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IdentificationPharmacologyInteractionsReferencesTrialsEconomicsPropertiesSpectraTaxonomyIdentification
- 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
Structure for DB09291 (Rolapitant)
- Synonyms
- Not Available
- Product Ingredients
Ingredient UNII CAS InChI Key Rolapitant hydrochloride J7Z9DBN8J0 858102-79-1 VEWAWEMXVUFANV-PVBCUUEWSA-N Rolapitant hydrochloride monohydrate 57O5S1QSAQ 914462-92-3 GZQWMYVDLCUBQX-WVZIYJGPSA-N - Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Varubi Tablet 90 mg/1 Oral Tesaro, Inc. 2015-10-07 Not applicable US 
Varubi Injection, emulsion 1.8 mg/mL Intravenous Tesaro, Inc. 2017-10-25 Not applicable US - International/Other Brands
- Varubi (Tesoro)
- Categories
- BCRP/ABCG2 Inhibitors
- Cytochrome P-450 CYP2D6 Inhibitors
- Cytochrome P-450 CYP2D6 Inhibitors (moderate)
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 CYP3A4 Substrates (strength unknown)
- Cytochrome P-450 Enzyme Inhibitors
- Neurokinin-1 Receptor Antagonists
- Neurotransmitter Agents
- P-glycoprotein/ABCB1 Inhibitors
- Substance P/Neurokinin-1 Receptor Antagonist
- 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.
Target Actions Organism ANeurokinin-1 Receptor (NK1R) antagonistHuman - 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
Drug Interaction Drug group 4-Methoxyamphetamine The metabolism of 4-Methoxyamphetamine can be decreased when combined with Rolapitant. Experimental, Illicit Abemaciclib The serum concentration of Abemaciclib can be increased when it is combined with Rolapitant. Approved, Investigational Acetyl sulfisoxazole The metabolism of Rolapitant can be decreased when combined with Acetyl sulfisoxazole. Approved, Vet Approved Acetylcholine The metabolism of Acetylcholine can be decreased when combined with Rolapitant. Approved Afatinib The serum concentration of Afatinib can be increased when it is combined with Rolapitant. Approved Ajmaline The metabolism of Ajmaline can be decreased when combined with Rolapitant. Approved, Investigational Almotriptan The metabolism of Almotriptan can be decreased when combined with Rolapitant. Approved, Investigational Alogliptin The metabolism of Alogliptin can be decreased when combined with Rolapitant. Approved Alprenolol The metabolism of Alprenolol can be decreased when combined with Rolapitant. Approved, Withdrawn Alvocidib The serum concentration of Alvocidib can be increased when it is combined with Rolapitant. Experimental, Investigational Aminophenazone The metabolism of Aminophenazone can be decreased when combined with Rolapitant. Approved, Withdrawn Amiodarone The metabolism of Rolapitant can be decreased when combined with Amiodarone. Approved, Investigational Amitriptyline The metabolism of Amitriptyline can be decreased when combined with Rolapitant. Approved Amoxapine The metabolism of Amoxapine can be decreased when combined with Rolapitant. Approved Amphetamine The metabolism of Amphetamine can be decreased when combined with Rolapitant. Approved, Illicit, Investigational Amprenavir The metabolism of Amprenavir can be decreased when combined with Rolapitant. Approved, Investigational Amsacrine The metabolism of Amsacrine can be decreased when combined with Rolapitant. Approved, Investigational Antipyrine The metabolism of Antipyrine can be decreased when combined with Rolapitant. Approved, Investigational Apalutamide The serum concentration of Rolapitant can be decreased when it is combined with Apalutamide. Approved, Investigational Apixaban The serum concentration of Apixaban can be increased when it is combined with Rolapitant. Approved Aprepitant The serum concentration of Rolapitant can be increased when it is combined with Aprepitant. Approved, Investigational Aprindine The metabolism of Aprindine can be decreased when combined with Rolapitant. Approved Arformoterol The metabolism of Arformoterol can be decreased when combined with Rolapitant. Approved, Investigational Aripiprazole The serum concentration of Aripiprazole can be increased when it is combined with Rolapitant. Approved, Investigational Artemether The metabolism of Artemether can be decreased when combined with Rolapitant. Approved Astemizole The metabolism of Astemizole can be decreased when combined with Rolapitant. Approved, Withdrawn Asunaprevir The metabolism of Asunaprevir can be decreased when combined with Rolapitant. Approved, Investigational, Withdrawn Atazanavir The metabolism of Rolapitant can be decreased when combined with Atazanavir. Approved, Investigational Atomoxetine The metabolism of Rolapitant can be decreased when combined with Atomoxetine. Approved Azelastine The metabolism of Azelastine can be decreased when combined with Rolapitant. Approved Baricitinib The serum concentration of Baricitinib can be increased when it is combined with Rolapitant. Approved, Investigational Betaxolol The metabolism of Betaxolol can be decreased when combined with Rolapitant. Approved, Investigational Bisoprolol The metabolism of Bisoprolol can be decreased when combined with Rolapitant. Approved Boceprevir The metabolism of Rolapitant can be decreased when combined with Boceprevir. Approved, Withdrawn Bortezomib The metabolism of Rolapitant can be decreased when combined with Bortezomib. Approved, Investigational Bosentan The serum concentration of Rolapitant can be decreased when it is combined with Bosentan. Approved, Investigational Bosutinib The serum concentration of Bosutinib can be increased when it is combined with Rolapitant. Approved Brentuximab vedotin The serum concentration of Brentuximab vedotin can be increased when it is combined with Rolapitant. Approved, Investigational Brexpiprazole The serum concentration of Brexpiprazole can be increased when