1042:
627:
604:
29:
2366:
916:
antagonist, most side effects had comparable frequencies in both groups, and differed more between chemotherapy regimens than between rolapitant and placebo groups. Common side effects included decreased appetite (9% under rolapitant vs. 7% under placebo),
1184:
Duffy RA, Morgan C, Naylor R, Higgins GA, Varty GB, Lachowicz JE, Parker EM (July 2012). "Rolapitant (SCH 619734): a potent, selective and orally active neurokinin NK1 receptor antagonist with centrally-mediated antiemetic effects in ferrets".
1080:-hydroxylated rolapitant) and a number of inactive metabolites. Rolapitant is mainly excreted via the feces (52–89%) in unchanged form, and to a lesser extent via the urine (9–20%) in form of its inactive metabolites.
744:
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
1425:
702:
1387:
952:
have increased threefold when combined with rolapitant; and increased concentrations of other substrates are expected. The drug also inhibits the transporter proteins
1996:
1298:"Efficacy and safety of rolapitant for prevention of chemotherapy-induced nausea and vomiting over multiple cycles of moderately or highly emetogenic chemotherapy"
2175:
236:
1436:
1337:
Chasen MR, Rapoport BL (March 2016). "Rolapitant for the treatment of chemotherapy-induced nausea and vomiting: a review of the clinical evidence".
170:
864:(anti-vomiting) agents in adults for the prevention of delayed nausea and vomiting associated with initial and repeat courses of emetogenic cancer
1398:
2210:
2195:
119:
1160:"International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended International Nonproprietary Names (Rec. INN): List 59"
2338:
2333:
2095:
1989:
716:
2155:
2145:
2140:
2135:
2120:
2115:
2075:
2303:
2190:
2080:
2070:
2065:
2170:
2125:
2060:
2205:
2100:
845:
1982:
976:
868:, including, but not limited to, highly emetogenic chemotherapy. The approved antiemetic combination consists of rolapitant plus
1133:
892:, whose inactivation could be inhibited by rolapitant. Under the European approval, it is contraindicated in combination with
1497:
2411:
852:
showed it to have similar or improved efficacy and some improvement in safety over existing drugs for this application.
2401:
187:
2396:
1842:
1061:
Rolapitant is practically completely absorbed from the gut, independently of food intake. It undergoes no measurable
801:
763:
736:
87:
987:, this effect was almost 90% in a study. Inhibitors of CYP3A4 have no relevant effect on rolapitant concentrations.
1269:
Nasir SS, Schwartzberg LS (August 2016). "Recent
Advances in Preventing Chemotherapy-Induced Nausea and Vomiting".
1230:"Recent developments in the prevention of chemotherapy-induced nausea and vomiting (CINV): a comprehensive review"
381:
266:
151:
1069:
concentrations are reached after about four hours. When in the bloodstream, 99.8% of the substance are bound to
1159:
464:
622:
515:
583:
921:(9% vs. 8% or 7% vs. 6%, depending on the kind of chemotherapy), dizziness (6% vs. 4%), indigestion and
2391:
2356:
1490:
1432:
1394:
831:
165:
599:
2406:
1890:
1602:
1015:
841:
823:
225:
198:
101:
2416:
1076:
It is metabolized by the liver enzyme CYP3A4, resulting in the major active metabolite M19 (C4-
318:
572:
2421:
2284:
2235:
2016:
1081:
1023:
1007:
835:
504:
455:
1296:
Rapoport B, Schwartzberg L, Chasen M, Powers D, Arora S, Navari R, Schnadig I (April 2016).
419:
2426:
2386:
1798:
1713:
1638:
1483:
996:
524:
350:
626:
603:
8:
2005:
1845:
1728:
1041:
1019:
410:
205:
2008:
1210:
893:
960:(P-gp), which has been shown to increase plasma concentrations of the ABCG2 substrate
1779:
1464:
1354:
1319:
1278:
1251:
1202:
1062:
1046:
980:
444:
281:
209:
143:
1214:
1774:
1769:
1519:
1346:
1309:
1241:
1194:
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873:
772:
639:
300:
249:
46:
129:
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1974:
1864:
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1054:
815:
328:
308:
1943:
1812:
1759:
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1653:
1314:
1297:
1070:
957:
933:
Up to eightfold therapeutic doses have been given in studies without problems.
