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pirtobrutinib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| agammaglobulinaemia tyrosine kinase (Bruton tyrosine kinase) inhibitors | 5709 | 2101700-15-4 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
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.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.20 | g | O |
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2A,ACVR2B,ALK,AURKA,AXL,BRAF,CAMK2B,CAMK2D,CDK9,CSF1R,DDR1,DYRK1B,EGFR,EIF2AK3,ERBB2,FLT3,GRK2,ITK,JAK1,KDR,LYN,MAP3K1,MAP3K10,MAP3K11,MAP3K21,MAP4K1,MAP4K3,MAPK10,MAPK7,MARK4,MET,NTRK1,PDK1,PDK2,PDK4,PIK3CA,PIK3CB,PIK3CD,PIK3CG,PRKCD,PRKDC,SIK2,SIK3,STK33,TGFBR1,TNIK,TTK,ULK1 | 48 | |||
| kinase-selectivity-class | AURKC,AXL,EIF2AK3,GRK2,PDK1,SIK2,SIK3 | 7 | |||
| mdck-mdr1-bcrp-efflux | MDCK-MDR1-BCRP efflux ratio | 15.205 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 1 | |||
| rat-kpuu-brain | Rat brain Kpuu | 0.020 | % | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 27, 2023 | FDA | LOXO ONCOLOGY INC | |
| Oct. 30, 2023 | EMA | ELI LILLY NEDERLAND B.V. |
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:
| Source | Code | Description |
|---|---|---|
| ATC | L01EL05 | ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS Bruton's tyrosine kinase (BTK) inhibitors |
| MeSH PA | D000092004 | Tyrosine Kinase Inhibitors |
| 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 |
| CHEBI has role | CHEBI:35610 | antineoplastic agent |
| CHEBI has role | CHEBI:35705 | immunosuppressive agent |
| CHEBI has role | CHEBI:68495 | apoptosis inducer |
| CHEBI has role | CHEBI:76617 | EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor |
Related Drugs by ATC class:
L01EL Bruton's tyrosine kinase (BTK) inhibitors 4 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| 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 strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
|---|---|---|---|---|---|---|---|---|---|---|
| 100MG | JAYPIRCA | LOXO ONCOL | N216059 | Jan. 27, 2023 | RX | TABLET | ORAL | 10464905 | Dec. 16, 2036 | TREATMENT OF ADULT PATIENTS WITH RELAPSED OR REFRACTORY CHRONIC LYMPHOCYTIC LEUKEMIA OR SMALL LYMPHOCYTIC LYMPHOMA (CLL/SLL) WHO HAVE PREVIOUSLY BEEN TREATED WITH A COVALENT BTK INHIBITOR |
| 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 CHRONIC LYMPHOCYTIC LEUKEMIA OR SMALL LYMPHOCYTIC LYMPHOMA (CLL/SLL) WHO HAVE PREVIOUSLY BEEN TREATED WITH A COVALENT 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 CHRONIC LYMPHOCYTIC LEUKEMIA OR SMALL LYMPHOCYTIC LYMPHOMA (CLL/SLL) WHO HAVE PREVIOUSLY BEEN TREATED WITH A COVALENT 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 |
| 100MG | JAYPIRCA | LOXO ONCOL | N216059 | Jan. 27, 2023 | RX | TABLET | ORAL | 12220401 | Dec. 16, 2036 | TREATMENT OF ADULT PATIENTS WITH RELAPSED OR REFRACTORY CHRONIC LYMPHOCYTIC LEUKEMIA OR SMALL LYMPHOCYTIC LYMPHOMA (CLL/SLL) WHO HAVE PREVIOUSLY BEEN TREATED WITH A COVALENT BTK INHIBITOR |
| 100MG | JAYPIRCA | LOXO ONCOL | N216059 | Jan. 27, 2023 | RX | TABLET | ORAL | 12220401 | 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 CHRONIC LYMPHOCYTIC LEUKEMIA OR SMALL LYMPHOCYTIC LYMPHOMA (CLL/SLL) WHO HAVE PREVIOUSLY BEEN TREATED WITH A COVALENT 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 CHRONIC LYMPHOCYTIC LEUKEMIA OR SMALL LYMPHOCYTIC LYMPHOMA (CLL/SLL) WHO HAVE PREVIOUSLY BEEN TREATED WITH A COVALENT 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 CHRONIC LYMPHOCYTIC LEUKEMIA OR SMALL LYMPHOCYTIC LYMPHOMA (CLL/SLL) WHO HAVE PREVIOUSLY BEEN TREATED WITH A COVALENT 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 |
