Identification

Name
Rolapitant
Accession Number
DB09291
Type
Small Molecule
Groups
Approved, Investigational
Description

Rolapitant is a potent, highly selective, long-acting Neurokinin-1 (NK-1) receptor antagonist approved for the prevention of delayed chemotherapy-induced nausea and vomiting (CINV) in adults. Delayed-phase CINV typically occurs >24 hours after chemotherapy treatment and is principally mediated by Neurokinin-1 and its ligand Substance P, which is released in the gut following chemotherapy administration. Neurokinin-1 is also known as Tachykinin Receptor 1 (TACR1), Neurokinin 1 Receptor (NK1R), and Substance P Receptor (SPR). By blocking Substance P from interacting with NK-1 receptors in the gut and the central nervous system, rolapitant prevents late-phase CINV. Unlike other available NK-1 receptor antagonists, rolapitant is not an inhibitor of Cytochrome P450 enzyme CYP3A4 and has a long elimination half-life, allowing a single dose to prevent both acute and late-phase CINV during the first 120 hours post-chemotherapy.

Structure
Thumb
Synonyms
Not Available
Product Ingredients
IngredientUNIICASInChI Key
Rolapitant hydrochlorideJ7Z9DBN8J0858102-79-1VEWAWEMXVUFANV-PVBCUUEWSA-N
Rolapitant hydrochloride monohydrate57O5S1QSAQ914462-92-3GZQWMYVDLCUBQX-WVZIYJGPSA-N
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
VarubiTablet90 mg/1OralTesaro, Inc.2015-10-07Not applicableUs
VarubiInjection, emulsion1.8 mg/mLIntravenousTesaro, Inc.2017-10-25Not applicableUs
International/Other Brands
Varubi (Tesoro)
Categories
UNII
NLE429IZUC
CAS number
552292-08-7
Weight
Average: 500.485
Monoisotopic: 500.189847063
Chemical Formula
C25H26F6N2O2
InChI Key
FIVSJYGQAIEMOC-ZGNKEGEESA-N
InChI
InChI=1S/C25H26F6N2O2/c1-16(17-11-19(24(26,27)28)13-20(12-17)25(29,30)31)35-15-23(18-5-3-2-4-6-18)10-9-22(14-32-23)8-7-21(34)33-22/h2-6,11-13,16,32H,7-10,14-15H2,1H3,(H,33,34)/t16-,22-,23-/m1/s1
IUPAC Name
(5S,8S)-8-{[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]methyl}-8-phenyl-1,7-diazaspiro[4.5]decan-2-one
SMILES
C[C@@H](OC[C@]1(CC[C@]2(CCC(=O)N2)CN1)C1=CC=CC=C1)C1=CC(=CC(=C1)C(F)(F)F)C(F)(F)F

Pharmacology

Indication

Rolapitant is indicated in combination with other antiemetic agents in adults for the prevention of delayed nausea and vomiting associated with initial and repeat courses of emetogenic cancer chemotherapy, including, but not limited to, highly emetogenic chemotherapy.

Associated Conditions
Pharmacodynamics
Not Available
Mechanism of action

Rolapitant is an orally active, highly selective Neurokinin-1 Receptor (NK1R) antagonist. NK1 receptors are located primarily in the gut and central nervous system and are activated by Substance P following chemotherapy administration. By binding to the NK1 receptor, rolapitant prevents binding of its ligand Substance P, which is released in the gut following chemotherapy administration.

TargetActionsOrganism
ANeurokinin-1 Receptor (NK1R)
antagonist
Human
Absorption

Following administration of rolapitant, plasma concentrations reached peak levels in about 4 hours.

Volume of distribution

460 L

Protein binding

Rolapitant is 99.8% bound to human plasma protein.

Metabolism

Rolapitant is metabolized primarily by Cytochrome P450 enzyme 3A4 (CYP3A4) to its major active and circulating metabolite M19 (C4-pyrrolidine-hydroxylated rolapitant).

Route of elimination

Rolapitant was found to be 14.2% renally excreted and 73% fecally excreted. Of the fecally excreted compounds

Half life

Mean terminal half life ranged from 169 to 183 hours (~7 days).

Clearance

0.96 L/hour

Toxicity

Most common adverse reactions occurring in >3% of patients receiving moderately emetogenic chemotherapy and combinations of anthracycline and cyclophosphamide included decreased appetite, neutropenia, dizziness, dyspepsia, urinary tract infection, stomatitis, and anemia. Most common adverse reactions occurring in patients receiving cisplatin-based highly emetogenic chemotherapy included neutropenia, hiccups, and abdominal pain.

