Identification

Name
Icatibant
Accession Number
DB06196
Type
Small Molecule
Groups
Approved
Description

Icatibant (Firazyr) is a synthetic peptidomimetic drug consisting of ten amino acids, and acts as an effective and specific antagonist of bradykinin B2 receptors. It has been approved in the EU for use in hereditary angioedema, and is under investigation for a number of other conditions in which bradykinin is thought to play a significant role. Icatibant currently has orphan drug status in the United States and FDA approved on August 25, 2011.

Structure
Thumb
Synonyms
  • HOE 140
Product Ingredients
IngredientUNIICASInChI Key
Icatibant Acetate325O8467XK138614-30-9DKYJWPPYONLYTF-DZJWSCHMSA-N
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
FirazyrInjection, solution30 mg/3mLSubcutaneousShire2011-08-25Not applicableUs
FirazyrSolution10 mgSubcutaneousShire Orphan Therapies Inc2014-07-14Not applicableCanada
Categories
UNII
7PG89G35Q7
CAS number
130308-48-4
Weight
Average: 1304.522
Monoisotopic: 1303.660794719
Chemical Formula
C59H89N19O13S
InChI Key
QURWXBZNHXJZBE-MCDGZUPGSA-N
InChI
InChI=1S/C59H89N19O13S/c60-37(14-5-19-67-57(61)62)48(82)72-38(15-6-20-68-58(63)64)52(86)75-22-8-18-43(75)54(88)77-30-35(80)26-44(77)50(84)70-28-47(81)71-40(27-36-13-9-23-92-36)49(83)74-41(31-79)53(87)76-29-34-12-2-1-10-32(34)24-46(76)55(89)78-42-17-4-3-11-33(42)25-45(78)51(85)73-39(56(90)91)16-7-21-69-59(65)66/h1-2,9-10,12-13,23,33,35,37-46,79-80H,3-8,11,14-22,24-31,60H2,(H,70,84)(H,71,81)(H,72,82)(H,73,85)(H,74,83)(H,90,91)(H4,61,62,67)(H4,63,64,68)(H4,65,66,69)/t33-,35+,37+,38?,39-,40-,41-,42-,43?,44?,45?,46?/m0/s1
IUPAC Name
(2S)-2-{[(3aS,7aS)-1-{2-[(2S)-2-[(2S)-2-(2-{[(4R)-1-(1-{2-[(2R)-2-amino-5-[(diaminomethylidene)amino]pentanamido]-5-[(diaminomethylidene)amino]pentanoyl}pyrrolidine-2-carbonyl)-4-hydroxypyrrolidin-2-yl]formamido}acetamido)-3-(thiophen-2-yl)propanamido]-3-hydroxypropanoyl]-1,2,3,4-tetrahydroisoquinoline-3-carbonyl}-octahydro-1H-indol-2-yl]formamido}-5-[(diaminomethylidene)amino]pentanoic acid
SMILES
[H][[email protected]]12CC(N(C(=O)C3CC4=CC=CC=C4CN3C(=O)[[email protected]](CO)NC(=O)[[email protected]](CC3=CC=CS3)NC(=O)CNC(=O)C3C[[email protected]@H](O)CN3C(=O)C3CCCN3C(=O)C(CCCN=C(N)N)NC(=O)[[email protected]](N)CCCN=C(N)N)[[email protected]@]1([H])CCCC2)C(=O)N[[email protected]@H](CCCN=C(N)N)C(O)=O

Pharmacology

Indication

Approved for use in acute attacks of hereditary angioedema (HAE). Investigated for use/treatment in angioedema, liver disease, and burns and burn infections.

Structured Indications
Pharmacodynamics

Icatibant is a potent, specific, competitive, and selective peptidomimetic bradykinin beta2-receptor antagonist (pA2 = 9.04). It has a modified peptide structure, and is the first bradykinin receptor antagonist to act on the guinea-pig trachea without demonstrating agonist effects. It also inhibits aminopeptidase N (Ki = 9.1 μM). If an IV dose of 0.4 and 0.8 mg/kg was infused over 4 hours, one may observe an inhibited response to bradykinin challenge for 6 - 8 hours following completion of infusion.

Mechanism of action

Bradykinin is a peptide-based hormone that is formed locally in tissues, very often in response to a trauma. It increases vessel permeability, dilates blood vessels and causes smooth muscle cells to contract. Bradykinin plays an important role in the mediation of pain. Surplus bradykinin is responsible for the typical symptoms of inflammation, such as swelling, redness, overheating and pain. These symptoms are mediated by activation of bradykinin B2 receptors. In patients with HAE, they have an absent or dysfunctional C1-esterase inhibitor. This inhibitor is responsible for the production of bradykinin in which displacement of bradykinin from B2 receptors by icatibant has an inhibitory effect on the receptor for a relatively long time.

TargetActionsOrganism
AB2 bradykinin receptor
antagonist
Human
UAminopeptidase N
inhibitor
Human
Absorption

The absolute bioavailability of icatibant following a 30 mg subcutaneous dose is approximately 97%. Maximum plasma concentrations (Cmax) of 974 ± 280 ng/mL was reached when a single subcutaneous dose of 30 mg was administered. The AUC was 2165 ± 568 ng∙hr/mL. Icatibant did not accumulate following multiple doses.

Volume of distribution

Vdss, subcutaneous injection = 29.0 ± 8.7 L.

Protein binding
Not Available
Metabolism

Icatibant is metabolized by proteolytic enzymes into inactive metabolites. The cytochrome P450 enzyme system is not involved with the metabolism of icatibant.

Route of elimination

Urine (<10% unchanged)

Half life

After subcutaneous administration, mean elimination half-life was 1.4 ± 0.4 hours.

Clearance

Plasma clearance following subcutaneous administration was 245 ± 58 mL/min.