| 50MG | JAYPIRCA | LOXO ONCOL | N216059 | Jan. 27, 2023 | RX | TABLET | ORAL | 12220401 | Dec. 16, 2036 | TREATMENT OF ADULT PATIENTS WITH RELAPSED OR REFRACTORY CHRONIC LYMPHOCYTIC LEUKEMIA OR SMALL LYMPHOCYTIC LYMPHOMA (CLL/SLL) WHO HAVE PREVIOUSLY BEEN TREATED WITH A COVALENT BTK INHIBITOR |
| 50MG | JAYPIRCA | LOXO ONCOL | N216059 | Jan. 27, 2023 | RX | TABLET | ORAL | 12220401 | 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 strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| 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 | Dec. 2, 2028 | EXPANSION TO THE TREATMENT OF ADULT PATIENTS WITH CHRONIC LYMPHOCYTIC LEUKEMIA OR SMALL LYMPHOCYTIC LYMPHOMA (CLL/SLL) INDICATION |
| 50MG | JAYPIRCA | LOXO ONCOL | N216059 | Jan. 27, 2023 | RX | TABLET | ORAL | Dec. 2, 2028 | EXPANSION TO THE TREATMENT OF ADULT PATIENTS WITH CHRONIC LYMPHOCYTIC LEUKEMIA OR SMALL LYMPHOCYTIC LYMPHOMA (CLL/SLL) INDICATION |
| 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 |
| 100MG | JAYPIRCA | LOXO ONCOL | N216059 | Jan. 27, 2023 | RX | TABLET | ORAL | Dec. 1, 2030 | TREATMENT OF ADULT PATIENTS WITH CHRONIC LYMPHOCYTIC LEUKEMIA OR SMALL LYMPHOCYTIC LYMPHOMA (CLL/SLL) WHO HAVE RECEIVED AT LEAST TWO PRIOR LINES OF THERAPY, INCLUDING A BTK INHIBITOR AND A BCL-2 INHIBITOR |
| 50MG | JAYPIRCA | LOXO ONCOL | N216059 | Jan. 27, 2023 | RX | TABLET | ORAL | Dec. 1, 2030 | TREATMENT OF ADULT PATIENTS WITH CHRONIC LYMPHOCYTIC LEUKEMIA OR SMALL LYMPHOCYTIC LYMPHOMA (CLL/SLL) WHO HAVE RECEIVED AT LEAST TWO PRIOR LINES OF THERAPY, INCLUDING A BTK INHIBITOR AND A BCL-2 INHIBITOR |
| 100MG | JAYPIRCA | LOXO ONCOL | N216059 | Jan. 27, 2023 | RX | TABLET | ORAL | Dec. 3, 2032 | TREATMENT OF ADULT PATIENTS WITH RELAPSED OR REFRACTORY CHRONIC LYMPHOCYTIC LEUKEMIA OR SMALL LYMPHOCYTIC LYMPHOMA (CLL/SLL) WHO HAVE PREVIOUSLY BEEN TREATED WITH A COVALENT BTK INHIBITOR, EXCLUDING PATIENTS WHO HAVE RECEIVED AT LEAST TWO PRIOR LINES OF THERAPY, INCLUDING A BTK INHIBITOR AND A BCL-2 INHIBITOR |
| 50MG | JAYPIRCA | LOXO ONCOL | N216059 | Jan. 27, 2023 | RX | TABLET | ORAL | Dec. 3, 2032 | TREATMENT OF ADULT PATIENTS WITH RELAPSED OR REFRACTORY CHRONIC LYMPHOCYTIC LEUKEMIA OR SMALL LYMPHOCYTIC LYMPHOMA (CLL/SLL) WHO HAVE PREVIOUSLY BEEN TREATED WITH A COVALENT BTK INHIBITOR, EXCLUDING PATIENTS WHO HAVE RECEIVED AT LEAST TWO PRIOR LINES OF THERAPY, INCLUDING A BTK INHIBITOR AND A BCL-2 INHIBITOR |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Tyrosine-protein kinase BTK | Kinase | INHIBITOR | IC50 | 8.50 | DRUG LABEL | DRUG LABEL |
External reference:
| ID | Source |
|---|---|
| CHEBI:229212 | CHEBI |
| Y7W | PDB_CHEM_ID |
| CHEMBL4650485 | ChEMBL_ID |
| C000723100 | MESH_SUPPLEMENTAL_RECORD_UI |
| 11628 | IUPHAR_LIGAND_ID |
| 1351539006 | SNOMEDCT_US |
| 4042010 | VANDF |
| C5554559 | UMLSCUI |
| 11681 | INN_ID |
| 129269915 | PUBCHEM_CID |
| 364958 | MMSL |
| 41212 | MMSL |
| d09984 | MMSL |
| 019282 | NDDF |
| D12050 | KEGG_DRUG |
| JNA39I7ZVB | UNII |
| 2629338 | RXNORM |
| JNA39I7ZVB | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| JAYPIRCA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0002-6902 | TABLET, COATED | 50 mg | ORAL | NDA | 30 sections |
| JAYPIRCA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0002-7026 | TABLET, COATED | 100 mg | ORAL | NDA | 30 sections |