tovorafenib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
Raf (Rapidely Accelerated Fibrosarcoma) kinase inhibitors 5819 1096708-71-2

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • tovorafenib
  • ojemda
  • DAY101
  • TAK-580
  • MLN2480
Tovorafenib is a Type II RAF kinase inhibitor of mutant BRAF V600E, wild-type BRAF, and wild-type CRAF kinases. Tovorafenib exhibited antitumor activity in cultured cells and xenograft tumor models harboring BRAF V600E and V600D mutations, and in a xenograft model harboring a BRAF fusion.
  • Molecular weight: 506.29
  • Formula: C17H12Cl2F3N7O2S
  • CLOGP: 3.98
  • LIPINSKI: 1
  • HAC: 9
  • HDO: 3
  • TPSA: 135.78
  • ALOGS:
  • ROTB: 6

  • Status: ONP

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

Drug dosage:

None

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

None

Approvals:

DateAgencyCompanyOrphan
April 23, 2024 FDA Day One Biopharmaceuticals, Inc.
April 20, 2026 EMA Ipsen Pharma

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:

SourceCodeDescription
ATC L01EC04 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
PROTEIN KINASE INHIBITORS
B-Raf serine-threonine kinase (BRAF) inhibitors
FDA EPC N0000175605 Kinase Inhibitor
FDA MoA N0000190118 Cytochrome P450 3A Inducers
FDA MoA N0000194133 Type II RAF Kinase Inhibitors
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:68495 apoptosis inducer
CHEBI has role CHEBI:75047 B-Raf inhibitor

Related Drugs by ATC class:

L01EC B-Raf serine-threonine kinase (BRAF) inhibitors 3 drugs

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

DiseaseRelationSNOMED_IDDOID
Relapsed or refractory pediatric low-grade glioma indication 74532006




🐶 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)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
100MG OJEMDA DAY ONE BIOPHARMS N217700 April 23, 2024 RX TABLET ORAL April 23, 2029 NEW CHEMICAL ENTITY
25MG/ML OJEMDA DAY ONE BIOPHARMS N218033 April 23, 2024 RX FOR SUSPENSION ORAL April 23, 2029 NEW CHEMICAL ENTITY
100MG OJEMDA DAY ONE BIOPHARMS N217700 April 23, 2024 RX TABLET ORAL April 23, 2031 TREATMENT OF PATIENTS 6 MONTHS OF AGE AND OLDER WITH RELAPSED OR REFRACTORY PEDIATRIC LOW-GRADE GLIOMA (LGG) HARBORING A BRAF FUSION OR REARRANGEMENT, OR BRAF V600 MUTATION
25MG/ML OJEMDA DAY ONE BIOPHARMS N218033 April 23, 2024 RX FOR SUSPENSION ORAL April 23, 2031 TREATMENT OF PATIENTS 6 MONTHS OF AGE AND OLDER WITH RELAPSED OR REFRACTORY PEDIATRIC LOW-GRADE GLIOMA (LGG) HARBORING A BRAF FUSION OR REARRANGEMENT, OR BRAF V600 MUTATION

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
RAF proto-oncogene serine/threonine-protein kinase Kinase INHIBITOR IC50 9.15 DRUG LABEL DRUG LABEL
Serine/threonine-protein kinase B-raf Kinase INHIBITOR IC50 8.08 DRUG LABEL DRUG LABEL
Breakpoint cluster region protein Kinase Kd 6.53 CHEMBL
Ephrin type-A receptor 2 Kinase Kd 6.09 CHEMBL
Myosin light chain kinase, smooth muscle Kinase Kd 5.36 CHEMBL
LIM domain kinase 1 Kinase Kd 5.99 CHEMBL
Abelson tyrosine-protein kinase 2 Kinase Kd 7 CHEMBL
Mitogen-activated protein kinase 11 Kinase Kd 6.17 CHEMBL
Mitogen-activated protein kinase 14 Kinase Kd 6.45 CHEMBL
Tyrosine-protein kinase FRK Kinase Kd 6.76 CHEMBL
Dual specificity protein kinase CLK1 Kinase Kd 6.03 CHEMBL
Epithelial discoidin domain-containing receptor 1 Kinase Kd 7.20 CHEMBL
Platelet-derived growth factor receptor beta Kinase Kd 4.95 CHEMBL
TGF-beta receptor type-2 Kinase Kd 5.79 CHEMBL
Wee1-like protein kinase Kinase Kd 6.60 CHEMBL
Mitogen-activated protein kinase kinase kinase MLT Kinase Kd 6.35 CHEMBL
Discoidin domain-containing receptor 2 Kinase Kd 6.64 CHEMBL
Dual specificity mitogen-activated protein kinase kinase 4 Kinase Kd 6.84 CHEMBL
Ephrin type-A receptor 1 Kinase Kd 5.97 CHEMBL
Dual specificity tyrosine-phosphorylation-regulated kinase 1A Kinase Kd 5.49 CHEMBL
Ephrin type-B receptor 6 Kinase Kd 5.48 CHEMBL
Mitogen-activated protein kinase kinase kinase 1 Kinase Kd 5.68 CHEMBL
Receptor-interacting serine/threonine-protein kinase 3 Kinase Kd 5.75 CHEMBL
Ephrin type-B receptor 4 Kinase Kd 5.03 CHEMBL
Tyrosine-protein kinase ABL1 Kinase Kd 6.30 CHEMBL

External reference:

IDSource
QOP PDB_CHEM_ID
CHEMBL3348923 ChEMBL_ID
C000626518 MESH_SUPPLEMENTAL_RECORD_UI
DB15266 DRUGBANK_ID
4043091 VANDF
C4287814 UMLSCUI
11985 INN_ID
25161177 PUBCHEM_CID
384705 MMSL
42790 MMSL
d10185 MMSL
019731 NDDF
9977 IUPHAR_LIGAND_ID
ZN90E4027M UNII
2682434 RXNORM
D12291 KEGG_DRUG
CHEBI:167672 CHEBI
ZN90E4027M INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
OJEMDA HUMAN PRESCRIPTION DRUG LABEL 1 82950-001 TABLET, FILM COATED 100 mg ORAL NDA 32 sections