Details of Drug

Drug General Information (ID: D1423)
Drug Name	Rolapitant
Drug Type	Small molecule
Drug Synonymous	Rolapitant; 552292-08-7; Sch 619734; Varubi; UNII-NLE429IZUC; SCH-619734; NLE429IZUC; 914462-92-3; (5S,8S)-8-(((R)-1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)methyl)-8-phenyl-1,7-diazaspiro[4.5]decan-2-one; (5S,8S)-8-[[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]methyl]-8-phenyl-1,9-diazaspiro[4.5]decan-2-one; Rolapitant [USAN:INN]; Varuby; Varubi (TN); Rolapitant (USAN/INN); Rolapitant(sch619734); SCHEMBL354305; GTPL5749; CHEMBL3707331; CHEBI:90908; DTXSID90203740; MolPort-035-942-975; EX-A1288; BCP09609; ZINC3816514 Click to Show/Hide
Disease Class	MD90: Nausea/vomiting
Therapeutic Class	Nk1 Receptor Antagonists
Structure
Structure	3D Structure		2D Structure
Formula	C25H26F6N2O2
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
InChIKey	FIVSJYGQAIEMOC-ZGNKEGEESA-N
Canonical SMILES	CC(C1=CC(=CC(=C1)C(F)(F)F)C(F)(F)F)OCC2(CCC3(CCC(=O)N3)CN2)C4=CC=CC=C4
External Link
	Pubchem ID	10311306
	CAS Number	552292-08-7
	CHEBI ID	90908
	TTD ID	D0CF0Y

Drug-Drug Interaction Network
Sunburst Graph		Legend Information AM002 Affected cellular transport AM004 Affected intra/extra-hepatic metabolism BM010 Transporter inhibition BM017 CYP450 enzyme inhibition BM022 CYP450 enzyme induction
Relation Graph

Full list of drugs interacting with Rolapitant
Affected cellular transport
	Transporter inhibition					Drug Num: 78
Drug ID		Drug Name	Formula	Pubchem ID	Severity Level		Interaction Detail	REF
D0380		Colchicine	C22H25NO6	6167	Major		Inter Info	[3], [4], [5]
D0551		Edoxaban	C24H30ClN7O4S	10280735	Major		Inter Info	[1], [6], [7], [8]
D0171		Berotralstat	C30H26F4N6O	137528262	Major		Inter Info	[14]
D0176		Betrixaban	C23H22ClN5O3	10275777	Major		Inter Info	[15], [16], [17]
D1211		Ozanimod	C23H24N4O3	52938427	Major		Inter Info	[11], [19]
D1388		Relugolix	C29H27F2N7O5S	10348973	Major		Inter Info	[20]
D1688		Venetoclax	C45H50ClN7O7S	49846579	Major		Inter Info	[11], [1], [21]
D0038		Aliskiren	C30H53N3O6	5493444	Moderate		Inter Info	[2]
D0096		Apixaban	C25H25N5O4	10182969	Moderate		Inter Info	[2]
D0109		Artesunate	C19H28O8	6917864	Moderate		Inter Info	[2]
D0195		Bosutinib	C26H29Cl2N5O3	5328940	Moderate		Inter Info	[2]
D0199		Brentuximab vedotin	NA	NA	Moderate		Inter Info	[68], [69]
D0302		Ceritinib	C28H36ClN5O3S	57379345	Moderate		Inter Info	[2]
D0376		Cobimetinib	C21H21F3IN3O2	16222096	Moderate		Inter Info	[2]
D0402		Cyclosporine	C62H111N11O12	5284373	Moderate		Inter Info	[2]
D0408		Daclatasvir	C40H50N8O6	25154714	Moderate		Inter Info	[2]
D0429		Daunorubicin	C27H29NO10	30323	Moderate		Inter Info	[2]
D0430		Daunorubicin (liposomal)	C27H29NO10	30323	Moderate		Inter Info	[82], [83], [84]
D0491		Digoxin	C41H64O14	2724385	Moderate		Inter Info	[2]
D0511		Docetaxel	C43H53NO14	148124	Moderate		Inter Info	[2]
D0528		Doxorubicin	C27H29NO11	31703	Moderate		Inter Info	[2]
D0529		Doxorubicin (liposomal)	C27H29NO11	31703	Moderate		Inter Info	[2]
