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

Stem definitionDrug idCAS RN
agammaglobulinaemia tyrosine kinase (Bruton tyrosine kinase) inhibitors 5709 2101700-15-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • pirtobrutinib
  • jaypirca
  • LOXO-305
  • LY3527727
  • RXC005
Pirtobrutinib is a small molecule, noncovalent inhibitor of BTK. BTK is a signaling protein of the B-cell antigen receptor (BCR) and cytokine receptor pathways. In B-cells, BTK signaling results in activation of pathways necessary for B-cell proliferation, trafficking, chemotaxis, and adhesion. Pirtobrutinib binds to wild type BTK and BTK harboring C481 mutations, leading to inhibition of BTK kinase activity. In nonclinical studies, pirtobrutinib inhibited BTK-mediated B-cell CD69 expression and inhibited malignant B-cell proliferation. Pirtobrutinib showed dose-dependent anti-tumor activities in BTK wild type and BTK C481S mutant mouse xenograft models.
  • Molecular weight: 479.44
  • Formula: C22H21F4N5O3
  • CLOGP:
  • LIPINSKI: 0
  • HAC: 8
  • HDO: 3
  • TPSA: 125.26
  • ALOGS:
  • ROTB: 8
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Jan. 27, 2023 FDA LOXO ONCOLOGY 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:

SourceCodeDescription
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D047428 Protein Kinase Inhibitors
FDA EPC N0000175605 Kinase Inhibitor
FDA MoA N0000182140 Cytochrome P450 2C19 Inhibitors
FDA MoA N0000185503 P-Glycoprotein Inhibitors
FDA MoA N0000187062 Cytochrome P450 2C8 Inhibitors
FDA MoA N0000190113 Breast Cancer Resistance Protein Inhibitors
FDA MoA N0000190114 Cytochrome P450 3A Inhibitors
FDA MoA N0000193934 Brutons Tyrosine Kinase Inhibitors

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

DiseaseRelationSNOMED_IDDOID
Relapsed or refractory mantle cell lymphoma (MCL) indication 443487006




🐶 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
100MG JAYPIRCA LOXO ONCOL N216059 Jan. 27, 2023 RX TABLET ORAL 10464905 Dec. 16, 2036 TREATMENT OF ADULT PATIENTS WITH RELAPSED OR REFRACTORY MANTLE CELL LYMPHOMA (MCL) AFTER AT LEAST TWO LINES OF SYSTEMIC THERAPY, INCLUDING A BTK INHIBITOR
100MG JAYPIRCA LOXO ONCOL N216059 Jan. 27, 2023 RX TABLET ORAL 10695323 Dec. 16, 2036 TREATMENT OF ADULT PATIENTS WITH RELAPSED OR REFRACTORY MANTLE CELL LYMPHOMA (MCL) AFTER AT LEAST TWO LINES OF SYSTEMIC THERAPY, INCLUDING A BTK INHIBITOR
100MG JAYPIRCA LOXO ONCOL N216059 Jan. 27, 2023 RX TABLET ORAL 10918622 Dec. 16, 2036 TREATMENT OF ADULT PATIENTS WITH RELAPSED OR REFRACTORY MANTLE CELL LYMPHOMA (MCL) AFTER AT LEAST TWO LINES OF SYSTEMIC THERAPY, INCLUDING A BTK INHIBITOR
50MG JAYPIRCA LOXO ONCOL N216059 Jan. 27, 2023 RX TABLET ORAL 10464905 Dec. 16, 2036 TREATMENT OF ADULT PATIENTS WITH RELAPSED OR REFRACTORY MANTLE CELL LYMPHOMA (MCL) AFTER AT LEAST TWO LINES OF SYSTEMIC THERAPY, INCLUDING A BTK INHIBITOR
50MG JAYPIRCA LOXO ONCOL N216059 Jan. 27, 2023 RX TABLET ORAL 10695323 Dec. 16, 2036 TREATMENT OF ADULT PATIENTS WITH RELAPSED OR REFRACTORY MANTLE CELL LYMPHOMA (MCL) AFTER AT LEAST TWO LINES OF SYSTEMIC THERAPY, INCLUDING A BTK INHIBITOR
50MG JAYPIRCA LOXO ONCOL N216059 Jan. 27, 2023 RX TABLET ORAL 10918622 Dec. 16, 2036 TREATMENT OF ADULT PATIENTS WITH RELAPSED OR REFRACTORY MANTLE CELL LYMPHOMA (MCL) AFTER AT LEAST TWO LINES OF SYSTEMIC THERAPY, INCLUDING A BTK INHIBITOR

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
100MG JAYPIRCA LOXO ONCOL N216059 Jan. 27, 2023 RX TABLET ORAL Jan. 27, 2028 NEW CHEMICAL ENTITY
50MG JAYPIRCA LOXO ONCOL N216059 Jan. 27, 2023 RX TABLET ORAL Jan. 27, 2028 NEW CHEMICAL ENTITY
100MG JAYPIRCA LOXO ONCOL N216059 Jan. 27, 2023 RX TABLET ORAL Jan. 27, 2030 TREATMENT OF ADULT PATIENTS WITH RELAPSED OR REFRACTORY MANTLE CELL LYMPHOMA (MCL) AFTER AT LEAST TWO LINES OF SYSTEMIC THERAPY, INCLUDING A BTK INHIBITOR
50MG JAYPIRCA LOXO ONCOL N216059 Jan. 27, 2023 RX TABLET ORAL Jan. 27, 2030 TREATMENT OF ADULT PATIENTS WITH RELAPSED OR REFRACTORY MANTLE CELL LYMPHOMA (MCL) AFTER AT LEAST TWO LINES OF SYSTEMIC THERAPY, INCLUDING A BTK INHIBITOR

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Tyrosine-protein kinase BTK Kinase INHIBITOR IC50 8.50 DRUG LABEL DRUG LABEL

External reference:

IDSource
Y7W PDB_CHEM_ID
CHEMBL4650485 ChEMBL_ID
C000723100 MESH_SUPPLEMENTAL_RECORD_UI
11628 IUPHAR_LIGAND_ID
019282 NDDF
4042010 VANDF
C5554559 UMLSCUI
11681 INN_ID
129269915 PUBCHEM_CID
2629338 RXNORM
D12050 KEGG_DRUG
JNA39I7ZVB UNII
364958 MMSL
41212 MMSL
d09984 MMSL

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
JAYPIRCA HUMAN PRESCRIPTION DRUG LABEL 1 0002-6902 TABLET, COATED 50 mg ORAL NDA 29 sections
JAYPIRCA HUMAN PRESCRIPTION DRUG LABEL 1 0002-7026 TABLET, COATED 100 mg ORAL NDA 29 sections