Toxicity
Not Available
Affected organisms
  • Humans and other mammals
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 Icatibant is combined with 16-Bromoepiandrosterone.Investigational
19-norandrostenedioneThe risk or severity of adverse effects can be increased when Icatibant is combined with 19-norandrostenedione.Experimental, Illicit
5-androstenedioneThe risk or severity of adverse effects can be increased when Icatibant is combined with 5-androstenedione.Experimental, Illicit
AbciximabIcatibant may increase the anticoagulant activities of Abciximab.Approved
AcebutololIcatibant may decrease the antihypertensive activities of Acebutolol.Approved
AceclofenacThe risk or severity of adverse effects can be increased when Icatibant is combined with Aceclofenac.Approved, Investigational
AcemetacinThe risk or severity of adverse effects can be increased when Icatibant is combined with Acemetacin.Approved
AcenocoumarolIcatibant may increase the anticoagulant activities of Acenocoumarol.Approved
Acetylsalicylic acidThe risk or severity of adverse effects can be increased when Acetylsalicylic acid is combined with Icatibant.Approved, Vet Approved
AclarubicinIcatibant may decrease the excretion rate of Aclarubicin which could result in a higher serum level.Investigational
AdapaleneThe risk or severity of adverse effects can be increased when Adapalene is combined with Icatibant.Approved
AlclofenacThe risk or severity of adverse effects can be increased when Icatibant is combined with Alclofenac.Approved, Withdrawn
AlclometasoneThe risk or severity of adverse effects can be increased when Icatibant is combined with Alclometasone.Approved
AldosteroneThe risk or severity of adverse effects can be increased when Icatibant is combined with Aldosterone.Experimental, Investigational
Alendronic acidThe risk or severity of adverse effects can be increased when Icatibant is combined with Alendronic acid.Approved
AliskirenIcatibant may decrease the antihypertensive activities of Aliskiren.Approved, Investigational
AlminoprofenThe risk or severity of adverse effects can be increased when Icatibant is combined with Alminoprofen.Experimental
AlprenololIcatibant may decrease the antihypertensive activities of Alprenolol.Approved, Withdrawn
AlprostadilThe therapeutic efficacy of Alprostadil can be decreased when used in combination with Icatibant.Approved, Investigational
AmcinonideThe risk or severity of adverse effects can be increased when Icatibant is combined with Amcinonide.Approved
AmikacinIcatibant may decrease the excretion rate of Amikacin which could result in a higher serum level.Approved, Vet Approved
AmilorideIcatibant may decrease the antihypertensive activities of Amiloride.Approved
AmrubicinIcatibant may decrease the excretion rate of Amrubicin which could result in a higher serum level.Approved, Investigational
AncrodIcatibant may increase the anticoagulant activities of Ancrod.Investigational
AndrographolideThe risk or severity of adverse effects can be increased when Andrographolide is combined with Icatibant.Investigational
AndrostenedioneThe risk or severity of adverse effects can be increased when Icatibant is combined with Androstenedione.Experimental, Illicit
AnecortaveThe risk or severity of adverse effects can be increased when Icatibant is combined with Anecortave.Investigational
anecortave acetateThe risk or severity of adverse effects can be increased when Icatibant is combined with anecortave acetate.Investigational
AnisodamineThe risk or severity of adverse effects can be increased when Icatibant is combined with Anisodamine.Investigational
annamycinIcatibant may decrease the excretion rate of annamycin which could result in a higher serum level.Investigational
AntipyrineThe risk or severity of adverse effects can be increased when Antipyrine is combined with Icatibant.Approved
Antithrombin III humanIcatibant may increase the anticoagulant activities of Antithrombin III human.Approved
ApixabanIcatibant may increase the anticoagulant activities of Apixaban.Approved
ApocyninThe risk or severity of adverse effects can be increased when Icatibant is combined with Apocynin.Investigational
ApramycinIcatibant may decrease the excretion rate of Apramycin which could result in a higher serum level.Experimental, Vet Approved
ApremilastThe risk or severity of adverse effects can be increased when Apremilast is combined with Icatibant.Approved, Investigational
ArbekacinIcatibant may decrease the excretion rate of Arbekacin which could result in a higher serum level.Approved, Investigational
ArdeparinIcatibant may increase the anticoagulant activities of Ardeparin.Approved, Investigational, Withdrawn
ArgatrobanIcatibant may increase the anticoagulant activities of Argatroban.Approved, Investigational
ArotinololIcatibant may decrease the antihypertensive activities of Arotinolol.Approved, Investigational
AtamestaneThe risk or severity of adverse effects can be increased when Icatibant is combined with Atamestane.Investigational
AtenololIcatibant may decrease the antihypertensive activities of Atenolol.Approved
AzapropazoneThe risk or severity of adverse effects can be increased when Icatibant is combined with Azapropazone.Withdrawn
AzelastineThe risk or severity of adverse effects can be increased when Azelastine is combined with Icatibant.Approved
Azilsartan medoxomilThe risk or severity of adverse effects can be increased when Azilsartan medoxomil is combined with Icatibant.Approved
BalsalazideIcatibant may increase the nephrotoxic activities of Balsalazide.Approved, Investigational
BCG vaccineThe therapeutic efficacy of BCG vaccine can be decreased when used in combination with Icatibant.Investigational
BecaplerminIcatibant may increase the anticoagulant activities of Becaplermin.Approved, Investigational
Beclomethasone dipropionateThe risk or severity of adverse effects can be increased when Icatibant is combined with Beclomethasone dipropionate.Approved, Investigational
BefunololIcatibant may decrease the antihypertensive activities of Befunolol.Experimental
BekanamycinIcatibant may decrease the excretion rate of Bekanamycin which could result in a higher serum level.Experimental
BenazeprilIcatibant may decrease the antihypertensive activities of Benazepril.Approved, Investigational
BendazacThe risk or severity of adverse effects can be increased when Icatibant is combined with Bendazac.Experimental
BendroflumethiazideThe therapeutic efficacy of Bendroflumethiazide can be decreased when used in combination with Icatibant.Approved
BenorilateThe risk or severity of adverse effects can be increased when Icatibant is combined with Benorilate.Experimental
BenoxaprofenThe risk or severity of adverse effects can be increased when Benoxaprofen is combined with Icatibant.Withdrawn
BenzydamineThe risk or severity of adverse effects can be increased when Icatibant is combined with Benzydamine.Approved
BeraprostThe therapeutic efficacy of Beraprost can be decreased when used in combination with Icatibant.Investigational
BetamethasoneThe risk or severity of adverse effects can be increased when Icatibant is combined with Betamethasone.Approved, Vet Approved
BetaxololIcatibant may decrease the antihypertensive activities of Betaxolol.Approved
BevantololIcatibant may decrease the antihypertensive activities of Bevantolol.Approved
BevoniumThe risk or severity of adverse effects can be increased when Icatibant is combined with Bevonium.Experimental
BimatoprostThe therapeutic efficacy of Bimatoprost can be decreased when used in combination with Icatibant.Approved, Investigational
BisoprololIcatibant may decrease the antihypertensive activities of Bisoprolol.Approved
BivalirudinIcatibant may increase the anticoagulant activities of Bivalirudin.Approved, Investigational
BopindololIcatibant may decrease the antihypertensive activities of Bopindolol.Approved
BromfenacThe risk or severity of adverse effects can be increased when Bromfenac is combined with Icatibant.Approved
BucillamineThe risk or severity of adverse effects can be increased when Icatibant is combined with Bucillamine.Investigational
BucindololIcatibant may decrease the antihypertensive activities of Bucindolol.Investigational
BudesonideThe risk or severity of adverse effects can be increased when Icatibant is combined with Budesonide.Approved
BufexamacThe risk or severity of adverse effects can be increased when Icatibant is combined with Bufexamac.Experimental
BufuralolIcatibant may decrease the antihypertensive activities of Bufuralol.Experimental, Investigational
BumadizoneThe risk or severity of adverse effects can be increased when Icatibant is combined with Bumadizone.Experimental
BumetanideIcatibant may decrease the diuretic activities of Bumetanide.Approved
BupranololIcatibant may decrease the antihypertensive activities of Bupranolol.Approved
CandesartanThe risk or severity of adverse effects can be increased when Candesartan is combined with Icatibant.Experimental
Candesartan cilexetilThe risk or severity of adverse effects can be increased when Candesartan cilexetil is combined with Icatibant.Approved
CandoxatrilIcatibant may decrease the antihypertensive activities of Candoxatril.Experimental
CaptoprilIcatibant may decrease the antihypertensive activities of Captopril.Approved
Carbaspirin calciumThe risk or severity of adverse effects can be increased when Icatibant is combined with Carbaspirin calcium.Experimental, Investigational
Carboprost TromethamineThe therapeutic efficacy of Carboprost Tromethamine can be decreased when used in combination with Icatibant.Approved
CarprofenThe risk or severity of adverse effects can be increased when Carprofen is combined with Icatibant.Approved, Vet Approved, Withdrawn
CarteololIcatibant may decrease the antihypertensive activities of Carteolol.Approved
CarvedilolIcatibant may decrease the antihypertensive activities of Carvedilol.Approved, Investigational
CastanospermineThe risk or severity of adverse effects can be increased when Castanospermine is combined with Icatibant.Experimental
CelecoxibThe risk or severity of adverse effects can be increased when Celecoxib is combined with Icatibant.Approved, Investigational
