Identification

Name
Icatibant
Accession Number
DB06196
Type
Small Molecule
Groups
Approved, Investigational
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][C@]12CC(N(C(=O)C3CC4=CC=CC=C4CN3C(=O)[C@H](CO)NC(=O)[C@H](CC3=CC=CS3)NC(=O)CNC(=O)C3C[C@@H](O)CN3C(=O)C3CCCN3C(=O)C(CCCN=C(N)N)NC(=O)[C@H](N)CCCN=C(N)N)[C@@]1([H])CCCC2)C(=O)N[C@@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.

Associated Conditions
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
(4R)-limoneneThe risk or severity of adverse effects can be increased when Icatibant is combined with (4R)-limonene.Investigational
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, Investigational
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, Experimental, Investigational
AcenocoumarolIcatibant may increase the anticoagulant activities of Acenocoumarol.Approved, Investigational
Acetylsalicylic acidThe risk or severity of adverse effects can be increased when Icatibant is combined with Acetylsalicylic acid.Approved, Vet Approved
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
AmilorideIcatibant may decrease the antihypertensive activities of Amiloride.Approved
Aminosalicylic AcidThe risk or severity of adverse effects can be increased when Icatibant is combined with Aminosalicylic Acid.Approved
AncrodIcatibant may increase the anticoagulant activities of Ancrod.Approved, 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
Anthrax immune globulin humanThe risk or severity of adverse effects can be increased when Icatibant is combined with Anthrax immune globulin human.Approved
AntipyrineThe risk or severity of adverse effects can be increased when Icatibant is combined with Antipyrine.Approved, Investigational
Antithrombin III humanIcatibant may increase the anticoagulant activities of Antithrombin III human.Approved
AntrafenineThe risk or severity of adverse effects can be increased when Icatibant is combined with Antrafenine.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.Investigational
AsenapineIcatibant may decrease the antihypertensive activities of Asenapine.Approved
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
Azficel-TThe risk or severity of adverse effects can be increased when Icatibant is combined with Azficel-T.Approved, Investigational
Azilsartan medoxomilThe risk or severity of adverse effects can be increased when Azilsartan medoxomil is combined with Icatibant.Approved, Investigational
AzosemideThe therapeutic efficacy of Azosemide can be decreased when used in combination with Icatibant.Investigational
Bacillus calmette-guerin substrain connaught live antigenThe risk or severity of adverse effects can be increased when Icatibant is combined with Bacillus calmette-guerin substrain connaught live antigen.Approved, Investigational
Bacillus calmette-guerin substrain tice live antigenThe risk or severity of adverse effects can be increased when Icatibant is combined with Bacillus calmette-guerin substrain tice live antigen.Approved
BalsalazideThe risk or severity of adverse effects can be increased when Icatibant is combined with 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
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
BenzthiazideThe therapeutic efficacy of Benzthiazide can be decreased when used in combination with Icatibant.Approved
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, Investigational
BetrixabanThe risk or severity of bleeding can be increased when Betrixaban is combined with Icatibant.Approved, Investigational
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 Icatibant is combined with Bromfenac.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
BufexamacThe risk or severity of adverse effects can be increased when Icatibant is combined with Bufexamac.Approved, 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
BumetanideThe therapeutic efficacy of Bumetanide can be decreased when used in combination with Icatibant.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
CapsaicinThe risk or severity of adverse effects can be increased when Icatibant is combined with Capsaicin.Approved
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 Icatibant is combined with Carprofen.Approved, Vet Approved, Withdrawn
CarteololIcatibant may decrease the antihypertensive activities of Carteolol.Approved
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 Icatibant is combined with Celecoxib.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, Investigational, Vet Approved
ChlorothiazideThe therapeutic efficacy of Chlorothiazide can be decreased when used in combination with Icatibant.Approved, Vet Approved
ChlorphenesinThe risk or severity of adverse effects can be increased when Icatibant is combined with Chlorphenesin.Approved, Vet Approved, Withdrawn
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, Investigational
Choline magnesium trisalicylateThe risk or severity of adverse effects can be increased when Icatibant is combined with Choline magnesium trisalicylate.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
CimicoxibThe risk or severity of adverse effects can be increased when Icatibant is combined with Cimicoxib.Investigational
CinoxacinIcatibant may increase the neuroexcitatory activities of Cinoxacin.Approved, Investigational, Withdrawn
CisplatinThe risk or severity of adverse effects can be increased when Icatibant is combined with Cisplatin.Approved
ClobetasolThe risk or severity of adverse effects can be increased when Icatibant is combined with Clobetasol.Approved, 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 risk or severity of adverse effects can be increased when Icatibant is combined with Clostridium tetani toxoid antigen (formaldehyde inactivated).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, Investigational
