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Identification
NameIloperidone
Accession NumberDB04946
TypeSmall Molecule
GroupsApproved
Description

Iloperidone is an atypical antipsychotic for the treatment of schizophrenia symptoms. Hoechst Marion Roussel Inc. made initial inquiries into the drug; however, in May 1996, they discontinued research, and in June 1997 gave research rights to Titan Pharmaceuticals. Titan then handed over worldwide development, manufacturing and marketing rights to Novartis in August 1998. On June 9, 2004, Titan Pharmaceuticals announced that the Phase III development rights have been acquired by Vanda Pharmaceuticals. FDA approved on May 9, 2009.

Structure
Thumb
Synonyms
1-[4-[3-[4-(6-Fluoro-1,2-benzisoxazol-3-yl)-1- piperidinyl]propoxy]-3-methoxyphenyl]ethanone
4'-(3-(4-(6-Fluoro-1,2-benzisoxazol-3-yl)piperidino)propoxy)-3'-methoxyacetophenone
Fanapt
Fanapta
HP 873
Iloperidona
Iloperidonum
Zomaril
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Fanapttablet4 mg/1oralVanda Pharmaceuticals Inc.2015-12-15Not applicableUs
Fanapttablet1 mg/1oralNovartis Pharmaceuticals Corporation2009-10-01Not applicableUs
FanaptkitoralNovartis Pharmaceuticals Corporation2009-10-01Not applicableUs
Fanapttablet12 mg/1oralNovartis Pharmaceuticals Corporation2009-10-01Not applicableUs
Fanapttablet10 mg/1oralNovartis Pharmaceuticals Corporation2009-10-01Not applicableUs
Fanapttablet8 mg/1oralNovartis Pharmaceuticals Corporation2009-10-01Not applicableUs
Fanapttablet10 mg/1oralVanda Pharmaceuticals Inc.2016-01-15Not applicableUs
Fanapttablet6 mg/1oralNovartis Pharmaceuticals Corporation2009-10-01Not applicableUs
FanaptkitoralVanda Pharmaceuticals Inc.2015-12-01Not applicableUs
Fanapttablet4 mg/1oralNovartis Pharmaceuticals Corporation2009-10-01Not applicableUs
Fanapttablet8 mg/1oralVanda Pharmaceuticals Inc.2015-09-15Not applicableUs
Fanapttablet2 mg/1oralNovartis Pharmaceuticals Corporation2009-10-01Not applicableUs
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
FiaptaNot Available
ZomarilNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIVPO7KJ050N
CAS number133454-47-4
WeightAverage: 426.4806
Monoisotopic: 426.195485567
Chemical FormulaC24H27FN2O4
InChI KeyInChIKey=XMXHEBAFVSFQEX-UHFFFAOYSA-N
InChI
InChI=1S/C24H27FN2O4/c1-16(28)18-4-7-21(23(14-18)29-2)30-13-3-10-27-11-8-17(9-12-27)24-20-6-5-19(25)15-22(20)31-26-24/h4-7,14-15,17H,3,8-13H2,1-2H3
IUPAC Name
1-(4-{3-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]propoxy}-3-methoxyphenyl)ethan-1-one
SMILES
COC1=C(OCCCN2CCC(CC2)C2=NOC3=C2C=CC(F)=C3)C=CC(=C1)C(C)=O
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as benzisoxazoles. These are aromatic compounds containing a benzene ring fused to an isoxazole ring. Isoxazole is five-membered ring with three carbon atoms, and an oxygen atom next to a nitrogen atom.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassBenzisoxazoles
Sub ClassNot Available
Direct ParentBenzisoxazoles
Alternative Parents
Substituents
  • Benzisoxazole
  • Acetophenone
  • Methoxybenzene
  • Aryl alkyl ketone
  • Aryl ketone
  • Phenol ether
  • Benzoyl
  • Anisole
  • Aralkylamine
  • Fluorobenzene
  • Alkyl aryl ether
  • Benzenoid
  • Piperidine
  • Monocyclic benzene moiety
  • Aryl halide
  • Aryl fluoride
  • Heteroaromatic compound
  • Oxazole
  • Isoxazole
  • Azole
  • Tertiary aliphatic amine
  • Tertiary amine
  • Ketone
  • Oxacycle
  • Azacycle
  • Ether
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Organofluoride
  • Organohalogen compound
  • Carbonyl group
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationTreatment of acute schizophrenia.
