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

Stem definition	Drug id	CAS RN
	5336	1262449-58-0

Description:

Molecule	Description
Synonyms: andexanet alfa ondexxya PRT064445 PRT-064445 PRT-44545 PRT-4445 AndexXa AnXa IndexXa andexanet alfa (genetical recombination)	Andexanet alfa is a recombinant form of human FXa protein that has been modified to lack FXa enzymatic activity. The active site serine was substituted with alanine, rendering the molecule unable to cleave and activate prothrombin, and the gamma-carboxyglutamic acid (Gla) domain was removed to eliminate the ability of the protein to assemble into the prothrombinase complex, thus removing any anti-coagulant effects. Andexanet alfa is a specific reversal agent for FXa inhibitors. The predominant mechanism of action is the binding and sequestration of the FXa inhibitor, although there may be a minor contribution from the inhibition of tissue factor pathway inhibitor (TFPI) activity through binding to TFPI. The interaction between andexanet alfa and TFPI has not been fully characterized. Andexanet alfa binds direct FXa inhibitors with high affinity, making them unavailable to exert their anticoagulant effects Molecular weight: Formula: CLOGP: LIPINSKI: None HAC: None HDO: None TPSA: ALOGS: ROTB: None

Molecule

Description

Synonyms:

andexanet alfa
ondexxya
PRT064445
PRT-064445
PRT-44545
PRT-4445
AndexXa
AnXa
IndexXa
andexanet alfa (genetical recombination)

Andexanet alfa is a recombinant form of human FXa protein that has been modified to lack FXa enzymatic activity. The active site serine was substituted with alanine, rendering the molecule unable to cleave and activate prothrombin, and the gamma-carboxyglutamic acid (Gla) domain was removed to eliminate the ability of the protein to assemble into the prothrombinase complex, thus removing any anti-coagulant effects. Andexanet alfa is a specific reversal agent for FXa inhibitors. The predominant mechanism of action is the binding and sequestration of the FXa inhibitor, although there may be a minor contribution from the inhibition of tissue factor pathway inhibitor (TFPI) activity through binding to TFPI. The interaction between andexanet alfa and TFPI has not been fully characterized. Andexanet alfa binds direct FXa inhibitors with high affinity, making them unavailable to exert their anticoagulant effects

Molecular weight:
Formula:
CLOGP:
LIPINSKI: None
HAC: None
HDO: None
TPSA:
ALOGS:
ROTB: None

Drug dosage:

None

ADMET properties:

None

Approvals:

Date	Agency	Company
April 26, 2019	EMA	Portola Netherlands BV
May 3, 2018	FDA	Portola Pharamceuticals US
March 28, 2022	PMDA	Alexion Pharma G.K.

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
Cerebral infarction	150.33	123.31	28	114	23865	63465015

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
Cerebral infarction	97.46	58.98	24	183	27431	34929293
Heparin resistance	63.08	58.98	7	200	47	34956677

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
Cerebral infarction	219.03	76.07	50	379	45626	79698333
Heparin resistance	101.20	76.07	11	418	66	79743893

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	V03AB38	VARIOUS ALL OTHER THERAPEUTIC PRODUCTS ALL OTHER THERAPEUTIC PRODUCTS Antidotes

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

Disease	Relation	SNOMED_ID	DOID
Direct acting anticoagulant adverse reaction	indication	293332005

🐶 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
BI009E452R	UNII
C4079904	UMLSCUI
CHEMBL3301583	ChEMBL_ID
DB14562	DRUGBANK_ID
D11029	KEGG_DRUG
9883	INN_ID
7576	IUPHAR_LIGAND_ID
783678000	SNOMEDCT_US
783691004	SNOMEDCT_US
2045114	RXNORM
281836	MMSL
C580915	MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
ANDEXXA	HUMAN PRESCRIPTION DRUG LABEL	1	0310-3200	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	200 mg	INTRAVENOUS	BLA	27 sections
ANDEXXA	HUMAN PRESCRIPTION DRUG LABEL	1	0310-3200	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	200 mg	INTRAVENOUS	BLA	27 sections
ANDEXXA	HUMAN PRESCRIPTION DRUG LABEL	1	69853-0102	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	200 mg	INTRAVENOUS	BLA	28 sections
ANDEXXA	HUMAN PRESCRIPTION DRUG LABEL	1	69853-0102	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	200 mg	INTRAVENOUS	BLA	28 sections
ANDEXXA	HUMAN PRESCRIPTION DRUG LABEL	1	69853-0102	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	200 mg	INTRAVENOUS	BLA	28 sections
ANDEXXA	HUMAN PRESCRIPTION DRUG LABEL	1	69853-0102	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	200 mg	INTRAVENOUS	BLA	28 sections