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 |
|---|---|
|
Synonyms:
|
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.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
None
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| 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 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 | 464.41 | 60.04 | 72 | 431 | 4471 | 50600150 |
| Therapy cessation | 123.47 | 60.04 | 32 | 471 | 25979 | 50578642 |
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 |
|---|---|---|---|---|---|---|
| Sickle cell anaemia with crisis | 223.75 | 75.14 | 34 | 180 | 2574 | 29571739 |
| Therapy cessation | 80.80 | 75.14 | 19 | 195 | 14443 | 29559870 |
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 |
|---|---|---|---|---|---|---|
| Sickle cell anaemia with crisis | 571.65 | 65.11 | 84 | 373 | 5248 | 64493027 |
| Therapy cessation | 74.49 | 65.11 | 21 | 436 | 32468 | 64465807 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | B06AX03 | BLOOD AND BLOOD FORMING ORGANS OTHER HEMATOLOGICAL AGENTS OTHER HEMATOLOGICAL AGENTS Other hematological agents |
| MeSH PA | D006401 | Hematologic Agents |
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)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
|---|---|---|---|---|---|---|---|---|---|---|
| 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 |
| 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 strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| 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 |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA 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:
| ID | Source |
|---|---|
| 3ZO554A4Q8 | UNII |
| C4723629 | UMLSCUI |
| CHEMBL4101807 | ChEMBL_ID |
| 71602803 | PUBCHEM_CID |
| DB14975 | DRUGBANK_ID |
| D11330 | KEGG_DRUG |
| 10559 | IUPHAR_LIGAND_ID |
| 2265678 | RXNORM |
| 327648 | MMSL |
| 37796 | MMSL |
| d09458 | MMSL |
| 833284006 | SNOMEDCT_US |
| 833304007 | SNOMEDCT_US |
| 4038992 | VANDF |
| 018213 | NDDF |
| C000628792 | MESH_SUPPLEMENTAL_RECORD_UI |
| 10454 | INN_ID |
Pharmaceutical products:
| 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 | 72786-111 | TABLET, FOR SUSPENSION | 300 mg | ORAL | NDA | 30 sections |