Corynebacterium diphtheriae toxoid antigen (formaldehyde inactivated)The risk or severity of adverse effects can be increased when Icatibant is combined with Corynebacterium diphtheriae toxoid antigen (formaldehyde inactivated).Approved
CurcuminThe risk or severity of adverse effects can be increased when Icatibant is combined with Curcumin.Approved, Investigational
CyclopenthiazideThe therapeutic efficacy of Cyclopenthiazide can be decreased when used in combination with Icatibant.Experimental
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
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, Investigational
DelaprilIcatibant may decrease the antihypertensive activities of Delapril.Investigational
DenosumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Icatibant.Approved
DesipramineIcatibant may decrease the antihypertensive activities of Desipramine.Approved, Investigational
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
Dexamethasone isonicotinateThe risk or severity of adverse effects can be increased when Icatibant is combined with Dexamethasone isonicotinate.Vet Approved
DexibuprofenThe risk or severity of adverse effects can be increased when Icatibant is combined with Dexibuprofen.Approved, Investigational
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, Investigational, Vet Approved
DibekacinIcatibant may decrease the excretion rate of Dibekacin which could result in a higher serum level.Experimental
Dibotermin alfaThe risk or severity of adverse effects can be increased when Icatibant is combined with Dibotermin alfa.Approved, Investigational
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 Icatibant is combined with Diflunisal.Approved, Investigational
DifluocortoloneThe risk or severity of adverse effects can be increased when Icatibant is combined with Difluocortolone.Approved, Investigational, Withdrawn
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
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.Withdrawn
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
EpitizideThe therapeutic efficacy of Epitizide can be decreased when used in combination with Icatibant.Experimental
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
EsatenololIcatibant may decrease the antihypertensive activities of Esatenolol.Experimental
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 acidThe therapeutic efficacy of Etacrynic acid can be decreased when used in combination with Icatibant.Approved, Investigational
EtanerceptThe risk or severity of adverse effects can be increased when Icatibant is combined with Etanercept.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 Icatibant is combined with Etodolac.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 Icatibant is combined with Etoricoxib.Approved, Investigational
Evening primrose oilThe risk or severity of adverse effects can be increased when Icatibant is combined with Evening primrose oil.Investigational, Nutraceutical
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 Icatibant is combined with Fenoprofen.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, Investigational
FluindioneIcatibant may increase the anticoagulant activities of Fluindione.Approved, 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, Investigational
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 Icatibant is combined with Flurbiprofen.Approved, Investigational
FluticasoneThe risk or severity of adverse effects can be increased when Icatibant is combined with Fluticasone.Approved, Experimental, Investigational
Fluticasone furoateThe risk or severity of adverse effects can be increased when Icatibant is combined with Fluticasone furoate.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 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
G17DTThe risk or severity of adverse effects can be increased when Icatibant is combined with G17DT.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 risk or severity of adverse effects can be increased when Icatibant is combined with GI-5005.Investigational
GinsengThe risk or severity of adverse effects can be increased when Icatibant is combined with Ginseng.Approved, Investigational, Nutraceutical
GrepafloxacinIcatibant may increase the neuroexcitatory activities of Grepafloxacin.Approved, 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 risk or severity of adverse effects can be increased when Icatibant is combined with Hepatitis A Vaccine.Approved
Hepatitis B Vaccine (Recombinant)The risk or severity of adverse effects can be increased when Icatibant is combined with Hepatitis B Vaccine (Recombinant).Approved, Withdrawn
HigenamineThe risk or severity of adverse effects can be increased when Icatibant is combined with Higenamine.Investigational
Human rabies virus immune globulinThe risk or severity of adverse effects can be increased when Icatibant is combined with Human rabies virus immune globulin.Approved
HydralazineIcatibant may decrease the antihypertensive activities of Hydralazine.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
IbuproxamThe risk or severity of adverse effects can be increased when Icatibant is combined with Ibuproxam.Withdrawn
IcosapentThe risk or severity of adverse effects can be increased when Icatibant is combined with Icosapent.Approved, Nutraceutical
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 Icatibant is combined with Indomethacin.Approved, Investigational
IndoprofenThe risk or severity of adverse effects can be increased when Icatibant is combined with Indoprofen.Withdrawn
INGN 201The risk or severity of adverse effects can be increased when Icatibant is combined with INGN 201.Investigational
