Iksabepilon: Perbedaan antara revisi
Konten dihapus Konten ditambahkan
Tidak ada ringkasan suntingan Tag: Suntingan perangkat seluler Suntingan peramban seluler Suntingan seluler lanjutan |
Tidak ada ringkasan suntingan Tag: Suntingan perangkat seluler Suntingan peramban seluler Suntingan seluler lanjutan |
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| (6 revisi perantara oleh pengguna yang sama tidak ditampilkan) | |||
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| Verifiedfields = changed
| verifiedrevid = 477495917
| IUPAC_name = (1''R'',5''S'',6''S'',7''R'',10''S'',14''S'',16''S'')-6,10-
| image = Ixabepilone.svg
| width = 250
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| legal_US = Rx-only
| legal_status =
| routes_of_administration = [[
<!--Pharmacokinetic data-->
| bioavailability = N/A
| protein_bound = 67
| metabolism =
| elimination_half-life = 52
| excretion =
<!--Identifiers-->
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| StdInChIKey_Ref = {{stdinchicite|correct|chemspider}}
| StdInChIKey = FABUFPQFXZVHFB-PVYNADRNSA-N
| synonyms =
}}
'''Iksabepilon''' ([[Nama Generik Internasional|INN]]; juga dikenal sebagai
==Sejarah==
Iksabepilon adalah analog semi-sintetik dari epotilon B, senyawa kimia alami yang diproduksi oleh bakteri ''Sorangium cellulosum''.<ref name="pmid18463327">{{cite journal | vauthors = Goodin S | title = Novel cytotoxic agents: epothilones | journal = American Journal of Health-System Pharmacy | volume = 65 | issue = 10 Suppl 3 | pages = S10–S15 | date = May 2008 | pmid = 18463327 | doi = 10.2146/ajhp080089 }}</ref> Perbedaan struktural antara Epotilon B dan iksabepilon hanya terdiri dari substitusi oksigen-nitrogen satu atom yang mengubah ester menjadi amida. Epotilon B sendiri tidak dapat dikembangkan sebagai obat farmasi karena stabilitas metabolik dan [[farmakokinetika]]nya yang buruk. Iksabepilon dirancang melalui [[kimia medisinal]] untuk meningkatkan sifat-sifat ini.<ref name="pmid18347795">{{cite journal | vauthors = Lee FY, Borzilleri R, Fairchild CR, Kamath A, Smykla R, Kramer R, Vite G | title = Preclinical discovery of ixabepilone, a highly active antineoplastic agent | journal = Cancer Chemotherapy and Pharmacology | volume = 63 | issue = 1 | pages = 157–166 | date = December 2008 | pmid = 18347795 | doi = 10.1007/s00280-008-0724-8 | doi-access = free }}</ref>
==Farmakologi==
Seperti [[paklitaksel]], iksabepilon bertindak untuk menstabilkan [[mikrotubulus]].<ref>{{cite journal | vauthors = Lopus M, Smiyun G, Miller H, Oroudjev E, Wilson L, Jordan MA | title = Mechanism of action of ixabepilone and its interactions with the βIII-tubulin isotype | journal = Cancer Chemotherapy and Pharmacology | volume = 76 | issue = 5 | pages = 1013–1024 | date = November 2015 | pmid = 26416565 | doi = 10.1007/s00280-015-2863-z | s2cid = 1842156 }}</ref><ref name="pmid18321240">{{cite journal | vauthors = Denduluri N, Swain SM | title = Ixabepilone for the treatment of solid tumors: a review of clinical data | journal = Expert Opinion on Investigational Drugs | volume = 17 | issue = 3 | pages = 423–435 | date = March 2008 | pmid = 18321240 | doi = 10.1517/13543784.17.3.423 | s2cid = 71169099 }}</ref><ref name="pmid18945860">{{cite journal | vauthors = Goodin S | title = Ixabepilone: a novel microtubule-stabilizing agent for the treatment of metastatic breast cancer | journal = American Journal of Health-System Pharmacy | volume = 65 | issue = 21 | pages = 2017–2026 | date = November 2008 | pmid = 18945860 | doi = 10.2146/ajhp070628 }}</ref> Obat ini sangat kuat, mampu merusak sel kanker dalam konsentrasi yang sangat rendah, dan mempertahankan aktivitas dalam kasus di mana sel tumor tidak sensitif terhadap obat jenis taksana.<ref name="pancreas">{{cite journal | vauthors = Vulfovich M, Rocha-Lima C | title = Novel advances in pancreatic cancer treatment | journal = Expert Review of Anticancer Therapy | volume = 8 | issue = 6 | pages = 993–1002 | date = June 2008 | pmid = 18533808 | doi = 10.1586/14737140.8.6.993 | s2cid = 20049942 }}</ref>