849:
28:
1198:
2380:
2110:
2105:
1948:
1907:
1789:
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961:
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615:
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1764:
1683:
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1358:
1323:
1282:
1255:
1206:
1066:
904:
In studies comparing chemotherapy plus rolapitant, dexamethasone and a 5-HT
889:
865:
244:
20:
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2030:
1938:
1880:
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1623:
1593:
1583:
1568:
1548:
1100:
1096:
1077:
1050:
918:
888:
Under the US approval, rolapitant is contraindicated in combination with
213:
137:
484:
2328:
2274:
2269:
2225:
2180:
2165:
2160:
2150:
2090:
2055:
2050:
2040:
1917:
1912:
1902:
1703:
1663:
1628:
1618:
1613:
1608:
1588:
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1563:
1543:
1506:
984:
922:
861:
678:
495:
340:
229:
220:
1350:
1103:
crystalline powder. Its maximum solubility in aqueous solutions is at
2343:
2323:
2264:
2259:
2130:
1958:
1953:
1827:
1807:
1648:
1578:
1558:
1553:
1538:
1533:
430:
363:
123:
1475:
1963:
1859:
1708:
552:
544:
475:
182:
701:
1689:
1084:
is about seven days (169 to 183 hours) over a wide dosing range.
965:
909:
1295:
1033:, more than 1000-fold therapeutic concentrations are necessary.
724:
FC(F)(F)c(c4)cc(C(F)(F)F)cc4C(C)OCC3(c2ccccc2)NCC1(CC3)NC(=O)CC1
1030:
972:
942:
819:
333:
169:
896:, which is expected to accelerate inactivation of rolapitant.
953:
844:). It has been approved as a medication for the treatment of
787:
692:
563:
588:
793:
778:
535:
52:
814:
in the
European Union) is a drug originally developed by
73:
67:
61:
1183:
1006:
Both rolapitant and its active metabolite M19 block the
1104:
401:)-1-ethoxy}methyl)- 8-phenyl-1,7-diazaspirodecan-2-one
2354:
802:
88:
76:
1465:"Rolapitant Injection: MedlinePlus Drug Information"
790:
784:
775:
79:
70:
64:
58:
49:
781:
463:
55:
2004:
1420:
1418:
1128:
1126:
1124:
1122:
1120:
1268:
2378:
941:Rolapitant moderately inhibits the liver enzyme
443:
1415:
1227:
1117:
418:
1336:
345:C4-pyrrolidine-hydroxylated rolapitant (major)
1990:
1491:
956:(breast cancer resistance protein, BCRP) and
860:Rolapitant is used in combination with other
945:. Blood plasma concentrations of the CYP2D6
186:
1997:
1983:
1498:
1484:
625:
602:
503:
1426:"Varuby: EPAR – Public assessment report"
1313:
1245:
1029:or any other of 115 tested receptors and
818:and licensed for clinical development by
523:
1187:Pharmacology, Biochemistry, and Behavior
1040:
1022:: to block the closely related receptor
846:chemotherapy-induced nausea and vomiting
1228:Jordan K, Jahn F, Aapro M (June 2015).
1165:. World Health Organization. p. 64
1092:The drug is used in form of rolapitant
598:
483:
142:
2379:
1382:
1380:
1378:
1376:
1374:
1372:
1370:
1368:
616:
287:
160:
1978:
1505:
1479:
997:Aprepitant § Mechanism of action
571:
275:
177:
128:
1388:"Varuby: EPAR – Product Information"
971:Strong inducers of the liver enzyme
883:
248:
1365:
1036:
1001:
551:
543:
434:
13:
14:
2438:
1457:
1099:, a white to off-white, slightly
1057:of the hydroxyl group is unknown.
2364:
908:antagonist to chemotherapy plus
771:
662:
656:
650:
45:
27:
1053:-hydroxylated rolapitant). The
990:
964:twofold and the P-gp substrate
936:
899:
855:
749:Key:FIVSJYGQAIEMOC-ZGNKEGEESA-N
1330:
1289:
1262:
1221:
1177:
1152:
668:
644:
1:
1110:
368:Feces (52–89%), urine (9–20%)
1435:. 2017-05-31. Archived from
1397:. 2017-05-31. Archived from
1087:
822:, which acts as a selective
7:
1134:"Varubi- rolapitant tablet"
928:
10:
2443:
2412:Drugs developed by GSK plc
1315:10.1016/j.ejca.2015.12.023
1302:European Journal of Cancer
994:
912:, dexamethasone and a 5-HT
634:Chemical and physical data
2402:Trifluoromethyl compounds
2283:
2234:
2015:
1931:
1889:
1841:
1788:
1727:
1682:
1637:
1518:
1433:European Medicines Agency
1395:European Medicines Agency
1199:10.1016/j.pbb.2012.03.021
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136:
118:
110:
100:
40:
35:
26:
2397:NK1 receptor antagonists
1639:5-HT serotonin G-protein
226:NK1 receptor antagonists
106:Varubi (US), Varuby (EU)
1065:in the liver. Highest
1058:
979:of rolapitant and its
2176:Nolpitantium besilate
1247:10.1093/annonc/mdv138
1082:Elimination half-life
1044:
995:Further information:
1714:Tetrahydrocannabinol
1641:receptor antagonists
977:area under the curve
2006:Neurokinin receptor
1526:channel antagonists
828:receptor antagonist
23:
16:Pharmaceutical drug
1234:Annals of Oncology
1059:
983:(called M19); for
925:(both 4% vs. 2%).
