lutetium (177Lu) vipivotide tetraxetan 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
PSMA (prostate-specific membrane antigen, glutamate carboxypeptidase 2)-binding peptides; peptides and glycopeptides 5509 1703749-62-5

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • lutetium (177Lu) vipivotide tetraxetan
  • pluvicto
  • 177Lu-PSMA-617
  • JK-218
Lutetium Lu 177 vipivotide tetraxetan is a radioligand therapeutic agent. The active moiety of lutetium Lu 177 vipivotide tetraxetan is the radionuclide lutetium-177 which is linked to a moiety that binds to PSMA, a transmembrane protein that is expressed in prostate cancer, including mCRPC. Upon binding of lutetium Lu 177 vipivotide tetraxetan to PSMA- expressing cells, the beta-minus emission from lutetium-177 delivers radiation to PSMA-expressing cells, as well as to surrounding cells, and induces DNA damage which can lead to cell death.
  • Molecular weight: 1216.07
  • Formula: C49H68LuN9O16
  • CLOGP: -12.02
  • LIPINSKI: 3
  • HAC: 25
  • HDO: 8
  • TPSA: 336.30
  • ALOGS: -4.32
  • ROTB: 27
  • Status: ONP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2A,ACVR2B,AURKA,AXL,BRAF,BTK,CAMK2D,CDK4,CDK5,CDK9,DDR1,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,GRK2,ITK,JAK2,JAK3,MAP2K6,MAP3K21,MAP3K7,MAPK7,MAPKAPK2,NTRK2,PDK1,PDK2,PIK3CB,PIM2,PRKDC,SIK2,STK33,SYK,TEK,TGFBR1,ZAP70 37
kinase-selectivity-class AXL,BRAF,CDK9,EPHB4,GRK2,MAP2K6,MAPK7,PIK3CD,TEK,TGFBR1 10
pfas-class PFAS structural alert (1 = True, 0 = False) 0

Approvals:

DateAgencyCompanyOrphan
March 23, 2022 FDA AAA USA NOVARTIS
Dec. 9, 2022 EMA NOVARTIS EUROPHARM LIMITED

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
General physical health deterioration 866.61 33.21 365 3462 150881 42466627
Ill-defined disorder 820.16 33.21 206 3621 16090 42601418
Prostatic specific antigen increased 313.06 33.21 98 3729 16827 42600681
Malignant neoplasm progression 303.51 33.21 161 3666 108239 42509269
Disease progression 148.66 33.21 114 3713 143542 42473966
Death 143.71 33.21 192 3635 470993 42146515
Metastases to bone 87.56 33.21 37 3790 14772 42602736
Anaemia 84.43 33.21 114 3713 280164 42337344
Thrombocytopenia 65.85 33.21 83 3744 190196 42427312
Haemoglobin decreased 61.11 33.21 67 3760 132404 42485104
Laboratory test abnormal 60.67 33.21 33 3794 22945 42594563
Dry mouth 60.29 33.21 40 3787 39839 42577669
Illness 42.55 33.21 27 3800 24903 42592605
Prostate cancer metastatic 37.29 33.21 16 3811 6613 42610895
Acquired haemophilia 36.38 33.21 11 3816 1664 42615844
Metastases to liver 33.78 33.21 20 3807 16306 42601202

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
General physical health deterioration 365.73 43.01 183 2405 425112 110161599
Malignant neoplasm progression 255.20 43.01 109 2479 174458 110412253
Ill-defined disorder 239.32 43.01 101 2487 156752 110429959
Prostatic specific antigen increased 207.79 43.01 50 2538 12461 110574250
Metastases to bone 133.10 43.01 43 2545 31329 110555382
Anaemia 105.48 43.01 93 2495 546993 110039718
Prostate cancer metastatic 83.25 43.01 20 2568 4923 110581788
Death 82.64 43.01 91 2497 698778 109887933
Thrombocytopenia 80.75 43.01 66 2522 348819 110237892
Haemoglobin decreased 61.57 43.01 49 2539 248678 110338033
Hormone-dependent prostate cancer 58.47 43.01 9 2579 205 110586506
Metastases to nervous system 55.25 43.01 9 2579 297 110586414
Metastases to liver 47.80 43.01 21 2567 35365 110551346
Blood chromogranin A increased 47.40 43.01 9 2579 724 110585987
Acquired haemophilia 46.13 43.01 11 2577 2620 110584091