CeliprololIcatibant may decrease the antihypertensive activities of Celiprolol.Approved, Investigational
CertoparinIcatibant may increase the anticoagulant activities of Certoparin.Approved, Investigational
ChloroquineThe risk or severity of adverse effects can be increased when Chloroquine is combined with Icatibant.Approved, Vet Approved
ChlorothiazideThe therapeutic efficacy of Chlorothiazide can be decreased when used in combination with Icatibant.Approved, Vet Approved
ChlorthalidoneThe therapeutic efficacy of Chlorthalidone can be decreased when used in combination with Icatibant.Approved
CholestyramineCholestyramine can cause a decrease in the absorption of Icatibant resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Choline magnesium trisalicylateThe risk or severity of adverse effects can be increased when Choline magnesium trisalicylate is combined with Icatibant.Approved
CiclesonideThe risk or severity of adverse effects can be increased when Icatibant is combined with Ciclesonide.Approved, Investigational
CilazaprilIcatibant may decrease the antihypertensive activities of Cilazapril.Approved
CinoxacinIcatibant may increase the neuroexcitatory activities of Cinoxacin.Approved, Investigational, Withdrawn
Citric AcidIcatibant may increase the anticoagulant activities of Citric Acid.Approved, Nutraceutical, Vet Approved
ClobetasolThe risk or severity of adverse effects can be increased when Icatibant is combined with Clobetasol.Investigational
Clobetasol propionateThe risk or severity of adverse effects can be increased when Icatibant is combined with Clobetasol propionate.Approved
ClobetasoneThe risk or severity of adverse effects can be increased when Icatibant is combined with Clobetasone.Approved
ClocortoloneThe risk or severity of adverse effects can be increased when Icatibant is combined with Clocortolone.Approved
Clodronic AcidThe risk or severity of adverse effects can be increased when Icatibant is combined with Clodronic Acid.Approved, Investigational, Vet Approved
ClonixinThe risk or severity of adverse effects can be increased when Icatibant is combined with Clonixin.Approved
CloprostenolThe therapeutic efficacy of Cloprostenol can be decreased when used in combination with Icatibant.Vet Approved
CloranololIcatibant may decrease the antihypertensive activities of Cloranolol.Experimental
Clostridium tetani toxoid antigen (formaldehyde inactivated)The therapeutic efficacy of Clostridium tetani toxoid antigen (formaldehyde inactivated) can be decreased when used in combination with Icatibant.Approved
ColesevelamColesevelam can cause a decrease in the absorption of Icatibant resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
ColestipolColestipol can cause a decrease in the absorption of Icatibant resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Cortexolone 17α-propionateThe risk or severity of adverse effects can be increased when Icatibant is combined with Cortexolone 17α-propionate.Investigational
CorticosteroneThe risk or severity of adverse effects can be increased when Icatibant is combined with Corticosterone.Experimental
Cortisone acetateThe risk or severity of adverse effects can be increased when Icatibant is combined with Cortisone acetate.Approved
Corynebacterium diphtheriae toxoid antigen (formaldehyde inactivated)The therapeutic efficacy of Corynebacterium diphtheriae toxoid antigen (formaldehyde inactivated) can be decreased when used in combination with Icatibant.Approved
CurcuminThe risk or severity of adverse effects can be increased when Icatibant is combined with Curcumin.Investigational
CyclopenthiazideThe therapeutic efficacy of Cyclopenthiazide can be decreased when used in combination with Icatibant.Experimental
CyclosporineIcatibant may increase the nephrotoxic activities of Cyclosporine.Approved, Investigational, Vet Approved
D-LimoneneThe risk or severity of adverse effects can be increased when Icatibant is combined with D-Limonene.Investigational
Dabigatran etexilateIcatibant may increase the anticoagulant activities of Dabigatran etexilate.Approved
DalteparinIcatibant may increase the anticoagulant activities of Dalteparin.Approved
DanaparoidIcatibant may increase the anticoagulant activities of Danaparoid.Approved, Withdrawn
DarexabanIcatibant may increase the anticoagulant activities of Darexaban.Investigational
DaunorubicinIcatibant may decrease the excretion rate of Daunorubicin which could result in a higher serum level.Approved
DeferasiroxThe risk or severity of adverse effects can be increased when Icatibant is combined with Deferasirox.Approved, Investigational
DeflazacortThe risk or severity of adverse effects can be increased when Icatibant is combined with Deflazacort.Approved
DelaprilIcatibant may decrease the antihypertensive activities of Delapril.Experimental
DenosumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Icatibant.Approved
DesirudinIcatibant may increase the anticoagulant activities of Desirudin.Approved
DesmopressinThe risk or severity of adverse effects can be increased when Icatibant is combined with Desmopressin.Approved
DesonideThe risk or severity of adverse effects can be increased when Icatibant is combined with Desonide.Approved, Investigational
DesoximetasoneThe risk or severity of adverse effects can be increased when Icatibant is combined with Desoximetasone.Approved
Desoxycorticosterone acetateThe risk or severity of adverse effects can be increased when Icatibant is combined with Desoxycorticosterone acetate.Approved
Desoxycorticosterone PivalateThe risk or severity of adverse effects can be increased when Icatibant is combined with Desoxycorticosterone Pivalate.Experimental, Vet Approved
DexamethasoneThe risk or severity of adverse effects can be increased when Icatibant is combined with Dexamethasone.Approved, Investigational, Vet Approved
Dexamethasone isonicotinateThe risk or severity of adverse effects can be increased when Icatibant is combined with Dexamethasone isonicotinate.Vet Approved
DexketoprofenThe risk or severity of adverse effects can be increased when Dexketoprofen is combined with Icatibant.Approved, Investigational
DextranIcatibant may increase the anticoagulant activities of Dextran.Approved, Vet Approved
Dextran 40Icatibant may increase the anticoagulant activities of Dextran 40.Approved
Dextran 70Icatibant may increase the anticoagulant activities of Dextran 70.Approved
Dextran 75Icatibant may increase the anticoagulant activities of Dextran 75.Approved
DibekacinIcatibant may decrease the excretion rate of Dibekacin which could result in a higher serum level.Experimental
DiclofenacThe risk or severity of adverse effects can be increased when Diclofenac is combined with Icatibant.Approved, Vet Approved
DicoumarolIcatibant may increase the anticoagulant activities of Dicoumarol.Approved
DifenpiramideThe risk or severity of adverse effects can be increased when Icatibant is combined with Difenpiramide.Experimental
DiflorasoneThe risk or severity of adverse effects can be increased when Icatibant is combined with Diflorasone.Approved
DiflunisalThe risk or severity of adverse effects can be increased when Diflunisal is combined with Icatibant.Approved
DifluocortoloneThe risk or severity of adverse effects can be increased when Icatibant is combined with Difluocortolone.Approved, Investigational
DifluprednateThe risk or severity of adverse effects can be increased when Icatibant is combined with Difluprednate.Approved
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Icatibant.Approved
DihydrostreptomycinIcatibant may decrease the excretion rate of Dihydrostreptomycin which could result in a higher serum level.Investigational, Vet Approved
DinoprostThe therapeutic efficacy of Dinoprost can be decreased when used in combination with Icatibant.Investigational
Dinoprost TromethamineThe therapeutic efficacy of Dinoprost Tromethamine can be decreased when used in combination with Icatibant.Approved, Vet Approved
DinoprostoneThe therapeutic efficacy of Dinoprostone can be decreased when used in combination with Icatibant.Approved
DoxorubicinIcatibant may decrease the excretion rate of Doxorubicin which could result in a higher serum level.Approved, Investigational
DrospirenoneIcatibant may increase the hyperkalemic activities of Drospirenone.Approved
DroxicamThe risk or severity of adverse effects can be increased when Icatibant is combined with Droxicam.Approved
DuvelisibThe risk or severity of adverse effects can be increased when Icatibant is combined with Duvelisib.Investigational
E-6201The risk or severity of adverse effects can be increased when Icatibant is combined with E-6201.Investigational
Edetic AcidIcatibant may increase the anticoagulant activities of Edetic Acid.Approved, Vet Approved
EdoxabanIcatibant may increase the anticoagulant activities of Edoxaban.Approved
EnalaprilIcatibant may decrease the antihypertensive activities of Enalapril.Approved, Vet Approved
EnalaprilatIcatibant may decrease the antihypertensive activities of Enalaprilat.Approved
EnoxacinIcatibant may increase the neuroexcitatory activities of Enoxacin.Approved, Investigational
EnoxaparinIcatibant may increase the anticoagulant activities of Enoxaparin.Approved
EnprostilThe therapeutic efficacy of Enprostil can be decreased when used in combination with Icatibant.Experimental
EpanololIcatibant may decrease the antihypertensive activities of Epanolol.Experimental
EpirizoleThe risk or severity of adverse effects can be increased when Icatibant is combined with Epirizole.Approved
EpirubicinIcatibant may decrease the excretion rate of Epirubicin which could result in a higher serum level.Approved
EplerenoneIcatibant may decrease the antihypertensive activities of Eplerenone.Approved
EpoprostenolThe therapeutic efficacy of Epoprostenol can be decreased when used in combination with Icatibant.Approved
EprosartanThe risk or severity of adverse effects can be increased when Eprosartan is combined with Icatibant.Approved
EquileninThe risk or severity of adverse effects can be increased when Icatibant is combined with Equilenin.Experimental