D0584		Epirubicin	C27H29NO11	41867	Moderate		Inter Info	[2]
D0595		Erlotinib	C22H23N3O4	176870	Moderate		Inter Info	[2]
D0597		Erythromycin	C37H67NO13	12560	Moderate		Inter Info	[2]
D0627		Etoposide	C29H32O13	36462	Moderate		Inter Info	[2]
D0629		Everolimus	C53H83NO14	6442177	Moderate		Inter Info	[2]
D0656		Fexofenadine	C32H39NO4	3348	Moderate		Inter Info	[2]
D0665		Flibanserin	C20H21F3N4O	6918248	Moderate		Inter Info	[2]
D0788		Idarubicin	C26H27NO9	42890	Moderate		Inter Info	[2]
D0845		Irinotecan	C33H38N4O6	60838	Moderate		Inter Info	[2]
D0846		Irinotecan (liposomal)	C33H38N4O6	60838	Moderate		Inter Info	[2]
D0894		Lapatinib	C29H26ClFN4O4S	208908	Moderate		Inter Info	[2]
D0930		Linagliptin	C25H28N8O2	10096344	Moderate		Inter Info	[2]
D0947		Loperamide	C29H33ClN2O2	3955	Moderate		Inter Info	[2]
D0980		Maraviroc	C29H41F2N5O	3002977	Moderate		Inter Info	[2]
D1025		Methotrexate	C20H22N8O5	126941	Moderate		Inter Info	[2]
D1136		Nilotinib	C28H22F3N7O	644241	Moderate		Inter Info	[11], [91], [2]
D1139		Nintedanib	C31H33N5O4	135423438	Moderate		Inter Info	[2]
D1212		Paclitaxel	C47H51NO14	36314	Moderate		Inter Info	[2]
D1213		Paclitaxel (protein-bound)	C47H51NO14	36314	Moderate		Inter Info	[2]
D1232		Pazopanib	C21H23N7O2S	10113978	Moderate		Inter Info	[2]
D1315		Posaconazole	C37H42F2N8O4	468595	Moderate		Inter Info	[2]
D1371		Quinidine	C20H24N2O2	441074	Moderate		Inter Info	[2]
D1383		Ranolazine	C24H33N3O4	56959	Moderate		Inter Info	[2]
D1402		Rifaximin	C43H51N3O11	6436173	Moderate		Inter Info	[2]
D1417		Rivaroxaban	C19H18ClN3O5S	9875401	Moderate		Inter Info	[2]
D0181		Bictegravir	C21H18F3N3O5	90311989	Moderate		Inter Info	[2]
D0182		Binimetinib	C17H15BrF2N4O3	10288191	Moderate		Inter Info	[2]
D0720		Gilteritinib	C29H44N8O3	49803313	Moderate		Inter Info	[2]
D0896		Larotrectinib	C21H22F2N6O2	46188928	Moderate		Inter Info	[2]
D0901		Lemborexant	C22H20F2N4O2	56944144	Moderate		Inter Info	[2]
D0963		Lusutrombopag	C29H32Cl2N2O5S	49843517	Moderate		Inter Info	[2]
D1101		Naldemedine	C32H34N4O6	54732242	Moderate		Inter Info	[2]
D1140		Niraparib	C19H20N4O	24958200	Moderate		Inter Info	[2]
D1407		Rimegepant	C28H28F2N6O3	51049968	Moderate		Inter Info	[98]
D1409		Ripretinib	C24H21BrFN5O2	71584930	Moderate		Inter Info	[2]
D1532		Talazoparib	C19H14F2N6O	135565082	Moderate		Inter Info	[2]
D1663		Ubrogepant	C29H26F3N5O3	68748835	Moderate		Inter Info	[100], [2]
D1424		Romidepsin	C24H36N4O6S2	5352062	Moderate		Inter Info	[101], [2]
D1430		Rosuvastatin	C22H28FN3O6S	446157	Moderate		Inter Info	[2]
D1449		Saxagliptin	C18H25N3O2	11243969	Moderate		Inter Info	[2]
D1466		Silodosin	C25H32F3N3O4	5312125	Moderate		Inter Info	[2]
D1476		Sirolimus	C51H79NO13	5284616	Moderate		Inter Info	[2]
D1477		Sitagliptin	C16H15F6N5O	4369359	Moderate		Inter Info	[2]
D1517		Sulfasalazine	C18H14N4O5S	5339	Moderate		Inter Info	[2]
D1556		Teriflunomide	C12H9F3N2O2	54684141	Moderate		Inter Info	[2]
D1579		Ticagrelor	C23H28F2N6O4S	9871419	Moderate		Inter Info	[2]
D1592		Tipranavir	C31H33F3N2O5S	54682461	Moderate		Inter Info	[2]
