motixafortide 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
peptides and glycopeptides 5744 664334-36-5

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • motixafortide
  • motixafortide acetate
  • aphexda
  • BL-8040
  • BKT140
  • 4F-benzoyl-TN14003
  • TF14016
Motixafortide is an inhibitor of the C-X-C Motif Chemokine Receptor 4 (CXCR4) and blocks the binding of its cognate ligand, stromal-derived factor-1alfa (SDF-1alfa)/C-X-C Motif Chemokine Ligand 12 (CXCL12). SDF-1alfa and CXCR4 play a role in the trafficking and homing of human hematopoietic stem cells to the marrow compartment. Once in the marrow, stem cell CXCR4 can help anchor these cells to the marrow matrix, either directly via SDF-1alfa or through the induction of other adhesion molecules. Treatment with motixafortide resulted in leukocytosis, and elevations in circulating hematopoietic stem and progenitor cells into the peripheral circulation in mice, rats, dogs, and humans. Stem cells mobilized by motixafortide were capable of engraftment with long-term repopulating capacity in a rodent transplantation model.
  • Molecular weight: 2159.55
  • Formula: C97H144FN33O19S2
  • CLOGP:
  • LIPINSKI: 3
  • HAC: 52
  • HDO: 34
  • TPSA: 892.04
  • ALOGS:
  • ROTB: 49

Drug dosage:

None

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

None

Approvals:

DateAgencyCompanyOrphan
Sept. 8, 2023 FDA BIOLINERX, LTD.

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 L03AX23 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
IMMUNOSTIMULANTS
IMMUNOSTIMULANTS
Other immunostimulants
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:68495 apoptosis inducer
CHEBI has role CHEBI:145438 C-X-C chemokine receptor type 4 antagonist

Related Drugs by ATC class:

L03AX Other immunostimulants 15 drugs

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

DiseaseRelationSNOMED_IDDOID
Mobilize hematopoietic stem cells for autologous transplantation in patients with multiple myeloma indication 879912005




🐶 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)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 62MG BASE/VIAL APHEXDA AYRMID PHARMA N217159 Sept. 8, 2023 RX POWDER SUBCUTANEOUS Sept. 8, 2028 NEW CHEMICAL ENTITY
EQ 62MG BASE/VIAL APHEXDA AYRMID PHARMA N217159 Sept. 8, 2023 RX POWDER SUBCUTANEOUS Sept. 8, 2030 TO MOBILIZE HEMATOPOIETIC STEM CELLS TO THE PERIPHERAL BLOOD FOR COLLECTION AND SUBSEQUENT AUTOLOGOUS TRANSPLANTATION IN PATIENTS WITH MULTIPLE MYELOMA

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
C-X-C chemokine receptor type 4 GPCR ANTAGONIST Kd 11.10 DRUG LABEL DRUG LABEL

External reference:

IDSource
CHEBI:145536 CHEBI
CHEMBL5095030 ChEMBL_ID
C116977 MESH_SUPPLEMENTAL_RECORD_UI
10679 IUPHAR_LIGAND_ID
DB14939 DRUGBANK_ID
4042614 VANDF
C5139777 UMLSCUI
CHEMBL5095449 ChEMBL_ID
10935 INN_ID
D12281 KEGG_DRUG
2639893-42-6 SECONDARY_CAS_RN
91865076 PUBCHEM_CID
371181 MMSL
41953 MMSL
d10105 MMSL
019555 NDDF
019556 NDDF
DA9G065962 UNII
2664896 RXNORM
C477728 MESH_SUPPLEMENTAL_RECORD_UI
C577220 MESH_SUPPLEMENTAL_RECORD_UI
C577039 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
APHEXDA HUMAN PRESCRIPTION DRUG LABEL 1 73441-062 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 62 mg SUBCUTANEOUS NDA 28 sections
Aphexda HUMAN PRESCRIPTION DRUG LABEL 1 82737-073 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 62 mg SUBCUTANEOUS NDA 16 sections