mifamurtide 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
peptides and glycopeptides 2960 90825-43-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • MTP-PE
  • mifamurtide hydrate
  • muramyl tripeptide phosphatidyl ethanolamine
  • mepact
  • mifamurtide sodium
  • mifamurtide
  • junovan
  • L-MTP-PE
Mifamurtide (muramyl tripeptide phosphatidyl ethanolamine, MTP-PE) is a fully synthetic derivative of muramyl dipeptide (MDP), the smallest naturally-occurring immune stimulatory component of cell walls from Mycobacterium sp. It has similar immunostimulatory effects as natural MDP with the additional advantage of a longer half-life in plasma. Mifamurtide liposomal formulation is specifically designed for in vivo targeting to macrophages by intravenous infusion. MTP-PE is a specific ligand of NOD2, a receptor found primarily on monocytes, dendritic cells and macrophages. MTP-PE is a potent activator of monocytes and macrophages. Activation of human macrophages by mifamurtide is associated with production of cytokines, including tumour necrosis factor (TNF-alfa), interleukin-1 (IL-1beta), IL-6, IL-8, and IL-12 and adhesion molecules, including lymphocyte function-associated antigen-1 (LFA-1) and intercellular adhesion molecule-1 (ICAM-1). In vitro-treated human monocytes killed allogeneic and autologous tumour cells (including melanoma, ovarian, colon, and renal carcinoma), but had no toxicity towards normal cells.
  • Molecular weight: 1237.52
  • Formula: C59H109N6O19P
  • CLOGP: 10.59
  • LIPINSKI: 4
  • HAC: 25
  • HDO: 10
  • TPSA: 376.10
  • ALOGS: -6
  • ROTB: 54

Drug dosage:

DoseUnitRoute
0.70 mg P

ADMET properties:

PropertyValueReference
Vd (Volume of distribution) 5.80 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 48.70 mL/min/kg Lombardo F, Berellini G, Obach RS
t_half (Half-life) 2.05 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
March 6, 2009 EMA Takeda France SAS

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:

SourceCodeDescription
ATC L03AX15 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
IMMUNOSTIMULANTS
IMMUNOSTIMULANTS
Other immunostimulants
MeSH PA D000276 Adjuvants, Immunologic
MeSH PA D007155 Immunologic Factors

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

DiseaseRelationSNOMED_IDDOID
Osteosarcoma of bone indication 307576001 DOID:3376




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 0.61 acidic
pKa2 11.44 acidic
pKa3 12.45 acidic
pKa4 12.94 acidic
pKa5 13.24 acidic
pKa6 13.32 acidic
pKa7 13.64 acidic
pKa8 13.96 acidic
pKa9 13.98 acidic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Nucleotide-binding oligomerization domain-containing protein 2 Cytosolic other ACTIVATOR DRUG LABEL DRUG LABEL

External reference:

IDSource
D06619 KEGG_DRUG
C0129341 UMLSCUI
CHEBI:135906 CHEBI
CHEMBL2111100 ChEMBL_ID
CHEMBL2107354 ChEMBL_ID
DB13615 DRUGBANK_ID
C037144 MESH_SUPPLEMENTAL_RECORD_UI
8274 IUPHAR_LIGAND_ID
1LM890Q4FY UNII
72734343 PUBCHEM_CID
013385 NDDF
710284002 SNOMEDCT_US
838853-48-8 SECONDARY_CAS_RN

Pharmaceutical products:

None