User:Mr. Ibrahem/Everolimus

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Mr. Ibrahem/Everolimus
Clinical data
PronunciationEverolimus /ˌɛvəˈrləməs/
Trade namesAfinitor, Zortress, others
Other names42-O-(2-hydroxyethyl)rapamycin, RAD001
AHFS/Drugs.comMonograph
MedlinePlusa609032
License data
Pregnancy
category
Routes of
administration
By mouth
Drug classmTOR inhibitor, kinase inhibitor[2]
Legal status
Legal status
  • US: ℞-only
  • EU: Rx-only
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Elimination half-life~30 hours[3]
Identifiers
  • Dihydroxy-12-[(2R)-1-[(1S,3R,4R)-4-(2-hydroxyethoxy)-3-methoxycyclohexyl]propan-2-yl]-19,30-dimethoxy-15,17,21,23,29,35-hexamethyl-11,36-dioxa-4-azatricyclo[30.3.1.0 hexatriaconta-16,24,26,28-tetraene-2,3,10,14,20-pentone
Chemical and physical data
FormulaC53H83NO14
Molar mass958.240 g·mol−1
3D model (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 is a medication used to prevent rejection after an organ transplant and to treat certain types of cancer.[2] This includes after kidney, heart, and liver transplant.[4] It may be used for breast, kidney, and neuroendocrine tumors.[5] It is taken by mouth.[2]

Common side effects include mouth inflammation, respiratory tract infection, tiredness, vomiting, and diarrhea.[2] Other side effects may include hair loss, low white blood cells, bleeding, kidney problems, blood clotting, and heart failure.[4] It is likely that use during pregnancy would harm the baby.[6] It is a derivative of sirolimus and works similarly; by blocking mammalian target of rapamycin (mTOR).[5][7]

Everolimus was approved for medical use in the United States and Europe in 2009.[2][5] It is available as a generic medication.[4] It is on the World Health Organization's List of Essential Medicines.[8] In the United Kingdom a month of treatment post transplant costs about £450 while for certain types of cancer can be £2,900 as of 2020.[4] A similar amount to prevent transplant rejection costs about 450 USD in the United States as of 2021.[9] A generic version was approved in 2021 in the USA.[10]

References[edit]

  1. ^ a b Use During Pregnancy and Breastfeeding
  2. ^ a b c d e "Everolimus Monograph for Professionals". Drugs.com. Archived from the original on 17 April 2021. Retrieved 23 July 2021.
  3. ^ 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.
  4. ^ a b c d BNF (80 ed.). BMJ Group and the Pharmaceutical Press. September 2020 – March 2021. p. 1034. ISBN 978-0-85711-369-6.{{cite book}}: CS1 maint: date format (link)
  5. ^ a b c "Afinitor". Archived from the original on 8 April 2021. Retrieved 23 July 2021.
  6. ^ "Everolimus Use During Pregnancy". Drugs.com. Archived from the original on 17 April 2021. Retrieved 23 July 2021.
  7. ^ Wheeler, Derek S.; Wong, Hector R. (2007). Pediatric Critical Care Medicine: Basic Science And Clinical Evidence. Springer Science & Business Media. p. 1391. ISBN 978-1-84628-463-2. Archived from the original on 2021-08-28. Retrieved 2021-07-23.
  8. ^ World Health Organization (2021). World Health Organization model list of essential medicines: 22nd list (2021). Geneva: World Health Organization. hdl:10665/345533. WHO/MHP/HPS/EML/2021.02.
  9. ^ "Everolimus Prices, Coupons & Savings Tips - GoodRx". GoodRx. Retrieved 23 July 2021.
  10. ^ Research, Center for Drug Evaluation and (10 February 2022). "2021 First Generic Drug Approvals". FDA. Archived from the original on 21 June 2022. Retrieved 22 October 2022.