==Persetujuan==
Pada tanggal 16 Oktober 2007, [[Badan Pengawas Obat dan Makanan Amerika Serikat]] menyetujui iksabepilon untuk pengobatan [[kanker payudara]] [[metastasis]] agresif atau kanker payudara stadium lanjut yang tidak lagi merespons kemoterapi yang tersedia saat ini.<ref>{{cite web |url= https://www.medicalnewstoday.com/releases/85726.php |title=FDA Approves IXEMPRA(TM) (ixabepilone), A Semi-Synthetic Analog Of Epothilone B, For The Treatment Of Advanced Breast Cancer|website=Medical News Today}}</ref> Pada bulan November 2008, [[Badan Pengawas Obat Eropa|EMEA]] telah menolak otorisasi pemasaran untuk iksabepilon.<ref>{{cite web | work = European Medicines Agency | title = Questions and answers on recommendation for the refusal of the marketing authorisation for Ixempra | id = Doc. Ref. EMEA/602569/2008 | url = http://www.ema.europa.eu/docs/en_GB/document_library/Summary_of_opinion_Initial_authorisation/human/000930/WC500014746.pdf | location = London | date = 20 November 2008 }} </ref>
Iksabepilon diberikan melalui suntikan, dan dipasarkan dengan nama dagang Ixempra.
==Kegunaan klinis==
Dalam kombinasi dengan [[kapesitabin]], iksabepilon telah menunjukkan efektivitas dalam pengobatan kanker payudara metastasis atau stadium lanjut pada pasien setelah kegagalan pengobatan dengan [[antrasiklin]] dan taksana.<ref name="pmid17968020">{{cite journal | vauthors = Thomas ES, Gomez HL, Li RK, Chung HC, Fein LE, Chan VF, Jassem J, Pivot XB, Klimovsky JV, de Mendoza FH, Xu B, Campone M, Lerzo GL, Peck RA, Mukhopadhyay P, Vahdat LT, Roché HH | display-authors = 6 | title = Ixabepilone plus capecitabine for metastatic breast cancer progressing after anthracycline and taxane treatment | journal = Journal of Clinical Oncology | volume = 25 | issue = 33 | pages = 5210–5217 | date = November 2007 | pmid = 17968020 | doi = 10.1200/JCO.2007.12.6557 | doi-access = free }}</ref>
Iksabepilon telah diteliti untuk digunakan dalam pengobatan [[limfoma]] non-Hodgkin.<ref name="pmid17261851">{{cite journal | vauthors = Aghajanian C, Burris HA, Jones S, Spriggs DR, Cohen MB, Peck R, Sabbatini P, Hensley ML, Greco FA, Dupont J, O'Connor OA | display-authors = 6 | title = Phase I study of the novel epothilone analog ixabepilone (BMS-247550) in patients with advanced solid tumors and lymphomas | journal = Journal of Clinical Oncology | volume = 25 | issue = 9 | pages = 1082–1088 | date = March 2007 | pmid = 17261851 | doi = 10.1200/JCO.2006.08.7304 | doi-access = free }}</ref> Dalam uji klinis [[kanker pankreas]] fase dua, obat ini menunjukkan beberapa hasil yang menjanjikan (digunakan sendiri). Uji klinis terapi kombinasi masih berlangsung.<ref name="pancreas"/>
==Referensi==
{{Reflist}}
Baris 67 ⟶ 80:
* [http://www.ixempra.com/ Ixempra product website]
* [https://web.archive.org/web/20160129134623/http://packageinserts.bms.com/pi/pi_ixempra.pdf Ixempra prescribing information]
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[[Kategori:Penghambat mitotik]]
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