Details of Drug

Drug General Information (ID: D1324)
Drug Name	Pralsetinib
Drug Type	Small molecule
Drug Synonymous	GBLBJPZSROAGMF-SIYOEGHHSA-N; Blu667; 2097132-94-8; SCHEMBL18806610; SCHEMBL18789229; SCHEMBL18789228; GTPL10033; BLU-668; EX-A1944; HY-112301; CS-0044766; N-[(1S)-1-[6-(4-fluoropyrazol-1-yl)pyridin-3-yl]ethyl]-1-methoxy-4-[4-methyl-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl]cyclohexane-1-carboxamide Click to Show/Hide
Disease Class	2A00-2F9Z: Solid tumour/cancer; 2C25: Lung cancer
Therapeutic Class	Multikinase Inhibitors
Structure
Structure	3D Structure		2D Structure
Formula	C27H32FN9O2
InChI	1S/C27H32FN9O2/c1-16-11-22(33-23-12-17(2)35-36-23)34-25(31-16)19-7-9-27(39-4,10-8-19)26(38)32-18(3)20-5-6-24(29-13-20)37-15-21(28)14-30-37/h5-6,11-15,18-19H,7-10H2,1-4H3,(H,32,38)(H2,31,33,34,35,36)/t18-,19?,27?/m0/s1
InChIKey	GBLBJPZSROAGMF-SIYOEGHHSA-N
Canonical SMILES	CC1=CC(=NN1)NC2=NC(=NC(=C2)C)C3CCC(CC3)(C(=O)NC(C)C4=CN=C(C=C4)N5C=C(C=N5)F)OC
External Link
	Pubchem ID	129073603
	CAS Number	2097132-94-8
	TTD ID	D0OD2I

Drug-Drug Interaction Network
Sunburst Graph		Legend Information AM002 Affected cellular transport AM004 Affected intra/extra-hepatic metabolism AM006 Pharmacodynamic additive effects BM010 Transporter inhibition BM017 CYP450 enzyme inhibition BM022 CYP450 enzyme induction BM055 Increased risk of hepatotoxicity
Relation Graph

Full list of drugs interacting with Pralsetinib
Affected cellular transport
	Transporter inhibition					Drug Num: 4
Drug ID		Drug Name	Formula	Pubchem ID	Severity Level		Interaction Detail	REF
D0044		Alpelisib	C19H22F3N5O2S	56649450	Moderate		Inter Info	[10], [11], [12]
D0720		Gilteritinib	C29H44N8O3	49803313	Moderate		Inter Info	[16], [10], [30]
D0725		Glasdegib	C21H22N6O	25166913	Moderate		Inter Info	[10], [31]
D1608		Tolvaptan	C26H25ClN2O3	216237	Moderate		Inter Info	[16], [10], [42], [43]
Affected intra/extra-hepatic metabolism
	CYP450 enzyme inhibition					Drug Num: 78
Drug ID		Drug Name	Formula	Pubchem ID	Severity Level		Interaction Detail	REF
D0080		Amprenavir	C25H35N3O6S	65016	Major		Inter Info	[1], [2]
D0116		Atazanavir	C38H52N6O7	148192	Major		Inter Info	[1]
D0192		Boceprevir	C27H45N5O5	10324367	Major		Inter Info	[1], [2]
D0302		Ceritinib	C28H36ClN5O3S	57379345	Major		Inter Info	[1]
D0349		Clarithromycin	C38H69NO13	84029	Major		Inter Info	[1]
D0375		Cobicistat	C40H53N7O5S2	25151504	Major		Inter Info	[1]
D0386		Conivaptan	C32H26N4O2	151171	Major		Inter Info	[1]
D0439		Delavirdine	C22H28N6O3S	5625	Major		Inter Info	[1], [2]
D0692		Fosamprenavir	C25H36N3O9PS	131536	Major		Inter Info	[1]
D0789		Idelalisib	C22H18FN7O	11625818	Major		Inter Info	[1]
D0799		Indinavir	C36H47N5O4	5362440	Major		Inter Info	[1]
D0867		Itraconazole	C35H38Cl2N8O4	55283	Major		Inter Info	[1]
