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

Stem definitionDrug idCAS RN
agammaglobulinaemia tyrosine kinase (Bruton tyrosine kinase) inhibitors 5797 1575596-30-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • rilzabrutinib
  • wayrilz
  • PRN1008
  • SAR444671
Rilzabrutinib is a selective, covalent, reversible inhibitor of BTK, with a tailored residence time at BTK to reduce off-target effects. In ITP, rilzabrutinib mediates its therapeutic effect through multi-immune modulation by inhibiting B cell activation, interruption of FcgammaR mediated phagocytosis, and potentially amelioration of chronic inflammation associated with ITP.
  • Molecular weight: 665.77
  • Formula: C36H40FN9O3
  • CLOGP: 4.42
  • LIPINSKI: 2
  • HAC: 12
  • HDO: 1
  • TPSA: 138.66
  • ALOGS:
  • ROTB: 8
  • 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
Aug. 29, 2025 FDA Genzyme Corporation
Dec. 12, 2025 EMA Sanofi B.V.

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
Platelet count decreased 76.45 56.26 21 125 136948 90491353

FDA Adverse Event Reporting System (Male)

None

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
Platelet count decreased 116.86 57.76 36 233 230407 110358623
Diarrhoea 72.28 57.76 40 229 1139465 109449565
Nausea 61.16 57.76 37 232 1235653 109353377

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
MeSH PA D000092004 Tyrosine Kinase Inhibitors
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D047428 Protein Kinase Inhibitors
FDA EPC N0000175605 Kinase Inhibitor
FDA MoA N0000185503 P-Glycoprotein Inhibitors
FDA MoA N0000190107 Organic Anion Transporting Polypeptide 1B1 Inhibitors
FDA MoA N0000190108 Organic Anion Transporting Polypeptide 1B3 Inhibitors
FDA MoA N0000190113 Breast Cancer Resistance Protein Inhibitors
FDA MoA N0000190114 Cytochrome P450 3A Inhibitors
FDA MoA N0000193845 Bile Salt Export Pump Inhibitors
FDA MoA N0000193934 Brutons Tyrosine Kinase Inhibitors
CHEBI has role CHEBI:50177 dermatologic drug
CHEBI has role CHEBI:65023 anti-asthmatic agent
CHEBI has role CHEBI:67079 anti-inflammatory agent
CHEBI has role CHEBI:75835 anti-anaemic agent

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

DiseaseRelationSNOMED_IDDOID
Immune thrombocytopenia indication 2897005 DOID:1587




🐶 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 strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
400MG WAYRILZ GENZYME CORP N219685 Aug. 29, 2025 RX TABLET ORAL 8940744 Sept. 6, 2033 METHOD OF TREATMENT OF ADULT PATIENTS WITH PERSISTENT OR CHRONIC IMMUNE THROMBOCYTOPENIA (ITP) WHO HAVE HAD AN INSUFFICIENT RESPONSE TO A PREVIOUS TREATMENT
400MG WAYRILZ GENZYME CORP N219685 Aug. 29, 2025 RX TABLET ORAL 9266895 Sept. 6, 2033 METHOD OF INHIBITING BRUTONS TYROSINE KINASE ACTIVITY IN ADULT PATIENTS WITH PERSISTENT OR CHRONIC IMMUNE THROMBOCYTOPENIA (ITP) WHO HAVE HAD AN INSUFFICIENT RESPONSE TO A PREVIOUS TREATMENT
400MG WAYRILZ GENZYME CORP N219685 Aug. 29, 2025 RX TABLET ORAL 9994576 Sept. 6, 2033 METHOD OF INHIBITING BRUTONS TYROSINE KINASE ACTIVITY IN ADULT PATIENTS WITH PERSISTENT OR CHRONIC IMMUNE THROMBOCYTOPENIA (ITP) WHO HAVE HAD AN INSUFFICIENT RESPONSE TO A PREVIOUS TREATMENT
400MG WAYRILZ GENZYME CORP N219685 Aug. 29, 2025 RX TABLET ORAL 9994576 Sept. 6, 2033 METHOD OF TREATING PERSISTENT OR CHRONIC IMMUNE THROMBOCYTOPENIA (ITP) IN ADULT PATIENTS WHO HAVE HAD AN INSUFFICIENT RESPONSE TO A PREVIOUS TREATMENT
400MG WAYRILZ GENZYME CORP N219685 Aug. 29, 2025 RX TABLET ORAL 12178818 Oct. 13, 2040 METHOD FOR TREATING ADULT PATIENTS WITH PERSISTENT OR CHRONIC IMMUNE THROMBOCYTOPENIA (ITP) WHO HAVE HAD AN INSUFFICIENT RESPONSE TO A PREVIOUS TREATMENT, BY ACHIEVING A PLATELET COUNT OF AT LEAST 50,000/UL

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
400MG WAYRILZ GENZYME CORP N219685 Aug. 29, 2025 RX TABLET ORAL Aug. 29, 2030 NEW CHEMICAL ENTITY
400MG WAYRILZ GENZYME CORP N219685 Aug. 29, 2025 RX TABLET ORAL Aug. 29, 2032 TREATMENT OF ADULT PATIENTS WITH PERSISTENT OR CHRONIC IMMUNE THROMBOCYTOPENIA (ITP) WHO HAVE HAD AN INSUFFICIENT RESPONSE TO A PREVIOUS TREATMENT

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Tyrosine-protein kinase BTK Kinase INHIBITOR IC50 8.89 DRUG LABEL DRUG LABEL
Tyrosine-protein kinase Blk Kinase IC50 8.20 CHEMBL
Cytoplasmic tyrosine-protein kinase BMX Kinase IC50 9 CHEMBL
Tyrosine-protein kinase Tec Kinase IC50 9.10 CHEMBL
Tyrosine-protein kinase TXK Kinase IC50 8.92 CHEMBL

External reference:

IDSource
1575591-66-0 SECONDARY_CAS_RN
R1L PDB_CHEM_ID
CHEMBL3702854 ChEMBL_ID
C000731875 MESH_SUPPLEMENTAL_RECORD_UI
4044241 VANDF
C5420945 UMLSCUI
CHEBI:755717 CHEBI
10966 INN_ID
73388818 PUBCHEM_CID
397499 MMSL
44371 MMSL
d10311 MMSL
020213 NDDF
9993 IUPHAR_LIGAND_ID
NWN58M4F5T UNII
2722398 RXNORM
D11873 KEGG_DRUG

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
WAYRILZ HUMAN PRESCRIPTION DRUG LABEL 1 58468-0251 TABLET, FILM COATED 400 mg ORAL NDA 31 sections