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

Interactions

Drug Interactions
DrugInteractionDrug group
4-MethoxyamphetamineThe metabolism of 4-Methoxyamphetamine can be decreased when combined with Rolapitant.Experimental, Illicit
AbemaciclibThe serum concentration of Abemaciclib can be increased when it is combined with Rolapitant.Approved, Investigational
Acetyl sulfisoxazoleThe metabolism of Rolapitant can be decreased when combined with Acetyl sulfisoxazole.Approved, Vet Approved
AcetylcholineThe metabolism of Acetylcholine can be decreased when combined with Rolapitant.Approved
AfatinibThe serum concentration of Afatinib can be increased when it is combined with Rolapitant.Approved
AjmalineThe metabolism of Ajmaline can be decreased when combined with Rolapitant.Approved, Investigational
AlmotriptanThe metabolism of Almotriptan can be decreased when combined with Rolapitant.Approved, Investigational
AlogliptinThe metabolism of Alogliptin can be decreased when combined with Rolapitant.Approved
AlprenololThe metabolism of Alprenolol can be decreased when combined with Rolapitant.Approved, Withdrawn
AlvocidibThe serum concentration of Alvocidib can be increased when it is combined with Rolapitant.Experimental, Investigational
AminophenazoneThe metabolism of Aminophenazone can be decreased when combined with Rolapitant.Approved, Withdrawn
AmiodaroneThe metabolism of Rolapitant can be decreased when combined with Amiodarone.Approved, Investigational
AmitriptylineThe metabolism of Amitriptyline can be decreased when combined with Rolapitant.Approved
AmoxapineThe metabolism of Amoxapine can be decreased when combined with Rolapitant.Approved
AmphetamineThe metabolism of Amphetamine can be decreased when combined with Rolapitant.Approved, Illicit, Investigational
AmprenavirThe metabolism of Amprenavir can be decreased when combined with Rolapitant.Approved, Investigational
AmsacrineThe metabolism of Amsacrine can be decreased when combined with Rolapitant.Approved, Investigational
AntipyrineThe metabolism of Antipyrine can be decreased when combined with Rolapitant.Approved, Investigational
ApalutamideThe serum concentration of Rolapitant can be decreased when it is combined with Apalutamide.Approved, Investigational
ApixabanThe serum concentration of Apixaban can be increased when it is combined with Rolapitant.Approved
AprepitantThe serum concentration of Rolapitant can be increased when it is combined with Aprepitant.Approved, Investigational
AprindineThe metabolism of Aprindine can be decreased when combined with Rolapitant.Approved
ArformoterolThe metabolism of Arformoterol can be decreased when combined with Rolapitant.Approved, Investigational
AripiprazoleThe serum concentration of Aripiprazole can be increased when it is combined with Rolapitant.Approved, Investigational
ArtemetherThe metabolism of Artemether can be decreased when combined with Rolapitant.Approved
AstemizoleThe metabolism of Astemizole can be decreased when combined with Rolapitant.Approved, Withdrawn
AsunaprevirThe metabolism of Asunaprevir can be decreased when combined with Rolapitant.Approved, Investigational, Withdrawn
AtazanavirThe metabolism of Rolapitant can be decreased when combined with Atazanavir.Approved, Investigational
AtomoxetineThe metabolism of Rolapitant can be decreased when combined with Atomoxetine.Approved
AzelastineThe metabolism of Azelastine can be decreased when combined with Rolapitant.Approved
BaricitinibThe serum concentration of Baricitinib can be increased when it is combined with Rolapitant.Approved, Investigational
BetaxololThe metabolism of Betaxolol can be decreased when combined with Rolapitant.Approved, Investigational
BisoprololThe metabolism of Bisoprolol can be decreased when combined with Rolapitant.Approved
BoceprevirThe metabolism of Rolapitant can be decreased when combined with Boceprevir.Approved, Withdrawn
BortezomibThe metabolism of Rolapitant can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Rolapitant can be decreased when it is combined with Bosentan.Approved, Investigational
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Rolapitant.Approved
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Rolapitant.Approved, Investigational
BrexpiprazoleThe serum concentration of Brexpiprazole can be increased when it is combined with Rolapitant.Approved, Investigational
BrigatinibThe serum concentration of Brigatinib can be increased when it is combined with Rolapitant.Approved, Investigational
BufuralolThe metabolism of Bufuralol can be decreased when combined with Rolapitant.Experimental, Investigational
BupivacaineThe metabolism of Bupivacaine can be decreased when combined with Rolapitant.Approved, Investigational
BuprenorphineThe metabolism of Buprenorphine can be decreased when combined with Rolapitant.Approved, Illicit, Investigational, Vet Approved
BupropionThe metabolism of Bupropion can be decreased when combined with Rolapitant.Approved
BuspironeThe metabolism of Buspirone can be decreased when combined with Rolapitant.Approved, Investigational
CamptothecinThe serum concentration of Camptothecin can be increased when it is combined with Rolapitant.Experimental
CaptoprilThe metabolism of Captopril can be decreased when combined with Rolapitant.Approved
CarbamazepineThe serum concentration of Rolapitant can be decreased when it is combined with Carbamazepine.Approved, Investigational
CarboplatinThe serum concentration of Carboplatin can be increased when it is combined with Rolapitant.Approved
CariprazineThe metabolism of Cariprazine can be decreased when combined with Rolapitant.Approved, Investigational
CarteololThe metabolism of Carteolol can be decreased when combined with Rolapitant.Approved
CarvedilolThe metabolism of Carvedilol can be decreased when combined with Rolapitant.Approved, Investigational
CephalexinThe metabolism of Cephalexin can be decreased when combined with Rolapitant.Approved, Investigational, Vet Approved
CeritinibThe serum concentration of Rolapitant can be increased when it is combined with Ceritinib.Approved
CerivastatinThe serum concentration of Cerivastatin can be increased when it is combined with Rolapitant.Approved, Withdrawn
CevimelineThe metabolism of Cevimeline can be decreased when combined with Rolapitant.Approved
ChlordiazepoxideThe metabolism of Chlordiazepoxide can be decreased when combined with Rolapitant.Approved, Illicit, Investigational
ChloroquineThe metabolism of Chloroquine can be decreased when combined with Rolapitant.Approved, Investigational, Vet Approved
ChlorpromazineThe metabolism of Chlorpromazine can be decreased when combined with Rolapitant.Approved, Investigational, Vet Approved
ChlorzoxazoneThe metabolism of Chlorzoxazone can be decreased when combined with Rolapitant.Approved
CholesterolThe serum concentration of Cholesterol can be increased when it is combined with Rolapitant.Approved, Investigational