INGN 225The risk or severity of adverse effects can be increased when Icatibant is combined with INGN 225.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
Japanese encephalitis virus strain sa 14-14-2 antigen (formaldehyde inactivated)The risk or severity of adverse effects can be increased when Icatibant is combined with Japanese encephalitis virus strain sa 14-14-2 antigen (formaldehyde inactivated).Approved
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 Icatibant is combined with Ketoprofen.Approved, Vet Approved
LandiololIcatibant may decrease the antihypertensive activities of Landiolol.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
LevobetaxololIcatibant may decrease the antihypertensive activities of Levobetaxolol.Approved, 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
Lithium cationThe serum concentration of Lithium can be increased when it is combined with Icatibant.Experimental
LomefloxacinIcatibant may increase the neuroexcitatory activities of Lomefloxacin.Approved, Investigational
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
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 Icatibant is combined with Lumiracoxib.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 Icatibant is combined with Magnesium salicylate.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 Icatibant is combined with Meclofenamic acid.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 Icatibant is combined with Mefenamic acid.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 Icatibant is combined with Meloxicam.Approved, Vet Approved
MepindololIcatibant may decrease the antihypertensive activities of Mepindolol.Experimental
MesalazineThe risk or severity of adverse effects can be increased when Icatibant is combined with Mesalazine.Approved
MetamizoleThe risk or severity of adverse effects can be increased when Metamizole is combined with Icatibant.Approved, 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
MetipranololIcatibant may decrease the antihypertensive activities of Metipranolol.Approved
MetolazoneThe therapeutic efficacy of Metolazone can be decreased when used in combination with Icatibant.Approved
MicronomicinIcatibant may decrease the excretion rate of Micronomicin which could result in a higher serum level.Experimental
MifamurtideThe therapeutic efficacy of Mifamurtide can be decreased when used in combination with Icatibant.Approved, 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 Icatibant is combined with Nabumetone.Approved
NadololIcatibant may decrease the antihypertensive activities of Nadolol.Approved
NadroparinIcatibant may increase the anticoagulant activities of Nadroparin.Approved, Investigational
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
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
NepafenacThe risk or severity of adverse effects can be increased when Icatibant is combined with Nepafenac.Approved, Investigational
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 Icatibant is combined with Niflumic Acid.Approved
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
OcrelizumabOcrelizumab may increase the immunosuppressive activities of Icatibant.Approved, Investigational
OfloxacinIcatibant may increase the neuroexcitatory activities of Ofloxacin.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 bleeding can be increased when Icatibant is combined with Omacetaxine mepesuccinate.Approved, Investigational
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 Icatibant is combined with Oxaprozin.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
PalmidrolThe risk or severity of adverse effects can be increased when Icatibant is combined with Palmidrol.Experimental, Nutraceutical
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
ParthenolideThe risk or severity of adverse effects can be increased when Icatibant is combined with Parthenolide.Approved, 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 Icatibant is combined with Phenylbutazone.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, Investigational
Pipemidic acidIcatibant may increase the neuroexcitatory activities of Pipemidic acid.Experimental
PiretanideThe therapeutic efficacy of Piretanide can be decreased when used in combination with Icatibant.Approved
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 Icatibant is combined with Piroxicam.Approved, Investigational
PirprofenThe risk or severity of adverse effects can be increased when Icatibant is combined with Pirprofen.Experimental
PitolisantThe risk or severity of adverse effects can be increased when Icatibant is combined with Pitolisant.Approved, Investigational
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.Approved, Investigational
PolythiazideThe therapeutic efficacy of Polythiazide can be decreased when used in combination with Icatibant.Approved
PomalidomideThe risk or severity of adverse effects can be increased when Icatibant is combined with Pomalidomide.Approved
Potassium CitrateIcatibant may increase the anticoagulant activities of Potassium Citrate.Approved, Investigational, Vet 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, Investigational
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, Investigational, 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, Investigational
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.Approved, Experimental, Investigational
ProbenecidThe serum concentration of Icatibant can be increased when it is combined with Probenecid.Approved, Investigational
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
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, Investigational
Rabies virus inactivated antigen, AThe therapeutic efficacy of Rabies virus inactivated antigen, A can be decreased when used in combination with Icatibant.Approved, Investigational