D0880		Ketoconazole	C26H28Cl2N4O4	456201	Major		Inter Info	[1]
D0946		Lonafarnib	C27H31Br2ClN4O2	148195	Major		Inter Info	[1], [4]
D1119		Nelfinavir	C32H45N3O4S	64143	Major		Inter Info	[1]
D1315		Posaconazole	C37H42F2N8O4	468595	Major		Inter Info	[1]
D1415		Ritonavir	C37H48N6O5S2	392622	Major		Inter Info	[1]
D1444		Saquinavir	C38H50N6O5	441243	Major		Inter Info	[1]
D1541		Telaprevir	C36H53N7O6	3010818	Major		Inter Info	[1], [2]
D1544		Telithromycin	C43H65N5O10	3002190	Major		Inter Info	[1], [2]
D1653		Troleandomycin	C41H67NO15	202225	Major		Inter Info	[1], [2]
D1660		Tucatinib	C26H24N8O2	51039094	Major		Inter Info	[1], [2]
D1706		Voriconazole	C16H14F3N5O	71616	Major		Inter Info	[1]
D0002		Abametapir (topical)	C12H12N2	15664	Moderate		Inter Info	[1]
D0007		Abiraterone	C24H31NO	132971	Moderate		Inter Info	[1]
D0030		Aldesleukin	NA	NA	Moderate		Inter Info	[1]
D0066		Amiodarone	C25H29I2NO3	2157	Moderate		Inter Info	[1]
D0069		Amlodipine	C20H25ClN2O5	2162	Moderate		Inter Info	[1]
D0100		Aprepitant	C23H21F7N4O3	135413536	Moderate		Inter Info	[1]
D0180		Bicalutamide	C18H14F4N2O4S	2375	Moderate		Inter Info	[1]
D0313		Chloramphenicol	C11H12Cl2N2O5	5959	Moderate		Inter Info	[1]
D0337		Cimetidine	C10H16N6S	2756	Moderate		Inter Info	[1]
D0341		Ciprofloxacin	C17H18FN3O3	2764	Moderate		Inter Info	[1]
D0367		Clotrimazole	C22H17ClN2	2812	Moderate		Inter Info	[1]
D0393		Crizotinib	C21H22Cl2FN5O	11626560	Moderate		Inter Info	[1]
D0402		Cyclosporine	C62H111N11O12	5284373	Moderate		Inter Info	[1]
D0413		Dalfopristin	C34H50N4O9S	6323289	Moderate		Inter Info	[1]
D0416		Danazol	C22H27NO2	28417	Moderate		Inter Info	[1]
D0426		Darunavir	C27H37N3O7S	213039	Moderate		Inter Info	[1]
D0428		Dasatinib	C22H26ClN7O2S	3062316	Moderate		Inter Info	[1]
D0497		Diltiazem	C22H26N2O4S	39186	Moderate		Inter Info	[1]
D0534		Dronedarone	C31H44N2O5S	208898	Moderate		Inter Info	[1]
D0597		Erythromycin	C37H67NO13	12560	Moderate		Inter Info	[1]
D0638		Fedratinib	C27H36N6O3S	16722836	Moderate		Inter Info	[1]
D0665		Flibanserin	C20H21F3N4O	6918248	Moderate		Inter Info	[1]
D0667		Fluconazole	C13H12F2N6O	3365	Moderate		Inter Info	[1]
D0687		Fluvoxamine	C15H21F3N2O2	5324346	Moderate		Inter Info	[1]
D0693		Fosaprepitant	C23H22F7N4O6P	135413538	Moderate		Inter Info	[1]
D0696		Fosnetupitant	C31H35F6N4O5P	71544786	Moderate		Inter Info	[1]
D0721		Ginger	C30H40O6	442138	Moderate		Inter Info	[1]
D0740		Grepafloxacin	C19H22FN3O3	72474	Moderate		Inter Info	[1]
D0793		Imatinib	C29H31N7O	5291	Moderate		Inter Info	[1]
D0852		Isavuconazonium	C35H35F2N8O5S+	6918606	Moderate		Inter Info	[1]
D0858		Isoniazid	C6H7N3O	3767	Moderate		Inter Info	[1]
D0869		Ivacaftor	C24H28N2O3	16220172	Moderate		Inter Info	[1]
D0891		Lanreotide	C54H69N11O10S2	71349	Moderate		Inter Info	[1]