19:
2392:CYP2D6 inhibitors
2352:
2351:
1972:
1971:
1780:Trimethobenzamide
1471:. 20 August 2020.
1351:10.2217/fon.16.11
1063:first-pass effect
1047:active metabolite
981:active metabolite
884:Contraindications
757:
756:
703:Interactive image
584:CompTox Dashboard
291:
279:
180:
163:
2434:
2369:
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1999:
1992:
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1975:
1851:anticholinergics
1775:Thiethylperazine
1770:Prochlorperazine
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1037:Pharmacokinetics
1002:Pharmacodynamics
950:dextromethorphan
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2407:Spiro compounds
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2288:
2279:
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2020:
2011:
2003:
1973:
1968:
1927:
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1865:Diphenhydramine
1848:
1837:
1818:Diphenhydramine
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1339:Future Oncology
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1222:
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1153:
1143:
1141:
1140:. 6 August 2019
1132:
1131:
1118:
1113:
1090:
1071:plasma proteins
1055:stereochemistry
1039:
1027:
1011:
1004:
999:
993:
939:
931:
915:
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894:St. John's Wort
886:
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858:
850:clinical trials
839:
827:
816:Schering-Plough
804:
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319:Protein binding
309:Bioavailability
301:Pharmacokinetic
295:
256:
200:
193:
90:
48:
44:
17:
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11:
5:
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1944:Cerium oxalate
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1813:Dimenhydrinate
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1799:antihistamines
1791:
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1783:
1782:
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1760:Metoclopramide
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1458:External links
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1240:(6): 1081–90.
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958:P-glycoprotein
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2137:
2134:
2132:
2129:
2127:
2124:
2122:
2119:
2117:
2114:
2112:
2111:Fosnetupitant
2109:
2107:
2106:Fosaprepitant
2104:
2102:
2099:
2097:
2094:
2092:
2089:
2087:
2084:
2082:
2079:
2077:
2074:
2072:
2069:
2067:
2064:
2062:
2059:
2057:
2054:
2052:
2049:
2047:
2044:
2042:
2039:
2036:
2035:
2032:
2029:
2026:
2025:
2023:
2021:
2014:
2010:
2007:
2000:
1995:
1993:
1988:
1986:
1981:
1980:
1977:
1965:
1962:
1960:
1957:
1955:
1952:
1950:
1949:Dexamethasone
1947:
1945:
1942:
1940:
1937:
1936:
1934:
1930:
1924:
1921:
1919:
1916:
1914:
1911:
1909:
1908:Fosaprepitant
1906:
1904:
1901:
1900:
1898:
1896:
1888:
1882:
1879:
1877:
1874:
1871:
1868:
1866:
1863:
1861:
1858:
1857:
1855:
1852:
1847:
1844:
1840:
1834:
1831:
1829:
1826:
1824:
1821:
1819:
1816:
1814:
1811:
1809:
1806:
1805:
1803:
1800:
1795:
1787:
1781:
1778:
1776:
1773:
1771:
1768:
1766:
1763:
1761:
1758:
1756:
1753:
1751:
1748:
1746:
1743:
1742:
1740:
1738:
1726:
1719:
1715:
1712:
1710:
1707:
1705:
1702:
1701:
1699:
1696:
1691:
1688:
1681:
1675:
1672:
1670:
1667:
1665:
1662:
1660:
1657:
1655:
1652:
1650:
1647:
1646:
1644:
1642:
1636:
1630:
1627:
1625:
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1620:
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1615:
1612:
1610:
1607:
1604:
1600:
1597:
1595:
1592:
1590:
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1585:
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1577:
1575:
1572:
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1567:
1565:
1562:
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1552:
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1547:
1545:
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1524:serotonin ion
1517:
1512:
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1501:
1496:
1494:
1489:
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1461:
1442:on 2018-03-18
1438:
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1427:
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1419:
1404:on 2018-03-18
1400:
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1389:
1383:
1381:
1379:
1377:
1375:
1373:
1371:
1369:
1360:
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1352:
1348:
1345:(6): 763–78.