CilostazolThe metabolism of Cilostazol can be decreased when combined with Rolapitant.Approved, Investigational
CimetidineThe serum concentration of Cimetidine can be increased when it is combined with Rolapitant.Approved, Investigational
CiprofloxacinThe serum concentration of Ciprofloxacin can be increased when it is combined with Rolapitant.Approved, Investigational
CisplatinThe serum concentration of Cisplatin can be increased when it is combined with Rolapitant.Approved
CitalopramThe metabolism of Citalopram can be decreased when combined with Rolapitant.Approved
CladribineThe serum concentration of Cladribine can be increased when it is combined with Rolapitant.Approved, Investigational
ClarithromycinThe metabolism of Rolapitant can be decreased when combined with Clarithromycin.Approved
ClofarabineThe serum concentration of Clofarabine can be increased when it is combined with Rolapitant.Approved, Investigational
ClomipramineThe metabolism of Clomipramine can be decreased when combined with Rolapitant.Approved, Investigational, Vet Approved
ClonidineThe metabolism of Clonidine can be decreased when combined with Rolapitant.Approved
ClotrimazoleThe metabolism of Rolapitant can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineThe metabolism of Clozapine can be decreased when combined with Rolapitant.Approved
CobicistatThe metabolism of Rolapitant can be decreased when combined with Cobicistat.Approved
CodeineThe therapeutic efficacy of Codeine can be decreased when used in combination with Rolapitant.Approved, Illicit
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Rolapitant.Approved
ConivaptanThe serum concentration of Conivaptan can be increased when it is combined with Rolapitant.Approved, Investigational
Conjugated estrogensThe serum concentration of Conjugated estrogens can be increased when it is combined with Rolapitant.Approved
CopanlisibThe serum concentration of Copanlisib can be increased when it is combined with Rolapitant.Approved, Investigational
CrizotinibThe metabolism of Rolapitant can be decreased when combined with Crizotinib.Approved
CurcuminThe metabolism of Rolapitant can be decreased when combined with Curcumin.Approved, Investigational
CyclobenzaprineThe metabolism of Cyclobenzaprine can be decreased when combined with Rolapitant.Approved
CyclophosphamideThe metabolism of Cyclophosphamide can be decreased when combined with Rolapitant.Approved, Investigational
CyclosporineThe serum concentration of Cyclosporine can be increased when it is combined with Rolapitant.Approved, Investigational, Vet Approved
Dabigatran etexilateThe serum concentration of the active metabolites of Dabigatran etexilate can be increased when Dabigatran etexilate is used in combination with Rolapitant.Approved
DabrafenibThe serum concentration of Rolapitant can be decreased when it is combined with Dabrafenib.Approved, Investigational
DactinomycinThe serum concentration of Dactinomycin can be increased when it is combined with Rolapitant.Approved, Investigational
DapagliflozinThe serum concentration of Dapagliflozin can be increased when it is combined with Rolapitant.Approved
DarifenacinThe metabolism of Darifenacin can be decreased when combined with Rolapitant.Approved, Investigational
DarunavirThe metabolism of Rolapitant can be decreased when combined with Darunavir.Approved
DasabuvirThe metabolism of Dasabuvir can be decreased when combined with Rolapitant.Approved
DasatinibThe serum concentration of Dasatinib can be increased when it is combined with Rolapitant.Approved, Investigational
DaunorubicinThe serum concentration of Daunorubicin can be increased when it is combined with Rolapitant.Approved
DebrisoquinThe metabolism of Debrisoquin can be decreased when combined with Rolapitant.Approved, Investigational
DeferasiroxThe serum concentration of Rolapitant can be decreased when it is combined with Deferasirox.Approved, Investigational
DelafloxacinThe serum concentration of Delafloxacin can be increased when it is combined with Rolapitant.Approved, Investigational
DelavirdineThe metabolism of Rolapitant can be decreased when combined with Delavirdine.Approved
DesipramineThe metabolism of Desipramine can be decreased when combined with Rolapitant.Approved, Investigational
DeutetrabenazineThe metabolism of Deutetrabenazine can be decreased when combined with Rolapitant.Approved, Investigational
DexamethasoneThe serum concentration of Rolapitant can be decreased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
Dexchlorpheniramine maleateThe metabolism of Dexchlorpheniramine maleate can be decreased when combined with Rolapitant.Approved
DexfenfluramineThe metabolism of Dexfenfluramine can be decreased when combined with Rolapitant.Approved, Illicit, Investigational, Withdrawn
DextroamphetamineThe metabolism of Dextroamphetamine can be decreased when combined with Rolapitant.Approved, Illicit
DextromethorphanThe metabolism of Dextromethorphan can be decreased when combined with Rolapitant.Approved
DihydrocodeineThe metabolism of Dihydrocodeine can be decreased when combined with Rolapitant.Approved, Illicit
DihydroergotamineThe metabolism of Rolapitant can be decreased when combined with Dihydroergotamine.Approved, Investigational
DiltiazemThe metabolism of Rolapitant can be decreased when combined with Diltiazem.Approved, Investigational
DocetaxelThe serum concentration of Docetaxel can be increased when it is combined with Rolapitant.Approved, Investigational
DolasetronThe metabolism of Dolasetron can be decreased when combined with Rolapitant.Approved, Investigational
DolutegravirThe serum concentration of Dolutegravir can be increased when it is combined with Rolapitant.Approved
DomperidoneThe metabolism of Domperidone can be decreased when combined with Rolapitant.Approved, Investigational, Vet Approved
DonepezilThe metabolism of Donepezil can be decreased when combined with Rolapitant.Approved
DopamineThe metabolism of Dopamine can be decreased when combined with Rolapitant.Approved
DoxepinThe metabolism of Doxepin can be decreased when combined with Rolapitant.Approved, Investigational
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Rolapitant.Approved, Investigational
DoxycyclineThe metabolism of Rolapitant can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronedaroneThe metabolism of Rolapitant can be decreased when combined with Dronedarone.Approved
DuloxetineThe metabolism of Duloxetine can be decreased when combined with Rolapitant.Approved
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Rolapitant.Approved
EletriptanThe metabolism of Eletriptan can be decreased when combined with Rolapitant.Approved, Investigational
EliglustatThe serum concentration of Eliglustat can be increased when it is combined with Rolapitant.Approved
EnasidenibThe serum concentration of Enasidenib can be increased when it is combined with Rolapitant.Approved, Investigational
