Lutetium (177Lu) oxodotreotide

Lutetium (177Lu) dotatate
INN: lutetium (177Lu) oxodotreotide
Clinical data
Trade namesLutathera
AHFS/Drugs.comMonograph
License data
Routes of
administration
Intravenous
Drug classRadiolabeled somatostatin analog
ATC code
Legal status
Legal status
  • CA: Rx-only / Schedule C
  • UK: POM (Prescription only)
  • US: ℞-only
  • EU: Rx-only
  • In general: ℞ (Prescription only)
Identifiers
  • (177Lu)lutetium(3+) 2-[4-({[(1R)-1-{[(4R,7S,10S,13R,16S,19R)-10-(4-aminobutyl)-4-{[(1S,2R)-1-carboxy-2-hydroxypropyl]-C-hydroxycarbonimidoyl}-6,9,12,15,18-pentahydroxy-7-[(1R)-1-hydroxyethyl]-13-[(1H-indol-3-yl)methyl]-16-[(4-oxidophenyl)methyl]-1,2-dithia-5,8,11,14,17-pentaazacycloicosa-5,8,11,14,17-pentaen-19-yl]-C-hydroxycarbonimidoyl}-2-phenylethyl]-C-hydroxycarbonimidoyl}methyl)-7,10-bis(carboxymethyl)-1,4,7,10-tetraazacyclododecan-1-yl]acetate
CAS Number
PubChem CID
DrugBank
UNII
KEGG
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC65H87LuN14O19S2
Molar mass1607.58 g·mol−1
3D model (JSmol)
  • CC(C1C(=O)NC(CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CCCCN)CC2=CNC3=CC=CC=C32)CC4=CC=C(C=C4)O)NC(=O)C(CC5=CC=CC=C5)NC(=O)CN6CCN(CCN(CCN(CC6)CC(=O)[O-])CC(=O)[O-])CC(=O)[O-])C(=O)NC(C(C)O)C(=O)O)O.[Lu+3]
  • InChI=1S/C65H90N14O19S2.Lu/c1-38(80)56-64(96)73-51(63(95)75-57(39(2)81)65(97)98)37-100-99-36-50(72-59(91)47(28-40-10-4-3-5-11-40)68-52(83)32-76-20-22-77(33-53(84)85)24-26-79(35-55(88)89)27-25-78(23-21-76)34-54(86)87)62(94)70-48(29-41-15-17-43(82)18-16-41)60(92)71-49(30-42-31-67-45-13-7-6-12-44(42)45)61(93)69-46(58(90)74-56)14-8-9-19-66;/h3-7,10-13,15-18,31,38-39,46-51,56-57,67,80-82H,8-9,14,19-30,32-37,66H2,1-2H3,(H,68,83)(H,69,93)(H,70,94)(H,71,92)(H,72,91)(H,73,96)(H,74,90)(H,75,95)(H,84,85)(H,86,87)(H,88,89)(H,97,98);/q;+3/p-3/t38-,39-,46+,47-,48+,49-,50+,51+,56+,57+;/m1./s1/i;1+2
  • Key:MXDPZUIOZWKRAA-PRDSJKGBSA-K

Lutetium (177Lu) oxodotreotide (INN) or 177Lu dotatate, brand name Lutathera, is a chelated complex of a radioisotope of the element lutetium with dotatate, used in peptide receptor radionuclide therapy. Specifically, it is used in the treatment of cancers which express somatostatin receptors. It is a radiolabeled somatostatin analog.

Alternatives to 177Lu-dotatate include yttrium-90 dotatate or DOTATOC. The longer range of the beta particles emitted by 90Y, which deliver the therapeutic effect, may make it more suitable for large tumors with 177Lu reserved for smaller volumes

The US Food and Drug Administration (FDA) considers 177Lu dotatate to be a first-in-class medication.