it is combined with Rolapitant. Approved, Investigational Brigatinib The serum concentration of Brigatinib can be increased when it is combined with Rolapitant. Approved, Investigational Bufuralol The metabolism of Bufuralol can be decreased when combined with Rolapitant. Experimental, Investigational Bupivacaine The metabolism of Bupivacaine can be decreased when combined with Rolapitant. Approved, Investigational Buprenorphine The metabolism of Buprenorphine can be decreased when combined with Rolapitant. Approved, Illicit, Investigational, Vet Approved Bupropion The metabolism of Bupropion can be decreased when combined with Rolapitant. Approved Buspirone The metabolism of Buspirone can be decreased when combined with Rolapitant. Approved, Investigational Camptothecin The serum concentration of Camptothecin can be increased when it is combined with Rolapitant. Experimental Captopril The metabolism of Captopril can be decreased when combined with Rolapitant. Approved Carbamazepine The serum concentration of Rolapitant can be decreased when it is combined with Carbamazepine. Approved, Investigational Carboplatin The serum concentration of Carboplatin can be increased when it is combined with Rolapitant. Approved Cariprazine The metabolism of Cariprazine can be decreased when combined with Rolapitant. Approved, Investigational Carteolol The metabolism of Carteolol can be decreased when combined with Rolapitant. Approved Carvedilol The metabolism of Carvedilol can be decreased when combined with Rolapitant. Approved, Investigational Cephalexin The metabolism of Cephalexin can be decreased when combined with Rolapitant. Approved, Investigational, Vet Approved Ceritinib The serum concentration of Rolapitant can be increased when it is combined with Ceritinib. Approved Cerivastatin The serum concentration of Cerivastatin can be increased when it is combined with Rolapitant. Approved, Withdrawn Cevimeline The metabolism of Cevimeline can be decreased when combined with Rolapitant. Approved Chlordiazepoxide The metabolism of Chlordiazepoxide can be decreased when combined with Rolapitant. Approved, Illicit, Investigational Chloroquine The metabolism of Chloroquine can be decreased when combined with Rolapitant. Approved, Investigational, Vet Approved Chlorpromazine The metabolism of Chlorpromazine can be decreased when combined with Rolapitant. Approved, Investigational, Vet Approved Chlorzoxazone The metabolism of Chlorzoxazone can be decreased when combined with Rolapitant. Approved Cholesterol The serum concentration of Cholesterol can be increased when it is combined with Rolapitant. Approved, Investigational Cilostazol The metabolism of Cilostazol can be decreased when combined with Rolapitant. Approved, Investigational Cimetidine The serum concentration of Cimetidine can be increased when it is combined with Rolapitant. Approved, Investigational Ciprofloxacin The serum concentration of Ciprofloxacin can be increased when it is combined with Rolapitant. Approved, Investigational Cisplatin The serum concentration of Cisplatin can be increased when it is combined with Rolapitant. Approved Citalopram The metabolism of Citalopram can be decreased when combined with Rolapitant. Approved Cladribine The serum concentration of Cladribine can be increased when it is combined with Rolapitant. Approved, Investigational Clarithromycin The metabolism of Rolapitant can be decreased when combined with Clarithromycin. Approved Clofarabine The serum concentration of Clofarabine can be increased when it is combined with Rolapitant. Approved, Investigational Clomipramine The metabolism of Clomipramine can be decreased when combined with Rolapitant. Approved, Investigational, Vet Approved Clonidine The metabolism of Clonidine can be decreased when combined with Rolapitant. Approved Clotrimazole The metabolism of Rolapitant can be decreased when combined with Clotrimazole. Approved, Vet Approved Clozapine The metabolism of Clozapine can be decreased when combined with Rolapitant. Approved Cobicistat The metabolism of Rolapitant can be decreased when combined with Cobicistat. Approved Codeine The therapeutic efficacy of Codeine can be decreased when used in combination with Rolapitant. Approved, Illicit Colchicine The serum concentration of Colchicine can be increased when it is combined with Rolapitant. Approved Conivaptan The serum concentration of Conivaptan can be increased when it is combined with Rolapitant. Approved, Investigational Conjugated estrogens The serum concentration of Conjugated estrogens can be increased when it is combined with Rolapitant. Approved Copanlisib The serum concentration of Copanlisib can be increased when it is combined with Rolapitant. Approved, Investigational Crizotinib The metabolism of Rolapitant can be decreased when combined with Crizotinib. Approved Curcumin The metabolism of Rolapitant can be decreased when combined with Curcumin. Approved, Investigational Cyclobenzaprine The metabolism of Cyclobenzaprine can be decreased when combined with Rolapitant. Approved Cyclophosphamide The metabolism of Cyclophosphamide can be decreased when combined with Rolapitant. Approved, Investigational Cyclosporine The serum concentration of Cyclosporine can be increased when it is combined with Rolapitant. Approved, Investigational, Vet Approved Dabigatran etexilate The serum concentration of the active metabolites of Dabigatran etexilate can be increased when Dabigatran etexilate is used in combination with Rolapitant. Approved Dabrafenib The serum concentration of Rolapitant can be decreased when it is combined with Dabrafenib. Approved, Investigational Dactinomycin The serum concentration of Dactinomycin can be increased when it is combined with Rolapitant. Approved, Investigational