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

Stem definition	Drug id	CAS RN
	5356	1446321-46-5

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: voxelotor GBT440 oxbryta GTX-011	Voxelotor is a hemoglobin S (HbS) polymerization inhibitor that binds to HbS with a 1:1 stoichiometry and exhibits preferential partitioning to red blood cells (RBCs). By increasing the affinity of Hb for oxygen, voxelotor demonstrates dose-dependent inhibition of HbS polymerization. Nonclinical studies suggest that voxelotor may inhibit RBC sickling, improve RBC deformability, and reduce whole blood viscosity. Molecular weight: 337.38 Formula: C19H19N3O3 CLOGP: 3.29 LIPINSKI: 0 HAC: 6 HDO: 1 TPSA: 77.24 ALOGS: -3.81 ROTB: 6 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

voxelotor
GBT440
oxbryta
GTX-011

Voxelotor is a hemoglobin S (HbS) polymerization inhibitor that binds to HbS with a 1:1 stoichiometry and exhibits preferential partitioning to red blood cells (RBCs). By increasing the affinity of Hb for oxygen, voxelotor demonstrates dose-dependent inhibition of HbS polymerization. Nonclinical studies suggest that voxelotor may inhibit RBC sickling, improve RBC deformability, and reduce whole blood viscosity.

Molecular weight: 337.38
Formula: C19H19N3O3
CLOGP: 3.29
LIPINSKI: 0
HAC: 6
HDO: 1
TPSA: 77.24
ALOGS: -3.81
ROTB: 6

Status: ONP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

None

ADMET properties:

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Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Bocci G, Oprea TI, Benet LZ
S (Water solubility)	0.03 mg/mL	Bocci G, Oprea TI, Benet LZ

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Approvals:

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Date	Agency	Company	Orphan
Feb. 14, 2022	EMA	GLOBAL BLOOD THERAPEUTICS NETHERLANDS B. V.
Nov. 25, 2019	FDA	GLOBAL BLOOD THERAPEUTICS INC

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FDA Adverse Event Reporting System (Female)

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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
Sickle cell anaemia with crisis	1799.53	64.02	271	1245	5732	63481774
Acute chest syndrome	319.52	64.02	47	1469	774	63486732
Therapy cessation	256.65	64.02	71	1445	30386	63457120
Diarrhoea	99.81	64.02	102	1414	715264	62772242
Hypersplenism	92.93	64.02	14	1502	270	63487236
Abdominal symptom	73.69	64.02	12	1504	388	63487118
Therapy interrupted	69.87	64.02	27	1489	32428	63455078

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FDA Adverse Event Reporting System (Male)

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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
Sickle cell anaemia with crisis	1761.29	78.70	264	932	3789	34951946
Acute chest syndrome	486.95	78.70	71	1125	756	34954979
Therapy cessation	272.94	78.70	71	1125	16902	34938833
Hypersplenism	145.45	78.70	23	1173	425	34955310
Priapism	90.15	78.70	23	1173	4971	34950764
Abdominal symptom	85.58	78.70	15	1181	526	34955209
Osteonecrosis	81.00	78.70	27	1169	14863	34940872

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FDA Adverse Event Reporting System (Geriatric)

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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
Sickle cell anaemia with crisis	3234.08	72.82	471	1588	7451	79734878
Acute chest syndrome	755.36	72.82	109	1950	1452	79740877
Hypersplenism	251.90	72.82	37	2022	551	79741778
Therapy cessation	210.30	72.82	65	1994	37497	79704832
Abdominal symptom	167.87	72.82	27	2032	746	79741583
Osteonecrosis	117.52	72.82	40	2019	31055	79711274
Pain	99.22	72.82	105	1954	703697	79038632
Therapy interrupted	75.79	72.82	29	2030	31312	79711017
Cholelithiasis	73.85	72.82	33	2026	52631	79689698

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FDA Adverse Event Reporting System (Pediatric)

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Pharmacologic Action:

