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

Stem definition	Drug id	CAS RN
transforming growth factor receptors	5364	1373715-00-4

Description:

Molecule	Description
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

Molecule

Description

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:

Dose	Unit	Route
3.33	mg	P

ADMET properties:

None

Approvals:

Date	Agency	Company	Orphan
June 25, 2020	EMA	Celgene Europe B.V.
Nov. 8, 2019	FDA	CELGENE CORP

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Extramedullary haemopoiesis	54.85	40.29	6	256	52	63488708
Haemoglobin decreased	40.96	40.29	17	245	145468	63343292

FDA Adverse Event Reporting System (Male)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Death	69.12	41.03	45	317	398004	34558565

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Death	77.11	36.15	49	545	566465	79177329
Haemoglobin decreased	62.24	36.15	31	563	222088	79521706
Extramedullary haemopoiesis	54.83	36.15	7	587	131	79743663

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
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

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

Disease	Relation	SNOMED_ID	DOID
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:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Growth/differentiation factor 11	Cytokine	O95390	GDF11_HUMAN	BINDING AGENT	Kd	10.13		SCIENTIFIC LITERATURE	DRUG LABEL
Growth/differentiation factor 8	Cytokine	O14793	GDF8_HUMAN	BINDING AGENT	Kd	9.69		SCIENTIFIC LITERATURE	DRUG LABEL

External reference:

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

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Reblozyl	HUMAN PRESCRIPTION DRUG LABEL	1	59572-711	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	25 mg	SUBCUTANEOUS	BLA	28 sections
Reblozyl	HUMAN PRESCRIPTION DRUG LABEL	1	59572-711	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	25 mg	SUBCUTANEOUS	BLA	28 sections
Reblozyl	HUMAN PRESCRIPTION DRUG LABEL	1	59572-711	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	25 mg	SUBCUTANEOUS	BLA	28 sections
Reblozyl	HUMAN PRESCRIPTION DRUG LABEL	1	59572-775	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	75 mg	SUBCUTANEOUS	BLA	28 sections
Reblozyl	HUMAN PRESCRIPTION DRUG LABEL	1	59572-775	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	75 mg	SUBCUTANEOUS	BLA	28 sections
Reblozyl	HUMAN PRESCRIPTION DRUG LABEL	1	59572-775	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	75 mg	SUBCUTANEOUS	BLA	28 sections