EquilinThe risk or severity of adverse effects can be increased when Icatibant is combined with Equilin.Approved
EsmololIcatibant may decrease the antihypertensive activities of Esmolol.Approved
EstroneThe risk or severity of adverse effects can be increased when Icatibant is combined with Estrone.Approved
Estrone sulfateThe risk or severity of adverse effects can be increased when Icatibant is combined with Estrone sulfate.Approved
Etacrynic acidIcatibant may decrease the diuretic activities of Etacrynic acid.Approved
EtanerceptThe risk or severity of adverse effects can be increased when Etanercept is combined with Icatibant.Approved, Investigational
EthenzamideThe risk or severity of adverse effects can be increased when Icatibant is combined with Ethenzamide.Experimental
Ethyl biscoumacetateIcatibant may increase the anticoagulant activities of Ethyl biscoumacetate.Withdrawn
Etidronic acidThe risk or severity of adverse effects can be increased when Icatibant is combined with Etidronic acid.Approved
EtodolacThe risk or severity of adverse effects can be increased when Etodolac is combined with Icatibant.Approved, Investigational, Vet Approved
EtofenamateThe risk or severity of adverse effects can be increased when Icatibant is combined with Etofenamate.Approved, Investigational
EtoricoxibThe risk or severity of adverse effects can be increased when Etoricoxib is combined with Icatibant.Approved, Investigational
Evening primrose oilThe risk or severity of adverse effects can be increased when Icatibant is combined with Evening primrose oil.Approved, Investigational
exisulindThe risk or severity of adverse effects can be increased when Icatibant is combined with exisulind.Investigational
FelbinacThe risk or severity of adverse effects can be increased when Icatibant is combined with Felbinac.Experimental
FenbufenThe risk or severity of adverse effects can be increased when Icatibant is combined with Fenbufen.Approved
FenoprofenThe risk or severity of adverse effects can be increased when Fenoprofen is combined with Icatibant.Approved
FenprostaleneThe therapeutic efficacy of Fenprostalene can be decreased when used in combination with Icatibant.Vet Approved
FentiazacThe risk or severity of adverse effects can be increased when Icatibant is combined with Fentiazac.Experimental
FeprazoneThe risk or severity of adverse effects can be increased when Icatibant is combined with Feprazone.Experimental
Ferulic acidIcatibant may increase the anticoagulant activities of Ferulic acid.Experimental
FimasartanThe risk or severity of adverse effects can be increased when Fimasartan is combined with Icatibant.Approved, Investigational
FingolimodIcatibant may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
FleroxacinIcatibant may increase the neuroexcitatory activities of Fleroxacin.Approved
FloctafenineThe risk or severity of adverse effects can be increased when Floctafenine is combined with Icatibant.Approved, Withdrawn
fluasteroneThe risk or severity of adverse effects can be increased when Icatibant is combined with fluasterone.Investigational
FludrocortisoneThe risk or severity of adverse effects can be increased when Icatibant is combined with Fludrocortisone.Approved
FluindioneIcatibant may increase the anticoagulant activities of Fluindione.Investigational
FlumequineIcatibant may increase the neuroexcitatory activities of Flumequine.Withdrawn
FlumethasoneThe risk or severity of adverse effects can be increased when Icatibant is combined with Flumethasone.Approved, Vet Approved
FlunisolideThe risk or severity of adverse effects can be increased when Icatibant is combined with Flunisolide.Approved, Investigational
FlunixinThe risk or severity of adverse effects can be increased when Icatibant is combined with Flunixin.Vet Approved
FlunoxaprofenThe risk or severity of adverse effects can be increased when Icatibant is combined with Flunoxaprofen.Experimental
Fluocinolone AcetonideThe risk or severity of adverse effects can be increased when Icatibant is combined with Fluocinolone Acetonide.Approved, Investigational, Vet Approved
FluocinonideThe risk or severity of adverse effects can be increased when Icatibant is combined with Fluocinonide.Approved, Investigational
FluocortoloneThe risk or severity of adverse effects can be increased when Icatibant is combined with Fluocortolone.Approved, Withdrawn
FluorometholoneThe risk or severity of adverse effects can be increased when Icatibant is combined with Fluorometholone.Approved
FluprednideneThe risk or severity of adverse effects can be increased when Icatibant is combined with Fluprednidene.Approved, Withdrawn
FluprednisoloneThe risk or severity of adverse effects can be increased when Icatibant is combined with Fluprednisolone.Approved
FluprostenolThe therapeutic efficacy of Fluprostenol can be decreased when used in combination with Icatibant.Vet Approved
FlurandrenolideThe risk or severity of adverse effects can be increased when Icatibant is combined with Flurandrenolide.Approved
FlurbiprofenThe risk or severity of adverse effects can be increased when Flurbiprofen is combined with Icatibant.Approved, Investigational
Fluticasone furoateThe risk or severity of adverse effects can be increased when Icatibant is combined with Fluticasone furoate.Approved
Fluticasone propionateThe risk or severity of adverse effects can be increased when Icatibant is combined with Fluticasone propionate.Approved
Folic AcidThe therapeutic efficacy of Folic Acid can be decreased when used in combination with Icatibant.Approved, Nutraceutical, Vet Approved
FondaparinuxIcatibant may increase the anticoagulant activities of Fondaparinux.Investigational
Fondaparinux sodiumIcatibant may increase the anticoagulant activities of Fondaparinux sodium.Approved, Investigational
ForasartanThe risk or severity of adverse effects can be increased when Forasartan is combined with Icatibant.Experimental
FormestaneThe risk or severity of adverse effects can be increased when Icatibant is combined with Formestane.Approved, Investigational, Withdrawn
FosinoprilIcatibant may decrease the antihypertensive activities of Fosinopril.Approved
FramycetinIcatibant may decrease the excretion rate of Framycetin which could result in a higher serum level.Approved
FurosemideIcatibant may decrease the diuretic activities of Furosemide.Approved, Vet Approved
G17DTThe therapeutic efficacy of G17DT can be decreased when used in combination with Icatibant.Investigational
GabexateIcatibant may increase the anticoagulant activities of Gabexate.Investigational
GarenoxacinIcatibant may increase the neuroexcitatory activities of Garenoxacin.Investigational
GatifloxacinIcatibant may increase the neuroexcitatory activities of Gatifloxacin.Approved, Investigational
GemeprostThe therapeutic efficacy of Gemeprost can be decreased when used in combination with Icatibant.Approved, Withdrawn
GemifloxacinIcatibant may increase the neuroexcitatory activities of Gemifloxacin.Approved, Investigational
GeneticinIcatibant may decrease the excretion rate of Geneticin which could result in a higher serum level.Experimental
GentamicinIcatibant may decrease the excretion rate of Gentamicin which could result in a higher serum level.Approved, Vet Approved
GENTAMICIN C1AIcatibant may decrease the excretion rate of GENTAMICIN C1A which could result in a higher serum level.Experimental
GI-5005The therapeutic efficacy of GI-5005 can be decreased when used in combination with Icatibant.Investigational
GPX-150Icatibant may decrease the excretion rate of GPX-150 which could result in a higher serum level.Investigational
GrepafloxacinIcatibant may increase the neuroexcitatory activities of Grepafloxacin.Investigational, Withdrawn
GuacetisalThe risk or severity of adverse effects can be increased when Icatibant is combined with Guacetisal.Experimental
HalcinonideThe risk or severity of adverse effects can be increased when Icatibant is combined with Halcinonide.Approved, Investigational, Withdrawn
HaloperidolThe risk or severity of adverse effects can be increased when Icatibant is combined with Haloperidol.Approved
HE3286The risk or severity of adverse effects can be increased when Icatibant is combined with HE3286.Investigational
HeparinIcatibant may increase the anticoagulant activities of Heparin.Approved, Investigational
Hepatitis A VaccineThe therapeutic efficacy of Hepatitis A Vaccine can be decreased when used in combination with Icatibant.Approved
Hepatitis B Vaccine (Recombinant)The therapeutic efficacy of Hepatitis B Vaccine (Recombinant) can be decreased when used in combination with Icatibant.Approved, Withdrawn
HigenamineThe risk or severity of adverse effects can be increased when Icatibant is combined with Higenamine.Investigational
HydralazineIcatibant may decrease the antihypertensive activities of Hydralazine.Approved
HydrochlorothiazideThe therapeutic efficacy of Hydrochlorothiazide can be decreased when used in combination with Icatibant.Approved, Vet Approved
HydrocortisoneThe risk or severity of adverse effects can be increased when Icatibant is combined with Hydrocortisone.Approved, Vet Approved
HydroflumethiazideThe therapeutic efficacy of Hydroflumethiazide can be decreased when used in combination with Icatibant.Approved, Investigational
Hygromycin BIcatibant may decrease the excretion rate of Hygromycin B which could result in a higher serum level.Vet Approved
IbandronateThe risk or severity of adverse effects can be increased when Icatibant is combined with Ibandronate.Approved, Investigational
IbuprofenThe risk or severity of adverse effects can be increased when Ibuprofen is combined with Icatibant.Approved
IbuproxamThe risk or severity of adverse effects can be increased when Icatibant is combined with Ibuproxam.Withdrawn
IdarubicinIcatibant may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved
IdraparinuxIcatibant may increase the anticoagulant activities of Idraparinux.Investigational
IloprostThe therapeutic efficacy of Iloprost can be decreased when used in combination with Icatibant.Approved, Investigational
ImidaprilIcatibant may decrease the antihypertensive activities of Imidapril.Investigational