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1333:
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1307:
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1299:
1292:
1284:
1280:
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1224:
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1200:
1196:
1193:(1): 95–100.
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1180:
1161:
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1129:
1127:
1125:
1123:
1121:
1116:
1108:
1106:
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1095:
1094:hydrochloride
1085:
1083:
1079:
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1072:
1068:
1064:
1056:
1052:
1048:
1043:
1034:
1032:
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1021:
1017:
1013:
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975:decrease the
974:
969:
967:
963:
962:sulfasalazine
959:
955:
951:
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934:
926:
924:
920:
911:
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895:
891:
881:
879:
871:
870:dexamethasone
867:
863:
853:
851:
848:(CINV) after
847:
843:
840:
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821:
817:
813:
809:
808:
798:
769:
766:, trade name
765:
761:
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643:
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632:
628:
624:
621:
619:
617:ECHA InfoCard
613:
605:
601:
597:
596:
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585:
581:
574:
570:
569:
567:
565:
561:
554:
550:as HCl:
549:
546:
542:
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539:
537:
533:
526:
522:
521:
519:
517:
513:
506:
502:
501:
499:
497:
493:
486:
482:
481:
479:
477:
473:
466:
462:
461:
459:
457:
453:
446:
442:
441:
439:
432:
428:
421:
417:
416:
414:
412:
408:
400:
396:
392:
387:
386:
383:
376:
371:
367:
365:
361:
358:169–183 hours
357:
355:
348:
344:
342:
338:
335:
332:
330:
326:
322:
320:
316:
312:
310:
306:
302:
298:
292: Rx-only
285:
283:
273:
272:
270:
268:
264:
259:
251:
246:
243:
242:
240:
238:
234:
231:
227:
224:
222:
218:
215:
211:
207:
204:
202:
196:
189:
184:
175:
172:
167:
158:
157:
155:
153:
149:
145:
141:
139:
135:
131:
127:
125:
121:
117:
113:
109:
105:
103:
99:
95:
94:
84:
43:
41:Pronunciation
39:
36:Clinical data
34:
30:
25:
2422:Pyrrolidones
2319:Fezolinetant
2314:Elinzanetant
2311:Antagonists:
2310:
2299:Neurokinin B
2295:
2257:Antagonists:
2256:
2250:Neurokinin A
2246:
2185:
2086:Elinzanetant
2046:Befetupitant
2038:Antagonists:
2037:
2027:
1922:
1833:Promethazine
1765:Metopimazine
1695:cannabinoids
1599:Palonosetron
1468:
1444:. Retrieved
1437:the original
1406:. Retrieved
1399:the original
1342:
1338:
1332:
1305:
1301:
1291:
1274:
1270:
1264:
1237:
1233:
1223:
1190:
1186:
1179:
1167:. Retrieved
1154:
1142:. Retrieved
1137:
1091:
1075:
1067:blood plasma
1060:
1005:
991:Pharmacology
970:
940:
937:Interactions
932:
903:
900:Side effects
890:thioridazine
887:
866:chemotherapy
859:
856:Medical uses
811:
767:
759:
758:
398:
394:
390:
351:Elimination
267:Legal status
261:Legal status
152:License data
2427:Piperidines
2387:Antiemetics
2221:Vestipitant
2216:Tradipitant
2211:Telmapitant
2201:Serlopitant
2196:SDZ NKT 343
2031:Substance P
1939:Amisulpride
1895:antagonists
1881:Scopolamine
1876:Hyoscyamine
1872:(very mild)
1870:Hydroxyzine
1846:antagonists
1823:Hydroxyzine
1794:antagonists
1755:Hydroxyzine
