Lu-PSMA-617

Lutetium (¹⁷⁷Lu) vipivotide tetraxetan
Clinical data
Trade names	Pluvicto
Other names	Lutetium (177Lu) vipivotide tetraxetan, Lutetium Lu 177 vipivotide tetraxetan (USAN US)
AHFS/Drugs.com	Micromedex Detailed Consumer Information
MedlinePlus	a622063
License data	US DailyMed: Pluvicto;
Pregnancy; category	AU: X (High risk);
Routes of; administration	Intravenous
Drug class	Radiopharmaceutical
ATC code	V10XX05 (WHO) ;
Legal status
Legal status	AU: S4 (Prescription only); CA: ℞-only / Schedule C; US: ℞-only; EU: Rx-only;
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	1703749-62-5;
PubChem CID	122706785;
DrugBank	DB16778;
ChemSpider	58828499;
UNII	G6UF363ECX;
KEGG	D12335;
Chemical and physical data
3D model (JSmol)	Interactive image;
	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). Lutetium (¹⁷⁷Lu) vipivotide tetraxetan is a targeted radioligand therapy.

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

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. Upon intravenous administration of Lu-PSMA-617, it targets and binds to PSMA-expressing tumor cells. Upon binding, PSMA-expressing tumor cells are destroyed by ¹⁷⁷Lu through the specific delivery of beta particle radiation. 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.

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