Imidazole salicylateThe risk or severity of adverse effects can be increased when Icatibant is combined with Imidazole salicylate.Experimental
IndapamideThe therapeutic efficacy of Indapamide can be decreased when used in combination with Icatibant.Approved
IndenololIcatibant may decrease the antihypertensive activities of Indenolol.Withdrawn
IndobufenThe risk or severity of adverse effects can be increased when Icatibant is combined with Indobufen.Investigational
IndomethacinThe risk or severity of adverse effects can be increased when Indomethacin is combined with Icatibant.Approved, Investigational
IndoprofenThe risk or severity of adverse effects can be increased when Icatibant is combined with Indoprofen.Withdrawn
INGN 201The therapeutic efficacy of INGN 201 can be decreased when used in combination with Icatibant.Investigational
INGN 225The therapeutic efficacy of INGN 225 can be decreased when used in combination with Icatibant.Investigational
INNO-206Icatibant may decrease the excretion rate of INNO-206 which could result in a higher serum level.Investigational
IrbesartanThe risk or severity of adverse effects can be increased when Irbesartan is combined with Icatibant.Approved, Investigational
IsepamicinIcatibant may decrease the excretion rate of Isepamicin which could result in a higher serum level.Experimental
IsoxicamThe risk or severity of adverse effects can be increased when Icatibant is combined with Isoxicam.Withdrawn
IstaroximeThe risk or severity of adverse effects can be increased when Icatibant is combined with Istaroxime.Investigational
KanamycinIcatibant may decrease the excretion rate of Kanamycin which could result in a higher serum level.Approved, Investigational, Vet Approved
KebuzoneThe risk or severity of adverse effects can be increased when Icatibant is combined with Kebuzone.Experimental
KetoprofenThe risk or severity of adverse effects can be increased when Ketoprofen is combined with Icatibant.Approved, Vet Approved
KetorolacThe risk or severity of adverse effects can be increased when Ketorolac is combined with Icatibant.Approved
LabetalolIcatibant may decrease the antihypertensive activities of Labetalol.Approved
LandiololIcatibant may decrease the antihypertensive activities of Landiolol.Investigational
LatanoprostThe therapeutic efficacy of Latanoprost can be decreased when used in combination with Icatibant.Approved, Investigational
Latanoprostene BunodThe therapeutic efficacy of Latanoprostene Bunod can be decreased when used in combination with Icatibant.Approved, Investigational
LeflunomideThe risk or severity of adverse effects can be increased when Icatibant is combined with Leflunomide.Approved, Investigational
LepirudinIcatibant may increase the anticoagulant activities of Lepirudin.Approved
LetaxabanIcatibant may increase the anticoagulant activities of Letaxaban.Investigational
LevobunololIcatibant may decrease the antihypertensive activities of Levobunolol.Approved
LevofloxacinIcatibant may increase the neuroexcitatory activities of Levofloxacin.Approved, Investigational
LimaprostThe therapeutic efficacy of Limaprost can be decreased when used in combination with Icatibant.Approved, Investigational
LisinoprilIcatibant may decrease the antihypertensive activities of Lisinopril.Approved, Investigational
LisofyllineThe risk or severity of adverse effects can be increased when Icatibant is combined with Lisofylline.Investigational
LithiumThe serum concentration of Lithium can be increased when it is combined with Icatibant.Approved
LonazolacThe risk or severity of adverse effects can be increased when Icatibant is combined with Lonazolac.Experimental
LornoxicamThe risk or severity of adverse effects can be increased when Icatibant is combined with Lornoxicam.Approved, Investigational
LosartanThe risk or severity of adverse effects can be increased when Losartan is combined with Icatibant.Approved
LoteprednolThe risk or severity of adverse effects can be increased when Icatibant is combined with Loteprednol.Approved
LoxoprofenThe risk or severity of adverse effects can be increased when Icatibant is combined with Loxoprofen.Approved, Investigational
LubiprostoneThe therapeutic efficacy of Lubiprostone can be decreased when used in combination with Icatibant.Approved, Investigational
LumiracoxibThe risk or severity of adverse effects can be increased when Lumiracoxib is combined with Icatibant.Approved, Investigational
LuprostiolThe therapeutic efficacy of Luprostiol can be decreased when used in combination with Icatibant.Vet Approved
Magnesium salicylateThe risk or severity of adverse effects can be increased when Magnesium salicylate is combined with Icatibant.Approved
MasoprocolThe risk or severity of adverse effects can be increased when Masoprocol is combined with Icatibant.Approved, Investigational
ME-609The risk or severity of adverse effects can be increased when Icatibant is combined with ME-609.Investigational
Meclofenamic acidThe risk or severity of adverse effects can be increased when Meclofenamic acid is combined with Icatibant.Approved, Vet Approved
MedrysoneThe risk or severity of adverse effects can be increased when Icatibant is combined with Medrysone.Approved
Mefenamic acidThe risk or severity of adverse effects can be increased when Mefenamic acid is combined with Icatibant.Approved
MelagatranIcatibant may increase the anticoagulant activities of Melagatran.Experimental
MelengestrolThe risk or severity of adverse effects can be increased when Icatibant is combined with Melengestrol.Vet Approved
MeloxicamThe risk or severity of adverse effects can be increased when Meloxicam is combined with Icatibant.Approved, Vet Approved
MepindololIcatibant may decrease the antihypertensive activities of Mepindolol.Experimental
MesalazineIcatibant may increase the nephrotoxic activities of Mesalazine.Approved
MetamizoleThe risk or severity of adverse effects can be increased when Metamizole is combined with Icatibant.Investigational, Withdrawn
MethotrexateThe serum concentration of Methotrexate can be increased when it is combined with Icatibant.Approved
MethyclothiazideThe therapeutic efficacy of Methyclothiazide can be decreased when used in combination with Icatibant.Approved
MethylprednisoloneThe risk or severity of adverse effects can be increased when Icatibant is combined with Methylprednisolone.Approved, Vet Approved
MetipranololIcatibant may decrease the antihypertensive activities of Metipranolol.Approved
MetolazoneThe therapeutic efficacy of Metolazone can be decreased when used in combination with Icatibant.Approved
MetoprololIcatibant may decrease the antihypertensive activities of Metoprolol.Approved, Investigational
MetrizamideIcatibant may decrease the excretion rate of Metrizamide which could result in a higher serum level.Approved
MicronomicinIcatibant may decrease the excretion rate of Micronomicin which could result in a higher serum level.Experimental
MisoprostolThe therapeutic efficacy of Misoprostol can be decreased when used in combination with Icatibant.Approved
MizoribineThe risk or severity of adverse effects can be increased when Icatibant is combined with Mizoribine.Investigational
MoexiprilIcatibant may decrease the antihypertensive activities of Moexipril.Approved
MofebutazoneThe risk or severity of adverse effects can be increased when Icatibant is combined with Mofebutazone.Experimental
MometasoneThe risk or severity of adverse effects can be increased when Icatibant is combined with Mometasone.Approved, Vet Approved
MorniflumateThe risk or severity of adverse effects can be increased when Morniflumate is combined with Icatibant.Approved
Mycophenolate mofetilThe risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Icatibant.Approved, Investigational
Mycophenolic acidThe risk or severity of adverse effects can be increased when Mycophenolic acid is combined with Icatibant.Approved
NabumetoneThe risk or severity of adverse effects can be increased when Nabumetone is combined with Icatibant.Approved
NadololIcatibant may decrease the antihypertensive activities of Nadolol.Approved
NadroparinIcatibant may increase the anticoagulant activities of Nadroparin.Approved
NafamostatIcatibant may increase the anticoagulant activities of Nafamostat.Approved, Investigational
NaftifineThe risk or severity of adverse effects can be increased when Naftifine is combined with Icatibant.Approved
Nalidixic AcidIcatibant may increase the neuroexcitatory activities of Nalidixic Acid.Approved, Investigational
NaproxenThe risk or severity of adverse effects can be increased when Naproxen is combined with Icatibant.Approved, Vet Approved
NatalizumabThe risk or severity of adverse effects can be increased when Icatibant is combined with Natalizumab.Approved, Investigational
NCX 1022The risk or severity of adverse effects can be increased when Icatibant is combined with NCX 1022.Investigational
NeamineIcatibant may decrease the excretion rate of Neamine which could result in a higher serum level.Experimental
NebivololIcatibant may decrease the antihypertensive activities of Nebivolol.Approved, Investigational
NemonoxacinIcatibant may increase the neuroexcitatory activities of Nemonoxacin.Investigational
NeomycinIcatibant may decrease the excretion rate of Neomycin which could result in a higher serum level.Approved, Vet Approved
NepafenacThe risk or severity of adverse effects can be increased when Nepafenac is combined with Icatibant.Approved
NetilmicinIcatibant may decrease the excretion rate of Netilmicin which could result in a higher serum level.Approved, Investigational
NifenazoneThe risk or severity of adverse effects can be increased when Icatibant is combined with Nifenazone.Experimental
Niflumic AcidThe risk or severity of adverse effects can be increased when Niflumic Acid is combined with Icatibant.Approved
NimesulideThe risk or severity of adverse effects can be increased when Nimesulide is combined with Icatibant.Approved, Investigational, Withdrawn
NitroaspirinThe risk or severity of adverse effects can be increased when Icatibant is combined with Nitroaspirin.Investigational