D1608		Tolvaptan	C26H25ClN2O3	216237	Moderate		Inter Info	[105]
D1610		Topotecan	C23H23N3O5	60700	Moderate		Inter Info	[2]
D1697		Vinblastine	C46H58N4O9	13342	Moderate		Inter Info	[2]
D1698		Vincristine	C46H56N4O10	5978	Moderate		Inter Info	[2]
D1699		Vincristine (liposome)	C46H56N4O10	5978	Moderate		Inter Info	[2]
D1700		Vinorelbine	C45H54N4O8	5311497	Moderate		Inter Info	[2]
D0658		Fidaxomicin	C52H74Cl2O18	10034073	Minor		Inter Info	[11], [1], [109]
D0797		Indacaterol	C24H28N2O3	6918554	Minor		Inter Info	[110]
D1104		Naloxegol	C34H53NO11	56959087	Minor		Inter Info	[111]
Affected intra/extra-hepatic metabolism
	CYP450 enzyme inhibition					Drug Num: 69
Drug ID		Drug Name	Formula	Pubchem ID	Severity Level		Interaction Detail	REF
D0559		Eliglustat	C23H36N2O4	23652731	Major		Inter Info	[9], [2]
D1292		Pimozide	C28H29F2N3O	16362	Major		Inter Info	[10], [11], [1], [12], [13], [2]
D1169		Oliceridine	C22H30N2O2S	66553195	Major		Inter Info	[18], [2]
D1533		Tamoxifen	C26H29NO	2733526	Major		Inter Info	[22], [23], [24], [25], [26], [27], [28], [29], [30], [31], [32], [33], [34], [35], [36], [37], [38], [39], [40], [41], [42], [43], [44], [45], [46], [47], [2], [48], [49], [50], [51], [52], [53], [54], [55]
D1574		Thioridazine	C21H26N2S2	5452	Major		Inter Info	[56], [57], [58], [59], [60], [61], [62], [63], [64], [65], [2], [66], [67]
D0068		Amitriptyline	C20H23N	2160	Moderate		Inter Info	[2]
D0074		Amphetamine	C9H13N	3007	Moderate		Inter Info	[2]
D0105		Aripiprazole	C23H27Cl2N3O2	60795	Moderate		Inter Info	[2]
D0119		Atomoxetine	C17H21NO	54841	Moderate		Inter Info	[2]
D0202		Brexpiprazole	C25H27N3O2S	11978813	Moderate		Inter Info	[2]
D0267		Carvedilol	C24H26N2O4	2585	Moderate		Inter Info	[2]
D0323		Chlorpheniramine	C16H19ClN2	2725	Moderate		Inter Info	[2]
D0324		Chlorpromazine	C17H19ClN2S	2726	Moderate		Inter Info	[2]
D0361		Clomipramine	C19H23ClN2	2801	Moderate		Inter Info	[2]
D0370		Clozapine	C18H19ClN4	135398737	Moderate		Inter Info	[2]
D0379		Codeine	C18H21NO3	5284371	Moderate		Inter Info	[70], [71], [72], [73], [74], [75], [2], [76], [77], [78], [79], [80], [81]
D0424		Darifenacin	C28H30N2O2	444031	Moderate		Inter Info	[2]
D0446		Desipramine	C18H22N2	2995	Moderate		Inter Info	[2]
D0457		Dexfenfluramine	C12H16F3N	66265	Moderate		Inter Info	[2]
D0466		Dextromethorphan	C18H25NO	5360696	Moderate		Inter Info	[2]
D0467		Dextropropoxyphene	C22H29NO2	10100	Moderate		Inter Info	[85], [2], [86]
D0502		Diphenhydramine	C17H21NO	3100	Moderate		Inter Info	[2]
D0525		Doxepin	C19H21NO	667477	Moderate		Inter Info	[2]
D0526		Doxepin (topical)	C19H21NO	667477	Moderate		Inter Info	[85], [2], [86]
D0539		Duloxetine	C18H19NOS	60835	Moderate		Inter Info	[2]
D0641		Fenfluramine	C12H16F3N	3337	Moderate		Inter Info	[2]
D0664		Flecainide	C17H20F6N2O3	3356	Moderate		Inter Info	[2]
D0676		Fluoxetine	C17H18F3NO	3386	Moderate		Inter Info	[2]
D0678		Fluphenazine	C22H26F3N3OS	3372	Moderate		Inter Info	[2]
D0687		Fluvoxamine	C15H21F3N2O2	5324346	Moderate		Inter Info	[2]