D0894		Lapatinib	C29H26ClFN4O4S	208908	Moderate		Inter Info	[1]
D0896		Larotrectinib	C21H22F2N6O2	46188928	Moderate		Inter Info	[1]
D0901		Lemborexant	C22H20F2N4O2	56944144	Moderate		Inter Info	[1]
D0906		Letermovir	C29H28F4N4O4	45138674	Moderate		Inter Info	[1]
D1063		Mifepristone	C29H35NO2	55245	Moderate		Inter Info	[1]
D1127		Netupitant	C30H32F6N4O	6451149	Moderate		Inter Info	[1]
D1163		Octreotide	C49H66N10O10S2	448601	Moderate		Inter Info	[1]
D1189		Osilodrostat	C13H10FN3	44139752	Moderate		Inter Info	[1]
D1190		Osimertinib	C28H33N7O2	71496458	Moderate		Inter Info	[1]
D1214		Palbociclib	C24H29N7O2	5330286	Moderate		Inter Info	[1]
D1230		Pasireotide	C58H66N10O9	9941444	Moderate		Inter Info	[1]
D1232		Pazopanib	C21H23N7O2S	10113978	Moderate		Inter Info	[1]
D0735		Goldenseal	NA	NA	Moderate		Inter Info	[1]
D1383		Ranolazine	C24H33N3O4	56959	Moderate		Inter Info	[1]
D1398		Ribociclib	C23H30N8O	44631912	Moderate		Inter Info	[1]
D1432		Rucaparib	C19H18FN3O	9931954	Moderate		Inter Info	[1]
D1505		Stiripentol	C14H18O3	5311454	Moderate		Inter Info	[1]
D1524		Suvorexant	C23H23ClN6O2	24965990	Moderate		Inter Info	[1]
D1579		Ticagrelor	C23H28F2N6O4S	9871419	Moderate		Inter Info	[1]
D1690		Verapamil	C27H38N2O4	2520	Moderate		Inter Info	[1]
D1709		Voxelotor	C19H19N3O3	71602803	Moderate		Inter Info	[1]
D1714		Zafirlukast	C31H33N3O6S	5717	Moderate		Inter Info	[1]
	CYP450 enzyme induction					Drug Num: 28
Drug ID		Drug Name	Formula	Pubchem ID	Severity Level		Interaction Detail	REF
D0095		Apalutamide	C21H15F4N5O2S	24872560	Major		Inter Info	[1]
D0255		Carbamazepine	C15H12N2O	2554	Major		Inter Info	[1]
D0578		Enzalutamide	C21H16F4N4O2S	15951529	Major		Inter Info	[1]
D0697		Fosphenytoin	C16H15N2O6P	56339	Major		Inter Info	[1]
D0958		Lumacaftor	C24H18F2N2O5	16678941	Major		Inter Info	[5], [1]
D1078		Mitotane	C14H10Cl4	4211	Major		Inter Info	[1]
D1265		Phenobarbital	C12H12N2O3	4763	Major		Inter Info	[1]
D1283		Phenytoin	C15H12N2O2	1775	Major		Inter Info	[1]
D1340		Primidone	C12H14N2O2	4909	Major		Inter Info	[1]
D1399		Rifabutin	C46H62N4O11	135398743	Major		Inter Info	[1]
D1400		Rifampicin	C43H58N4O12	135398735	Major		Inter Info	[5], [1]
D1401		Rifapentine	C47H64N4O12	135403821	Major		Inter Info	[1]
D1502		St. John's Wort	NA	NA	Major		Inter Info	[1]
D0194		Bosentan	C27H29N5O6S	104865	Moderate		Inter Info	[1]
D0300		Cenobamate	C10H10ClN5O2	11962412	Moderate		Inter Info	[1]
D0406		Dabrafenib	C23H20F3N5O2S2	44462760	Moderate		Inter Info	[1]
D0453		Dexamethasone	C22H29FO5	5743	Moderate		Inter Info	[1]
D0554		Efavirenz	C14H9ClF3NO2	64139	Moderate		Inter Info	[1]
D0601		Eslicarbazepine	C15H14N2O2	9881504	Moderate		Inter Info	[1]
D0628		Etravirine	C20H15BrN6O	193962	Moderate		Inter Info	[1]
D0953		Lorlatinib	C21H19FN6O2	71731823	Moderate		Inter Info	[1]
