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melphalan flufenamide 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2A,ACVR2B,AKT1,AKT2,AKT3,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,DDR1,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,IGF1R,ITK,JAK2,JAK3,MAP2K6,MAP3K21,MAP3K7,MAP4K1,MAPK10,MAPK12,MAPK7,MAPK9,MAPKAPK2,MARK4,MET,NTRK2,PAK4,PDK1,PDK2,PDK4,PDPK1,PIK3CA,PIK3CB,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK,ZAP70 | 56 | |||
| kinase-selectivity-class | AXL,EIF2AK3,GRK2,PDK4 | 4 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Feb. 26, 2021 | FDA | ONCOPEPTIDES AB | |
| Aug. 17, 2022 | EMA | 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 |
| CHEBI has role | CHEBI:35610 | antineoplastic agent |
Related Drugs by ATC class:
L01AA Nitrogen mustard analogues 8 drugs
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)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
None
External reference:
| ID | Source |
|---|---|
| D11865 | KEGG_DRUG |
| F70C5K4786 | UNII |
| 380449-54-7 | SECONDARY_CAS_RN |
| C1435749 | UMLSCUI |
| CHEBI:757647 | CHEBI |
| CHEMBL4303060 | ChEMBL_ID |
| 9935639 | PUBCHEM_CID |
| DB16627 | DRUGBANK_ID |
| CHEMBL4297403 | ChEMBL_ID |
| 9493 | INN_ID |
| C585069 | MESH_SUPPLEMENTAL_RECORD_UI |
| 11605 | IUPHAR_LIGAND_ID |
| 1149379008 | SNOMEDCT_US |
| 1179099000 | SNOMEDCT_US |
| 4040186 | VANDF |
| 344117 | MMSL |
| 39364 | MMSL |
| d09721 | MMSL |
| 018648 | NDDF |
| 018649 | NDDF |
| 2531369 | RXNORM |
Pharmaceutical products:
None