NorfloxacinIcatibant may increase the neuroexcitatory activities of Norfloxacin.Approved
Oleoyl-estroneThe risk or severity of adverse effects can be increased when Icatibant is combined with Oleoyl-estrone.Investigational
OlmesartanThe risk or severity of adverse effects can be increased when Olmesartan is combined with Icatibant.Approved, Investigational
OlopatadineThe risk or severity of adverse effects can be increased when Olopatadine is combined with Icatibant.Approved
OlsalazineIcatibant may increase the nephrotoxic activities of Olsalazine.Approved
Omacetaxine mepesuccinateThe risk or severity of adverse effects can be increased when Icatibant is combined with Omacetaxine mepesuccinate.Approved
OmapatrilatIcatibant may decrease the antihypertensive activities of Omapatrilat.Investigational
OrgoteinThe risk or severity of adverse effects can be increased when Icatibant is combined with Orgotein.Vet Approved
OtamixabanIcatibant may increase the anticoagulant activities of Otamixaban.Investigational
OxaprozinThe risk or severity of adverse effects can be increased when Oxaprozin is combined with Icatibant.Approved
Oxolinic acidIcatibant may increase the neuroexcitatory activities of Oxolinic acid.Experimental
OxprenololIcatibant may decrease the antihypertensive activities of Oxprenolol.Approved
OxyphenbutazoneThe risk or severity of adverse effects can be increased when Oxyphenbutazone is combined with Icatibant.Approved, Withdrawn
PamidronateThe risk or severity of adverse effects can be increased when Icatibant is combined with Pamidronate.Approved
ParamethasoneThe risk or severity of adverse effects can be increased when Icatibant is combined with Paramethasone.Approved
ParecoxibThe risk or severity of adverse effects can be increased when Icatibant is combined with Parecoxib.Approved
ParomomycinIcatibant may decrease the excretion rate of Paromomycin which could result in a higher serum level.Approved, Investigational
ParthenolideThe risk or severity of adverse effects can be increased when Icatibant is combined with Parthenolide.Investigational
PazufloxacinIcatibant may increase the neuroexcitatory activities of Pazufloxacin.Investigational
PefloxacinIcatibant may increase the neuroexcitatory activities of Pefloxacin.Approved
PenbutololIcatibant may decrease the antihypertensive activities of Penbutolol.Approved, Investigational
Pentaerythritol TetranitrateIcatibant may increase the anticoagulant activities of Pentaerythritol Tetranitrate.Approved
Pentosan PolysulfateIcatibant may increase the anticoagulant activities of Pentosan Polysulfate.Approved
PerindoprilIcatibant may decrease the antihypertensive activities of Perindopril.Approved
PhenindioneIcatibant may increase the anticoagulant activities of Phenindione.Approved, Investigational
PhenprocoumonIcatibant may increase the anticoagulant activities of Phenprocoumon.Approved, Investigational
PhenylbutazoneThe risk or severity of adverse effects can be increased when Phenylbutazone is combined with Icatibant.Approved, Vet Approved
PimecrolimusThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Icatibant.Approved, Investigational
PindololIcatibant may decrease the antihypertensive activities of Pindolol.Approved
Pipemidic acidIcatibant may increase the neuroexcitatory activities of Pipemidic acid.Experimental
PirarubicinIcatibant may decrease the excretion rate of Pirarubicin which could result in a higher serum level.Investigational
PiretanideIcatibant may decrease the diuretic activities of Piretanide.Experimental
PirfenidoneThe risk or severity of adverse effects can be increased when Pirfenidone is combined with Icatibant.Approved, Investigational
Piromidic acidIcatibant may increase the neuroexcitatory activities of Piromidic acid.Experimental
PiroxicamThe risk or severity of adverse effects can be increased when Piroxicam is combined with Icatibant.Approved, Investigational
PirprofenThe risk or severity of adverse effects can be increased when Icatibant is combined with Pirprofen.Experimental
Platelet Activating FactorIcatibant may decrease the antihypertensive activities of Platelet Activating Factor.Experimental
PlazomicinIcatibant may decrease the excretion rate of Plazomicin which could result in a higher serum level.Investigational
PlicamycinIcatibant may decrease the excretion rate of Plicamycin which could result in a higher serum level.Approved, Investigational, Withdrawn
PolythiazideThe therapeutic efficacy of Polythiazide can be decreased when used in combination with Icatibant.Approved
PractololIcatibant may decrease the antihypertensive activities of Practolol.Approved
PralatrexateThe serum concentration of Pralatrexate can be increased when it is combined with Icatibant.Approved
PranoprofenThe risk or severity of adverse effects can be increased when Icatibant is combined with Pranoprofen.Experimental, Investigational
PrasteroneThe risk or severity of adverse effects can be increased when Icatibant is combined with Prasterone.Approved, Nutraceutical
Prasterone sulfateThe risk or severity of adverse effects can be increased when Icatibant is combined with Prasterone sulfate.Investigational
PrednicarbateThe risk or severity of adverse effects can be increased when Icatibant is combined with Prednicarbate.Approved
PrednisoloneThe risk or severity of adverse effects can be increased when Icatibant is combined with Prednisolone.Approved, Vet Approved
PrednisoneThe risk or severity of adverse effects can be increased when Icatibant is combined with Prednisone.Approved, Vet Approved
PregnenoloneThe risk or severity of adverse effects can be increased when Icatibant is combined with Pregnenolone.Experimental, Investigational
ProbenecidThe serum concentration of Icatibant can be increased when it is combined with Probenecid.Approved
ProglumetacinThe risk or severity of adverse effects can be increased when Icatibant is combined with Proglumetacin.Experimental
PropacetamolThe risk or severity of adverse effects can be increased when Icatibant is combined with Propacetamol.Approved, Investigational
PropranololIcatibant may decrease the antihypertensive activities of Propranolol.Approved, Investigational
PropyphenazoneThe risk or severity of adverse effects can be increased when Icatibant is combined with Propyphenazone.Experimental
ProquazoneThe risk or severity of adverse effects can be increased when Icatibant is combined with Proquazone.Experimental
Prostaglandin B2The therapeutic efficacy of Prostaglandin B2 can be decreased when used in combination with Icatibant.Experimental
Prostaglandin G2The therapeutic efficacy of Prostaglandin G2 can be decreased when used in combination with Icatibant.Experimental
ProstaleneThe therapeutic efficacy of Prostalene can be decreased when used in combination with Icatibant.Vet Approved
Protein CIcatibant may increase the anticoagulant activities of Protein C.Approved
Protein S humanIcatibant may increase the anticoagulant activities of Protein S human.Approved
ProtocatechualdehydeIcatibant may increase the anticoagulant activities of Protocatechualdehyde.Approved
PrulifloxacinIcatibant may increase the neuroexcitatory activities of Prulifloxacin.Investigational
PTC299The risk or severity of adverse effects can be increased when PTC299 is combined with Icatibant.Investigational
PuromycinIcatibant may decrease the excretion rate of Puromycin which could result in a higher serum level.Experimental
QuinaprilIcatibant may decrease the antihypertensive activities of Quinapril.Approved, Investigational
QuinethazoneThe therapeutic efficacy of Quinethazone can be decreased when used in combination with Icatibant.Approved
Rabies virus inactivated antigen, AThe risk or severity of adverse effects can be increased when Icatibant is combined with Rabies virus inactivated antigen, A.Approved
Rabies virus inactivated antigen, AThe therapeutic efficacy of Rabies virus inactivated antigen, A can be decreased when used in combination with Icatibant.Approved
RamiprilIcatibant may decrease the antihypertensive activities of Ramipril.Approved
RescinnamineIcatibant may decrease the antihypertensive activities of Rescinnamine.Approved
ResveratrolThe risk or severity of adverse effects can be increased when Resveratrol is combined with Icatibant.Approved, Experimental, Investigational
ReviparinIcatibant may increase the anticoagulant activities of Reviparin.Approved, Investigational
RibostamycinIcatibant may decrease the excretion rate of Ribostamycin which could result in a higher serum level.Approved, Investigational
RimexoloneThe risk or severity of adverse effects can be increased when Icatibant is combined with Rimexolone.Approved
RindopepimutThe therapeutic efficacy of Rindopepimut can be decreased when used in combination with Icatibant.Investigational
RisedronateThe risk or severity of adverse effects can be increased when Icatibant is combined with Risedronate.Approved, Investigational
RivaroxabanIcatibant may increase the anticoagulant activities of Rivaroxaban.Approved
RofecoxibThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Icatibant.Investigational, Withdrawn
RoflumilastRoflumilast may increase the immunosuppressive activities of Icatibant.Approved
RosoxacinIcatibant may increase the neuroexcitatory activities of Rosoxacin.Approved, Investigational
Rotavirus VaccineThe therapeutic efficacy of Rotavirus Vaccine can be decreased when used in combination with Icatibant.Approved
Rubella virus vaccineThe therapeutic efficacy of Rubella virus vaccine can be decreased when used in combination with Icatibant.Approved
RufloxacinIcatibant may increase the neuroexcitatory activities of Rufloxacin.Experimental
SabarubicinIcatibant may decrease the excretion rate of Sabarubicin which could result in a higher serum level.Investigational
SacubitrilThe risk or severity of adverse effects can be increased when Sacubitril is combined with Icatibant.Approved
SalicylamideThe risk or severity of adverse effects can be increased when Icatibant is combined with Salicylamide.Approved
Salicylic acidThe risk or severity of adverse effects can be increased when Salicylic acid is combined with Icatibant.Approved, Vet Approved