1750:Haloperidol
1737:antagonists
1674:Ziprasidone
1669:Risperidone
1659:Hydroxyzine
1624:Tropisetron
1603:+netupitant
1594:Ondansetron
1584:Mirtazapine
1569:Granisetron
1549:Cilansetron
1507:Antiemetics
1469:MedlinePlus
1101:hygroscopic
1097:monohydrate
1078:pyrrolidine
1051:pyrrolidine
1020:selectivity
919:neutropenia
686: g·mol
623:100.243.022
573:CHEBI:90908
420:552292-08-7
373:Identifiers
341:Metabolites
313:nearly 100%
230:antiemetics
214:intravenous
138:MedlinePlus
111:Other names
102:Trade names
2381:Categories
2339:SB-222,200
2334:SB-218,795
2329:Pavinetant
2275:Saredutant
2270:Nepadutant
2226:Vofopitant
2186:Rolapitant
2181:Orvepitant
2166:Netupitant
2161:Maropitant
2151:Lanepitant
2096:Figopitant
2091:Ezlopitant
2056:Casopitant
2051:Burapitant
2041:Aprepitant
2009:modulators
1923:Rolapitant
1918:Netupitant
1913:Maropitant
1903:Aprepitant
1704:Dronabinol
1664:Olanzapine
1629:Zatosetron
1619:Ricasetron
1614:Ramosetron
1609:Quetiapine
1589:Olanzapine
1574:Lerisetron
1564:Dolasetron
1544:Bemesetron
1446:2017-10-11
1408:2017-10-11
1111:References
1049:, M19 (C4-
1045:The major
1014:with high
985:rifampicin
923:stomatitis
878:antagonist
862:antiemetic
832:antagonist
760:Rolapitant
691:3D model (
679:Molar mass
525:NLE429IZUC
496:ChemSpider
456:IUPHAR/BPS
411:CAS Number
382:IUPAC name
329:Metabolism
221:Drug class
188:Rolapitant
114:SCH 619734
21:Rolapitant
2344:Talnetant
2324:Osanetant
2296:Agonists:
2265:Ibodutant
2260:GR-159897
2247:Agonists:
2156:LY-306740
2146:L-758,298
2141:L-743,310
2136:L-741,671
2131:L-733,060
2121:GW-597599
2116:GR-203040
2076:CP-122721
2028:Agonists:
1959:Midazolam
1954:Lorazepam
1828:Meclizine
1808:Cyclizine
1649:Clozapine
1579:Mianserin
1559:Dazopride
1554:Clozapine
1539:Azasetron
1534:Alosetron
1308:: 23–30.
1169:5 October
1144:21 August
1088:Chemistry
947:substrate
364:Excretion
353:half-life
199:Routes of
130:Monograph
124:Drugs.com
2371:Medicine
2304:Senktide
2191:RP-67580
2081:Dapitant
2071:CP-99994
2066:CP-96345
1964:Propofol
1860:Atropine
1718:cannabis
1709:Nabilone
1690:agonists
1359:26842387
1324:26851398
1283:27539626
1271:Oncology
1256:25755107
1215:24357198
1207:22497992
1138:DailyMed
1016:affinity
1012:receptor
968:by 70%.
929:Overdose
842:receptor
834:for the
476:DrugBank
445:10311306
397:)-8-({(1
237:ATC code
206:By mouth
183:DailyMed
2171:NKP-608
2126:HSP-117
2061:CI-1021
1031:enzymes
966:digoxin
910:placebo
684:500.485
640:Formula
505:8486772
485:DB09291
431:PubChem
253:)
247: (
245:A04AD14
210:tablets
185::
168::
144:a615041
93:-i-tant
2357:Portal
2206:T-2328
2101:FK-888
1932:Others
1357:
1322:
1281:
1254:
1213:
1205:
973:CYP3A4
943:CYP2D6
872:and a
820:Tesaro
812:Varuby
768:Varubi
717:SMILES
553:D08988
545:D10742
334:CYP3A4
282:℞-only
280:
181:
171:by INN
164:
96:
1440:(PDF)
1429:(PDF)
1402:(PDF)
1391:(PDF)
1211:S2CID
1163:(PDF)
1107:2–4.
954:ABCG2
737:InChI
693:JSmol
564:ChEBI
323:99.8%
1843:mACh
1520:5-HT
1355:PMID
1320:PMID
1279:PMID
1252:PMID
1203:PMID
1171:2016
1146:2020
1018:and
874:5-HT
807:-bee
536:KEGG
516:UNII
465:5749
303:data
120:AHFS
89:roh-
1511:A04
1347:doi
1310:doi
1242:doi
1195:doi
1191:102
805:ROO
803:və-
764:INN
589:EPA
435:CID
250:WHO
212:),
166:EMA
91:LAP
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2017:NK
1891:NK
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1024:NK
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