Dapagliflozin The serum concentration of Dapagliflozin can be increased when it is combined with Rolapitant. Approved Darifenacin The metabolism of Darifenacin can be decreased when combined with Rolapitant. Approved, Investigational Darunavir The metabolism of Rolapitant can be decreased when combined with Darunavir. Approved Dasabuvir The metabolism of Dasabuvir can be decreased when combined with Rolapitant. Approved Dasatinib The serum concentration of Dasatinib can be increased when it is combined with Rolapitant. Approved, Investigational Daunorubicin The serum concentration of Daunorubicin can be increased when it is combined with Rolapitant. Approved Debrisoquin The metabolism of Debrisoquin can be decreased when combined with Rolapitant. Approved, Investigational Deferasirox The serum concentration of Rolapitant can be decreased when it is combined with Deferasirox. Approved, Investigational Delafloxacin The serum concentration of Delafloxacin can be increased when it is combined with Rolapitant. Approved, Investigational Delavirdine The metabolism of Rolapitant can be decreased when combined with Delavirdine. Approved Desipramine The metabolism of Desipramine can be decreased when combined with Rolapitant. Approved, Investigational Deutetrabenazine The metabolism of Deutetrabenazine can be decreased when combined with Rolapitant. Approved, Investigational Dexamethasone The serum concentration of Rolapitant can be decreased when it is combined with Dexamethasone. Approved, Investigational, Vet Approved Dexchlorpheniramine maleate The metabolism of Dexchlorpheniramine maleate can be decreased when combined with Rolapitant. Approved Dexfenfluramine The metabolism of Dexfenfluramine can be decreased when combined with Rolapitant. Approved, Illicit, Investigational, Withdrawn Dextroamphetamine The metabolism of Dextroamphetamine can be decreased when combined with Rolapitant. Approved, Illicit Dextromethorphan The metabolism of Dextromethorphan can be decreased when combined with Rolapitant. Approved Dihydrocodeine The metabolism of Dihydrocodeine can be decreased when combined with Rolapitant. Approved, Illicit Dihydroergotamine The metabolism of Rolapitant can be decreased when combined with Dihydroergotamine. Approved, Investigational Diltiazem The metabolism of Rolapitant can be decreased when combined with Diltiazem. Approved, Investigational Docetaxel The serum concentration of Docetaxel can be increased when it is combined with Rolapitant. Approved, Investigational Dolasetron The metabolism of Dolasetron can be decreased when combined with Rolapitant. Approved, Investigational Dolutegravir The serum concentration of Dolutegravir can be increased when it is combined with Rolapitant. Approved Domperidone The metabolism of Domperidone can be decreased when combined with Rolapitant. Approved, Investigational, Vet Approved Donepezil The metabolism of Donepezil can be decreased when combined with Rolapitant. Approved Dopamine The metabolism of Dopamine can be decreased when combined with Rolapitant. Approved Doxepin The metabolism of Doxepin can be decreased when combined with Rolapitant. Approved, Investigational Doxorubicin The serum concentration of Doxorubicin can be increased when it is combined with Rolapitant. Approved, Investigational Doxycycline The metabolism of Rolapitant can be decreased when combined with Doxycycline. Approved, Investigational, Vet Approved Dronedarone The metabolism of Rolapitant can be decreased when combined with Dronedarone. Approved Duloxetine The metabolism of Duloxetine can be decreased when combined with Rolapitant. Approved Edoxaban The serum concentration of Edoxaban can be increased when it is combined with Rolapitant. Approved Eletriptan The metabolism of Eletriptan can be decreased when combined with Rolapitant. Approved, Investigational Eliglustat The serum concentration of Eliglustat can be increased when it is combined with Rolapitant. Approved Enasidenib The serum concentration of Enasidenib can be increased when it is combined with Rolapitant. Approved, Investigational Encainide The metabolism of Encainide can be decreased when combined with Rolapitant. Approved, Investigational, Withdrawn Enclomiphene The metabolism of Enclomiphene can be decreased when combined with Rolapitant. Investigational Enzalutamide The serum concentration of Rolapitant can be decreased when it is combined with Enzalutamide. Approved Epinastine The metabolism of Epinastine can be decreased when combined with Rolapitant. Approved, Investigational Erlotinib The metabolism of Erlotinib can be decreased when combined with Rolapitant. Approved, Investigational Ertugliflozin The serum concentration of Ertugliflozin can be increased when it is combined with Rolapitant. Approved, Investigational Erythromycin The metabolism of Rolapitant can be decreased when combined with Erythromycin. Approved, Investigational, Vet Approved Escitalopram The metabolism of Escitalopram can be decreased when combined with Rolapitant. Approved, Investigational Esmirtazapine The metabolism of Esmirtazapine can be decreased when combined with Rolapitant. Investigational Estradiol The serum concentration of Estradiol can be increased when it is combined with Rolapitant. Approved, Investigational, Vet Approved Ethinyl Estradiol The serum concentration of Ethinyl Estradiol can be increased when it is combined with Rolapitant. Approved Ethylmorphine The metabolism of Ethylmorphine can be decreased when combined with Rolapitant. Approved, Illicit Etoposide The serum concentration of Etoposide can be increased when it is combined with Rolapitant. Approved Etoricoxib The metabolism of Etoricoxib can be decreased when combined with Rolapitant. Approved, Investigational Everolimus