EncainideThe metabolism of Encainide can be decreased when combined with Rolapitant.Approved, Investigational, Withdrawn
EnclomipheneThe metabolism of Enclomiphene can be decreased when combined with Rolapitant.Investigational
EnzalutamideThe serum concentration of Rolapitant can be decreased when it is combined with Enzalutamide.Approved
EpinastineThe metabolism of Epinastine can be decreased when combined with Rolapitant.Approved, Investigational
ErlotinibThe metabolism of Erlotinib can be decreased when combined with Rolapitant.Approved, Investigational
ErtugliflozinThe serum concentration of Ertugliflozin can be increased when it is combined with Rolapitant.Approved, Investigational
ErythromycinThe metabolism of Rolapitant can be decreased when combined with Erythromycin.Approved, Investigational, Vet Approved
EscitalopramThe metabolism of Escitalopram can be decreased when combined with Rolapitant.Approved, Investigational
EsmirtazapineThe metabolism of Esmirtazapine can be decreased when combined with Rolapitant.Investigational
EstradiolThe serum concentration of Estradiol can be increased when it is combined with Rolapitant.Approved, Investigational, Vet Approved
Ethinyl EstradiolThe serum concentration of Ethinyl Estradiol can be increased when it is combined with Rolapitant.Approved
EthylmorphineThe metabolism of Ethylmorphine can be decreased when combined with Rolapitant.Approved, Illicit
EtoposideThe serum concentration of Etoposide can be increased when it is combined with Rolapitant.Approved
EtoricoxibThe metabolism of Etoricoxib can be decreased when combined with Rolapitant.Approved, Investigational
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Rolapitant.Approved
EzetimibeThe serum concentration of Ezetimibe can be increased when it is combined with Rolapitant.Approved
FesoterodineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Rolapitant.Approved
FingolimodThe metabolism of Fingolimod can be decreased when combined with Rolapitant.Approved, Investigational
FlecainideThe metabolism of Flecainide can be decreased when combined with Rolapitant.Approved, Withdrawn
FluconazoleThe metabolism of Rolapitant can be decreased when combined with Fluconazole.Approved, Investigational
FluorouracilThe serum concentration of Fluorouracil can be increased when it is combined with Rolapitant.Approved
FluoxetineThe metabolism of Fluoxetine can be decreased when combined with Rolapitant.Approved, Vet Approved
FluphenazineThe metabolism of Fluphenazine can be decreased when combined with Rolapitant.Approved
Fluticasone propionateThe serum concentration of Fluticasone propionate can be increased when it is combined with Rolapitant.Approved
FluvoxamineThe metabolism of Rolapitant can be decreased when combined with Fluvoxamine.Approved, Investigational
Folic AcidThe serum concentration of Folic Acid can be increased when it is combined with Rolapitant.Approved, Nutraceutical, Vet Approved
FormoterolThe metabolism of Formoterol can be decreased when combined with Rolapitant.Approved, Investigational
FosamprenavirThe metabolism of Rolapitant can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Rolapitant can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe serum concentration of Rolapitant can be decreased when it is combined with Fosphenytoin.Approved, Investigational
FostamatinibThe serum concentration of Fostamatinib can be increased when it is combined with Rolapitant.Approved, Investigational
Fusidic AcidThe serum concentration of Rolapitant can be increased when it is combined with Fusidic Acid.Approved, Investigational
GalantamineThe metabolism of Galantamine can be decreased when combined with Rolapitant.Approved
GefitinibThe serum concentration of Gefitinib can be increased when it is combined with Rolapitant.Approved, Investigational
GlecaprevirThe serum concentration of Glecaprevir can be increased when it is combined with Rolapitant.Approved, Investigational
GranisetronThe metabolism of Granisetron can be decreased when combined with Rolapitant.Approved, Investigational
HalofantrineThe metabolism of Halofantrine can be decreased when combined with Rolapitant.Approved
HaloperidolThe metabolism of Haloperidol can be decreased when combined with Rolapitant.Approved
HalothaneThe metabolism of Halothane can be decreased when combined with Rolapitant.Approved, Vet Approved
HydrocodoneThe serum concentration of the active metabolites of Hydrocodone can be reduced when Hydrocodone is used in combination with Rolapitant resulting in a loss in efficacy.Approved, Illicit
HydrocortisoneThe serum concentration of Hydrocortisone can be increased when it is combined with Rolapitant.Approved, Vet Approved
HydromorphoneThe metabolism of Hydromorphone can be decreased when combined with Rolapitant.Approved, Illicit
IbrutinibThe metabolism of Ibrutinib can be decreased when combined with Rolapitant.Approved
IdarubicinThe metabolism of Idarubicin can be decreased when combined with Rolapitant.Approved
IdelalisibThe serum concentration of Idelalisib can be increased when it is combined with Rolapitant.Approved
IloperidoneThe metabolism of Iloperidone can be decreased when combined with Rolapitant.Approved
ImatinibThe serum concentration of Imatinib can be increased when it is combined with Rolapitant.Approved
ImipramineThe metabolism of Imipramine can be decreased when combined with Rolapitant.Approved
IndinavirThe metabolism of Rolapitant can be decreased when combined with Indinavir.Approved
IpecacThe metabolism of Ipecac can be decreased when combined with Rolapitant.Approved, Withdrawn
IsavuconazoleThe serum concentration of Rolapitant can be increased when it is combined with Isavuconazole.Approved, Investigational
IsavuconazoniumThe metabolism of Rolapitant can be decreased when combined with Isavuconazonium.Approved, Investigational
ItraconazoleThe metabolism of Rolapitant can be decreased when combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Rolapitant can be increased when it is combined with Ivacaftor.Approved
IvermectinThe serum concentration of Ivermectin can be increased when it is combined with Rolapitant.Approved, Investigational, Vet Approved
IxazomibThe metabolism of Ixazomib can be decreased when combined with Rolapitant.Approved, Investigational
KetoconazoleThe metabolism of Rolapitant can be decreased when combined with Ketoconazole.Approved, Investigational
LabetalolThe metabolism of Labetalol can be decreased when combined with Rolapitant.Approved
LamotrigineThe serum concentration of Lamotrigine can be increased when it is combined with Rolapitant.Approved, Investigational
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Rolapitant.Approved
LeflunomideThe serum concentration of Leflunomide can be increased when it is combined with Rolapitant.Approved, Investigational
