melphalan flufenamide 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antineoplastic, alkylating agents, (beta-chloroethyl)amine derivatives | 5445 | 380449-51-4 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Melphalan flufenamide is a peptide conjugated alkylating drug. Due to its lipophilicity, melphalan flufenamide is passively distributed into cells and thereafter enzymatically hydrolyzed to melphalan. Similar to other nitrogen mustard drugs, crosslinking of DNA is involved in the antitumor activity of melphalan flufenamide. In cellular assays, melphalan flufenamide inhibited proliferation and induced apoptosis of hematopoietic and solid tumor cells. Additionally, melphalan flufenamide showed synergistic cytotoxicity with dexamethasone in melphalan resistant and non-resistant multiple myeloma cell lines.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
None
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Aug. 17, 2022 | EMA | ONCOPEPTIDES AB | |
| Feb. 26, 2021 | FDA | ONCOPEPTIDES AB |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
None
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | L01AA10 | ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS ALKYLATING AGENTS Nitrogen mustard analogues |
| FDA MoA | N0000000236 | Alkylating Activity |
| FDA EPC | N0000175558 | Alkylating Drug |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Relapsed or refractory multiple myeloma | indication | 109989006 | DOID:9538 |
| Breastfeeding (mother) | contraindication | 413712001 |
🐶 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 |
|---|---|---|---|---|---|---|---|---|---|---|
| EQ 20MG BASE/VIAL | PEPAXTO | ONCOPEPTIDES AB | N214383 | Feb. 26, 2021 | DISCN | POWDER | INTRAVENOUS | 6992207 | June 25, 2024 | IN COMBINATION WITH DEXAMETHASONE TO TREAT RELAPSED OR REFRACTORY MULTIPLE MYELOMA (REFACTORY TO AT LEAST 1 PROTEASOME INHIBITOR, 1 IMMUNOMODULATORY AGENT, AND 1 ANTI-CD38 MAB) IN ADULTS WHO RECEIVED AT LEAST 4 PRIOR LINES OF THERAPY |
| EQ 20MG BASE/VIAL | PEPAXTO | ONCOPEPTIDES AB | N214383 | Feb. 26, 2021 | DISCN | POWDER | INTRAVENOUS | 10543274 | April 25, 2032 | IN COMBINATION WITH DEXAMETHASONE TO TREAT RELAPSED OR REFRACTORY MULTIPLE MYELOMA (REFACTORY TO AT LEAST 1 PROTEASOME INHIBITOR, 1 IMMUNOMODULATORY AGENT, AND 1 ANTI-CD38 MAB) IN ADULTS WHO RECEIVED AT LEAST 4 PRIOR LINES OF THERAPY |
| EQ 20MG BASE/VIAL | PEPAXTO | ONCOPEPTIDES AB | N214383 | Feb. 26, 2021 | DISCN | POWDER | INTRAVENOUS | 11344622 | April 25, 2032 | IN COMBINATION WITH DEXAMETHASONE TO TREAT RELAPSED OR REFRACTORY MULTIPLE MYELOMA (REFACTORY TO AT LEAST 1 PROTEASOME INHIBITOR, 1 IMMUNOMODULATORY AGENT, AND 1 ANTI-CD38 MAB) IN ADULTS WHO RECEIVED AT LEAST 4 PRIOR LINES OF THERAPY |
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| EQ 20MG BASE/VIAL | PEPAXTO | ONCOPEPTIDES AB | N214383 | Feb. 26, 2021 | DISCN | POWDER | INTRAVENOUS | Feb. 26, 2026 | NEW CHEMICAL ENTITY |
| EQ 20MG BASE/VIAL | PEPAXTO | ONCOPEPTIDES AB | N214383 | Feb. 26, 2021 | DISCN | POWDER | INTRAVENOUS | Feb. 26, 2028 | TREATMENT OF ADULT PATIENTS WITH RELAPSED OR REFRACTORY MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST FOUR PRIOR LINES OF THERAPY AND WHOSE DISEASE IS REFRACTORY TO AT LEAST ONE PROTEASOME INHIBITOR, ONE IMMUNOMODULATORY AGENT, AND ONE CD-38 DIRECTED MONOCLONAL ANTIBODY |
Bioactivity Summary:
None
External reference:
| ID | Source |
|---|---|
| D11865 | KEGG_DRUG |
| F70C5K4786 | UNII |
| 380449-54-7 | SECONDARY_CAS_RN |
| C1435749 | UMLSCUI |
| CHEMBL4303060 | ChEMBL_ID |
| 9935639 | PUBCHEM_CID |
| DB16627 | DRUGBANK_ID |
| CHEMBL4297403 | ChEMBL_ID |
| C585069 | MESH_SUPPLEMENTAL_RECORD_UI |
| 11605 | IUPHAR_LIGAND_ID |
| 018648 | NDDF |
| 018649 | NDDF |
| 1149379008 | SNOMEDCT_US |
| 1179099000 | SNOMEDCT_US |
| 4040186 | VANDF |
| 2531369 | RXNORM |
| 344117 | MMSL |
| 39364 | MMSL |
| d09721 | MMSL |
| 9493 | INN_ID |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Pepaxto | HUMAN PRESCRIPTION DRUG LABEL | 1 | 73657-020 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 20 mg | INTRAVENOUS | NDA | 30 sections |