The serum concentration of Everolimus can be increased when it is combined with Rolapitant. Approved Ezetimibe The serum concentration of Ezetimibe can be increased when it is combined with Rolapitant. Approved Fesoterodine The serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Rolapitant. Approved Fingolimod The metabolism of Fingolimod can be decreased when combined with Rolapitant. Approved, Investigational Flecainide The metabolism of Flecainide can be decreased when combined with Rolapitant. Approved, Withdrawn Fluconazole The metabolism of Rolapitant can be decreased when combined with Fluconazole. Approved, Investigational Fluorouracil The serum concentration of Fluorouracil can be increased when it is combined with Rolapitant. Approved Fluoxetine The metabolism of Fluoxetine can be decreased when combined with Rolapitant. Approved, Vet Approved Fluphenazine The metabolism of Fluphenazine can be decreased when combined with Rolapitant. Approved Fluticasone propionate The serum concentration of Fluticasone propionate can be increased when it is combined with Rolapitant. Approved Fluvoxamine The metabolism of Rolapitant can be decreased when combined with Fluvoxamine. Approved, Investigational Folic Acid The serum concentration of Folic Acid can be increased when it is combined with Rolapitant. Approved, Nutraceutical, Vet Approved Formoterol The metabolism of Formoterol can be decreased when combined with Rolapitant. Approved, Investigational Fosamprenavir The metabolism of Rolapitant can be decreased when combined with Fosamprenavir. Approved Fosaprepitant The serum concentration of Rolapitant can be increased when it is combined with Fosaprepitant. Approved Fosphenytoin The serum concentration of Rolapitant can be decreased when it is combined with Fosphenytoin. Approved, Investigational Fostamatinib The serum concentration of Fostamatinib can be increased when it is combined with Rolapitant. Approved, Investigational Fusidic Acid The serum concentration of Rolapitant can be increased when it is combined with Fusidic Acid. Approved, Investigational Galantamine The metabolism of Galantamine can be decreased when combined with Rolapitant. Approved Gefitinib The serum concentration of Gefitinib can be increased when it is combined with Rolapitant. Approved, Investigational Glecaprevir The serum concentration of Glecaprevir can be increased when it is combined with Rolapitant. Approved, Investigational Granisetron The metabolism of Granisetron can be decreased when combined with Rolapitant. Approved, Investigational Halofantrine The metabolism of Halofantrine can be decreased when combined with Rolapitant. Approved Haloperidol The metabolism of Haloperidol can be decreased when combined with Rolapitant. Approved Halothane The metabolism of Halothane can be decreased when combined with Rolapitant. Approved, Vet Approved Hydrocodone The 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 Hydrocortisone The serum concentration of Hydrocortisone can be increased when it is combined with Rolapitant. Approved, Vet Approved Hydromorphone The metabolism of Hydromorphone can be decreased when combined with Rolapitant. Approved, Illicit Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Rolapitant. Approved Idarubicin The metabolism of Idarubicin can be decreased when combined with Rolapitant. Approved Idelalisib The serum concentration of Idelalisib can be increased when it is combined with Rolapitant. Approved Iloperidone The metabolism of Iloperidone can be decreased when combined with Rolapitant. Approved Imatinib The serum concentration of Imatinib can be increased when it is combined with Rolapitant. Approved Imipramine The metabolism of Imipramine can be decreased when combined with Rolapitant. Approved Indinavir The metabolism of Rolapitant can be decreased when combined with Indinavir. Approved Ipecac The metabolism of Ipecac can be decreased when combined with Rolapitant. Approved, Withdrawn Isavuconazole The serum concentration of Rolapitant can be increased when it is combined with Isavuconazole. Approved, Investigational Isavuconazonium The metabolism of Rolapitant can be decreased when combined with Isavuconazonium. Approved, Investigational Itraconazole The metabolism of Rolapitant can be decreased when combined with Itraconazole. Approved, Investigational Ivacaftor The serum concentration of Rolapitant can be increased when it is combined with Ivacaftor. Approved Ivermectin The serum concentration of Ivermectin can be increased when it is combined with Rolapitant. Approved, Investigational, Vet Approved Ixazomib The metabolism of Ixazomib can be decreased when combined with Rolapitant. Approved, Investigational Ketoconazole The metabolism of Rolapitant can be decreased when combined with Ketoconazole. Approved, Investigational Labetalol The metabolism of Labetalol can be decreased when combined with Rolapitant. Approved Lamotrigine The serum concentration of Lamotrigine can be increased when it is combined with Rolapitant. Approved, Investigational Ledipasvir The serum concentration of Ledipasvir can be increased when it is combined with Rolapitant. Approved Leflunomide The serum concentration of Leflunomide can be increased when it is combined with Rolapitant. Approved, Investigational Lenvatinib The serum concentration of Lenvatinib can be increased when it is combined with Rolapitant. Approved, Investigational Letermovir The metabolism of Letermovir can be decreased when combined with Rolapitant. Approved, Investigational Levetiracetam The serum concentration of Levetiracetam can be increased when it is combined with Rolapitant. Approved, Investigational Levomilnacipran The metabolism of Levomilnacipran can be decreased when combined with