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Source	Code	Description
ATC	B06AX03	BLOOD AND BLOOD FORMING ORGANS OTHER HEMATOLOGICAL AGENTS OTHER HEMATOLOGICAL AGENTS Other hematological agents
FDA EPC	N0000194027	Hemoglobin S Polymerization Inhibitor
FDA MoA	N0000182141	Cytochrome P450 3A4 Inhibitors
FDA MoA	N0000194028	Hemoglobin S Polymerization Inhibitors
MeSH PA	D006401	Hematologic Agents

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

Disease	Relation	SNOMED_ID	DOID
Sickle cell disease	indication	417357006

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	8.15	acidic
pKa2	4.48	Basic
pKa3	2.17	Basic

Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
300MG	OXBRYTA	GLOBAL BLOOD THERAPS	N213137	Oct. 14, 2022	RX	TABLET	ORAL	9248199	Jan. 29, 2034	TREATMENT OF SICKLE CELL DISEASE BY ADMINISTERING VOXELOTOR, AS RECITED IN CLAIM 1
300MG	OXBRYTA	GLOBAL BLOOD THERAPS	N213137	Oct. 14, 2022	RX	TABLET	ORAL	9248199	Jan. 29, 2034	TREATMENT OF SICKLE CELL DISEASE BY ADMINISTERING VOXELOTOR, AS RECITED IN CLAIM 2
300MG	OXBRYTA	GLOBAL BLOOD THERAPS	N216157	Dec. 17, 2021	RX	TABLET, FOR SUSPENSION	ORAL	9248199	Jan. 29, 2034	TREATMENT OF SICKLE CELL DISEASE BY ADMINISTERING VOXELOTOR, AS RECITED IN CLAIM 1
300MG	OXBRYTA	GLOBAL BLOOD THERAPS	N216157	Dec. 17, 2021	RX	TABLET, FOR SUSPENSION	ORAL	9248199	Jan. 29, 2034	TREATMENT OF SICKLE CELL DISEASE BY ADMINISTERING VOXELOTOR, AS RECITED IN CLAIM 2
300MG	OXBRYTA	GLOBAL BLOOD THERAPS	N213137	Oct. 14, 2022	RX	TABLET	ORAL	11452720	Feb. 6, 2035	TREATING SICKLE CELL DISEASE BY ADMINISTERING VOXELOTOR AND ANOTHER ACTIVE AGENT
300MG	OXBRYTA	GLOBAL BLOOD THERAPS	N216157	Dec. 17, 2021	RX	TABLET, FOR SUSPENSION	ORAL	11452720	Feb. 6, 2035	TREATING SICKLE CELL DISEASE BY ADMINISTERING VOXELOTOR AND ANOTHER ACTIVE AGENT
300MG	OXBRYTA	GLOBAL BLOOD THERAPS	N213137	Oct. 14, 2022	RX	TABLET	ORAL	11020382	Dec. 2, 2036	INCREASING HEMOGLOBIN TO TREAT SICKLE CELL DISEASE BY ADMINISTERING 1500 MG OF VOXELOTOR ORALLY ONCE DAILY
300MG	OXBRYTA	GLOBAL BLOOD THERAPS	N213137	Oct. 14, 2022	RX	TABLET	ORAL	11020382	Dec. 2, 2036	TREATING SICKLE CELL DISEASE BY ADMINISTERING 1500 MG OF VOXELOTOR ORALLY ONCE DAILY
300MG	OXBRYTA	GLOBAL BLOOD THERAPS	N216157	Dec. 17, 2021	RX	TABLET, FOR SUSPENSION	ORAL	11020382	Dec. 2, 2036	INCREASING HEMOGLOBIN TO TREAT SICKLE CELL DISEASE BY ADMINISTERING 1500 MG OF VOXELOTOR ORALLY ONCE DAILY
300MG	OXBRYTA	GLOBAL BLOOD THERAPS	N216157	Dec. 17, 2021	RX	TABLET, FOR SUSPENSION	ORAL	11020382	Dec. 2, 2036	TREATING SICKLE CELL DISEASE BY ADMINISTERING 1500 MG OF VOXELOTOR ORALLY ONCE DAILY