D1081		Modafinil	C15H15NO2S	4236	Moderate		Inter Info	[1]
D1099		Nafcillin	C21H22N2O5S	8982	Moderate		Inter Info	[1]
D1128		Nevirapine	C15H14N4O	4463	Moderate		Inter Info	[1]
D1493		Somapacitan	C54H95N13O20S2	129894493	Moderate		Inter Info	[16], [10], [38]
D1494		Somatotropin	NA	NA	Moderate		Inter Info	[16], [10], [38]
D1495		Somatrem	C43H72N14O14	5487805	Moderate		Inter Info	[16], [10], [38]
D1546		Telotristat ethyl	C27H26ClF3N6O3	25181577	Moderate		Inter Info	[1], [39]
Pharmacodynamic additive effects
	Increased risk of hepatotoxicity					Drug Num: 19
Drug ID		Drug Name	Formula	Pubchem ID	Severity Level		Interaction Detail	REF
D0944		Lomitapide	C39H37F6N3O2	9853053	Major		Inter Info	[3]
D1258		Pexidartinib	C20H15ClF3N5	25151352	Major		Inter Info	[6]
D1556		Teriflunomide	C12H9F3N2O2	54684141	Major		Inter Info	[7], [8], [9]
D0113		Asparaginase Erwinia chrysanthemi	NA	NA	Moderate		Inter Info	[13], [14], [15], [16], [10], [17], [18], [19], [20], [21], [22], [23], [24]
D0114		Asparaginase Escherichia coli	NA	NA	Moderate		Inter Info	[14], [16], [23]
D0149		Bedaquiline	C32H31BrN2O2	5388906	Moderate		Inter Info	[25]
D0199		Brentuximab vedotin	NA	NA	Moderate		Inter Info	[26]
D0232		Calaspargase pegol	NA	NA	Moderate		Inter Info	[13], [14], [15], [16], [10], [17], [18], [19], [20], [21], [22], [23], [24]
D0248		Cannabidiol	C21H30O2	644019	Moderate		Inter Info	[10], [27]
D0357		Clofarabine	C10H11ClFN5O3	119182	Moderate		Inter Info	[28]
D0584		Epirubicin	C27H29NO11	41867	Moderate		Inter Info	[16], [10], [29]
D0826		Interferon beta-1a	NA	NA	Moderate		Inter Info	[32], [33], [34], [35]
D0827		Interferon beta-1b	NA	NA	Moderate		Inter Info	[32], [33], [34], [35]
D1025		Methotrexate	C20H22N8O5	126941	Moderate		Inter Info	[10], [36]
D1106		Naltrexone	C20H23NO4	5360515	Moderate		Inter Info	[37]
D1234		Pegaspargase	C14H19NO	436058	Moderate		Inter Info	[13], [14], [15], [16], [10], [17], [18], [19], [20], [21], [22], [23], [24]
D1239		Peginterferon beta-1a	NA	NA	Moderate		Inter Info	[32], [33], [34], [35]
D1589		Tioguanine	C5H5N5S	2723601	Moderate		Inter Info	[40], [41]
D1615		Trabectedin	C39H43N3O11S	108150	Moderate		Inter Info	[10], [44]

References
1	Product Information. Gavreto (pralsetinib). Blueprint Medicines Corporation, Cambridge, MA.
2	Wohlt PD, Zheng L, Gunderson S, Balzar SA, Johnson BD, Fish JT "Recommendations for the use of medications with continuous enteral nutrition." Am J Health Syst Pharm 66 (2009): 1438-67. [PMID: 19667002]
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4	Product Information. Zokinvy (lonafarnib). Eiger BioPharmaceuticals, Palo Alto, CA.
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6	Product Information. Turalio (pexidartinib). Daiichi Sankyo, Inc., Parsippany, NJ.
