
PA2 catalyzes the calcium-dependent hydrolysis of the 2-acyl groups in 3-sn-phosphoglycerides. Has a preference for arachidonic-containing phospholipids.
Gene Name
PLA2G2E
Uniprot ID
Q9NZK7
Uniprot Name
Group IIE secretory phospholipase A2
Molecular Weight
15988.525 Da
References
  1. Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [PubMed:10592235]
Kind
Protein
Organism
Mycobacterium tuberculosis
Pharmacological action
Unknown
Actions
Unknown
General Function
Not Available
Specific Function
2-amino-4-hydroxy-6-hydroxymethyldihydropteridine diphosphokinase activity
Gene Name
folK
Uniprot ID
P9WNC7
Uniprot Name
2-amino-4-hydroxy-6-hydroxymethyldihydropteridine pyrophosphokinase
Molecular Weight
20731.305 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Peroxidase activity
Specific Function
Part of the host defense system of polymorphonuclear leukocytes. It is responsible for microbicidal activity against a wide range of organisms. In the stimulated PMN, MPO catalyzes the production o...
Gene Name
MPO
Uniprot ID
P05164
Uniprot Name
Myeloperoxidase
Molecular Weight
83867.71 Da
References
  1. von Ritter C, Grisham MB, Granger DN: Sulfasalazine metabolites and dapsone attenuate formyl-methionyl-leucyl-phenylalanine-induced mucosal injury in rat ileum. Gastroenterology. 1989 Mar;96(3):811-6. [PubMed:2563347]
  2. Gorgulu S, Yagci G, Kaymakcioglu N, Ozkara M, Kurt B, Ozcan A, Kaya O, Sadir S, Tufan T: Hyperbaric oxygen enhances the efficiency of 5-aminosalicylic acid in acetic acid-induced colitis in rats. Dig Dis Sci. 2006 Mar;51(3):480-7. [PubMed:16614956]

Drug created on June 13, 2005 07:24 / Updated on December 01, 2017 17:36