Rolapitant. Approved, Investigational Lisuride The metabolism of Lisuride can be decreased when combined with Rolapitant. Approved, Investigational Lofexidine The metabolism of Lofexidine can be decreased when combined with Rolapitant. Approved, Investigational Lomustine The metabolism of Lomustine can be decreased when combined with Rolapitant. Approved, Investigational Loperamide The serum concentration of Loperamide can be increased when it is combined with Rolapitant. Approved Lopinavir The metabolism of Rolapitant can be decreased when combined with Lopinavir. Approved Lorcaserin The metabolism of Lorcaserin can be decreased when combined with Rolapitant. Approved Lorpiprazole The serum concentration of Rolapitant can be increased when it is combined with Lorpiprazole. Approved Losartan The serum concentration of Losartan can be increased when it is combined with Rolapitant. Approved Lovastatin The metabolism of Rolapitant can be decreased when combined with Lovastatin. Approved, Investigational Luliconazole The serum concentration of Rolapitant can be increased when it is combined with Luliconazole. Approved Lumacaftor The serum concentration of Rolapitant can be decreased when it is combined with Lumacaftor. Approved Maprotiline The metabolism of Maprotiline can be decreased when combined with Rolapitant. Approved, Investigational Mephenytoin The metabolism of Mephenytoin can be decreased when combined with Rolapitant. Investigational, Withdrawn Mequitazine The metabolism of Mequitazine can be decreased when combined with Rolapitant. Approved Mesoridazine The metabolism of Mesoridazine can be decreased when combined with Rolapitant. Approved, Investigational Methadone The metabolism of Methadone can be decreased when combined with Rolapitant. Approved Methamphetamine The metabolism of Methamphetamine can be decreased when combined with Rolapitant. Approved, Illicit Methotrexate The serum concentration of Methotrexate can be increased when it is combined with Rolapitant. Approved Methotrimeprazine The metabolism of Methotrimeprazine can be decreased when combined with Rolapitant. Approved, Investigational Methoxyflurane The metabolism of Methoxyflurane can be decreased when combined with Rolapitant. Approved, Investigational, Vet Approved Methylprednisolone The serum concentration of Methylprednisolone can be increased when it is combined with Rolapitant. Approved, Vet Approved Methyprylon The metabolism of Methyprylon can be decreased when combined with Rolapitant. Approved, Illicit, Withdrawn Metoprolol The serum concentration of Metoprolol can be increased when it is combined with Rolapitant. Approved, Investigational Mexiletine The metabolism of Mexiletine can be decreased when combined with Rolapitant. Approved, Investigational Mianserin The metabolism of Mianserin can be decreased when combined with Rolapitant. Approved, Investigational Mibefradil The metabolism of Rolapitant can be decreased when combined with Mibefradil. Investigational, Withdrawn Miconazole The metabolism of Rolapitant can be decreased when combined with Miconazole. Approved, Investigational, Vet Approved Mifepristone The serum concentration of Rolapitant can be increased when it is combined with Mifepristone. Approved, Investigational Minaprine The metabolism of Minaprine can be decreased when combined with Rolapitant. Approved Mirabegron The metabolism of Mirabegron can be decreased when combined with Rolapitant. Approved Mirtazapine The metabolism of Mirtazapine can be decreased when combined with Rolapitant. Approved Mitotane The serum concentration of Rolapitant can be decreased when it is combined with Mitotane. Approved Mitoxantrone The serum concentration of Mitoxantrone can be increased when it is combined with Rolapitant. Approved, Investigational Moclobemide The metabolism of Moclobemide can be decreased when combined with Rolapitant. Approved, Investigational Morphine The metabolism of Morphine can be decreased when combined with Rolapitant. Approved, Investigational Mycophenolate mofetil The serum concentration of Mycophenolate mofetil can be increased when it is combined with Rolapitant. Approved, Investigational Naloxegol The serum concentration of Naloxegol can be increased when it is combined with Rolapitant. Approved Nateglinide The metabolism of Nateglinide can be decreased when combined with Rolapitant. Approved, Investigational Nebivolol The serum concentration of Nebivolol can be increased when it is combined with Rolapitant. Approved, Investigational Nefazodone The metabolism of Rolapitant can be decreased when combined with Nefazodone. Approved, Withdrawn Nelfinavir The metabolism of Rolapitant can be decreased when combined with Nelfinavir. Approved Netupitant The serum concentration of Rolapitant can be increased when it is combined with Netupitant. Approved, Investigational Nevirapine The serum concentration of Rolapitant can be decreased when it is combined with Nevirapine. Approved Nicardipine The serum concentration of Nicardipine can be increased when it is combined with Rolapitant. Approved, Investigational Nicergoline The metabolism of Nicergoline can be decreased when combined with Rolapitant. Approved, Investigational Nifedipine The serum concentration of Nifedipine can be increased when it is combined with Rolapitant. Approved Nilotinib The serum concentration of Nilotinib can be increased when it is combined with Rolapitant. Approved, Investigational Nitrofural The metabolism of Nitrofural can be decreased when combined with Rolapitant. Approved, Investigational, Vet Approved Nitrofurantoin The serum concentration of Nitrofurantoin can be increased when it is combined with Rolapitant. Approved, Vet Approved Nortriptyline The metabolism of Nortriptyline can be decreased when combined