PharmacodynamicsIloperidone shows high affinity and maximal receptor occupancy for dopamine D2 receptors in the caudate nucleus and putamen of the brains of schizophrenic patients. The improvement in cognition is attributed to iloperidone's high affinity for α adrenergic receptors. Iloperidone also binds with high affinity to serotonin 5-HT2a and dopamine 3 receptors. Iloperidone binds with moderate affinity to dopamine D4, serotonin 5-HT6 and 5-HT7, and norepinephrine NEα1 receptors. Furthermore, iloperidone binds with weak affinity to serotonin 5-HT1A, dopamine D1, and histamine H1 receptors.
Mechanism of actionIloperidone is a dopamine D2 and 5-HT2A receptor antagonist and acts as a neuroleptic agent.
Related Articles
AbsorptionWell absorbed from the GI tract and Cmax is reached within 2-4 hours. Steady-state concentration is achieved in 3-4 days post-administration of iloperidone. Relative bioavailability of the tablet formulation compared to oral solution is 96%. Accumulation occurs in a predictable fashion.
Volume of distribution

Apparent Vd = 1340-2800 L

Protein binding95% of iloperidone is bound to protein. Percent bound is not altered by renal or hepatic impairment or combination therapy with ketoconazole.
Metabolism

Iloperidone is hepatically metabolized by cytochrome enzymes which mediates O-dealkylation (CYP3A4), hydroxylation (CYP2D6), and decarboxylation/reduction processes. Metabolites formed are P89, P95, and P88. The minor metabolite is P89, whereas P95 and P88 are the major ones. The affinity of the iloperidone metabolite P88 is generally equal or less than that of the parent compound. In contrast, the metabolite P95 only shows affinity for 5-HT2A (Ki value of 3.91) and the NEα1A, NEα1B, NEα1D, and NEα2C receptors (Ki values of 4.7, 2.7, 8.8 and 4.7 nM respectively).

Route of eliminationRenal (in which <1% of iloperidone is excreted unchanged).
Half lifeThe observed mean elimination half-lives for iloperidone, P88 and P95 in CYP2D6 extensive metabolizers (EM) are 18, 26 and 23 hours, respectively, and in poor metabolizers (PM) are 33, 37 and 31 hours, respectively.
Clearance

Apparent clearance (clearance/bioavilability) = 47-102 L/h.

ToxicityCommonly observed adverse reactions (incidence ≥5% and two-fold greater than placebo) were: dizziness, dry mouth, fatigue, nasal congestion, orthostatic hypotension, somnolence, tachycardia, and weight increased.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.9848
Caco-2 permeable+0.5513
P-glycoprotein substrateSubstrate0.6668
P-glycoprotein inhibitor IInhibitor0.8242
P-glycoprotein inhibitor IIInhibitor0.9268
Renal organic cation transporterInhibitor0.5726
CYP450 2C9 substrateNon-substrate0.9051
CYP450 2D6 substrateSubstrate0.892
CYP450 3A4 substrateSubstrate0.7409
CYP450 1A2 substrateNon-inhibitor0.6111
CYP450 2C9 inhibitorNon-inhibitor0.5061
CYP450 2D6 inhibitorNon-inhibitor0.886
CYP450 2C19 inhibitorInhibitor0.6257
CYP450 3A4 inhibitorInhibitor0.6777
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.9008
Ames testNon AMES toxic0.6314
CarcinogenicityNon-carcinogens0.8699
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.7862 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.6563
hERG inhibition (predictor II)Inhibitor0.7945
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
Kitoral
Tabletoral1 mg/1
Tabletoral10 mg/1
Tabletoral12 mg/1
Tabletoral2 mg/1
Tabletoral4 mg/1
Tabletoral6 mg/1
Tabletoral8 mg/1
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US8586610 No2007-11-022027-11-02Us
US8652776 No2010-08-312030-08-31Us
US8999638 No2010-10-282030-10-28Us
US9072742 No2011-01-162031-01-16Us
US9074254 No2011-12-282031-12-28Us
US9074255 No2010-12-172030-12-17Us
US9074256 No2011-02-102031-02-10Us