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Orange Book exclusivity data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
300MG	OXBRYTA	GLOBAL BLOOD THERAPS	N216157	Dec. 17, 2021	RX	TABLET, FOR SUSPENSION	ORAL	Nov. 25, 2024	NEW CHEMICAL ENTITY
300MG	OXBRYTA	GLOBAL BLOOD THERAPS	N213137	Oct. 14, 2022	RX	TABLET	ORAL	Dec. 17, 2028	FOR TREATMENT OF SICKLE CELL DISEASE (SCD) IN PEDIATRIC PATIENTS 4 YEARS OF AGE TO LESS THAN 12 YEARS OF AGE
300MG	OXBRYTA	GLOBAL BLOOD THERAPS	N216157	Dec. 17, 2021	RX	TABLET, FOR SUSPENSION	ORAL	Dec. 17, 2028	FOR TREATMENT OF SICKLE CELL DISEASE (SCD) IN PEDIATRIC PATIENTS 4 YEARS OF AGE TO LESS THAN 12 YEARS OF AGE
500MG	OXBRYTA	GLOBAL BLOOD THERAPS	N213137	Nov. 25, 2019	RX	TABLET	ORAL	Nov. 25, 2024	NEW CHEMICAL ENTITY
500MG	OXBRYTA	GLOBAL BLOOD THERAPS	N213137	Nov. 25, 2019	RX	TABLET	ORAL	Nov. 25, 2026	INDICATED FOR THE TREATMENT OF SICKLE CELL DISEASE (SCD) IN ADULTS AND PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER
500MG	OXBRYTA	GLOBAL BLOOD THERAPS	N213137	Nov. 25, 2019	RX	TABLET	ORAL	Dec. 17, 2028	FOR TREATMENT OF SICKLE CELL DISEASE (SCD) IN PEDIATRIC PATIENTS 4 YEARS OF AGE TO LESS THAN 12 YEARS OF AGE

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
hemoglobin subunit alpha	Transporter	P69905	HBA_HUMAN	INHIBITOR	EC50	5.09	SCIENTIFIC LITERATURE	DRUG LABEL
Cytochrome P450 3A4	Enzyme	P08684	CP3A4_HUMAN	INHIBITOR	IC50	4.90	IUPHAR
Cytochrome P450 2C8	Enzyme	P10632	CP2C8_HUMAN	INHIBITOR	IC50	5.10	IUPHAR
Cytochrome P450 2C9	Enzyme	P11712	CP2C9_HUMAN	INHIBITOR	IC50	5.07	IUPHAR

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External reference:

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ID	Source
018213	NDDF
10454	INN_ID
10559	IUPHAR_LIGAND_ID
2265678	RXNORM
327648	MMSL
37796	MMSL
3ZO554A4Q8	UNII
4038992	VANDF
71602803	PUBCHEM_CID
833284006	SNOMEDCT_US

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
OXBRYTA	HUMAN PRESCRIPTION DRUG LABEL	1	72786-101	TABLET, FILM COATED	500 mg	ORAL	NDA	30 sections
OXBRYTA	HUMAN PRESCRIPTION DRUG LABEL	1	72786-101	TABLET, FILM COATED	500 mg	ORAL	NDA	30 sections
OXBRYTA	HUMAN PRESCRIPTION DRUG LABEL	1	72786-101	TABLET, FILM COATED	500 mg	ORAL	NDA	30 sections
OXBRYTA	HUMAN PRESCRIPTION DRUG LABEL	1	72786-102	TABLET, FILM COATED	300 mg	ORAL	NDA	30 sections
OXBRYTA	HUMAN PRESCRIPTION DRUG LABEL	1	72786-102	TABLET, FILM COATED	300 mg	ORAL	NDA	30 sections
OXBRYTA	HUMAN PRESCRIPTION DRUG LABEL	1	72786-111	TABLET, FOR SUSPENSION	300 mg	ORAL	NDA	30 sections
OXBRYTA	HUMAN PRESCRIPTION DRUG LABEL	1	72786-111	TABLET, FOR SUSPENSION	300 mg	ORAL	NDA	30 sections
OXBRYTA	HUMAN PRESCRIPTION DRUG LABEL	1	72786-111	TABLET, FOR SUSPENSION	300 mg	ORAL	NDA	30 sections

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