Everolimus

Everolimus
Clinical data
Pronunciation	Everolimus /ˌɛvəˈroʊləməs/
Trade names	Afinitor, Zortress
Other names	42-O-(2-hydroxyethyl)rapamycin, RAD001
AHFS/Drugs.com	Monograph
MedlinePlus	a609032
License data	US DailyMed: Everolimus;
Pregnancy; category	AU: C;
Routes of; administration	By mouth
ATC code	L01EG02 (WHO) L04AH02 (WHO);
Legal status
Legal status	AU: S4 (Prescription only); UK: ; US: WARNINGRx-only; EU: Rx-only; In general: ℞ (Prescription only);
Pharmacokinetic data
Elimination half-life	~30 hours
Identifiers
	IUPAC name 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;
CAS Number	159351-69-6 ;
PubChem CID	6442177;
DrugBank	DB01590 ;
ChemSpider	21106307 ;
UNII	9HW64Q8G6G;
KEGG	D02714 ;
ChEBI	CHEBI:68478;
ChEMBL	ChEMBL1908360 ;
CompTox Dashboard (EPA)	DTXSID0040599 ;
ECHA InfoCard	100.149.896
Chemical and physical data
Formula	C53H83NO14
Molar mass	958.240 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES 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 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 ; Key:HKVAMNSJSFKALM-GKUWKFKPSA-N ;
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Everolimus, sold under the brand name Afinitor among others, is a medication used as an immunosuppressant to prevent rejection of organ transplants and as a targeted therapy in the treatment of renal cell cancer and other tumours.

This compound also has a use in cardiovascular drug-eluting stent technologies to inhibit restenosis.

It is the 40-O-(2-hydroxyethyl) derivative of sirolimus and works similarly to sirolimus as an inhibitor of mammalian target of rapamycin (mTOR).

It is marketed by Novartis under the trade names Zortress (US) and Certican (European Union and other countries) in transplantation medicine, and as Afinitor (general tumours) and Votubia (tumours as a result of Tuberous Sclerosis Complex (TSC)) in oncology.

It is on the World Health Organization's List of Essential Medicines. It is available as a generic medication.

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