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 Icatibant is combined with Resveratrol.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 risk or severity of adverse effects can be increased when Icatibant is combined with Rindopepimut.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 Icatibant is combined with Rofecoxib.Approved, Investigational, Withdrawn
RoflumilastRoflumilast may increase the immunosuppressive activities of Icatibant.Approved
RosoxacinIcatibant may increase the neuroexcitatory activities of Rosoxacin.Approved, Investigational
Rotavirus VaccineThe risk or severity of adverse effects can be increased when Icatibant is combined with Rotavirus Vaccine.Approved
Rubella virus vaccineThe risk or severity of adverse effects can be increased when Icatibant is combined with Rubella virus vaccine.Approved, Investigational
RufloxacinIcatibant may increase the neuroexcitatory activities of Rufloxacin.Experimental
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
Salmonella typhi ty2 vi polysaccharide antigenThe risk or severity of adverse effects can be increased when Icatibant is combined with Salmonella typhi ty2 vi polysaccharide antigen.Approved
Salmonella typhi Ty21a live antigenThe risk or severity of adverse effects can be increased when Icatibant is combined with Salmonella typhi ty21a live antigen.Approved
SalsalateThe risk or severity of adverse effects can be increased when Icatibant is combined with Salsalate.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
SarilumabSarilumab may increase the immunosuppressive activities of Icatibant.Approved, Investigational
SeliciclibThe risk or severity of adverse effects can be increased when Icatibant is combined with Seliciclib.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
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
SotalolIcatibant may decrease the antihypertensive activities of Sotalol.Approved
SparfloxacinIcatibant may increase the neuroexcitatory activities of Sparfloxacin.Approved, Investigational
SpiraprilIcatibant may decrease the antihypertensive activities of Spirapril.Approved
SRP 299The risk or severity of adverse effects can be increased when Icatibant is combined with SRP 299.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
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 Icatibant is combined with Suprofen.Approved, Withdrawn
SuxibuzoneThe risk or severity of adverse effects can be increased when Icatibant is combined with Suxibuzone.Experimental
TacrolimusTacrolimus may increase the immunosuppressive activities of Icatibant.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 risk or severity of adverse effects can be increased when Icatibant is combined with Tecemotide.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 Icatibant is combined with Tenoxicam.Approved
TepoxalinThe risk or severity of adverse effects can be increased when Icatibant is combined with Tepoxalin.Vet Approved
TerbutalineIcatibant may decrease the antihypertensive activities of Terbutaline.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 risk or severity of adverse effects can be increased when Icatibant is combined with TG4010.Investigational
Tiaprofenic acidThe risk or severity of adverse effects can be increased when Icatibant is combined with Tiaprofenic acid.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, Withdrawn
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
TolmetinThe risk or severity of adverse effects can be increased when Icatibant is combined with Tolmetin.Approved
TorasemideThe therapeutic efficacy of Torasemide can be decreased when used in combination with Icatibant.Approved
TrandolaprilIcatibant may decrease the antihypertensive activities of Trandolapril.Approved
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
Typhoid VaccineThe risk or severity of adverse effects can be increased when Icatibant is combined with Typhoid Vaccine.Approved
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, Investigational
ValdecoxibThe risk or severity of adverse effects can be increased when Icatibant is combined with Valdecoxib.Approved, Investigational, Withdrawn
ValsartanThe risk or severity of adverse effects can be increased when Valsartan is combined with Icatibant.Approved, Investigational
Varicella Zoster Vaccine (Live/Attenuated)The risk or severity of adverse effects can be increased when Icatibant is combined with Varicella Zoster Vaccine (Live/Attenuated).Approved
WarfarinIcatibant may increase the anticoagulant activities of Warfarin.Approved
XimelagatranIcatibant may increase the anticoagulant activities of Ximelagatran.Approved, Investigational, Withdrawn
Yellow Fever VaccineThe risk or severity of adverse effects can be increased when Icatibant is combined with Yellow Fever Vaccine.Approved, Investigational
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
ZomepiracThe risk or severity of adverse effects can be increased when Zomepirac is combined with Icatibant.Withdrawn
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
HMDB0015624
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
2WithdrawnBasic 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
2, 3CompletedPreventionCardiopulmonary Bypass / Fibrinolysis / General Surgery / Inflammatory Reaction1
3CompletedTreatmentAngioedema1
3CompletedTreatmentAngiotensin Converting Enzyme Inhibitor Induced Angioedema1
3CompletedTreatmentHereditary Angioedema3
3CompletedTreatmentHereditary Angioedema / Hereditary Angioedema (HAE)1
4CompletedTreatmentHereditary Angioedema1
4TerminatedTreatmentACE Inhibitor-associated Angioedema1

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 August 15, 2018 09:53