Lu-PSMA-617

Lutetium (177Lu) vipivotide tetraxetan
Clinical data
Trade namesPluvicto
Other namesLutetium (177Lu) vipivotide tetraxetan, Lutetium Lu 177 vipivotide tetraxetan (USAN US)
AHFS/Drugs.comMicromedex Detailed Consumer Information
MedlinePlusa622063
License data
Pregnancy
category
  • AU: X (High risk)[1]
Routes of
administration		Intravenous
Drug classRadiopharmaceutical
ATC code
Legal status
Legal status
Identifiers
IUPAC name
  • Lutetium-177 2-[4-[2-[[4-[[(2S)-1-[[(5S)-5-carboxy-5-[[(1S)-1,3-dicarboxypropyl]carbamoylamino]pentyl]amino]-3-naphthalen-2-yl-1-oxopropan-2-yl]carbamoyl]cyclohexyl]methylamino]-2-oxoethyl]-7,10-bis(carboxylatomethyl)-1,4,7,10-tetrazacyclododec-1-yl]acetate
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
Chemical and physical data
3D model (JSmol)
SMILES
  • [177Lu+3].OC(=O)CC[C@H](NC(=O)N[C@@H](CCCCNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@@H]3CC[C@@H](CNC(=O)CN4CCN(CC(=O)[O-])CCN(CC(=O)[O-])CCN(CC(=O)[O-])CC4)CC3)C(=O)O)C(=O)O
InChI
  • InChI=1S/C49H71N9O16.Lu/c59-40(28-55-17-19-56(29-42(62)63)21-23-58(31-44(66)67)24-22-57(20-18-55)30-43(64)65)51-27-32-8-12-35(13-9-32)45(68)52-39(26-33-10-11-34-5-1-2-6-36(34)25-33)46(69)50-16-4-3-7-37(47(70)71)53-49(74)54-38(48(72)73)14-15-41(60)61;/h1-2,5-6,10-11,25,32,35,37-39H,3-4,7-9,12-24,26-31H2,(H,50,69)(H,51,59)(H,52,68)(H,60,61)(H,62,63)(H,64,65)(H,66,67)(H,70,71)(H,72,73)(H2,53,54,74);/q;+3/p-3/t32-,35-,37-,38-,39-;/m0./s1/i;1+2
  • Key:RSTDSVVLNYFDHY-BGOLSCJMSA-K

Lu-PSMA-617, sold under the brand name Pluvicto, is a radiopharmaceutical medication used for the treatment of prostate-specific membrane antigen (PSMA)-positive metastatic castration-resistant prostate cancer (mCRPC).[5][6] Lutetium (177Lu) vipivotide tetraxetan is a targeted radioligand therapy.[6][8]

The most common adverse reactions include fatigue, dry mouth, nausea, anemia, decreased appetite, and constipation.[6][7]

Lu-PSMA-617 is a radioconjugate composed of PSMA-617, a human prostate-specific membrane antigen (PSMA)-targeting ligand, conjugated to the beta-emitting radioisotope lutetium-177, with potential antineoplastic activity against PSMA-expressing tumor cells.[9] Upon intravenous administration of Lu-PSMA-617, it targets and binds to PSMA-expressing tumor cells.[9] Upon binding, PSMA-expressing tumor cells are destroyed by 177Lu through the specific delivery of beta particle radiation.[9] PSMA, a tumor-associated antigen and type II transmembrane protein, is expressed on the membrane of prostatic epithelial cells and overexpressed on prostate tumor cells.[9]

Lu-PSMA-617 was approved for medical use in the United States in March 2022,[6][10] and in the European Union in December 2022.[7] The US Food and Drug Administration (FDA) considers it to be a first-in-class medication.[11][12]

  1. ^ a b "Pluvicto (Lutetium (177Lu) vipivotide tetraxetan)". Therapeutic Goods Administration (TGA). 31 July 2024. Retrieved 12 October 2024.
  2. ^ https://www.tga.gov.au/resources/prescription-medicines-registrations/pluvicto-novartis-pharmaceuticals-australia-pty-ltd
  3. ^ Advanced Accelerator Applications USA. "Pluvicto Product Monograph" (PDF). The Drug and Health Product Register. Government of Canada. Retrieved 12 October 2022.
  4. ^ "Summary Basis of Decision - Pluvicto". Health Canada. 23 October 2014. Archived from the original on 24 February 2023. Retrieved 23 February 2023.
  5. ^ a b "Pluvicto- lutetium lu 177 vipivotide tetraxetan injection, solution". DailyMed. 23 March 2022. Archived from the original on 5 April 2022. Retrieved 4 April 2022.
  6. ^ a b c d e "FDA approves Pluvicto for metastatic castration-resistant prostate cancer". U.S. Food and Drug Administration. 23 March 2022. Archived from the original on 24 March 2022. Retrieved 23 March 2022. This article incorporates text from this source, which is in the public domain.
  7. ^ a b c "Pluvicto EPAR". European Medicines Agency. 12 October 2022. Retrieved 21 December 2022. Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
  8. ^ Neels OC, Kopka K, Liolios C, Afshar-Oromieh A (December 2021). "Radiolabeled PSMA Inhibitors". Cancers. 13 (24): 6255. doi:10.3390/cancers13246255. PMC 8699044. PMID 34944875.
  9. ^ a b c d "Lutetium Lu 177 Vipivotide Tetraxetan (Code C148145)". NCI Thesaurus. 28 February 2022. Archived from the original on 15 April 2022. Retrieved 23 March 2022. This article incorporates text from this source, which is in the public domain.
  10. ^ "Novartis Pluvicto approved by FDA as first targeted radioligand therapy for treatment of progressive, PSMA positive metastatic castration-resistant prostate cancer" (Press release). Novartis. 23 March 2022. Archived from the original on 23 March 2022. Retrieved 23 March 2022.
  11. ^ "Advancing Health Through Innovation: New Drug Therapy Approvals 2022". U.S. Food and Drug Administration (FDA). 10 January 2023. Archived from the original on 10 January 2023. Retrieved 22 January 2023. This article incorporates text from this source, which is in the public domain.
  12. ^ New Drug Therapy Approvals 2022. U.S. Food and Drug Administration (FDA) (Report). January 2024. Archived from the original (PDF) on 14 January 2024. Retrieved 14 January 2024. This article incorporates text from this source, which is in the public domain.
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