with Rolapitant. Approved Olanzapine The metabolism of Olanzapine can be decreased when combined with Rolapitant. Approved, Investigational Olaparib The metabolism of Rolapitant can be decreased when combined with Olaparib. Approved Ombitasvir The serum concentration of Ombitasvir can be increased when it is combined with Rolapitant. Approved, Investigational Omeprazole The serum concentration of Omeprazole can be increased when it is combined with Rolapitant. Approved, Investigational, Vet Approved Ondansetron The serum concentration of Ondansetron can be increased when it is combined with Rolapitant. Approved Opium The metabolism of Opium can be decreased when combined with Rolapitant. Approved, Illicit Osimertinib The serum concentration of Rolapitant can be increased when it is combined with Osimertinib. Approved Oxaliplatin The serum concentration of Oxaliplatin can be increased when it is combined with Rolapitant. Approved, Investigational Oxycodone The metabolism of Oxycodone can be decreased when combined with Rolapitant. Approved, Illicit, Investigational Paclitaxel The serum concentration of Paclitaxel can be increased when it is combined with Rolapitant. Approved, Vet Approved Palbociclib The serum concentration of Rolapitant can be increased when it is combined with Palbociclib. Approved, Investigational Palonosetron The metabolism of Palonosetron can be decreased when combined with Rolapitant. Approved, Investigational Paroxetine The metabolism of Paroxetine can be decreased when combined with Rolapitant. Approved, Investigational Pazopanib The serum concentration of Pazopanib can be increased when it is combined with Rolapitant. Approved Pentamidine The metabolism of Pentamidine can be decreased when combined with Rolapitant. Approved, Investigational Pentobarbital The serum concentration of Rolapitant can be decreased when it is combined with Pentobarbital. Approved, Investigational, Vet Approved Perospirone The metabolism of Perospirone can be decreased when combined with Rolapitant. Approved Perphenazine The metabolism of Perphenazine can be decreased when combined with Rolapitant. Approved Pethidine The metabolism of Pethidine can be decreased when combined with Rolapitant. Approved Phenacetin The metabolism of Phenacetin can be decreased when combined with Rolapitant. Withdrawn Phenformin The metabolism of Phenformin can be decreased when combined with Rolapitant. Approved, Investigational, Withdrawn Phenobarbital The serum concentration of Rolapitant can be decreased when it is combined with Phenobarbital. Approved, Investigational Phenytoin The serum concentration of Rolapitant can be decreased when it is combined with Phenytoin. Approved, Vet Approved Pibrentasvir The serum concentration of Pibrentasvir can be increased when it is combined with Rolapitant. Approved, Investigational Pimozide The serum concentration of Pimozide can be increased when it is combined with Rolapitant. Approved Pindolol The metabolism of Pindolol can be decreased when combined with Rolapitant. Approved, Investigational Piperazine The metabolism of Piperazine can be decreased when combined with Rolapitant. Approved, Vet Approved Pipotiazine The metabolism of Pipotiazine can be decreased when combined with Rolapitant. Approved, Investigational Pitavastatin The serum concentration of Pitavastatin can be increased when it is combined with Rolapitant. Approved Pitolisant The serum concentration of Pitolisant can be increased when it is combined with Rolapitant. Approved, Investigational Ponatinib The serum concentration of Ponatinib can be increased when it is combined with Rolapitant. Approved, Investigational Posaconazole The metabolism of Rolapitant can be decreased when combined with Posaconazole. Approved, Investigational, Vet Approved Pravastatin The serum concentration of Pravastatin can be increased when it is combined with Rolapitant. Approved Prazosin The serum concentration of Prazosin can be increased when it is combined with Rolapitant. Approved Prednisolone The serum concentration of Prednisolone can be increased when it is combined with Rolapitant. Approved, Vet Approved Primidone The serum concentration of Rolapitant can be decreased when it is combined with Primidone. Approved, Vet Approved Procainamide The metabolism of Procainamide can be decreased when combined with Rolapitant. Approved Progesterone The metabolism of Progesterone can be decreased when combined with Rolapitant. Approved, Vet Approved Propafenone The serum concentration of Rolapitant can be increased when it is combined with Propafenone. Approved Propofol The metabolism of Propofol can be decreased when combined with Rolapitant. Approved, Investigational, Vet Approved Propranolol The serum concentration of Propranolol can be increased when it is combined with Rolapitant. Approved, Investigational Protriptyline The metabolism of Protriptyline can be decreased when combined with Rolapitant. Approved Prucalopride The serum concentration of Prucalopride can be increased when it is combined with Rolapitant. Approved Quetiapine The serum concentration of Quetiapine can be increased when it is combined with Rolapitant. Approved Quinine The metabolism of Quinine can be decreased when combined with Rolapitant. Approved Ranitidine The serum concentration of Ranitidine can be increased when it is combined with Rolapitant. Approved Ranolazine The serum concentration of Ranolazine can be increased when it is combined with Rolapitant. Approved, Investigational Remoxipride The metabolism of Remoxipride can be decreased when combined with Rolapitant. Approved, Withdrawn Repinotan The metabolism of Repinotan can be decreased when combined with Rolapitant. Investigational Rifabutin The serum concentration of Rolapitant