Salmonella typhi ty21a live antigenThe therapeutic efficacy of Salmonella typhi ty21a live antigen can be decreased when used in combination with Icatibant.Approved
SalsalateThe risk or severity of adverse effects can be increased when Salsalate is combined with Icatibant.Approved
SaprisartanThe risk or severity of adverse effects can be increased when Saprisartan is combined with Icatibant.Experimental
SaralasinThe risk or severity of adverse effects can be increased when Saralasin is combined with Icatibant.Investigational
SemapimodThe risk or severity of adverse effects can be increased when Icatibant is combined with Semapimod.Investigational
SeratrodastThe risk or severity of adverse effects can be increased when Icatibant is combined with Seratrodast.Approved
SerrapeptaseThe risk or severity of adverse effects can be increased when Icatibant is combined with Serrapeptase.Investigational
Sipuleucel-TThe therapeutic efficacy of Sipuleucel-T can be decreased when used in combination with Icatibant.Approved
SisomicinIcatibant may decrease the excretion rate of Sisomicin which could result in a higher serum level.Investigational
SitafloxacinIcatibant may increase the neuroexcitatory activities of Sitafloxacin.Experimental, Investigational
Sodium phosphateSodium phosphate may increase the nephrotoxic activities of Icatibant.Approved
SotalolIcatibant may decrease the antihypertensive activities of Sotalol.Approved
SP1049CIcatibant may decrease the excretion rate of SP1049C which could result in a higher serum level.Investigational
SparfloxacinIcatibant may increase the neuroexcitatory activities of Sparfloxacin.Approved, Investigational
SpectinomycinIcatibant may decrease the excretion rate of Spectinomycin which could result in a higher serum level.Approved, Investigational, Vet Approved
SpiraprilIcatibant may decrease the antihypertensive activities of Spirapril.Approved
SpironolactoneIcatibant may decrease the antihypertensive activities of Spironolactone.Approved
SRP 299The therapeutic efficacy of SRP 299 can be decreased when used in combination with Icatibant.Investigational
SRT501The risk or severity of adverse effects can be increased when SRT501 is combined with Icatibant.Investigational
StreptomycinIcatibant may decrease the excretion rate of Streptomycin which could result in a higher serum level.Approved, Vet Approved
StreptozocinIcatibant may decrease the excretion rate of Streptozocin which could result in a higher serum level.Approved
SulfasalazineThe risk or severity of adverse effects can be increased when Sulfasalazine is combined with Icatibant.Approved
SulindacThe risk or severity of adverse effects can be increased when Sulindac is combined with Icatibant.Approved
SulodexideIcatibant may increase the anticoagulant activities of Sulodexide.Approved, Investigational
SulprostoneThe therapeutic efficacy of Sulprostone can be decreased when used in combination with Icatibant.Investigational
SuprofenThe risk or severity of adverse effects can be increased when Suprofen is combined with Icatibant.Approved, Withdrawn
SuxibuzoneThe risk or severity of adverse effects can be increased when Icatibant is combined with Suxibuzone.Experimental
TacrolimusIcatibant may increase the nephrotoxic activities of Tacrolimus.Approved, Investigational
TafluprostThe therapeutic efficacy of Tafluprost can be decreased when used in combination with Icatibant.Approved
TalinololIcatibant may decrease the antihypertensive activities of Talinolol.Investigational
TalniflumateThe risk or severity of adverse effects can be increased when Talniflumate is combined with Icatibant.Approved
TarenflurbilThe risk or severity of adverse effects can be increased when Tarenflurbil is combined with Icatibant.Investigational
TasosartanThe risk or severity of adverse effects can be increased when Tasosartan is combined with Icatibant.Approved
TecemotideThe therapeutic efficacy of Tecemotide can be decreased when used in combination with Icatibant.Investigational
Technetium Tc-99m etidronateThe risk or severity of adverse effects can be increased when Icatibant is combined with Technetium Tc-99m etidronate.Approved
Technetium Tc-99m medronateThe risk or severity of adverse effects can be increased when Icatibant is combined with Technetium Tc-99m medronate.Approved
TelmisartanThe risk or severity of adverse effects can be increased when Telmisartan is combined with Icatibant.Approved, Investigational
TemafloxacinIcatibant may increase the neuroexcitatory activities of Temafloxacin.Withdrawn
TemocaprilIcatibant may decrease the antihypertensive activities of Temocapril.Experimental, Investigational
TenidapThe risk or severity of adverse effects can be increased when Icatibant is combined with Tenidap.Experimental
Tenofovir disoproxilThe risk or severity of adverse effects can be increased when Icatibant is combined with Tenofovir disoproxil.Approved, Investigational
TenoxicamThe risk or severity of adverse effects can be increased when Tenoxicam is combined with Icatibant.Approved
TepoxalinThe risk or severity of adverse effects can be increased when Icatibant is combined with Tepoxalin.Vet Approved
TeriflunomideThe risk or severity of adverse effects can be increased when Icatibant is combined with Teriflunomide.Approved
TertatololIcatibant may decrease the antihypertensive activities of Tertatolol.Experimental
TG4010The therapeutic efficacy of TG4010 can be decreased when used in combination with Icatibant.Investigational
Tiaprofenic acidThe risk or severity of adverse effects can be increased when Tiaprofenic acid is combined with Icatibant.Approved
Tiludronic acidThe risk or severity of adverse effects can be increased when Icatibant is combined with Tiludronic acid.Approved, Investigational, Vet Approved
TimololIcatibant may decrease the antihypertensive activities of Timolol.Approved
TinoridineThe risk or severity of adverse effects can be increased when Icatibant is combined with Tinoridine.Investigational
TixocortolThe risk or severity of adverse effects can be increased when Icatibant is combined with Tixocortol.Approved
TobramycinIcatibant may decrease the excretion rate of Tobramycin which could result in a higher serum level.Approved, Investigational
TofacitinibIcatibant may increase the immunosuppressive activities of Tofacitinib.Approved, Investigational
Tolfenamic AcidThe risk or severity of adverse effects can be increased when Icatibant is combined with Tolfenamic Acid.Approved
TolmetinThe risk or severity of adverse effects can be increased when Tolmetin is combined with Icatibant.Approved
TorasemideIcatibant may decrease the diuretic activities of Torasemide.Approved
TrandolaprilIcatibant may decrease the antihypertensive activities of Trandolapril.Approved
TranilastThe risk or severity of adverse effects can be increased when Icatibant is combined with Tranilast.Approved, Investigational
TrastuzumabTrastuzumab may increase the neutropenic activities of Icatibant.Approved, Investigational
TravoprostThe therapeutic efficacy of Travoprost can be decreased when used in combination with Icatibant.Approved
TreprostinilThe risk or severity of adverse effects can be increased when Treprostinil is combined with Icatibant.Approved, Investigational
TriamcinoloneThe risk or severity of adverse effects can be increased when Icatibant is combined with Triamcinolone.Approved, Vet Approved
TriamtereneIcatibant may decrease the antihypertensive activities of Triamterene.Approved
TribenosideThe risk or severity of adverse effects can be increased when Icatibant is combined with Tribenoside.Experimental
TrichlormethiazideThe therapeutic efficacy of Trichlormethiazide can be decreased when used in combination with Icatibant.Approved, Vet Approved
TriptolideThe risk or severity of adverse effects can be increased when Icatibant is combined with Triptolide.Investigational
TrovafloxacinIcatibant may increase the neuroexcitatory activities of Trovafloxacin.Approved, Investigational, Withdrawn
TroxerutinIcatibant may increase the anticoagulant activities of Troxerutin.Investigational
UlobetasolThe risk or severity of adverse effects can be increased when Icatibant is combined with Ulobetasol.Approved
UnoprostoneThe therapeutic efficacy of Unoprostone can be decreased when used in combination with Icatibant.Approved
ValdecoxibThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Icatibant.Investigational, Withdrawn
ValrubicinIcatibant may decrease the excretion rate of Valrubicin which could result in a higher serum level.Approved
ValsartanThe risk or severity of adverse effects can be increased when Valsartan is combined with Icatibant.Approved, Investigational
VancomycinThe serum concentration of Vancomycin can be increased when it is combined with Icatibant.Approved
WarfarinIcatibant may increase the anticoagulant activities of Warfarin.Approved
XimelagatranIcatibant may increase the anticoagulant activities of Ximelagatran.Approved, Investigational, Withdrawn
Yellow fever vaccineThe therapeutic efficacy of Yellow fever vaccine can be decreased when used in combination with Icatibant.Approved
ZaltoprofenThe risk or severity of adverse effects can be increased when Icatibant is combined with Zaltoprofen.Approved, Investigational
ZileutonThe risk or severity of adverse effects can be increased when Zileuton is combined with Icatibant.Approved, Investigational, Withdrawn
ZofenoprilIcatibant may decrease the antihypertensive activities of Zofenopril.Experimental
Zoledronic acidThe risk or severity of adverse effects can be increased when Icatibant is combined with Zoledronic acid.Approved
ZomepiracThe risk or severity of adverse effects can be increased when Zomepirac is combined with Icatibant.Withdrawn
Zoptarelin doxorubicinIcatibant may decrease the excretion rate of Zoptarelin doxorubicin which could result in a higher serum level.Investigational
ZorubicinIcatibant may decrease the excretion rate of Zorubicin which could result in a higher serum level.Experimental
Zoster vaccineThe therapeutic efficacy of Zoster vaccine can be decreased when used in combination with Icatibant.Approved
Food Interactions
Not Available

