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lurbinectedin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| ecteinascidin derivatives | 5398 | 497871-47-3 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Lurbinectedin is an alkylating drug that binds guanine residues in the minor groove of DNA, forming adducts and resulting in a bending of the DNA helix towards the major groove. Adduct formation triggers a cascade of events that can affect the subsequent activity of DNA binding proteins, including some transcription factors, and DNA repair pathways, resulting in perturbation of the cell cycle and eventual cell death.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Bocci G, Oprea TI, Benet LZ |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2A,ACVR2B,AKT2,AKT3,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK2,CDK4,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,GRK2,GSK3B,IGF1R,ITK,JAK2,JAK3,MAP2K6,MAP3K21,MAP3K7,MAPK10,MAPK7,MAPK9,MAPKAPK2,MET,MTOR,NTRK2,PDK1,PDK2,PDK4,PDPK1,PIK3CA,PIK3CB,PIK3CD,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK,ZAP70 | 53 | |||
| kinase-selectivity-class | GRK2,MAP2K6 | 2 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| June 15, 2020 | FDA | JAZZ |
FDA Adverse Event Reporting System (Female)
| 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 |
|---|---|---|---|---|---|---|
| Disease progression | 75.38 | 61.12 | 26 | 298 | 156589 | 90471534 |
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 |
|---|---|---|---|---|---|---|
| Disease progression | 78.05 | 54.81 | 38 | 539 | 143618 | 42477140 |
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 |
|---|---|---|---|---|---|---|
| Neutropenia | 68.29 | 48.17 | 40 | 825 | 374580 | 110213854 |
| Death | 65.06 | 48.17 | 49 | 816 | 698820 | 109889614 |
| Disease progression | 55.01 | 48.17 | 30 | 835 | 244004 | 110344430 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | L01XX69 | ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS OTHER ANTINEOPLASTIC AGENTS Other antineoplastic agents |
| FDA MoA | N0000000236 | Alkylating Activity |
| FDA EPC | N0000175558 | Alkylating Drug |
| CHEBI has role | CHEBI:35610 | antineoplastic agent |
Related Drugs by ATC class:
L01XX Other antineoplastic agents 33 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Small cell carcinoma of lung | indication | 254632001 | DOID:5409 |
🐶 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 |
|---|---|---|---|---|---|---|---|---|---|---|
| 4MG/VIAL | ZEPZELCA | JAZZ | N213702 | June 15, 2020 | RX | POWDER | INTRAVENOUS | 7763615 | Dec. 13, 2029 | MAINTENANCE TREATMENT OF ADULT PATIENTS WITH EXTENSIVE-STAGE SMALL CELL LUNG CANCER (ES-SCLC) WHOSE DISEASE HAS NOT PROGRESSED AFTER FIRST-LINE INDUCTION THERAPY |
| 4MG/VIAL | ZEPZELCA | JAZZ | N213702 | June 15, 2020 | RX | POWDER | INTRAVENOUS | 7763615 | Dec. 13, 2029 | TREATMENT OF ADULT PATIENTS WITH SMALL CELL LUNG CANCER (SCLC) WITH DISEASE PROGRESSION ON OR AFTER PLATINUM-BASED CHEMOTHERAPY. |
| 4MG/VIAL | ZEPZELCA | JAZZ | N213702 | June 15, 2020 | RX | POWDER | INTRAVENOUS | 12324806 | May 29, 2040 | TREATING METASTATIC SCLC AFTER PLATINUM CHEMOTHERAPY WITH LURBINECTEDIN MONOTHERAPY BY REDUCING THE DOSE FOR GRADE ≥3 HEPATOTOXICITY FROM 3.2 TO 2.6 MG/M2 AND 2.6 TO 2.0 MG/M2 LURBINECTEDIN WITHIN 35 DAYS OF THE HIGHER DOSE IF HEPATOTOXICITY ≤GRADE 1 |
| 4MG/VIAL | ZEPZELCA | JAZZ | N213702 | June 15, 2020 | RX | POWDER | INTRAVENOUS | 12433890 | May 29, 2040 | TREATING METASTATIC SCLC AFTER PLATINUM CHEMOTHERAPY WITH LURBINECTEDIN MONOTHERAPY BY REDUCING THE DOSE FOR GRADE 4 OR ANY GRADE FEBRILE NEUTROPENIA FROM 3.2 TO 2.6 MG/M2 AND 2.6 TO 2.0 MG/M2 LURBINECTEDIN WITHIN 35 DAYS OF THE HIGHER DOSE |
| 4MG/VIAL | ZEPZELCA | JAZZ | N213702 | June 15, 2020 | RX | POWDER | INTRAVENOUS | 12440490 | May 29, 2040 | TREATING METASTATIC SCLC AFTER PLATINUM CHEMOTHERAPY WITH LURBINECTEDIN MONOTHERAPY BY REDUCING THE DOSE FOR GRADE 4 THROMBOCYTOPENIA OR GRADE 3 WITH BLEEDING FROM 3.2 TO 2.6 MG/M2 AND 2.6 TO 2.0 MG/M2 LURBINECTEDIN WITHIN 35 DAYS OF THE HIGHER DOSE |
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| 4MG/VIAL | ZEPZELCA | JAZZ | N213702 | June 15, 2020 | RX | POWDER | INTRAVENOUS | June 15, 2027 | INDICATED FOR THE TREATMENT OF ADULT PATIENTS WITH METASTATIC SMALL CELL LUNG CANCER (SCLC) WITH DISEASE PROGRESSION ON OR AFTER PLATINUM-BASED CHEMOTHERAPY |
| 4MG/VIAL | ZEPZELCA | JAZZ | N213702 | June 15, 2020 | RX | POWDER | INTRAVENOUS | Oct. 2, 2028 | LURBINECTEDIN IN COMBINATION WITH ATEZOLIZUMAB OR ATEZOLIZUMAB AND HYALURONIDASE-TQJS, FOR MAINTENANCE TREATMENT OF ADULT PATIENTS WITH EXTENSIVE-STAGE SMALL CELL LUNG CANCER WHOSE DISEASE HAS NOT PROGRESSED AFTER FIRST-LINE INDUCTION THERAPY WITH ATEZOLIZUMAB OR ATEZOLIZUMAB AND HYALURONIDASE-TQJS, CARBOPLATIN, AND ETOPOSIDE |
Bioactivity Summary:
None
External reference:
| ID | Source |
|---|---|
| D11644 | KEGG_DRUG |
| 2CN60TN6ZS | UNII |
| 4039494 | VANDF |
| C3898565 | UMLSCUI |
| CHEMBL4297516 | ChEMBL_ID |
| 57327016 | PUBCHEM_CID |
| DB12674 | DRUGBANK_ID |
| 9397 | INN_ID |
| C568606 | MESH_SUPPLEMENTAL_RECORD_UI |
| 10681 | IUPHAR_LIGAND_ID |
| 879925002 | SNOMEDCT_US |
| 879932006 | SNOMEDCT_US |
| CHEBI:746908 | CHEBI |
| A1JUE | PDB_CHEM_ID |
| 335658 | MMSL |
| 38550 | MMSL |
| d09579 | MMSL |
| 018414 | NDDF |
| 2374729 | RXNORM |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| ZEPZELCA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68727-712 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 0.50 mg | INTRAVENOUS | NDA | 28 sections |