US9138432 No2005-09-302025-09-30Us
US9157121 No2010-04-052030-04-05Us
USRE39198 No1996-11-152016-11-15Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
water solubilityInsoluble FDA label
Predicted Properties
PropertyValueSource
Water Solubility0.0304 mg/mLALOGPS
logP4.26ALOGPS
logP3.22ChemAxon
logS-4.2ALOGPS
pKa (Strongest Acidic)16.14ChemAxon
pKa (Strongest Basic)7.91ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area64.8 Å2ChemAxon
Rotatable Bond Count8ChemAxon
Refractivity116.65 m3·mol-1ChemAxon
Polarizability46.51 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

DrugSyn.org

US5364866
General References
  1. Strupczewski JT, Bordeau KJ, Chiang Y, Glamkowski EJ, Conway PG, Corbett R, Hartman HB, Szewczak MR, Wilmot CA, Helsley GC: 3-[[(Aryloxy)alkyl]piperidinyl]-1,2-benzisoxazoles as D2/5-HT2 antagonists with potential atypical antipsychotic activity: antipsychotic profile of iloperidone (HP 873). J Med Chem. 1995 Mar 31;38(7):1119-31. [PubMed:7707315 ]
  2. Kongsamut S, Roehr JE, Cai J, Hartman HB, Weissensee P, Kerman LL, Tang L, Sandrasagra A: Iloperidone binding to human and rat dopamine and 5-HT receptors. Eur J Pharmacol. 1996 Dec 19;317(2-3):417-23. [PubMed:8997630 ]
  3. Hesselink JM: Iloperidone (Novartis). IDrugs. 2002 Jan;5(1):84-90. [PubMed:12861482 ]
  4. Hesselink JM: Iloperidone (Hoechst Marion Roussel Inc). IDrugs. 1999 Jun;2(6):584-90. [PubMed:16127622 ]
  5. Szewczak MR, Corbett R, Rush DK, Wilmot CA, Conway PG, Strupczewski JT, Cornfeldt M: The pharmacological profile of iloperidone, a novel atypical antipsychotic agent. J Pharmacol Exp Ther. 1995 Sep;274(3):1404-13. [PubMed:7562515 ]
  6. Bobo WV: Asenapine, iloperidone and lurasidone: critical appraisal of the most recently approved pharmacotherapies for schizophrenia in adults. Expert Rev Clin Pharmacol. 2013 Jan;6(1):61-91. doi: 10.1586/ecp.12.70. [PubMed:23272794 ]
  7. Citrome L: Iloperidone: chemistry, pharmacodynamics, pharmacokinetics and metabolism, clinical efficacy, safety and tolerability, regulatory affairs, and an opinion. Expert Opin Drug Metab Toxicol. 2010 Dec;6(12):1551-64. doi: 10.1517/17425255.2010.531259. Epub 2010 Nov 1. [PubMed:21034370 ]
External Links
ATC CodesN05AX14
AHFS Codes
  • 28:16.08.04
PDB EntriesNot Available
FDA labelDownload (352 KB)
MSDSDownload (480 KB)
Interactions
Drug Interactions
Drug
AbirateroneThe serum concentration of Iloperidone can be increased when it is combined with Abiraterone.
AcetohexamideThe therapeutic efficacy of Acetohexamide can be decreased when used in combination with Iloperidone.
AlogliptinThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Iloperidone.
AmisulprideThe risk or severity of adverse effects can be increased when Iloperidone is combined with Amisulpride.
AmphetamineIloperidone may decrease the stimulatory activities of Amphetamine.
AtazanavirThe serum concentration of the active metabolites of Iloperidone can be increased when Iloperidone is used in combination with Atazanavir.
AzelastineIloperidone may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
BaclofenThe risk or severity of adverse effects can be increased when Baclofen is combined with Iloperidone.
BoceprevirThe serum concentration of the active metabolites of Iloperidone can be increased when Iloperidone is used in combination with Boceprevir.
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Iloperidone.
BromocriptineThe therapeutic efficacy of Bromocriptine can be decreased when used in combination with Iloperidone.
BuprenorphineIloperidone may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
BupropionThe serum concentration of the active metabolites of Iloperidone can be increased when Iloperidone is used in combination with Bupropion.