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC V10XX05 VARIOUS
THERAPEUTIC RADIOPHARMACEUTICALS
OTHER THERAPEUTIC RADIOPHARMACEUTICALS
Various therapeutic radiopharmaceuticals
MeSH PA D007202 Indicators and Reagents
MeSH PA D019275 Radiopharmaceuticals
MeSH PA D064907 Diagnostic Uses of Chemicals

Related Drugs by ATC class:

V10XX Various therapeutic radiopharmaceuticals 4 drugs
ibritumomab tiuxetanlutetium (177Lu) oxodotreotideradium Ra 223 dichloridesodium phosphate (32P)

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
PSMA-positive metastatic castration-resistant prostate cancer indication 427492003




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
27mCi/ML PLUVICTO NOVARTIS N215833 March 23, 2022 RX SOLUTION INTRAVENOUS 10406240 Aug. 15, 2028 FOR TREATMENT OF ADULT PATIENTS WITH PROSTATE-SPECIFIC MEMBRANE ANTIGEN (PSMA)-POSITIVE METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC) WHO HAVE BEEN TREATED WITH ANDROGEN RECEPTOR PATHWAY INHIBITOR (ARPI) THERAPY
27mCi/ML PLUVICTO NOVARTIS N215833 March 23, 2022 RX SOLUTION INTRAVENOUS 11318121 Aug. 15, 2028 FOR TREATMENT OF ADULT PATIENTS WITH PROSTATE-SPECIFIC MEMBRANE ANTIGEN (PSMA)-POSITIVE METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC) WHO HAVE BEEN TREATED WITH ANDROGEN RECEPTOR PATHWAY INHIBITOR (ARPI) THERAPY
27mCi/ML PLUVICTO NOVARTIS N215833 March 23, 2022 RX SOLUTION INTRAVENOUS 11951190 Nov. 12, 2035 FOR TREATMENT OF ADULT PATIENTS WITH PROSTATE-SPECIFIC MEMBRANE ANTIGEN (PSMA)-POSITIVE METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC) WHO HAVE BEEN TREATED WITH ANDROGEN RECEPTOR PATHWAY INHIBITOR (ARPI) THERAPY
27mCi/ML PLUVICTO NOVARTIS N215833 March 23, 2022 RX SOLUTION INTRAVENOUS 12208102 Sept. 18, 2041 FOR TREATMENT OF ADULT PATIENTS WITH PROSTATE-SPECIFIC MEMBRANE ANTIGEN (PSMA)-POSITIVE METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC) WHO HAVE BEEN TREATED WITH ANDROGEN RECEPTOR PATHWAY INHIBITOR (ARPI) THERAPY

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
27mCi/ML PLUVICTO NOVARTIS N215833 March 23, 2022 RX SOLUTION INTRAVENOUS March 23, 2027 NEW CHEMICAL ENTITY
27mCi/ML PLUVICTO NOVARTIS N215833 March 23, 2022 RX SOLUTION INTRAVENOUS March 28, 2028 TREATMENT OF ADULT PATIENTS WITH PROSTATE-SPECIFIC MEMBRANE ANTIGEN (PSMA)-POSITIVE METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC) WHO HAVE BEEN TREATED WITH ANDROGEN RECEPTOR PATHWAY INHIBITOR (ARPI) THERAPY, AND ARE CONSIDERED APPROPRIATE TO DELAY TAXANE-BASED CHEMOTHERAPY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Prostate-specific antigen Surface antigen BINDING AGENT Kd 8.33 DRUG LABEL DRUG LABEL

External reference:

IDSource
CHEBI:757895 CHEBI
CHEMBL4594406 ChEMBL_ID
C000610110 MESH_SUPPLEMENTAL_RECORD_UI
DB16778 DRUGBANK_ID
C4308025 UMLSCUI
D12335 KEGG_DRUG
122706785 PUBCHEM_CID
357907 MMSL
40557 MMSL
d09868 MMSL
018885 NDDF
11010 INN_ID
13645 INN_ID
11429 INN_ID
2597047 RXNORM
4YM1W0EGQ5 UNII
7P5C02S4X8 UNII
AB6DQ43TKE UNII
G6UF363ECX UNII
UH4J18XEL3 UNII

Pharmaceutical products:

None