Knowledge

Icatibant

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InChI=1S/C59H89N19O13S/c60-37(14-5-19-67-57(61)62)48(82)72-38(15-6-20-68-58(63)64)52(86)75-22-8-18-43(75)54(88)77-30-35(80)26-44(77)50(84)70-28-47(81)71-40(27-36-13-9-23-92-36)49(83)74-41(31-79)53(87)76-29-34-12-2-1-10-32(34)24-46(76)55(89)78-42-17-4-3-11-33(42)25-45(78)51(85)73-39(56(90)91)16-7-21-69-59(65)66/h1-2,9-10,12-13,23,33,35,37-46,79-80H,3-8,11,14-22,24-31,60H2,(H,70,84)(H,71,81)(H,72,82)(H,73,85)(H,74,83)(H,90,91)(H4,61,62,67)(H4,63,64,68)(H4,65,66,69)/t33-,35+,37+,38-,39-,40-,41-,42-,43-,44-,45-,46+/m0/s1
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to market Firazyr in the European Union's 27 member states, as well as Switzerland, Liechtenstein and Iceland, making it the first product to be approved in all EU countries for the treatment of hereditary angioedema. In the US, the drug was granted FDA approval in August 2011.
205: 260:)-2-amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]-4-hydroxypyrrolidine-2-carbonyl]amino]acetyl]amino]-3-thiophen-2-ylpropanoyl]amino]-3-hydroxypropanoyl]-3,4-dihydro-1 1287: 160: 1044: 618: 872: 72: 574: 582:
C1CC2(C1)C(N2C(=O)3CC4=CC=CC=C4CN3C(=O)(CO)NC(=O)(CC5=CC=CS5)NC(=O)CNC(=O)6C(CN6C(=O)7CCCN7C(=O)(CCCN=C(N)N)NC(=O)(CCCN=C(N)N)N)O)C(=O)N(CCCN=C(N)N)C(=O)O
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Bradykinin is a peptide-based hormone that is formed locally in tissues, very often in response to a trauma. It increases vessel permeability,
796: 1030: 1272: 594: 811: 248: 190: 90: 1277: 378: 264:-isoquinoline-3-carbonyl]-2,3,3a,4,5,6,7,7a-octahydroindole-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoic acid 459: 1092: 109: 704:
receptors. Icatibant acts as a bradykinin inhibitor by blocking the binding of native bradykinin to the bradykinin B
1242: 1203: 845: 1198: 1188: 327: 146: 900:"Randomized Trial of Icatibant for Angiotensin-Converting Enzyme Inhibitor-Induced Upper Airway Angioedema" 669: 448: 153: 797:
https://www.tga.gov.au/resources/prescription-medicines-registrations/icatibant-wkt-wockhardt-bio-pty-ltd
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Sinert R, Levy P, Bernstein JA, Body R, Sivilotti ML, Moellman J, et al. (September–October 2017).
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status in Australia, the EU, Switzerland, and the US for the treatment of hereditary angioedema (HAE).
1005:"FDA Approves Shire's Firazyr (icatibant injection) for Acute Attacks of Hereditary Angioedema (HAE)" 475: 1170: 273: 1083: 779: 689: 120: 986: 921: 873:"Jerini Receives European Commission Approval for Firazyr (Icatibant) in the Treatment of HAE" 771: 428: 367: 218: 54: 1175: 976: 966: 911: 840: 763: 496: 282: 387: 1256: 1004: 82: 479: 981: 954: 658: 1266: 1193: 1144: 1103: 1098: 767: 651: 783: 307: 1179: 1139: 1134: 1125: 1088: 1078: 1064: 1054: 1022: 955:"Management of acute attacks of hereditary angioedema: potential role of icatibant" 685: 647: 173: 168: 700:, overheating and pain. These symptoms are mediated by activation of bradykinin B 692:
to contract. Bradykinin plays an important role as the mediator of pain. Surplus
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receptor. Little is known about the effects of icatibant on the bradykinin B
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deficiency. It is not effective in angioedema caused by medication from the
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is responsible for the typical symptoms of inflammation, such as swelling,
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In the EU, the approval by the European Commission (July 2008) allows
41: 876: 439: 642:, is a medication for the symptomatic treatment of acute attacks of 408: 1229: 559: 550: 419: 398: 224: 1026: 212: 99: 464: 904:
The Journal of Allergy and Clinical Immunology. In Practice
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Shire 686:dilates blood vessels 648:C1-esterase-inhibitor 646:(HAE) in adults with 644:hereditary angioedema 1278:Peptide therapeutics 1171:sickle cell disease 1093:+desoxyribonuclease 910:(5): 1402–1409.e3. 850:. 17 September 2018 725:Icatibant received 716:Society and culture 690:smooth muscle cells 680:Mechanism of action 208:(Prescription only) 36: 27:Pharmaceutical drug 1084:Desoxyribonuclease 972:10.2147/vhrm.s4332 818:. 16 December 2019 762:(6): 343–8. 2004. 661:consisting of ten 1238: 1237: 875:(Press release). 633: 632: 561:Interactive image 460:CompTox Dashboard 228: 216: 203: 135: 102: 16:(Redirected from 1295: 1255: 1254: 1253: 1246: 1176:beta thalassemia 1047: 1040: 1033: 1024: 1017: 1016: 1014: 1012: 1001: 995: 994: 984: 974: 950: 944: 943: 937: 929: 919: 895: 889: 888: 886: 884: 869: 860: 859: 857: 855: 837: 828: 827: 825: 823: 808: 799: 794: 788: 787: 756:Drugs in R&D 751: 629: 628: 621: 563: 543: 541: 527: 521: 515: 509: 503: 483: 482: 468: 466: 451: 431: 411: 390: 370: 350: 330: 310: 300: 299: 285: 226: 223: 214: 211: 201: 198: 176: 133: 130: 112: 101: 98: 85: 44: 37: 35: 21: 1303: 1302: 1298: 1297: 1296: 1294: 1293: 1292: 1263: 1262: 1261: 1251: 1249: 1241: 1239: 1234: 1218: 1173: 1164: 1121: 1113: 1058: 1051: 1021: 1020: 1010: 1008: 1003: 1002: 998: 952: 951: 947: 930: 897: 896: 892: 882: 880: 871: 870: 863: 853: 851: 839: 838: 831: 821: 819: 810: 809: 802: 795: 791: 753: 752: 748: 743: 723: 718: 711: 707: 703: 682: 673: 624: 622: 619:(what is this?) 616: 611: 608: 603: 598: 597: 586: 583: 578: 577: 566: 539: 537: 524: 518: 512: 506: 486: 462: 454: 434: 414: 393: 373: 353: 333: 313: 296: 288: 268: 265: 252: 251: 235: 180: 148: 141: 122: 115: 67:Hoe 140, JE 049 28: 23: 22: 15: 12: 11: 5: 1301: 1299: 1291: 1290: 1285: 1280: 1275: 1265: 1264: 1260: 1259: 1236: 1235: 1233: 1232: 1226: 1224: 1220: 1219: 1217: 1216: 1211: 1206: 1201: 1196: 1191: 1185: 1183: 1169:Drugs used in 1166: 1165: 1163: 1162: 1157: 1152: 1147: 1142: 1137: 1131: 1129: 1118:Drugs used in 1115: 1114: 1112: 1111: 1106: 1101: 1096: 1086: 1081: 1076: 1070: 1068: 1060: 1059: 1052: 1050: 1049: 1042: 1035: 1027: 1019: 1018: 996: 945: 890: 879:. 