CanagliflozinThe therapeutic efficacy of Canagliflozin can be decreased when used in combination with Iloperidone.
CathinoneIloperidone may decrease the stimulatory activities of Cathinone.
ChlorpropamideThe therapeutic efficacy of Chlorpropamide can be decreased when used in combination with Iloperidone.
CinacalcetThe serum concentration of the active metabolites of Iloperidone can be increased when Iloperidone is used in combination with Cinacalcet.
CitalopramCitalopram may increase the QTc-prolonging activities of Iloperidone.
CobicistatThe serum concentration of the active metabolites of Iloperidone can be increased when Iloperidone is used in combination with Cobicistat.
CocaineThe serum concentration of the active metabolites of Iloperidone can be increased when Iloperidone is used in combination with Cocaine.
DarunavirThe serum concentration of the active metabolites of Iloperidone can be increased when Iloperidone is used in combination with Darunavir.
DelavirdineThe serum concentration of the active metabolites of Iloperidone can be increased when Iloperidone is used in combination with Delavirdine.
DofetilideDofetilide may increase the QTc-prolonging activities of Iloperidone.
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Iloperidone.
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Iloperidone.
EthanolIloperidone may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
FlibanserinThe serum concentration of Flibanserin can be increased when it is combined with Iloperidone.
FluoxetineThe serum concentration of the active metabolites of Iloperidone can be increased when Iloperidone is used in combination with Fluoxetine.
FluvoxamineThe risk or severity of adverse effects can be increased when Fluvoxamine is combined with Iloperidone.
GliclazideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Iloperidone.
GlimepirideThe therapeutic efficacy of Glimepiride can be decreased when used in combination with Iloperidone.
GliquidoneThe therapeutic efficacy of Gliquidone can be decreased when used in combination with Iloperidone.
GlyburideThe therapeutic efficacy of Glyburide can be decreased when used in combination with Iloperidone.
GoserelinGoserelin may increase the QTc-prolonging activities of Iloperidone.
HydrocodoneIloperidone may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
IdelalisibThe serum concentration of the active metabolites of Iloperidone can be increased when Iloperidone is used in combination with Idelalisib.
IndinavirThe serum concentration of the active metabolites of Iloperidone can be increased when Iloperidone is used in combination with Indinavir.
Insulin AspartThe therapeutic efficacy of Insulin Aspart can be decreased when used in combination with Iloperidone.
Insulin DetemirThe therapeutic efficacy of Insulin Detemir can be decreased when used in combination with Iloperidone.
Insulin GlargineThe therapeutic efficacy of Insulin Glargine can be decreased when used in combination with Iloperidone.
Insulin GlulisineThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Iloperidone.
Insulin HumanThe therapeutic efficacy of Insulin Regular can be decreased when used in combination with Iloperidone.
Insulin LisproThe therapeutic efficacy of Insulin Lispro can be decreased when used in combination with Iloperidone.
ItraconazoleThe serum concentration of the active metabolites of Iloperidone can be increased when Iloperidone is used in combination with Itraconazole.
IvabradineIvabradine may increase the QTc-prolonging activities of Iloperidone.
KetoconazoleThe serum concentration of the active metabolites of Iloperidone can be increased when Iloperidone is used in combination with Ketoconazole.
LeuprolideLeuprolide may increase the QTc-prolonging activities of Iloperidone.
LinagliptinThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Iloperidone.
LomitapideThe serum concentration of Lomitapide can be increased when it is combined with Iloperidone.
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Iloperidone.
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Iloperidone.
MetforminThe therapeutic efficacy of Metformin can be decreased when used in combination with Iloperidone.
MethotrimeprazineThe serum concentration of the active metabolites of Iloperidone can be increased when Iloperidone is used in combination with Methotrimeprazine.
MethylphenidateThe risk or severity of adverse effects can be increased when Iloperidone is combined with Methylphenidate.
MetoclopramideThe risk or severity of adverse effects can be increased when Metoclopramide is combined with Iloperidone.
MetyrosineIloperidone may increase the sedative activities of Metyrosine.
MifepristoneMifepristone may increase the QTc-prolonging activities of Iloperidone.
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Iloperidone.
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Iloperidone.