LenvatinibThe serum concentration of Lenvatinib can be increased when it is combined with Rolapitant.Approved, Investigational
LetermovirThe metabolism of Letermovir can be decreased when combined with Rolapitant.Approved, Investigational
LevetiracetamThe serum concentration of Levetiracetam can be increased when it is combined with Rolapitant.Approved, Investigational
LevomilnacipranThe metabolism of Levomilnacipran can be decreased when combined with Rolapitant.Approved, Investigational
LisurideThe metabolism of Lisuride can be decreased when combined with Rolapitant.Approved, Investigational
LofexidineThe metabolism of Lofexidine can be decreased when combined with Rolapitant.Approved, Investigational
LomustineThe metabolism of Lomustine can be decreased when combined with Rolapitant.Approved, Investigational
LoperamideThe serum concentration of Loperamide can be increased when it is combined with Rolapitant.Approved
LopinavirThe metabolism of Rolapitant can be decreased when combined with Lopinavir.Approved
LorcaserinThe metabolism of Lorcaserin can be decreased when combined with Rolapitant.Approved
LorpiprazoleThe serum concentration of Rolapitant can be increased when it is combined with Lorpiprazole.Approved
LosartanThe serum concentration of Losartan can be increased when it is combined with Rolapitant.Approved
LovastatinThe metabolism of Rolapitant can be decreased when combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Rolapitant can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of Rolapitant can be decreased when it is combined with Lumacaftor.Approved
MaprotilineThe metabolism of Maprotiline can be decreased when combined with Rolapitant.Approved, Investigational
MephenytoinThe metabolism of Mephenytoin can be decreased when combined with Rolapitant.Investigational, Withdrawn
MequitazineThe metabolism of Mequitazine can be decreased when combined with Rolapitant.Approved
MesoridazineThe metabolism of Mesoridazine can be decreased when combined with Rolapitant.Approved, Investigational
MethadoneThe metabolism of Methadone can be decreased when combined with Rolapitant.Approved
MethamphetamineThe metabolism of Methamphetamine can be decreased when combined with Rolapitant.Approved, Illicit
MethotrexateThe serum concentration of Methotrexate can be increased when it is combined with Rolapitant.Approved
MethotrimeprazineThe metabolism of Methotrimeprazine can be decreased when combined with Rolapitant.Approved, Investigational
MethoxyfluraneThe metabolism of Methoxyflurane can be decreased when combined with Rolapitant.Approved, Investigational, Vet Approved
MethylprednisoloneThe serum concentration of Methylprednisolone can be increased when it is combined with Rolapitant.Approved, Vet Approved
MethyprylonThe metabolism of Methyprylon can be decreased when combined with Rolapitant.Approved, Illicit, Withdrawn
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Rolapitant.Approved, Investigational
MexiletineThe metabolism of Mexiletine can be decreased when combined with Rolapitant.Approved, Investigational
MianserinThe metabolism of Mianserin can be decreased when combined with Rolapitant.Approved, Investigational
MibefradilThe metabolism of Rolapitant can be decreased when combined with Mibefradil.Investigational, Withdrawn
MiconazoleThe metabolism of Rolapitant can be decreased when combined with Miconazole.Approved, Investigational, Vet Approved
MifepristoneThe serum concentration of Rolapitant can be increased when it is combined with Mifepristone.Approved, Investigational
MinaprineThe metabolism of Minaprine can be decreased when combined with Rolapitant.Approved
MirabegronThe metabolism of Mirabegron can be decreased when combined with Rolapitant.Approved
MirtazapineThe metabolism of Mirtazapine can be decreased when combined with Rolapitant.Approved
MitotaneThe serum concentration of Rolapitant can be decreased when it is combined with Mitotane.Approved
MitoxantroneThe serum concentration of Mitoxantrone can be increased when it is combined with Rolapitant.Approved, Investigational
MoclobemideThe metabolism of Moclobemide can be decreased when combined with Rolapitant.Approved, Investigational
MorphineThe metabolism of Morphine can be decreased when combined with Rolapitant.Approved, Investigational
Mycophenolate mofetilThe serum concentration of Mycophenolate mofetil can be increased when it is combined with Rolapitant.Approved, Investigational
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Rolapitant.Approved
NateglinideThe metabolism of Nateglinide can be decreased when combined with Rolapitant.Approved, Investigational
NebivololThe serum concentration of Nebivolol can be increased when it is combined with Rolapitant.Approved, Investigational
NefazodoneThe metabolism of Rolapitant can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe metabolism of Rolapitant can be decreased when combined with Nelfinavir.Approved
NetupitantThe serum concentration of Rolapitant can be increased when it is combined with Netupitant.Approved, Investigational
NevirapineThe serum concentration of Rolapitant can be decreased when it is combined with Nevirapine.Approved
NicardipineThe serum concentration of Nicardipine can be increased when it is combined with Rolapitant.Approved, Investigational
NicergolineThe metabolism of Nicergoline can be decreased when combined with Rolapitant.Approved, Investigational
NifedipineThe serum concentration of Nifedipine can be increased when it is combined with Rolapitant.Approved
NilotinibThe serum concentration of Nilotinib can be increased when it is combined with Rolapitant.Approved, Investigational
NitrofuralThe metabolism of Nitrofural can be decreased when combined with Rolapitant.Approved, Investigational, Vet Approved
NitrofurantoinThe serum concentration of Nitrofurantoin can be increased when it is combined with Rolapitant.Approved, Vet Approved
NortriptylineThe metabolism of Nortriptyline can be decreased when combined with Rolapitant.Approved
OlanzapineThe metabolism of Olanzapine can be decreased when combined with Rolapitant.Approved, Investigational
OlaparibThe metabolism of Rolapitant can be decreased when combined with Olaparib.Approved
OmbitasvirThe serum concentration of Ombitasvir can be increased when it is combined with Rolapitant.Approved, Investigational
OmeprazoleThe serum concentration of Omeprazole can be increased when it is combined with Rolapitant.Approved, Investigational, Vet Approved
OndansetronThe serum concentration of Ondansetron can be increased when it is combined with Rolapitant.Approved
OpiumThe metabolism of Opium can be decreased when combined with Rolapitant.Approved, Illicit
OsimertinibThe serum concentration of Rolapitant can be increased when it is combined with Osimertinib.Approved
OxaliplatinThe serum concentration of Oxaliplatin can be increased when it is combined with Rolapitant.Approved, Investigational