D0707		Galantamine	C17H21NO3	9651	Moderate		Inter Info	[2]
D0750		Haloperidol	C21H23ClFNO2	3559	Moderate		Inter Info	[2]
D0791		Iloperidone	C24H27FN2O4	71360	Moderate		Inter Info	[2]
D0795		Imipramine	C19H24N2	3696	Moderate		Inter Info	[2]
D0979		Maprotiline	C20H23N	4011	Moderate		Inter Info	[2]
D0987		Meclizine	C25H27ClN2	4034	Moderate		Inter Info	[2]
D1010		Mesoridazine	C21H26N2OS2	4078	Moderate		Inter Info	[2]
D1012		Metamfetamine	C10H15N	10836	Moderate		Inter Info	[85], [2], [86]
D1026		Methotrimeprazine	C19H24N2OS	72287	Moderate		Inter Info	[2]
D1046		Metoclopramide	C14H22ClN3O2	4168	Moderate		Inter Info	[2]
D1049		Metoprolol	C15H25NO3	4171	Moderate		Inter Info	[2]
D1054		Mexiletine	C11H17NO	4178	Moderate		Inter Info	[2]
D1061		Midodrine	C12H18N2O4	4195	Moderate		Inter Info	[2]
D1075		Mirtazapine	C17H19N3	4205	Moderate		Inter Info	[87], [88], [2], [89], [90]
D1114		Nebivolol	C22H25F2NO4	71301	Moderate		Inter Info	[2]
D1158		Nortriptyline	C19H21N	4543	Moderate		Inter Info	[2]
D1229		Paroxetine	C19H20FNO3	43815	Moderate		Inter Info	[2]
D1257		Perphenazine	C21H26ClN3OS	4748	Moderate		Inter Info	[2]
D1299		Pirfenidone	C12H11NO	40632	Moderate		Inter Info	[1], [92], [2]
D1352		Promethazine	C17H20N2S	4927	Moderate		Inter Info	[2]
D1353		Propafenone	C21H27NO3	4932	Moderate		Inter Info	[2]
D1357		Propranolol	C16H21NO2	4946	Moderate		Inter Info	[2]
D1361		Protriptyline	C19H21N	4976	Moderate		Inter Info	[2]
D1413		Risperidone	C23H27FN4O2	5073	Moderate		Inter Info	[2]
D1415		Ritonavir	C37H48N6O5S2	392622	Moderate		Inter Info	[2]
D0002		Abametapir (topical)	C12H12N2	15664	Moderate		Inter Info	[93]
D0699		Fostamatinib	C23H26FN6O9P	11671467	Moderate		Inter Info	[95]
D0899		Lefamulin	C28H45NO5S	25185057	Moderate		Inter Info	[85], [96], [86]
D1302		Pitolisant	C17H26ClNO	9948102	Moderate		Inter Info	[1], [2], [97]
D1534		Tamsulosin	C20H28N2O5S	129211	Moderate		Inter Info	[102], [103], [104], [2]
D1560		Tetrabenazine	C19H27NO3	6018	Moderate		Inter Info	[2]
D1585		Timolol	C13H24N4O3S	33624	Moderate		Inter Info	[2]
D1586		Timolol (ophthalmic)	C13H24N4O3S	33624	Moderate		Inter Info	[85], [2], [86]
D1616		Tramadol	C16H25NO2	33741	Moderate		Inter Info	[2]
D1624		Trazodone	C19H22ClN5O	5533	Moderate		Inter Info	[2]
D1647		Trimipramine	C20H26N2	5584	Moderate		Inter Info	[2]
D1708		Vortioxetine	C18H22N2S	9966051	Moderate		Inter Info	[2]
D0516		Donepezil	C24H29NO3	3152	Minor		Inter Info	[106], [2], [107], [108]
D1607		Tolterodine	C22H31NO	443879	Minor		Inter Info	[112], [113], [2]
	CYP450 enzyme induction					Drug Num: 51
Drug ID		Drug Name	Formula	Pubchem ID	Severity Level		Interaction Detail	REF
D0255		Carbamazepine	C15H12N2O	2554	Major		Inter Info	[1], [2]
D0578		Enzalutamide	C21H16F4N4O2S	15951529	Major		Inter Info	[1], [2]
D0697		Fosphenytoin	C16H15N2O6P	56339	Major		Inter Info	[1], [2]
D0958		Lumacaftor	C24H18F2N2O5	16678941	Major		Inter Info	[1], [2]
D1078		Mitotane	C14H10Cl4	4211	Major		Inter Info	[1], [2]
D1265		Phenobarbital	C12H12N2O3	4763	Major		Inter Info	[1], [2]
D1283		Phenytoin	C15H12N2O2	1775	Major		Inter Info	[1], [2]