can be decreased when it is combined with Rifabutin. Approved, Investigational Rifampicin The serum concentration of Rolapitant can be decreased when it is combined with Rifampicin. Approved Rifapentine The serum concentration of Rolapitant can be decreased when it is combined with Rifapentine. Approved, Investigational Rifaximin The serum concentration of Rifaximin can be increased when it is combined with Rolapitant. Approved, Investigational Riluzole The serum concentration of Riluzole can be increased when it is combined with Rolapitant. Approved, Investigational Riociguat The serum concentration of Riociguat can be increased when it is combined with Rolapitant. Approved Risperidone The metabolism of Risperidone can be decreased when combined with Rolapitant. Approved, Investigational Ritonavir The metabolism of Ritonavir can be decreased when combined with Rolapitant. Approved, Investigational Ropivacaine The metabolism of Ropivacaine can be decreased when combined with Rolapitant. Approved Rotigotine The metabolism of Rotigotine can be decreased when combined with Rolapitant. Approved Rucaparib The serum concentration of Rucaparib can be increased when it is combined with Rolapitant. Approved, Investigational Rupatadine The metabolism of Rupatadine can be decreased when combined with Rolapitant. Approved Safinamide The serum concentration of Safinamide can be increased when it is combined with Rolapitant. Approved, Investigational Saquinavir The metabolism of Rolapitant can be decreased when combined with Saquinavir. Approved, Investigational Sarilumab The therapeutic efficacy of Rolapitant can be decreased when used in combination with Sarilumab. Approved, Investigational Sertindole The metabolism of Sertindole can be decreased when combined with Rolapitant. Approved, Investigational, Withdrawn Sertraline The metabolism of Sertraline can be decreased when combined with Rolapitant. Approved Sildenafil The metabolism of Rolapitant can be decreased when combined with Sildenafil. Approved, Investigational Silodosin The serum concentration of Silodosin can be increased when it is combined with Rolapitant. Approved Siltuximab The serum concentration of Rolapitant can be decreased when it is combined with Siltuximab. Approved, Investigational Simeprevir The serum concentration of Rolapitant can be increased when it is combined with Simeprevir. Approved Simvastatin The metabolism of Simvastatin can be decreased when combined with Rolapitant. Approved Sitagliptin The serum concentration of Sitagliptin can be increased when it is combined with Rolapitant. Approved, Investigational Sofosbuvir The serum concentration of Sofosbuvir can be increased when it is combined with Rolapitant. Approved Sorafenib The serum concentration of Sorafenib can be increased when it is combined with Rolapitant. Approved, Investigational Sparteine The metabolism of Sparteine can be decreased when combined with Rolapitant. Experimental St. John's Wort The serum concentration of Rolapitant can be decreased when it is combined with St. John's Wort. Approved, Investigational, Nutraceutical Stiripentol The serum concentration of Rolapitant can be increased when it is combined with Stiripentol. Approved Sulfisoxazole The metabolism of Rolapitant can be decreased when combined with Sulfisoxazole. Approved, Vet Approved Sumatriptan The serum concentration of Sumatriptan can be increased when it is combined with Rolapitant. Approved, Investigational Tamoxifen The 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 Tamsulosin The metabolism of Tamsulosin can be decreased when combined with Rolapitant. Approved, Investigational Tapentadol The metabolism of Tapentadol can be decreased when combined with Rolapitant. Approved Tegaserod The metabolism of Tegaserod can be decreased when combined with Rolapitant. Approved, Investigational, Withdrawn Telaprevir The metabolism of Rolapitant can be decreased when combined with Telaprevir. Approved, Withdrawn Telithromycin The metabolism of Rolapitant can be decreased when combined with Telithromycin. Approved Teniposide The serum concentration of Teniposide can be increased when it is combined with Rolapitant. Approved Terfenadine The metabolism of Terfenadine can be decreased when combined with Rolapitant. Approved, Withdrawn Teriflunomide The serum concentration of Teriflunomide can be increased when it is combined with Rolapitant. Approved Tesmilifene The metabolism of Tesmilifene can be decreased when combined with Rolapitant. Investigational Testosterone The serum concentration of Testosterone can be increased when it is combined with Rolapitant. Approved, Investigational Testosterone cypionate The serum concentration of Testosterone cypionate can be increased when it is combined with Rolapitant. Approved Testosterone enanthate The serum concentration of Testosterone enanthate can be increased when it is combined with Rolapitant. Approved Testosterone undecanoate The serum concentration of Testosterone undecanoate can be increased when it is combined with Rolapitant. Approved, Investigational Tetrabenazine The metabolism of Tetrabenazine can be decreased when combined with Rolapitant. Approved, Investigational Tetracycline The serum concentration of Tetracycline can be increased when it is combined with Rolapitant. Approved, Vet Approved Theophylline The metabolism of Theophylline can be decreased when combined with Rolapitant. Approved Thioridazine The serum concentration of Thioridazine can be increased when it is combined with Rolapitant. Approved, Withdrawn Ticlopidine The metabolism of Rolapitant can be decreased when combined with Ticlopidine. Approved Timolol The metabolism of Timolol can be decreased when combined with Rolapitant. Approved Tiotropium The