15 July 2008 861: 841:"Firazyr EPAR" 829: 800: 789: 745: 744: 742: 739: 722: 719: 717: 714: 709: 705: 701: 681: 678: 671: 659:peptidomimetic 631: 630: 613: 612: 610: 609: 606: 604: 601: 593: 592: 591: 588: 587: 585: 584: 581: 573: 572: 571: 568: 567: 565: 564: 556: 554: 546: 545: 535: 529: 528: 522: 516: 510: 504: 499: 493: 492: 488: 487: 485: 484: 476:DTXSID20903963 471: 469: 456: 455: 453: 452: 444: 442: 436: 435: 433: 432: 424: 422: 416: 415: 413: 412: 406:as salt:  403: 401: 395: 394: 392: 391: 383: 381: 375: 374: 372: 371: 363: 361: 355: 354: 352: 351: 343: 341: 335: 334: 332: 331: 323: 321: 315: 314: 312: 311: 303: 301: 290: 289: 287: 286: 278: 276: 270: 269: 267: 266: 255: 247: 246: 245: 242: 241: 237: 236: 234: 233: 230: 221: 209: 195: 193: 187: 186: 182: 181: 179: 178: 165: 163: 157: 156: 151: 149:administration 143: 142: 140: 139: 137: 127: 125: 117: 116: 114: 113: 95: 93: 87: 86: 79: 69: 68: 65: 61: 60: 57: 51: 50: 46: 45: 26: 24: 14: 13: 10: 9: 6: 4: 3: 2: 1300: 1289: 1286: 1284: 1281: 1279: 1276: 1274: 1271: 1270: 1268: 1258: 1248: 1244: 1231: 1228: 1227: 1225: 1221: 1215: 1212: 1210: 1207: 1205: 1202: 1200: 1197: 1195: 1194:Crizanlizumab 1192: 1190: 1187: 1186: 1184: 1181: 1177: 1172: 1167: 1161: 1158: 1156: 1153: 1151: 1148: 1146: 1145:Conestat alfa 1143: 1141: 1138: 1136: 1133: 1132: 1130: 1127: 1123: 1116: 1110: 1107: 1105: 1104:Streptokinase 1102: 1100: 1099:Hyaluronidase 1097: 1094: 1090: 1087: 1085: 1082: 1080: 1077: 1075: 1072: 1071: 1069: 1066: 1061: 1056: 1048: 1043: 1041: 1036: 1034: 1029: 1028: 1025: 1006: 1000: 997: 992: 988: 983: 978: 973: 968: 964: 960: 956: 949: 946: 941: 935: 927: 923: 918: 913: 909: 905: 901: 894: 891: 878: 874: 868: 866: 862: 849: 847: 842: 836: 834: 830: 817: 813: 807: 805: 801: 798: 793: 790: 785: 781: 777: 773: 769: 765: 761: 757: 750: 747: 740: 738: 735: 730: 728: 720: 715: 713: 699: 695: 691: 687: 679: 677: 675: 668: 664: 660: 655: 653: 652:ACE inhibitor 649: 645: 641: 637: 627: 620: 614: 605: 600: 596: 589: 580: 576: 569: 562: 558: 557: 555: 552: 547: 536: 534: 530: 500: 498: 494: 489: 481: 477: 473: 472: 470: 461: 457: 450: 449:ChEMBL1743581 446: 445: 443: 441: 437: 430: 426: 425: 423: 421: 417: 410: 405: 404: 402: 400: 396: 389: 385: 384: 382: 380: 376: 369: 365: 364: 362: 360: 356: 349: 345: 344: 342: 340: 336: 329: 325: 324: 322: 320: 316: 309: 305: 304: 302: 295: 291: 284: 280: 279: 277: 275: 271: 263: 259: 254: 250: 243: 238: 231: 229: Rx-only 222: 220: 210: 207: 197: 