D1340		Primidone	C12H14N2O2	4909	Major		Inter Info	[1], [2]
D1399		Rifabutin	C46H62N4O11	135398743	Major		Inter Info	[1], [2]
D1400		Rifampicin	C43H58N4O12	135398735	Major		Inter Info	[1], [2]
D1401		Rifapentine	C47H64N4O12	135403821	Major		Inter Info	[1], [2]
D0095		Apalutamide	C21H15F4N5O2S	24872560	Major		Inter Info	[1], [2]
D1502		St. John's Wort	NA	NA	Major		Inter Info	[1], [2]
D0061		Aminoglutethimide	C13H16N2O2	2145	Moderate		Inter Info	[2]
D0071		Amobarbital	C11H18N2O3	2164	Moderate		Inter Info	[2]
D0106		Armodafinil	C15H15NO2S	9690109	Moderate		Inter Info	[2]
D0178		Bexarotene	C24H28O2	82146	Moderate		Inter Info	[2]
D0194		Bosentan	C27H29N5O6S	104865	Moderate		Inter Info	[1], [2]
D0224		Butabarbital	C10H16N2O3	2479	Moderate		Inter Info	[2]
D0225		Butalbital	C11H16N2O3	2481	Moderate		Inter Info	[2]
D0300		Cenobamate	C10H10ClN5O2	11962412	Moderate		Inter Info	[2]
D0432		Deferasirox	C21H15N3O4	214348	Moderate		Inter Info	[2]
D0453		Dexamethasone	C22H29FO5	5743	Moderate		Inter Info	[1], [2]
D0554		Efavirenz	C14H9ClF3NO2	64139	Moderate		Inter Info	[1], [2]
D0628		Etravirine	C20H15BrN6O	193962	Moderate		Inter Info	[1], [2]
D0639		Felbamate	C11H14N2O4	3331	Moderate		Inter Info	[2]
D0741		Griseofulvin	C17H17ClO6	441140	Moderate		Inter Info	[2]
D1040		Methylphenobarbital	C13H14N2O3	8271	Moderate		Inter Info	[2]
D1050		Metreleptin	NA	NA	Moderate		Inter Info	[2]
D1081		Modafinil	C15H15NO2S	4236	Moderate		Inter Info	[1], [2]
D1099		Nafcillin	C21H22N2O5S	8982	Moderate		Inter Info	[2]
D1128		Nevirapine	C15H14N4O	4463	Moderate		Inter Info	[1], [2]
D1198		Oxcarbazepine	C15H12N2O2	34312	Moderate		Inter Info	[2]
D1248		Pentobarbital	C11H18N2O3	4737	Moderate		Inter Info	[2]
D1274		Phenylbutazone	C19H20N2O2	4781	Moderate		Inter Info	[2]
D0545		Echinacea	NA	NA	Moderate		Inter Info	[11], [94]
D0555		Elagolix	C32H30F5N3O5	11250647	Moderate		Inter Info	[2]
D0601		Eslicarbazepine	C15H14N2O2	9881504	Moderate		Inter Info	[1], [2]
D0872		Ivosidenib	C28H22ClF3N6O3	71657455	Moderate		Inter Info	[2]
D0953		Lorlatinib	C21H19FN6O2	71731823	Moderate		Inter Info	[2]
D1258		Pexidartinib	C20H15ClF3N5	25151352	Moderate		Inter Info	[2]
D1493		Somapacitan	C54H95N13O20S2	129894493	Moderate		Inter Info	[2]
D1538		Tazemetostat	C34H44N4O4	66558664	Moderate		Inter Info	[2]
D1546		Telotristat ethyl	C27H26ClF3N6O3	25181577	Moderate		Inter Info	[1], [99]
D1433		Rufinamide	C10H8F2N4O	129228	Moderate		Inter Info	[2]
D1453		Secobarbital	C12H18N2O3	5193	Moderate		Inter Info	[2]
D1494		Somatotropin	NA	NA	Moderate		Inter Info	[2]
D1495		Somatrem	C43H72N14O14	5487805	Moderate		Inter Info	[2]
D1518		Sulfinpyrazone	C23H20N2O3S	5342	Moderate		Inter Info	[2]
D1652		Troglitazone	C24H27NO5S	5591	Moderate		Inter Info	[2]
D1687		Vemurafenib	C23H18ClF2N3O3S	42611257	Moderate		Inter Info	[2]

References
1	Cerner Multum, Inc. "UK Summary of Product Characteristics.".
2	Product Information. Varubi (rolapitant). Tesaro Inc., Waltham, MA.
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