OxycodoneThe metabolism of Oxycodone can be decreased when combined with Rolapitant.Approved, Illicit, Investigational
PaclitaxelThe serum concentration of Paclitaxel can be increased when it is combined with Rolapitant.Approved, Vet Approved
PalbociclibThe serum concentration of Rolapitant can be increased when it is combined with Palbociclib.Approved, Investigational
PalonosetronThe metabolism of Palonosetron can be decreased when combined with Rolapitant.Approved, Investigational
ParoxetineThe metabolism of Paroxetine can be decreased when combined with Rolapitant.Approved, Investigational
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Rolapitant.Approved
PentamidineThe metabolism of Pentamidine can be decreased when combined with Rolapitant.Approved, Investigational
PentobarbitalThe serum concentration of Rolapitant can be decreased when it is combined with Pentobarbital.Approved, Investigational, Vet Approved
PerospironeThe metabolism of Perospirone can be decreased when combined with Rolapitant.Approved
PerphenazineThe metabolism of Perphenazine can be decreased when combined with Rolapitant.Approved
PethidineThe metabolism of Pethidine can be decreased when combined with Rolapitant.Approved
PhenacetinThe metabolism of Phenacetin can be decreased when combined with Rolapitant.Withdrawn
PhenforminThe metabolism of Phenformin can be decreased when combined with Rolapitant.Approved, Investigational, Withdrawn
PhenobarbitalThe serum concentration of Rolapitant can be decreased when it is combined with Phenobarbital.Approved, Investigational
PhenytoinThe serum concentration of Rolapitant can be decreased when it is combined with Phenytoin.Approved, Vet Approved
PibrentasvirThe serum concentration of Pibrentasvir can be increased when it is combined with Rolapitant.Approved, Investigational
PimozideThe serum concentration of Pimozide can be increased when it is combined with Rolapitant.Approved
PindololThe metabolism of Pindolol can be decreased when combined with Rolapitant.Approved, Investigational
PiperazineThe metabolism of Piperazine can be decreased when combined with Rolapitant.Approved, Vet Approved
PipotiazineThe metabolism of Pipotiazine can be decreased when combined with Rolapitant.Approved, Investigational
PitavastatinThe serum concentration of Pitavastatin can be increased when it is combined with Rolapitant.Approved
PitolisantThe serum concentration of Pitolisant can be increased when it is combined with Rolapitant.Approved, Investigational
PonatinibThe serum concentration of Ponatinib can be increased when it is combined with Rolapitant.Approved, Investigational
PosaconazoleThe metabolism of Rolapitant can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
PravastatinThe serum concentration of Pravastatin can be increased when it is combined with Rolapitant.Approved
PrazosinThe serum concentration of Prazosin can be increased when it is combined with Rolapitant.Approved
PrednisoloneThe serum concentration of Prednisolone can be increased when it is combined with Rolapitant.Approved, Vet Approved
PrimidoneThe serum concentration of Rolapitant can be decreased when it is combined with Primidone.Approved, Vet Approved
ProcainamideThe metabolism of Procainamide can be decreased when combined with Rolapitant.Approved
ProgesteroneThe metabolism of Progesterone can be decreased when combined with Rolapitant.Approved, Vet Approved
PropafenoneThe serum concentration of Rolapitant can be increased when it is combined with Propafenone.Approved
PropofolThe metabolism of Propofol can be decreased when combined with Rolapitant.Approved, Investigational, Vet Approved
PropranololThe serum concentration of Propranolol can be increased when it is combined with Rolapitant.Approved, Investigational
ProtriptylineThe metabolism of Protriptyline can be decreased when combined with Rolapitant.Approved
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Rolapitant.Approved
QuetiapineThe serum concentration of Quetiapine can be increased when it is combined with Rolapitant.Approved
QuinineThe metabolism of Quinine can be decreased when combined with Rolapitant.Approved
RanitidineThe serum concentration of Ranitidine can be increased when it is combined with Rolapitant.Approved
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Rolapitant.Approved, Investigational
RemoxiprideThe metabolism of Remoxipride can be decreased when combined with Rolapitant.Approved, Withdrawn
RepinotanThe metabolism of Repinotan can be decreased when combined with Rolapitant.Investigational
RifabutinThe serum concentration of Rolapitant can be decreased when it is combined with Rifabutin.Approved, Investigational
RifampicinThe serum concentration of Rolapitant can be decreased when it is combined with Rifampicin.Approved
RifapentineThe serum concentration of Rolapitant can be decreased when it is combined with Rifapentine.Approved, Investigational
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Rolapitant.Approved, Investigational
RiluzoleThe serum concentration of Riluzole can be increased when it is combined with Rolapitant.Approved, Investigational
RiociguatThe serum concentration of Riociguat can be increased when it is combined with Rolapitant.Approved
RisperidoneThe metabolism of Risperidone can be decreased when combined with Rolapitant.Approved, Investigational
RitonavirThe metabolism of Ritonavir can be decreased when combined with Rolapitant.Approved, Investigational
RopivacaineThe metabolism of Ropivacaine can be decreased when combined with Rolapitant.Approved
RotigotineThe metabolism of Rotigotine can be decreased when combined with Rolapitant.Approved
RucaparibThe serum concentration of Rucaparib can be increased when it is combined with Rolapitant.Approved, Investigational
RupatadineThe metabolism of Rupatadine can be decreased when combined with Rolapitant.Approved
SafinamideThe serum concentration of Safinamide can be increased when it is combined with Rolapitant.Approved, Investigational
SaquinavirThe metabolism of Rolapitant can be decreased when combined with Saquinavir.Approved, Investigational
SarilumabThe therapeutic efficacy of Rolapitant can be decreased when used in combination with Sarilumab.Approved, Investigational
SertindoleThe metabolism of Sertindole can be decreased when combined with Rolapitant.Approved, Investigational, Withdrawn
SertralineThe metabolism of Sertraline can be decreased when combined with Rolapitant.Approved
SildenafilThe metabolism of Rolapitant can be decreased when combined with Sildenafil.Approved, Investigational
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Rolapitant.Approved
SiltuximabThe serum concentration of Rolapitant can be decreased when it is combined with Siltuximab.Approved, Investigational
SimeprevirThe serum concentration of Rolapitant can be increased when it is combined with Simeprevir.Approved
