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

Stem definitionDrug idCAS RN
transforming growth factor receptors 5364 1373715-00-4

Description:

MoleculeDescription

Synonyms:

  • luspatercept
  • luspatercept-aamt
  • reblozyl
  • ACE-536
  • ACE536
Luspatercept-aamt is a receptor fusion protein consisting of a modified extracellular domain of the human activin receptor type IIB linked to a human IgG1 Fc domain with a calculated molecular mass of approximately 76 kD. Luspatercept is produced in Chinese hamster ovary cells by recombinant DNA technology. It binds several endogenous TGF-beta superfamily ligands, thereby diminishing Smad2/3 signaling. Luspatercept-aamt promoted erythroid maturation through differentiation of late-stage erythroid precursors (normoblasts) in mice. In a model of beta-thalassemia, luspatercept-aamt decreased abnormally elevated Smad2/3 signaling and improved hematology parameters associated with ineffective erythropoiesis in mice.
  • Molecular weight:
  • Formula:
  • CLOGP:
  • LIPINSKI: None
  • HAC: None
  • HDO: None
  • TPSA:
  • ALOGS:
  • ROTB: None

Drug dosage:

DoseUnitRoute
3.33 mg P

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

None

Approvals:

DateAgencyCompanyOrphan
June 25, 2020 EMA Celgene Europe B.V.
Nov. 8, 2019 FDA CELGENE CORP

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Haemoglobin decreased 80.32 41.36 33 599 161923 90465892
Death 68.12 41.36 41 591 456510 90171305
Extramedullary haemopoiesis 51.68 41.36 7 625 224 90627591

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Death 94.29 37.50 82 941 471103 42149209
Extramedullary haemopoiesis 92.90 37.50 13 1010 145 42620167
Transformation to acute myeloid leukaemia 67.64 37.50 13 1010 1092 42619220
Haemoglobin decreased 60.05 37.50 38 985 132433 42487879
Weight decreased 44.67 37.50 38 985 207910 42412402

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Death 159.63 38.11 107 1476 698762 109888954
Haemoglobin decreased 111.20 38.11 59 1524 248668 110339048
Extramedullary haemopoiesis 105.27 38.11 15 1568 332 110587384
Transformation to acute myeloid leukaemia 96.32 38.11 17 1566 1506 110586210
Weight decreased 61.91 38.11 52 1531 468005 110119711
Off label use 45.12 38.11 78 1505 1500107 109087609
Hospitalisation 39.86 38.11 25 1558 142468 110445248

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC B03XA06 BLOOD AND BLOOD FORMING ORGANS
ANTIANEMIC PREPARATIONS
OTHER ANTIANEMIC PREPARATIONS
Other antianemic preparations
MeSH PA D006397 Hematinics
MeSH PA D006401 Hematologic Agents
FDA PE N0000009319 Increased Erythroid Cell Production
FDA EPC N0000194025 Erythroid Maturation Agent
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:75835 anti-anaemic agent

Related Drugs by ATC class:

B03XA Other antianemic preparations 8 drugs
daprodustatdarbepoetin alfaepoetin alfamethoxy polyethylene glycol-epoetin betamolidustatpeginesatideroxadustatvadadustat

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

DiseaseRelationSNOMED_IDDOID
beta Thalassemia indication 65959000 DOID:12241
Myelodysplastic syndrome indication 109995007




🐶 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:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Growth/differentiation factor 11 Cytokine BINDING AGENT Kd 10.13 SCIENTIFIC LITERATURE DRUG LABEL
Growth/differentiation factor 8 Cytokine BINDING AGENT Kd 9.69 SCIENTIFIC LITERATURE DRUG LABEL

External reference:

IDSource
4038947 VANDF
4038948 VANDF
CHEBI:755086 CHEBI
CHEMBL3039545 ChEMBL_ID
D11701 KEGG_DRUG
C000621232 MESH_SUPPLEMENTAL_RECORD_UI
10538 IUPHAR_LIGAND_ID
DB12281 DRUGBANK_ID
830158005 SNOMEDCT_US
830211009 SNOMEDCT_US
C4086553 UMLSCUI
9823 INN_ID
326571 MMSL
37653 MMSL
37654 MMSL
d09430 MMSL
018185 NDDF
AQK7UBA1LS UNII
2262543 RXNORM

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Reblozyl HUMAN PRESCRIPTION DRUG LABEL 1 59572-711 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 25 mg SUBCUTANEOUS BLA 27 sections
Reblozyl HUMAN PRESCRIPTION DRUG LABEL 1 59572-775 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 75 mg SUBCUTANEOUS BLA 27 sections