metabolism of Tiotropium can be decreased when combined with Rolapitant. Approved Tipranavir The metabolism of Tipranavir can be decreased when combined with Rolapitant. Approved, Investigational Tocilizumab The serum concentration of Rolapitant can be decreased when it is combined with Tocilizumab. Approved Tolterodine The metabolism of Tolterodine can be decreased when combined with Rolapitant. Approved, Investigational Topiramate The serum concentration of Topiramate can be increased when it is combined with Rolapitant. Approved Topotecan The serum concentration of Topotecan can be increased when it is combined with Rolapitant. Approved, Investigational Trabectedin The metabolism of Trabectedin can be decreased when combined with Rolapitant. Approved, Investigational Tramadol The therapeutic efficacy of Tramadol can be decreased when used in combination with Rolapitant. Approved, Investigational Trazodone The metabolism of Trazodone can be decreased when combined with Rolapitant. Approved, Investigational Trimipramine The metabolism of Trimipramine can be decreased when combined with Rolapitant. Approved Umeclidinium The metabolism of Umeclidinium can be decreased when combined with Rolapitant. Approved Valbenazine The metabolism of Valbenazine can be decreased when combined with Rolapitant. Approved, Investigational Vecuronium The serum concentration of Vecuronium can be increased when it is combined with Rolapitant. Approved Velpatasvir The serum concentration of Velpatasvir can be increased when it is combined with Rolapitant. Approved, Investigational Vemurafenib The serum concentration of Rolapitant can be decreased when it is combined with Vemurafenib. Approved Venetoclax The serum concentration of Venetoclax can be increased when it is combined with Rolapitant. Approved, Investigational Venlafaxine The serum concentration of Venlafaxine can be increased when it is combined with Rolapitant. Approved Verapamil The serum concentration of Verapamil can be increased when it is combined with Rolapitant. Approved Vernakalant The metabolism of Vernakalant can be decreased when combined with Rolapitant. Approved, Investigational Vilazodone The metabolism of Vilazodone can be decreased when combined with Rolapitant. Approved Vinblastine The metabolism of Vinblastine can be decreased when combined with Rolapitant. Approved Vincristine The serum concentration of Vincristine can be increased when it is combined with Rolapitant. Approved, Investigational Vincristine The excretion of Vincristine can be decreased when combined with Rolapitant. Approved, Investigational Vinorelbine The metabolism of Vinorelbine can be decreased when combined with Rolapitant. Approved, Investigational Voriconazole The metabolism of Rolapitant can be decreased when combined with Voriconazole. Approved, Investigational Vortioxetine The metabolism of Vortioxetine can be decreased when combined with Rolapitant. Approved, Investigational Voxilaprevir The serum concentration of Voxilaprevir can be increased when it is combined with Rolapitant. Approved, Investigational Yohimbine The metabolism of Yohimbine can be decreased when combined with Rolapitant. Approved, Investigational, Vet Approved Zalcitabine The metabolism of Zalcitabine can be decreased when combined with Rolapitant. Approved, Investigational Ziprasidone The metabolism of Rolapitant can be decreased when combined with Ziprasidone. Approved Zuclopenthixol The metabolism of Zuclopenthixol can be decreased when combined with Rolapitant. Approved, Investigational - Food Interactions
- Not Available
References
- General References
- Syed YY: Rolapitant: first global approval. Drugs. 2015 Nov;75(16):1941-5. doi: 10.1007/s40265-015-0485-8. [PubMed:26467681]
- 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]
- 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
Phase Status Purpose Conditions Count 1 Completed Basic Science Prophylaxis of acute chemotherapy induced nausea and vomiting 1 1 Completed Prevention Prophylaxis of acute chemotherapy induced nausea and vomiting 2 2 Completed Prevention Nausea / Vomiting 1 2 Completed Treatment Coughing 1 2 Recruiting Supportive Care Chemo-radiation Induced Nausea and Vomiting 1 2 Recruiting Supportive Care Sarcomas 1 3 Completed Prevention Prophylaxis of acute chemotherapy induced nausea and vomiting 3
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage forms
Form Route Strength Injection, emulsion Intravenous 1.8 mg/mL Tablet Oral 90 mg/1 - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) US8470842 No 2009-01-18 2029-01-18 US US8404702 No 2009-10-09 2029-10-09 US US8796299 No 2002-12-17 2022-12-17 US US7049320 No 2003-12-08 2023-12-08 US US7981905 No 2007-04-04 2027-04-04 US US8361500 No 2009-10-09 2029-10-09 US US7563801 No 2007-04-04 2027-04-04 US US8178550 No 2007-04-04 2027-04-04 US US9101615 No 2012-07-14 2032-07-14 US
Properties
- State
- Solid
- Experimental Properties
- Not Available
- Predicted Properties
Property Value Source Water Solubility 0.00166 mg/mL ALOGPS logP 4.07 ALOGPS logP 5 ChemAxon logS -5.5 ALOGPS pKa (Strongest Acidic) 14.15 ChemAxon pKa (Strongest Basic) 8.3 ChemAxon Physiological Charge 1 ChemAxon Hydrogen Acceptor Count 3 ChemAxon Hydrogen Donor Count 2 ChemAxon Polar Surface Area 50.36 Å2 ChemAxon Rotatable Bond Count 7 ChemAxon Refractivity 118.28 m3·mol-1 ChemAxon Polarizability 46.2 Å3 ChemAxon Number of Rings 4 ChemAxon Bioavailability 0 ChemAxon Rule of Five No ChemAxon Ghose Filter No ChemAxon Veber's Rule No ChemAxon MDDR-like Rule Yes ChemAxon - Predicted ADMET features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not 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)
Yes
Antagonist
References
- 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