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

Stem definitionDrug idCAS RN
5356 1446321-46-5

Description:

MoleculeDescription

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:

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

Approvals:

DateAgencyCompanyOrphan
Feb. 14, 2022 EMA GLOBAL BLOOD THERAPEUTICS NETHERLANDS B. V.
Nov. 25, 2019 FDA GLOBAL BLOOD THERAPEUTICS INC

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
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

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
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

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
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

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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

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

DiseaseRelationSNOMED_IDDOID
Sickle cell disease indication 417357006




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.15 acidic
pKa2 4.48 Basic
pKa3 2.17 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent 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
500MG OXBRYTA GLOBAL BLOOD THERAPS N213137 Nov. 25, 2019 RX TABLET ORAL 9248199 Jan. 29, 2034 TREATMENT OF SICKLE CELL DISEASE BY ADMINISTERING VOXELOTOR, AS RECITED IN CLAIM 1
500MG OXBRYTA GLOBAL BLOOD THERAPS N213137 Nov. 25, 2019 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
500MG OXBRYTA GLOBAL BLOOD THERAPS N213137 Nov. 25, 2019 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
500MG OXBRYTA GLOBAL BLOOD THERAPS N213137 Nov. 25, 2019 RX TABLET ORAL 11020382 Dec. 2, 2036 INCREASING HEMOGLOBIN TO TREAT SICKLE CELL DISEASE BY ADMINISTERING 1500 MG OF VOXELOTOR ORALLY ONCE DAILY
500MG OXBRYTA GLOBAL BLOOD THERAPS N213137 Nov. 25, 2019 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

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
500MG OXBRYTA GLOBAL BLOOD THERAPS N213137 Nov. 25, 2019 RX TABLET ORAL Nov. 25, 2024 NEW CHEMICAL ENTITY
300MG OXBRYTA GLOBAL BLOOD THERAPS N216157 Dec. 17, 2021 RX TABLET, FOR SUSPENSION 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
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
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
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

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
hemoglobin subunit alpha Transporter INHIBITOR EC50 5.09 SCIENTIFIC LITERATURE DRUG LABEL
Cytochrome P450 3A4 Enzyme INHIBITOR IC50 4.90 IUPHAR
Cytochrome P450 2C8 Enzyme INHIBITOR IC50 5.10 IUPHAR
Cytochrome P450 2C9 Enzyme INHIBITOR IC50 5.07 IUPHAR

External reference:

IDSource
3ZO554A4Q8 UNII
C4723629 UMLSCUI
CHEMBL4101807 ChEMBL_ID
71602803 PUBCHEM_CID
DB14975 DRUGBANK_ID
D11330 KEGG_DRUG
10454 INN_ID
10559 IUPHAR_LIGAND_ID
018213 NDDF
833284006 SNOMEDCT_US
833304007 SNOMEDCT_US
4038992 VANDF
2265678 RXNORM
327648 MMSL
37796 MMSL
d09458 MMSL
C000628792 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
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