Drug Libraray

DRACPC ID DRACPC0028

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

Type Small Molecule

Disease Metastatic Castration-Resistant Prostate Cancer (mCRPC)

Classification

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

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]

PubChem CID 122706785

DrugBank Accession Number DB16778

NCI Thesaurus Code C148145

UNII G6UF363ECX GSRS

CAS 1703749-62-5

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.