Lutetium Lu-177 vipivotide tetraxetan

DCTPepD ID  DCTPepD0028

Active Ingredients   Lutetium Lu-177 vipivotide tetraxetan

Description  A radioconjugate composed of PSMA-617, a human prostate-specific membrane antigen (PSMA)-targeting ligand, conjugated to the beta-emitting radioisotope lutetium Lu 177 (177Lu), with potential antineoplastic activity against PSMA-expressing tumor cells. Upon intravenous administration of lutetium Lu 177 vipivotide tetraxetan, vipivotide tetraxetan 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.

Synonyms  177Lu-labeled PSMA-617; 177Lu-PSMA-617; Lu177-PSMA-617; Lutetium Lu 177 Vipivotide Tetraxetan; Lutetium Lu 177-PSMA-617; Pluvicto; Lutetium Lu-177 vipivotide tetraxetan

Disease  Metastatic Castration-Resistant Prostate Cancer (mCRPC)

Classification

  

Peptide and derivative Peptide Receptor Radionuclide Therapy(PPRT) Cancer targeted Radioconjugates

Structure Information


Molecular Formula  C49H68LuN9O16

Molecular Weight  1216.1

Active Sequence  Not available

Sequence Length  Not available

Modification  Not available

Structure

 

Show IUPAC/InChI/SMILES

IUPAC Name  lutetium(III)-177Lu rac-2,2',2''-(10-(2-((((1R,4r)-4-(((R)-1-(((R)-5-carboxy-5-(3-((R)-1,3-dicarboxypropyl)ureido)pentyl)amino)-3-(naphthalen-2-yl)-1-oxopropan-2-yl)carbamoyl)cyclohexyl)methyl)amino)-2-oxoethyl)-1,4,7,10-tetraazacyclododecane-1,4,7-triyl)triacetate

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

InChI_Key RSTDSVVLNYFDHY-BGOLSCJMSA-K

SMILES  O=C([C@H](CCCCNC([C@H](CC1=CC=C2C=CC=CC2=C1)NC([C@@H](CC3)CC[C@H]3CNC(CN4CCN(CC([O-])=O)CCN(CCN(CC4)CC([O-])=O)CC([O-])=O)=O)=O)=O)NC(N[C@@H](CCC(O)=O)C(O)=O)=O)O.[177Lu+3]

External Codes


PubChem CID  122706785

DrugBank Accession Number  DB16778

NCI Thesaurus Code  C148145  

UNII  G6UF363ECX   GSRS

CAS  1703749-62-5



Drug approval


Drug indication
    Lutetium Lu 177 vipivotide tetraxetan is a radioligand therapeutic agent indicated for the treatment of adult patients with prostate-specific membrane antigen (PSMA)-positive metastatic castration-resistant prostate cancer (mCRPC) who have been treated with androgen receptor (AR) pathway inhibition and taxane-based chemotherapy.

Drug Name Strength Dosage Form/Route Company Marketing Status Drug ID Approval year
Pluvicto 27mci/ml Solution; Intravenous Aaa Usa Novartis Prescription NDA: 215833 2022

ClinicalTrials.gov Identifier Title Condition or disease Phase Purpose
NCT05113537 Phase I/II Study of CDK4/6 Inhibition With Abemaciclib to Upregulate PSMA Expression Prior to 177Lu-PSMA-617 Treatment in Patients With Metastatic Castrate Resistant Prostate Cancer (mCRPC) Previously Treated With Novel Hormonal Agents and Chemotherapy Castration-Resistant Prostate Carcinoma; Metastatic Prostate Adenocarcinoma; Stage IV Prostate Cancer AJCC v8; Stage IVA Prostate Cancer AJCC v8; Stage IVB Prostate Cancer AJCC v8; Metastatic Castration-resistant Prostate Carcinoma; Metastatic Castration-resistant Prostate Cancer Phase 1/2 Treatment
NCT05658003 An Open-label, Multi-center, Randomized, Phase II Study Evaluating [177Lu]Lu-PSMA-617 vs. a Change of Androgen Receptor-directed Therapy in the Treatment of Taxane Naive Chinese Male Patients With Progressive Metastatic Castrate Resistant Prostate Cancer Metastatic Castration-Resistant Prostate Cancer (mCRPC) Phase 2 Treatment

    More clinical information is obtained from ClinicalTrials.gov.





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