References

General References
  1. Cockcroft JR, Chowienczyk PJ, Brett SE, Bender N, Ritter JM: Inhibition of bradykinin-induced vasodilation in human forearm vasculature by icatibant, a potent B2-receptor antagonist. Br J Clin Pharmacol. 1994 Oct;38(4):317-21. [PubMed:7833220]
  2. Bork K, Frank J, Grundt B, Schlattmann P, Nussberger J, Kreuz W: Treatment of acute edema attacks in hereditary angioedema with a bradykinin receptor-2 antagonist (Icatibant). J Allergy Clin Immunol. 2007 Jun;119(6):1497-503. Epub 2007 Apr 5. [PubMed:17418383]
External Links
Human Metabolome Database
HMDB15624
KEGG Drug
D04492
PubChem Compound
71364
PubChem Substance
99443237
ChemSpider
64461
BindingDB
50142947
ChEBI
68564
ChEMBL
CHEMBL2028850
Therapeutic Targets Database
DCL000131
PharmGKB
PA164749185
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Icatibant
ATC Codes
B06AC02 — Icatibant
AHFS Codes
  • 92:32.00 — Complement Inhibitors
FDA label
Download (543 KB)
MSDS
Download (87.6 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedTreatmentHereditary Angioedema (HAE)1
1TerminatedTreatmentAngioneurotic Edema1
2Active Not RecruitingPreventionHemodialysis-Induced Symptom / Mitochondrial Diseases1
2CompletedTreatmentAngioedema1
2, 3CompletedPreventionCardiopulmonary Bypass / Fibrinolysis / General Surgery / Inflammatory Reaction1
3Active Not RecruitingTreatmentHereditary Angioedema / Hereditary Angioedema (HAE)1
3CompletedTreatmentAngioedema1
3CompletedTreatmentAngiotensin Converting Enzyme Inhibitor Induced Angioedema1
3CompletedTreatmentHereditary Angioedema3
4CompletedTreatmentHereditary Angioedema1
4TerminatedTreatmentACE Inhibitor-associated Angioedema1
Not AvailableRecruitingBasic ScienceChronic heart failure with reduced ejection fraction (NYHA Class II) / Chronic heart failure with reduced ejection fraction (NYHA Class III) / NYHA Class I Congestive heart failure1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
Injection, solutionSubcutaneous30 mg/3mL
SolutionSubcutaneous10 mg
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5648333No1999-07-152019-07-15Us

Properties

State
Solid
Experimental Properties
PropertyValueSource
water solubility1 mg/mL MSDS
Predicted Properties
PropertyValueSource
Water Solubility0.057 mg/mLALOGPS
logP-2.3ALOGPS
logP-8ChemAxon
logS-4.4ALOGPS
pKa (Strongest Acidic)3.46ChemAxon
pKa (Strongest Basic)11.45ChemAxon
Physiological Charge3ChemAxon
Hydrogen Acceptor Count23ChemAxon
Hydrogen Donor Count15ChemAxon
Polar Surface Area523.72 Å2ChemAxon
Rotatable Bond Count30ChemAxon
Refractivity332.91 m3·mol-1ChemAxon
Polarizability137.03 Å3ChemAxon
Number of Rings7ChemAxon
Bioavailability0ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.5123
Blood Brain Barrier-0.8713
Caco-2 permeable-0.8198
P-glycoprotein substrateSubstrate0.8421
P-glycoprotein inhibitor INon-inhibitor0.8961
P-glycoprotein inhibitor IINon-inhibitor0.9801
Renal organic cation transporterNon-inhibitor0.6176
CYP450 2C9 substrateNon-substrate0.7753
CYP450 2D6 substrateNon-substrate0.7828
CYP450 3A4 substrateNon-substrate0.5958
CYP450 1A2 substrateNon-inhibitor0.661
CYP450 2C9 inhibitorNon-inhibitor0.8477
CYP450 2D6 inhibitorNon-inhibitor0.876
CYP450 2C19 inhibitorNon-inhibitor0.796
CYP450 3A4 inhibitorNon-inhibitor0.729
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9691
Ames testNon AMES toxic0.6483
CarcinogenicityNon-carcinogens0.8963
BiodegradationNot ready biodegradable0.898
Rat acute toxicity2.4262 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9506
hERG inhibition (predictor II)Inhibitor0.5187
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
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

Taxonomy

Description
This compound belongs to the class of organic compounds known as oligopeptides. These are organic compounds containing a sequence of between three and ten alpha-amino acids joined by peptide bonds.
Kingdom
Organic compounds
Super Class
Organic acids and derivatives
Class
Carboxylic acids and derivatives
Sub Class
Amino acids, peptides, and analogues
Direct Parent
Oligopeptides
Alternative Parents
N-acyl-L-alpha-amino acids / Proline and derivatives / Alpha amino acid amides / Tetrahydroisoquinolines / Indoles and derivatives / N-acylpyrrolidines / Pyrrolidinecarboxamides / Benzenoids / N-acyl amines / Thiophenes
show 17 more
Substituents
Alpha-oligopeptide / Proline or derivatives / N-acyl-alpha-amino acid / N-acyl-alpha amino acid or derivatives / N-acyl-l-alpha-amino acid / Alpha-amino acid amide / N-substituted-alpha-amino acid / Alpha-amino acid or derivatives / Tetrahydroisoquinoline / Indole or derivatives
show 38 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
Not Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Antagonist
General Function
Type 1 angiotensin receptor binding
Specific Function
Receptor for bradykinin. It is associated with G proteins that activate a phosphatidylinositol-calcium second messenger system.
Gene Name
BDKRB2
Uniprot ID
P30411
Uniprot Name
B2 bradykinin receptor
Molecular Weight
44460.15 Da
References
  1. Privitera PJ, Beckstead RM, Yates P, Walgren R: Autoradiographic localization of [125I-Tyr0]bradykinin binding sites in brains of Wistar-Kyoto and spontaneously hypertensive rats. Cell Mol Neurobiol. 2003 Oct;23(4-5):805-15. [PubMed:14514033]
  2. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Zinc ion binding
Specific Function
Broad specificity aminopeptidase. Plays a role in the final digestion of peptides generated from hydrolysis of proteins by gastric and pancreatic proteases. May play a critical role in the pathogen...
Gene Name
ANPEP
Uniprot ID
P15144
Uniprot Name
Aminopeptidase N
Molecular Weight
109538.68 Da
References
  1. Bawolak MT, Fortin JP, Vogel LK, Adam A, Marceau F: The bradykinin B2 receptor antagonist icatibant (Hoe 140) blocks aminopeptidase N at micromolar concentrations: off-target alterations of signaling mediated by the bradykinin B1 and angiotensin receptors. Eur J Pharmacol. 2006 Dec 3;551(1-3):108-11. Epub 2006 Sep 8. [PubMed:17026984]

Drug created on March 19, 2008 10:16 / Updated on November 19, 2017 20:34