SimvastatinThe metabolism of Simvastatin can be decreased when combined with Rolapitant.Approved
SitagliptinThe serum concentration of Sitagliptin can be increased when it is combined with Rolapitant.Approved, Investigational
SofosbuvirThe serum concentration of Sofosbuvir can be increased when it is combined with Rolapitant.Approved
SorafenibThe serum concentration of Sorafenib can be increased when it is combined with Rolapitant.Approved, Investigational
SparteineThe metabolism of Sparteine can be decreased when combined with Rolapitant.Experimental
St. John's WortThe serum concentration of Rolapitant can be decreased when it is combined with St. John's Wort.Approved, Investigational, Nutraceutical
StiripentolThe serum concentration of Rolapitant can be increased when it is combined with Stiripentol.Approved
SulfisoxazoleThe metabolism of Rolapitant can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
SumatriptanThe serum concentration of Sumatriptan can be increased when it is combined with Rolapitant.Approved, Investigational
TamoxifenThe serum concentration of the active metabolites of Tamoxifen can be reduced when Tamoxifen is used in combination with Rolapitant resulting in a loss in efficacy.Approved
TamsulosinThe metabolism of Tamsulosin can be decreased when combined with Rolapitant.Approved, Investigational
TapentadolThe metabolism of Tapentadol can be decreased when combined with Rolapitant.Approved
TegaserodThe metabolism of Tegaserod can be decreased when combined with Rolapitant.Approved, Investigational, Withdrawn
TelaprevirThe metabolism of Rolapitant can be decreased when combined with Telaprevir.Approved, Withdrawn
TelithromycinThe metabolism of Rolapitant can be decreased when combined with Telithromycin.Approved
TeniposideThe serum concentration of Teniposide can be increased when it is combined with Rolapitant.Approved
TerfenadineThe metabolism of Terfenadine can be decreased when combined with Rolapitant.Approved, Withdrawn
TeriflunomideThe serum concentration of Teriflunomide can be increased when it is combined with Rolapitant.Approved
TesmilifeneThe metabolism of Tesmilifene can be decreased when combined with Rolapitant.Investigational
TestosteroneThe serum concentration of Testosterone can be increased when it is combined with Rolapitant.Approved, Investigational
Testosterone cypionateThe serum concentration of Testosterone cypionate can be increased when it is combined with Rolapitant.Approved
Testosterone enanthateThe serum concentration of Testosterone enanthate can be increased when it is combined with Rolapitant.Approved
Testosterone undecanoateThe serum concentration of Testosterone undecanoate can be increased when it is combined with Rolapitant.Approved, Investigational
TetrabenazineThe metabolism of Tetrabenazine can be decreased when combined with Rolapitant.Approved, Investigational
TetracyclineThe serum concentration of Tetracycline can be increased when it is combined with Rolapitant.Approved, Vet Approved
TheophyllineThe metabolism of Theophylline can be decreased when combined with Rolapitant.Approved
ThioridazineThe serum concentration of Thioridazine can be increased when it is combined with Rolapitant.Approved, Withdrawn
TiclopidineThe metabolism of Rolapitant can be decreased when combined with Ticlopidine.Approved
TimololThe metabolism of Timolol can be decreased when combined with Rolapitant.Approved
TiotropiumThe metabolism of Tiotropium can be decreased when combined with Rolapitant.Approved
TipranavirThe metabolism of Tipranavir can be decreased when combined with Rolapitant.Approved, Investigational
TocilizumabThe serum concentration of Rolapitant can be decreased when it is combined with Tocilizumab.Approved
TolterodineThe metabolism of Tolterodine can be decreased when combined with Rolapitant.Approved, Investigational
TopiramateThe serum concentration of Topiramate can be increased when it is combined with Rolapitant.Approved
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Rolapitant.Approved, Investigational
TrabectedinThe metabolism of Trabectedin can be decreased when combined with Rolapitant.Approved, Investigational
TramadolThe therapeutic efficacy of Tramadol can be decreased when used in combination with Rolapitant.Approved, Investigational
TrazodoneThe metabolism of Trazodone can be decreased when combined with Rolapitant.Approved, Investigational
TrimipramineThe metabolism of Trimipramine can be decreased when combined with Rolapitant.Approved
UmeclidiniumThe metabolism of Umeclidinium can be decreased when combined with Rolapitant.Approved
ValbenazineThe metabolism of Valbenazine can be decreased when combined with Rolapitant.Approved, Investigational
VecuroniumThe serum concentration of Vecuronium can be increased when it is combined with Rolapitant.Approved
VelpatasvirThe serum concentration of Velpatasvir can be increased when it is combined with Rolapitant.Approved, Investigational
VemurafenibThe serum concentration of Rolapitant can be decreased when it is combined with Vemurafenib.Approved
VenetoclaxThe serum concentration of Venetoclax can be increased when it is combined with Rolapitant.Approved, Investigational
VenlafaxineThe serum concentration of Venlafaxine can be increased when it is combined with Rolapitant.Approved
VerapamilThe serum concentration of Verapamil can be increased when it is combined with Rolapitant.Approved
VernakalantThe metabolism of Vernakalant can be decreased when combined with Rolapitant.Approved, Investigational
VilazodoneThe metabolism of Vilazodone can be decreased when combined with Rolapitant.Approved
VinblastineThe metabolism of Vinblastine can be decreased when combined with Rolapitant.Approved
VincristineThe serum concentration of Vincristine can be increased when it is combined with Rolapitant.Approved, Investigational
VincristineThe excretion of Vincristine can be decreased when combined with Rolapitant.Approved, Investigational
VinorelbineThe metabolism of Vinorelbine can be decreased when combined with Rolapitant.Approved, Investigational
VoriconazoleThe metabolism of Rolapitant can be decreased when combined with Voriconazole.Approved, Investigational
VortioxetineThe metabolism of Vortioxetine can be decreased when combined with Rolapitant.Approved, Investigational
VoxilaprevirThe serum concentration of Voxilaprevir can be increased when it is combined with Rolapitant.Approved, Investigational
YohimbineThe metabolism of Yohimbine can be decreased when combined with Rolapitant.Approved, Investigational, Vet Approved
ZalcitabineThe metabolism of Zalcitabine can be decreased when combined with Rolapitant.Approved, Investigational
ZiprasidoneThe metabolism of Rolapitant can be decreased when combined with Ziprasidone.Approved
ZuclopenthixolThe metabolism of Zuclopenthixol can be decreased when combined with Rolapitant.Approved, Investigational
Food Interactions
Not Available