NefazodoneThe serum concentration of the active metabolites of Iloperidone can be increased when Iloperidone is used in combination with Nefazodone.
NelfinavirThe serum concentration of the active metabolites of Iloperidone can be increased when Iloperidone is used in combination with Nelfinavir.
NimodipineThe serum concentration of Nimodipine can be increased when it is combined with Iloperidone.
OctreotideOctreotide may increase the QTc-prolonging activities of Iloperidone.
OrphenadrineIloperidone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
ParaldehydeIloperidone may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
ParoxetineThe serum concentration of the active metabolites of Iloperidone can be increased when Iloperidone is used in combination with Paroxetine.
Peginterferon alfa-2bThe serum concentration of Iloperidone can be decreased when it is combined with Peginterferon alfa-2b.
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Iloperidone.
PhenelzinePhenelzine may increase the orthostatic hypotensive activities of Iloperidone.
PimozideThe serum concentration of Pimozide can be increased when it is combined with Iloperidone.
PosaconazoleThe serum concentration of the active metabolites of Iloperidone can be increased when Iloperidone is used in combination with Posaconazole.
QuinagolideThe therapeutic efficacy of Quinagolide can be decreased when used in combination with Iloperidone.
RepaglinideThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Iloperidone.
RitonavirThe serum concentration of the active metabolites of Iloperidone can be increased when Iloperidone is used in combination with Ritonavir.
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Iloperidone.
SaxagliptinThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Iloperidone.
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Iloperidone.
StiripentolThe serum concentration of the active metabolites of Iloperidone can be increased when Iloperidone is used in combination with Stiripentol.
SulpirideThe risk or severity of adverse effects can be increased when Iloperidone is combined with Sulpiride.
SuvorexantIloperidone may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
TacrineTacrine may increase the central neurotoxic activities of Iloperidone.
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Iloperidone.
TelaprevirThe serum concentration of the active metabolites of Iloperidone can be increased when Iloperidone is used in combination with Telaprevir.
TerbinafineThe serum concentration of the active metabolites of Iloperidone can be increased when Iloperidone is used in combination with Terbinafine.
ThalidomideIloperidone may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
TiclopidineThe metabolism of Iloperidone can be decreased when combined with Ticlopidine.
TipranavirThe serum concentration of the active metabolites of Iloperidone can be increased when Iloperidone is used in combination with Tipranavir.
TolbutamideThe therapeutic efficacy of Tolbutamide can be decreased when used in combination with Iloperidone.
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with Iloperidone.
TranylcypromineTranylcypromine may increase the orthostatic hypotensive activities of Iloperidone.
VildagliptinThe therapeutic efficacy of Vildagliptin can be decreased when used in combination with Iloperidone.
VoriconazoleThe serum concentration of the active metabolites of Iloperidone can be increased when Iloperidone is used in combination with Voriconazole.
ZolpidemIloperidone may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Food Interactions
  • Administration of iloperidone with a standard high-fat meal did not significantly affect the Cmax or AUC of iloperidone, P88, or P95, but delayed Tmax by 1 hour for iloperidone, 2 hours for P88 and 6 hours for P95.
  • Can be taken with or without meals

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Virus receptor activity
Specific Function:
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including mescaline, psilocybin, 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI) and lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates...
Gene Name:
HTR2A
Uniprot ID:
P28223
Molecular Weight:
52602.58 Da
References
  1. Kongsamut S, Roehr JE, Cai J, Hartman HB, Weissensee P, Kerman LL, Tang L, Sandrasagra A: Iloperidone binding to human and rat dopamine and 5-HT receptors. Eur J Pharmacol. 1996 Dec 19;317(2-3):417-23. [PubMed:8997630 ]
  2. Hesselink JM: Iloperidone (Novartis). IDrugs. 2002 Jan;5(1):84-90. [PubMed:12861482 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Potassium channel regulator activity
Specific Function:
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase.
Gene Name:
DRD2
Uniprot ID:
P14416
Molecular Weight:
50618.91 Da
References
  1. Kongsamut S, Roehr JE, Cai J, Hartman HB, Weissensee P, Kerman LL, Tang L, Sandrasagra A: Iloperidone binding to human and rat dopamine and 5-HT receptors. Eur J Pharmacol. 1996 Dec 19;317(2-3):417-23. [PubMed:8997630 ]
  2. Hesselink JM: Iloperidone (Novartis). IDrugs. 2002 Jan;5(1):84-90. [PubMed:12861482 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
G-protein coupled amine receptor activity
Specific Function:
Dopamine receptor whose activity is mediated by G proteins which activate adenylyl cyclase.
