Everolimus

Everolimus
Data klinis
PengucapanEverolimus /ˌɛvəˈroʊləməs/
Nama dagangAfinitor, Certican, Everonat, Zortress
Nama lain42-O-(2-hidroksietil)rapamisin, RAD001
AHFS/Drugs.commonograph
MedlinePlusa609032
License data
Kategori
kehamilan
Rute
pemberian		Oral
Kode ATC
Status hukum
Status hukum
Data farmakokinetika
Waktu paruh eliminasi~30 jam[8]
Pengenal
  • Dihidroksi-12-[(2R)-1-[(1S,3R,4R)-4-(2-hidroksietoksi)-3-metoksisikloheksil]propan-2-il]-19,30-dimetoksi-15,17,21,23,29,35-heksametil-11,36-dioksa-4-azatrisiklo[30.3.1.0 heksatriakonta-16,24,26,28-tetraena-2,3,10,14,20-pentona
Nomor CAS
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.149.896 Sunting di Wikidata
Data sifat kimia dan fisik
RumusC53H83NO14
Massa molar958,24 g·mol−1
Model 3D (JSmol)
  • OCCO[C@@H]1CC[C@H](C[C@H]1OC)C[C@@H](C)[C@@H]4CC(=O)[C@H](C)/C=C(\C)[C@@H](O)[C@@H](OC)C(=O)[C@H](C)C[C@H](C)\C=C\C=C\C=C(/C)[C@@H](OC)C[C@@H]2CC[C@@H](C)[C@@](O)(O2)C(=O)C(=O)N3CCCC[C@H]3C(=O)O4
  • InChI=1S/C53H83NO14/c1-32-16-12-11-13-17-33(2)44(63-8)30-40-21-19-38(7)53(62,68-40)50(59)51(60)54-23-15-14-18-41(54)52(61)67-45(35(4)28-39-20-22-43(66-25-24-55)46(29-39)64-9)31-42(56)34(3)27-37(6)48(58)49(65-10)47(57)36(5)26-32/h11-13,16-17,27,32,34-36,38-41,43-46,48-49,55,58,62H,14-15,18-26,28-31H2,1-10H3/b13-11+,16-12+,33-17+,37-27+/t32-,34-,35-,36-,38-,39+,40+,41+,43-,44+,45+,46-,48-,49+,53-/m1/s1 checkY
  • Key:HKVAMNSJSFKALM-GKUWKFKPSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Everolimus adalah obat yang digunakan sebagai imunosupresan untuk mencegah penolakan transplantasi organ[9] dan sebagai terapi bertarget dalam pengobatan kanker sel ginjal dan tumor lainnya.[10]

Obat ini adalah turunan 40-O-(2-hidroksietil) dari sirolimus dan bekerja serupa dengan sirolimus sebagai penghambat target rapamisin manusia dan mamalia.[11]

Obat ini tercantum dalam Daftar Obat Esensial Organisasi Kesehatan Dunia.[12] Obat ini tersedia sebagai obat generik.[13]

Referensi

  1. ^
  2. ^ "Prescription medicines: registration of new generic medicines and biosimilar medicines, 2017". Therapeutic Goods Administration (TGA). 21 June 2022. Diakses tanggal 30 March 2024.
  3. ^ "Summary of Product Characteristics (SmPC) - (emc)". Certican Tablets. 15 January 2021. Diakses tanggal 30 December 2021.
  4. ^ "Afinitor- everolimus tablet Afinitor Disperz- everolimus tablet, for suspension". DailyMed. Diakses tanggal 30 December 2021.
  5. ^ "Zortress- everolimus tablet". DailyMed. Diakses tanggal 30 December 2021.
  6. ^ "Afinitor EPAR". European Medicines Agency. 17 September 2018. Diakses tanggal 30 December 2021.
  7. ^ "Votubia EPAR". European Medicines Agency. 17 September 2018. Diakses tanggal 30 December 2021.
  8. ^ Formica RN, Lorber KM, Friedman AL, Bia MJ, Lakkis F, Smith JD, Lorber MI (March 2004). "The evolving experience using everolimus in clinical transplantation". Transplantation Proceedings. 36 (2 Suppl): 495S – 499S. doi:10.1016/j.transproceed.2004.01.015. PMID 15041395.
  9. ^ Tedesco-Silva H, Saliba F, Barten MJ, De Simone P, Potena L, Gottlieb J, Gawai A, Bernhardt P, Pascual J (January 2022). "An overview of the efficacy and safety of everolimus in adult solid organ transplant recipients". Transplantation Reviews. 36 (1) 100655. Orlando, Fla. doi:10.1016/j.trre.2021.100655. hdl:10230/53730. PMID 34696930. S2CID 239887236.
  10. ^ Hasskarl J (2018). "Everolimus". Small Molecules in Oncology. Recent Results in Cancer Research. Vol. 211. hlm. 101–123. doi:10.1007/978-3-319-91442-8_8. ISBN 978-3-319-91441-1. PMID 30069763.
  11. ^ Hasskarl J (2018). "Everolimus". Dalam Martens UM (ed.). Small Molecules in Oncology (Edisi Third). Heidelberg: Springer. hlm. 101–124. ISBN 978-3-319-91442-8.
  12. ^ World Health Organization (2023). The selection and use of essential medicines 2023: web annex A: World Health Organization model list of essential medicines: 23rd list (2023). Geneva: World Health Organization. hdl:10665/371090. WHO/MHP/HPS/EML/2023.02.
  13. ^ "First Generic Drug Approvals". U.S. Food and Drug Administration (FDA). 15 November 2021. Diarsipkan dari asli tanggal 12 June 2019. Diakses tanggal 30 December 2021.

Bacaan lebih lanjut

  • Sedrani R, Cottens S, Kallen J, Schuler W (August 1998). "Chemical modification of rapamycin: the discovery of SDZ RAD". Transplantation Proceedings. 30 (5): 2192–2194. doi:10.1016/S0041-1345(98)00587-9. PMID 9723437.

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