References

General References
  1. Syed YY: Rolapitant: first global approval. Drugs. 2015 Nov;75(16):1941-5. doi: 10.1007/s40265-015-0485-8. [PubMed:26467681]
  2. Duffy RA, Morgan C, Naylor R, Higgins GA, Varty GB, Lachowicz JE, Parker EM: Rolapitant (SCH 619734): a potent, selective and orally active neurokinin NK1 receptor antagonist with centrally-mediated antiemetic effects in ferrets. Pharmacol Biochem Behav. 2012 Jul;102(1):95-100. doi: 10.1016/j.pbb.2012.03.021. Epub 2012 Mar 31. [PubMed:22497992]
  3. Gan TJ, Gu J, Singla N, Chung F, Pearman MH, Bergese SD, Habib AS, Candiotti KA, Mo Y, Huyck S, Creed MR, Cantillon M: Rolapitant for the prevention of postoperative nausea and vomiting: a prospective, double-blinded, placebo-controlled randomized trial. Anesth Analg. 2011 Apr;112(4):804-12. doi: 10.1213/ANE.0b013e31820886c3. Epub 2011 Mar 8. [PubMed:21385988]
External Links
KEGG Drug
D10742
PubChem Compound
10311306
PubChem Substance
310265183
ChemSpider
8486772
ChEBI
90908
ChEMBL
CHEMBL3707331
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Rolapitant
FDA label
Download (315 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedBasic ScienceProphylaxis of acute chemotherapy induced nausea and vomiting1
1CompletedPreventionProphylaxis of acute chemotherapy induced nausea and vomiting2
2CompletedPreventionNausea / Vomiting1
2CompletedTreatmentCoughing1
2RecruitingSupportive CareChemo-radiation Induced Nausea and Vomiting1
2RecruitingSupportive CareSarcomas1
3CompletedPreventionProphylaxis of acute chemotherapy induced nausea and vomiting3

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
Injection, emulsionIntravenous1.8 mg/mL
TabletOral90 mg/1
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US8470842No2009-01-182029-01-18Us
US8404702No2009-10-092029-10-09Us
US8796299No2002-12-172022-12-17Us
US7049320No2003-12-082023-12-08Us
US7981905No2007-04-042027-04-04Us
US8361500No2009-10-092029-10-09Us
US7563801No2007-04-042027-04-04Us
US8178550No2007-04-042027-04-04Us
US9101615No2012-07-142032-07-14Us

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.00166 mg/mLALOGPS
logP4.07ALOGPS
logP5ChemAxon
logS-5.5ALOGPS
pKa (Strongest Acidic)14.15ChemAxon
pKa (Strongest Basic)8.3ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area50.36 Å2ChemAxon
Rotatable Bond Count7ChemAxon
Refractivity118.28 m3·mol-1ChemAxon
Polarizability46.2 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability0ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
Not Available

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 delta amino acids and derivatives. These are compounds containing a carboxylic acid group and an amino group at the C5 carbon atom.
Kingdom
Organic compounds
Super Class
Organic acids and derivatives
Class
Carboxylic acids and derivatives
Sub Class
Amino acids, peptides, and analogues
Direct Parent
Delta amino acids and derivatives
Alternative Parents
Phenylpiperidines / Trifluoromethylbenzenes / Azaspirodecane derivatives / Benzylethers / Aralkylamines / Pyrrolidine-2-ones / Secondary carboxylic acid amides / Lactams / Azacyclic compounds / Dialkylamines
show 7 more
Substituents
Delta amino acid or derivatives / Phenylpiperidine / Azaspirodecane / Trifluoromethylbenzene / Benzylether / Aralkylamine / Monocyclic benzene moiety / Piperidine / Benzenoid / Pyrrolidone
show 25 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
Not Available

Targets

1. Neurokinin-1 Receptor (NK1R)
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Antagonist
References
  1. Duffy RA, Morgan C, Naylor R, Higgins GA, Varty GB, Lachowicz JE, Parker EM: Rolapitant (SCH 619734): a potent, selective and orally active neurokinin NK1 receptor antagonist with centrally-mediated antiemetic effects in ferrets. Pharmacol Biochem Behav. 2012 Jul;102(1):95-100. doi: 10.1016/j.pbb.2012.03.021. Epub 2012 Mar 31. [PubMed:22497992]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Inhibitor
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...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
Molecular Weight
55768.94 Da
Kind
Protein
Organism
Human
Pharmacological action
No
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 react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da

Transporters

Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Inhibitor
General Function
Xenobiotic-transporting atpase activity
Specific Function
High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both fro...
Gene Name
ABCG2
Uniprot ID
Q9UNQ0
Uniprot Name
ATP-binding cassette sub-family G member 2
Molecular Weight
72313.47 Da
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Inhibitor
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da

Drug created on October 29, 2015 15:22 / Updated on August 15, 2018 10:01