lutetium (177Lu) vipivotide tetraxetan 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| PSMA (prostate-specific membrane antigen, glutamate carboxypeptidase 2)-binding peptides; peptides and glycopeptides | 5509 | 1703749-62-5 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
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.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
None
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Dec. 9, 2022 | EMA | NOVARTIS EUROPHARM LIMITED | |
| March 23, 2022 | FDA | AAA USA NOVARTIS |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Ill-defined disorder | 160.33 | 39.08 | 36 | 371 | 13873 | 34942651 |
| Malignant neoplasm progression | 47.03 | 39.08 | 22 | 385 | 88024 | 34868500 |
FDA Adverse Event Reporting System (Geriatric)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Ill-defined disorder | 65.06 | 44.78 | 18 | 209 | 65857 | 79678304 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | V10XX05 | VARIOUS THERAPEUTIC RADIOPHARMACEUTICALS OTHER THERAPEUTIC RADIOPHARMACEUTICALS Various therapeutic radiopharmaceuticals |
| MeSH PA | D064907 | Diagnostic Uses of Chemicals |
| MeSH PA | D007202 | Indicators and Reagents |
| MeSH PA | D019275 | Radiopharmaceuticals |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| 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 strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
|---|---|---|---|---|---|---|---|---|---|---|
| 27mCi/ML | PLUVICTO | AAA USA 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 (AR) PATHWAY INHIBITION AND TAXANE-BASED CHEMOTHERAPY |
| 27mCi/ML | PLUVICTO | AAA USA 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 (AR) PATHWAY INHIBITION AND TAXANE-BASED CHEMOTHERAPY |
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| 27mCi/ML | PLUVICTO | AAA USA NOVARTIS | N215833 | March 23, 2022 | RX | SOLUTION | INTRAVENOUS | March 23, 2027 | NEW CHEMICAL ENTITY |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Prostate-specific antigen | Surface antigen | BINDING AGENT | Kd | 8.33 | DRUG LABEL | DRUG LABEL |
External reference:
| ID | Source |
|---|---|
| CHEMBL4594406 | ChEMBL_ID |
| C000610110 | MESH_SUPPLEMENTAL_RECORD_UI |
| DB16778 | DRUGBANK_ID |
| 018885 | NDDF |
| C5577600 | UMLSCUI |
| D12335 | KEGG_DRUG |
| 11010 | INN_ID |
| 11429 | INN_ID |
| 122706785 | PUBCHEM_CID |
| 2597047 | RXNORM |
| 357907 | MMSL |
| 40557 | MMSL |
| d09868 | MMSL |
| 4YM1W0EGQ5 | UNII |
| 7P5C02S4X8 | UNII |
| G6UF363ECX | UNII |
| UH4J18XEL3 | UNII |
Pharmaceutical products:
None