225Ac-PSMA-617

225Ac-PSMA-617
Clinical data
Other namesActinium (225Ac) PSMA-617, UH4J18XEL3, Actinium vipivotide tetraxetan
Routes of
administration		Intravenous
Drug classRadiopharmaceutical
ATC code
Identifiers
  • actinium-225;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
UNII
Chemical and physical data
FormulaC49H68AcN9O16
3D model (JSmol)
  • C1CC(CCC1CNC(=O)CN2CCN(CCN(CCN(CC2)CC(=O)[O-])CC(=O)[O-])CC(=O)[O-])C(=O)N[C@@H](CC4=CC3=CC=CC=C3C=C4)C(=O)NCCCC[C@@H](C(=O)O)NC(=O)N[C@@H](CCC(=O)O)C(=O)O.[225Ac+3]
  • InChI=1S/C49H71N9O16.Ac/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);/p-3/t32?,35?,37-,38-,39-;/m0./s1/i;1-2
  • Key:PNFYWACVZSJSKR-DCZFPAOOSA-K

225Ac-PSMA-617 is an investigational radiopharmaceutical used in targeted alpha therapy (TAT) for metastatic castration-resistant prostate cancer (mCRPC) and, more recently, for metastatic hormone-sensitive prostate cancer (mHSPC). Initially developed by the German Cancer Research Center and University Hospital Heidelberg, it combines actinium-225 (225Ac), an alpha-emitting radionuclide, with PSMA-617, a small-molecule ligand that targets prostate-specific membrane antigen (PSMA), a protein overexpressed in prostate cancer cells. The therapy delivers high-energy alpha radiation to induce DNA damage in cancer cells while leveraging the short tissue penetration of alpha particles to minimize damage to healthy tissues. As of May 2025, 225Ac-PSMA-617 remains in early-phase clinical trials and has not yet received regulatory approval.

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