196: 194: 192: 188: 183: 175: 170: 167: 166: 164: 162: 158: 155: 152: 150: 144: 138: 129: 128: 126: 124: 118: 111: 106: 97: 96: 94: 92: 88: 84: 80: 78: 74: 70: 66: 62: 58: 56: 52: 49:Clinical data 47: 43: 38: 30: 19: 1283:Orphan drugs 1154: 1140:C1-inhibitor 1135:Berotralstat 1089:Fibrinolysin 1079:Chymotrypsin 1009:. Retrieved 999: 962: 958: 948: 934:cite journal 907: 903: 893: 881:. Retrieved 852:. Retrieved 844: 820:. Retrieved 815: 792: 759: 755: 749: 731: 724: 721:Legal status 683: 656: 639: 635: 634: 623:   617:   261: 257: 191:Legal status 185:Legal status 154:Subcutaneous 91:License data 29: 1160:Lanadelumab 1150:Ecallantide 965:: 795–802. 727:orphan drug 688:and causes 663:amino acids 544: g·mol 429:CHEBI:68556 283:130308-48-4 240:Identifiers 64:Other names 55:Trade names 1267:Categories 1122:angioedema 1120:hereditary 741:References 712:receptor. 694:bradykinin 667:bradykinin 549:3D model ( 533:Molar mass 388:7PG89G35Q7 359:ChemSpider 319:IUPHAR/BPS 274:CAS Number 249:IUPAC name 1214:Voxelotor 1209:Mitapivat 1155:Icatibant 1074:Bromelain 1063:Enzymes ( 1011:28 August 877:Jerini AG 674:receptors 636:Icatibant 147:Routes of 121:Pregnancy 110:Icatibant 83:Monograph 77:Drugs.com 34:Icatibant 1257:Medicine 991:20859548 926:28552382 854:17 April 822:17 April 816:DailyMed 784:25491021 776:15563238 657:It is a 626:(verify) 368:16736634 339:DrugBank 161:ATC code 123:category 105:DailyMed 1109:Trypsin 982:2941790 883:22 July 698:redness 654:class. 640:Firazyr 497:Formula 348:DB06196 308:6918173 294:PubChem 177:) 171: ( 169:B06AC02 136: C 107::  59:Firazyr 18:Firazyr 1243:Portal 1223:Others 989:  979:  924:  782:  774:  734:Jerini 575:SMILES 440:ChEMBL 409:D04492 219:℞-only 217: 204: 103:  1230:Hemin 1180:B06AX 1126:B06AC 1065:B06AA 848:(EMA) 780:S2CID 595:InChI 551:JSmol 420:ChEBI 1174:and 1013:2011 987:PMID 940:link 922:PMID 885:2008 856:2020 824:2020 772:PMID 399:KEGG 379:UNII 73:AHFS 1055:B06 977:PMC 967:doi 912:doi 764:doi 542:.54 540:304 465:EPA 328:667 298:CID 174:WHO 1269:: 985:. 975:. 961:. 957:. 936:}} 932:{{ 920:. 906:. 902:. 864:^ 843:. 832:^ 814:. 803:^ 778:. 770:. 758:. 676:. 523:13 517:19 511:89 505:59 256:(2 225:EU 213:US 206:S4 200:AU 132:AU 100:US 1245:: 1182:) 1178:( 1128:) 1124:( 1095:) 1091:( 1067:) 1057:) 1046:e 1039:t 1032:v 1015:. 993:. 969:: 963:6 942:) 928:. 914:: 908:5 887:. 858:. 826:. 786:. 766:: 760:5 710:1 706:2 702:2 672:2 670:B 553:) 538:1 526:S 520:O 514:N 508:H 502:C 467:) 463:( 262:H 258:S 227:: 215:: 202:: 134:: 75:/ 20:)

Index

Firazyr

Trade names
AHFS
Drugs.com
Monograph
License data
DailyMed
Icatibant
Pregnancy
category

Routes of
administration

Subcutaneous
ATC code
B06AC02
WHO
Legal status
S4
℞-only
IUPAC name
CAS Number
130308-48-4
PubChem
6918173
IUPHAR/BPS
667
DrugBank
DB06196
ChemSpider
16736634
UNII

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