Gene Name:
DRD1
Uniprot ID:
P21728
Molecular Weight:
49292.765 Da
References
  1. Bobo WV: Asenapine, iloperidone and lurasidone: critical appraisal of the most recently approved pharmacotherapies for schizophrenia in adults. Expert Rev Clin Pharmacol. 2013 Jan;6(1):61-91. doi: 10.1586/ecp.12.70. [PubMed:23272794 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
G-protein coupled amine receptor activity
Specific Function:
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase. Promotes cell proliferation.
Gene Name:
DRD3
Uniprot ID:
P35462
Molecular Weight:
44224.335 Da
References
  1. George M, Amrutheshwar R, Rajkumar RP, Kattimani S, Dkhar SA: Newer antipsychotics and upcoming molecules for schizophrenia. Eur J Clin Pharmacol. 2013 Aug;69(8):1497-509. doi: 10.1007/s00228-013-1498-4. Epub 2013 Apr 2. [PubMed:23545936 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Sh3 domain binding
Specific Function:
Dopamine receptor responsible for neuronal signaling in the mesolimbic system of the brain, an area of the brain that regulates emotion and complex behavior. Its activity is mediated by G proteins which inhibit adenylyl cyclase. Modulates the circadian rhythm of contrast sensitivity by regulating the rhythmic expression of NPAS2 in the retinal ganglion cells (By similarity).
Gene Name:
DRD4
Uniprot ID:
P21917
Molecular Weight:
48359.86 Da
References
  1. Bobo WV: Asenapine, iloperidone and lurasidone: critical appraisal of the most recently approved pharmacotherapies for schizophrenia in adults. Expert Rev Clin Pharmacol. 2013 Jan;6(1):61-91. doi: 10.1586/ecp.12.70. [PubMed:23272794 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Serotonin receptor activity
Specific Function:
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Beta-arrestin family members inhibit signaling via G pro...
Gene Name:
HTR1A
Uniprot ID:
P08908
Molecular Weight:
46106.335 Da
References
  1. Bobo WV: Asenapine, iloperidone and lurasidone: critical appraisal of the most recently approved pharmacotherapies for schizophrenia in adults. Expert Rev Clin Pharmacol. 2013 Jan;6(1):61-91. doi: 10.1586/ecp.12.70. [PubMed:23272794 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Serotonin receptor activity
Specific Function:
This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor is mediated by G proteins that stimulate adenylate cyclase. It has a high affinity for tricyclic psychotropic drugs (By similarity). Controls pyramidal neurons migration during corticogenesis, through...
Gene Name:
HTR6
Uniprot ID:
P50406
Molecular Weight:
46953.625 Da
References
  1. Bobo WV: Asenapine, iloperidone and lurasidone: critical appraisal of the most recently approved pharmacotherapies for schizophrenia in adults. Expert Rev Clin Pharmacol. 2013 Jan;6(1):61-91. doi: 10.1586/ecp.12.70. [PubMed:23272794 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Serotonin receptor activity
Specific Function:
This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor is mediated by G proteins that stimulate adenylate cyclase.
Gene Name:
HTR7
Uniprot ID:
P34969
Molecular Weight:
53554.43 Da
References
  1. Bobo WV: Asenapine, iloperidone and lurasidone: critical appraisal of the most recently approved pharmacotherapies for schizophrenia in adults. Expert Rev Clin Pharmacol. 2013 Jan;6(1):61-91. doi: 10.1586/ecp.12.70. [PubMed:23272794 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Protein heterodimerization activity
Specific Function:
This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) proteins. Nuclear ADRA1A-ADRA1B heterooligomers regulate phenylephrine(PE)-stimulated ERK signaling in cardiac myocytes.