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9	Product Information. Arava (leflunomide). Hoechst Marion-Roussel Inc, Kansas City, MO.
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11	Product Information. Diovan (valsartan). Novartis Pharmaceuticals, East Hanover, NJ.
12	Product Information. Piqray (alpelisib). Novartis Pharmaceuticals, East Hanover, NJ.
13	Al-Nawakil C, Willems L, Mauprivez C, et.al "Successful treatment of l-asparaginase-induced severe acute hepatotoxicity using mitochondrial cofactors." Leuk Lymphoma 55 (2014): 1670-4. [PMID: 24090500]
14	Bodmer M, Sulz M, Stadlmann S, Droll A, Terracciano L, Krahenbuhl S "Fatal liver failure in an adult patient with acute lymphoblastic leukemia following treatment with L-asparaginase." Digestion 74 (2006): epub. [PMID: 16988508]
15	Cerner Multum, Inc "ANVISA Bulario Eletrnico.".
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17	Christ TN, Stock W, Knoebel RW "Incidence of asparaginase-related hepatotoxicity, pancreatitis, and thrombotic events in adults with acute lymphoblastic leukemia treated with a pediatric-inspired regimen." J Oncol Pharm Pract 24 (2018): 299-308. [PMID: 28355969]
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20	Product Information. Asparlas (calaspargase pegol). Servier, Boston, MA.
21	Product Information. Elspar (asparaginase). Merck & Co, Inc, West Point, PA.
22	Product Information. Erwinaze (asparaginase Erwinia chrysanthemi). EUSA Pharma, Newtown, PA.
23	Product Information. Oncaspar (pegaspargase). Rhone-Poulenc Rorer, Collegeville, PA.
24	Burke PW, Aldoss I, Lunning MA, et.al "High-grade PEGylated asparaginase-related hepatotoxicity occurrence in a pediatric-inspired adult acute lymphoblastic leukemia regimen does not necessarily predict recurrent hepatotoxicity in subsequent cycles." Blood 122 (2013): 2671. [PMID: 29407583]
25	Product Information. Sirturo (bedaquiline). Janssen Pharmaceuticals, Titusville, NJ.
26	Product Information. Adcetris (brentuximab vedotin). Seattle Genetics Inc, Bothell, WA.
27	Product Information. Epidiolex (cannabidiol). Greenwich Biosciences Inc, Carlsbad, CA.
28	Product Information. Clolar (clofarabine). sanofi-aventis, Bridgewater, NJ.
29	Product Information. Ellence (epirubicin) Pharmacia and Upjohn, Kalamazoo, MI.
30	Product Information. Xospata (gilteritinib). Astellas Pharma US, Inc, Deerfield, IL.
31	Product Information. Daurismo (glasdegib). Pfizer U.S. Pharmaceuticals Group, New York, NY.
32	Product Information. Avonex (interferon beta-1a). Biogen, Cambridge, MA.
33	Product Information. Betaseron (interferon beta-1b). Berlex, Richmond, CA.
34	Product Information. Plegridy (peginterferon beta-1a). Biogen Idec Inc, Cambridge, MA.
35	Product Information. Rebif (interferon beta-1a). Serono Laboratories Inc, Norwell, MA.
36	Product Information. Methotrexate (methotrexate). Lederle Laboratories, Wayne, NJ.
37	Product Information. ReVia (naltrexone). DuPont Pharmaceuticals, Wilmington, DE.
38	Product Information. Zorbtive (somatropin). Serono Laboratories Inc, Rockland, MA.
39	Product Information. Xermelo (telotristat ethyl). Lexicon Pharmaceuticals, Inc., The Woodlands, TX.
40	Product Information. Aubagio (teriflunomide). Genzyme Corporation, Cambridge, MA.
41	Product Information. Tabloid (thioguanine). Prasco Laboratories, Cincinnati, OH.
42	Product Information. Jynarque (tolvaptan). Otsuka American Pharmaceuticals Inc, Rockville, MD.
43	Product Information. Samsca (tolvaptan). Otsuka American Pharmaceuticals Inc, Rockville, MD.
44	Product Information. Yondelis (trabectedin). Janssen Pharmaceuticals, Titusville, NJ.

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