olutasidenib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| isocitrate dehydrogenase inhibitors | 5693 | 1887014-12-1 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Olutasidenib is a small-molecule inhibitor of mutated isocitrate dehydrogenase-1 (IDH1). In patients with AML, susceptible IDH1 mutations are defined as those leading to increased levels of 2- hydroxyglutarate (2-HG) in the leukemia cells and where efficacy is predicted by 1) clinically meaningful remissions with the recommended dose of olutasidenib and/or 2) inhibition of mutant IDH1 enzymatic activity at concentrations of olutasidenib sustainable at the recommended dosage according to validated methods. The most common of such mutations in patients with AML are R132H and R132C substitutions. In vitro, olutasidenib inhibited mutated IDH1 R132H, R132L, R132S, R132G, and R132C proteins; wild-type IDH1 or mutated IDH2 proteins were not inhibited. Olutasidenib inhibition of mutant IDH1 led to decreased 2-HG levels in vitro and in in vivo xenograft models.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
None
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Dec. 1, 2022 | FDA | RIGEL PHARMS INC |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
None
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
None
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Acute myeloid leukemia, disease | indication | 91861009 | |
| Relapsing acute myeloid leukemia with a susceptible IDH1 mutation | indication | ||
| Refractory acute myeloid leukemia with a susceptible IDH1 mutation | indication |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
None
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 |
|---|---|---|---|---|---|---|---|---|---|---|
| 150MG | REZLIDHIA | RIGEL PHARMS INC | N215814 | Dec. 1, 2022 | RX | CAPSULE | ORAL | 9834539 | Sept. 18, 2035 | A METHOD OF TREATING A CANCER WHERE THE CANCER IS ACUTE MYELOID LEUKEMIA (AML) |
| 150MG | REZLIDHIA | RIGEL PHARMS INC | N215814 | Dec. 1, 2022 | RX | CAPSULE | ORAL | 11013733 | May 16, 2039 | A METHOD OF TREATING A CANCER CHARACTERIZED BY AN IDH1 MUTATION WHERE THE CANCER IS ACUTE MYELOID LEUKEMIA (AML) |
| 150MG | REZLIDHIA | RIGEL PHARMS INC | N215814 | Dec. 1, 2022 | RX | CAPSULE | ORAL | 11013734 | May 16, 2039 | A METHOD OF TREATING ACUTE MYELOID LEUKEMIA (AML) IN PATIENTS WITH AN ISOCITRATE DEHYDROGENASE-1 (IDH1) MUTATION |
| 150MG | REZLIDHIA | RIGEL PHARMS INC | N215814 | Dec. 1, 2022 | RX | CAPSULE | ORAL | 11376246 | May 16, 2039 | A METHOD OF TREATING ACUTE MYELOID LEUKEMIA (AML) IN PATIENTS WITH AN ISOCITRATE DEHYDROGENASE-1 (IDH1) MUTATION |
| 150MG | REZLIDHIA | RIGEL PHARMS INC | N215814 | Dec. 1, 2022 | RX | CAPSULE | ORAL | 11497743 | May 16, 2039 | A METHOD OF TREATING ACUTE MYELOID LEUKEMIA (AML) IN PATIENTS WITH AN ISOCITRATE DEHYDROGENASE-1 (IDH1) MUTATION |
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| 150MG | REZLIDHIA | RIGEL PHARMS INC | N215814 | Dec. 1, 2022 | RX | CAPSULE | ORAL | Dec. 1, 2027 | NEW CHEMICAL ENTITY |
| 150MG | REZLIDHIA | RIGEL PHARMS INC | N215814 | Dec. 1, 2022 | RX | CAPSULE | ORAL | Dec. 1, 2029 | TREATMENT OF ADULT PATIENTS WITH RELAPSED OR REFRACTORY ACUTE MYELOID LEUKEMIA (AML) WITH A SUSCEPTIBLE ISOCITRATE DEHYDROGENASE-1 (IDH1) MUTATION AS DETECTED BY AN FDA-APPROVED TEST |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Isocitrate dehydrogenase [NADP] cytoplasmic | Enzyme | INHIBITOR | IC50 | 7.67 | SCIENTIFIC LITERATURE | DRUG LABEL | |||
| Isocitrate dehydrogenase [NADP], mitochondrial | Enzyme | IC50 | 4.56 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| PWV | PDB_CHEM_ID |
| CHEMBL4297610 | ChEMBL_ID |
| C000710173 | MESH_SUPPLEMENTAL_RECORD_UI |
| 10319 | IUPHAR_LIGAND_ID |
| DB16267 | DRUGBANK_ID |
| 019241 | NDDF |
| 4041886 | VANDF |
| C5235389 | UMLSCUI |
| 11036 | INN_ID |
| D12483 | KEGG_DRUG |
| 118955396 | PUBCHEM_CID |
| 2623641 | RXNORM |
| 364106 | MMSL |
| 41136 | MMSL |
| d09955 | MMSL |
| 0T4IMT8S5Z | UNII |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| REZLIDHIA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 71332-005 | CAPSULE | 150 mg | ORAL | NDA | 28 sections |