Gene Name:
ADRA1A
Uniprot ID:
P35348
Molecular Weight:
51486.005 Da
References
  1. George M, Amrutheshwar R, Rajkumar RP, Kattimani S, Dkhar SA: Newer antipsychotics and upcoming molecules for schizophrenia. Eur J Clin Pharmacol. 2013 Aug;69(8):1497-509. doi: 10.1007/s00228-013-1498-4. Epub 2013 Apr 2. [PubMed:23545936 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Histamine receptor activity
Specific Function:
In peripheral tissues, the H1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamine release from adrenal medulla, as well as mediating neurotransmission in the central nervous system.
Gene Name:
HRH1
Uniprot ID:
P35367
Molecular Weight:
55783.61 Da
References
  1. Bobo WV: Asenapine, iloperidone and lurasidone: critical appraisal of the most recently approved pharmacotherapies for schizophrenia in adults. Expert Rev Clin Pharmacol. 2013 Jan;6(1):61-91. doi: 10.1586/ecp.12.70. [PubMed:23272794 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Protein homodimerization activity
Specific Function:
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins.
Gene Name:
ADRA2C
Uniprot ID:
P18825
Molecular Weight:
49521.585 Da
References
  1. FDA label

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
Molecular Weight:
55768.94 Da
References
  1. Mutlib AE, Klein JT: Application of liquid chromatography/mass spectrometry in accelerating the identification of human liver cytochrome P450 isoforms involved in the metabolism of iloperidone. J Pharmacol Exp Ther. 1998 Sep;286(3):1285-93. [PubMed:9732390 ]
  2. Citrome L: Iloperidone: chemistry, pharmacodynamics, pharmacokinetics and metabolism, clinical efficacy, safety and tolerability, regulatory affairs, and an opinion. Expert Opin Drug Metab Toxicol. 2010 Dec;6(12):1551-64. doi: 10.1517/17425255.2010.531259. Epub 2010 Nov 1. [PubMed:21034370 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Mutlib AE, Klein JT: Application of liquid chromatography/mass spectrometry in accelerating the identification of human liver cytochrome P450 isoforms involved in the metabolism of iloperidone. J Pharmacol Exp Ther. 1998 Sep;286(3):1285-93. [PubMed:9732390 ]
  2. Citrome L: Iloperidone: chemistry, pharmacodynamics, pharmacokinetics and metabolism, clinical efficacy, safety and tolerability, regulatory affairs, and an opinion. Expert Opin Drug Metab Toxicol. 2010 Dec;6(12):1551-64. doi: 10.1517/17425255.2010.531259. Epub 2010 Nov 1. [PubMed:21034370 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxygen binding
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A5
Uniprot ID:
P20815
Molecular Weight:
57108.065 Da
References
  1. Mutlib AE, Klein JT: Application of liquid chromatography/mass spectrometry in accelerating the identification of human liver cytochrome P450 isoforms involved in the metabolism of iloperidone. J Pharmacol Exp Ther. 1998 Sep;286(3):1285-93. [PubMed:9732390 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxygen binding
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A7
Uniprot ID:
P24462
Molecular Weight:
57525.03 Da
References
  1. Mutlib AE, Klein JT: Application of liquid chromatography/mass spectrometry in accelerating the identification of human liver cytochrome P450 isoforms involved in the metabolism of iloperidone. J Pharmacol Exp Ther. 1998 Sep;286(3):1285-93. [PubMed:9732390 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Metabolizes several precarcinogens, drugs, and solvents to reactive metabolites. Inactivates a number of drugs and xenobiotics and also bioactivates many xenobiotic substrates to their hepatotoxic or carcinogenic forms.
Gene Name:
CYP2E1
Uniprot ID:
P05181
Molecular Weight:
56848.42 Da
References
  1. Mutlib AE, Klein JT: Application of liquid chromatography/mass spectrometry in accelerating the identification of human liver cytochrome P450 isoforms involved in the metabolism of iloperidone. J Pharmacol Exp Ther. 1998 Sep;286(3):1285-93. [PubMed:9732390 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
Molecular Weight:
58293.76 Da
References
  1. Mutlib AE, Klein JT: Application of liquid chromatography/mass spectrometry in accelerating the identification of human liver cytochrome P450 isoforms involved in the metabolism of iloperidone. J Pharmacol Exp Ther. 1998 Sep;286(3):1285-93. [PubMed:9732390 ]
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Drug created on October 21, 2007 16:23 / Updated on May 31, 2016 02:12