ritlecitinib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| Janus kinase inhibitors, antineoplastics | 5728 | 1792180-81-4 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Ritlecitinib irreversibly inhibits Janus kinase 3 (JAK3) and the tyrosine kinase expressed in hepatocellular carcinoma (TEC) kinase family by blocking the adenosine triphosphate (ATP) binding site. In cellular settings, ritlecitinib inhibits cytokine induced STAT phosphorylation mediated by JAK3-dependent receptors. Additionally, ritlecitinib inhibits signaling of immune receptors dependent on TEC kinase family members. The relevance of inhibition of specific JAK or TEC family enzymes to therapeutic effectiveness is not currently known.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
None
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| June 23, 2023 | FDA | PFIZER 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 |
|---|---|---|---|
| Alopecia areata | indication | 68225006 | DOID:986 |
🐶 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 strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| EQ 50MG BASE | LITFULO | PFIZER | N215830 | June 23, 2023 | RX | CAPSULE | ORAL | June 23, 2028 | NEW CHEMICAL ENTITY |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Tyrosine-protein kinase JAK3 | Kinase | INHIBITOR | IC50 | 7.48 | DRUG LABEL | DRUG LABEL | |||
| Receptor tyrosine-protein kinase erbB-4 | Kinase | IC50 | 4.60 | CHEMBL | |||||
| Cytoplasmic tyrosine-protein kinase BMX | Kinase | Ki | 6.26 | CHEMBL | |||||
| Tyrosine-protein kinase ITK/TSK | Kinase | Ki | 7.57 | CHEMBL | |||||
| Tyrosine-protein kinase JAK1 | Kinase | INHIBITOR | IC50 | 5.79 | IUPHAR | ||||
| Tyrosine-protein kinase Tec | Kinase | IC50 | 6.23 | CHEMBL | |||||
| Tyrosine-protein kinase TXK | Kinase | Ki | 6.88 | CHEMBL | |||||
| Tyrosine-protein kinase Blk | Kinase | IC50 | 4.72 | CHEMBL | |||||
| Tyrosine-protein kinase BTK | Kinase | IC50 | 6.22 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| CHEMBL4085457 | ChEMBL_ID |
| C000614924 | MESH_SUPPLEMENTAL_RECORD_UI |
| 9559 | IUPHAR_LIGAND_ID |
| DB14924 | DRUGBANK_ID |
| 019479 | NDDF |
| 019480 | NDDF |
| 4042382 | VANDF |
| C5418278 | UMLSCUI |
| 11170 | INN_ID |
| 2192215-81-7 | SECONDARY_CAS_RN |
| 118115473 | PUBCHEM_CID |
| 2641595 | RXNORM |
| D11970 | KEGG_DRUG |
| 2OYE00PC25 | UNII |
| 41733 | MMSL |
| d10074 | MMSL |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Litfulo | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0069-0334 | CAPSULE | 50 mg | ORAL | NDA | 30 sections |
| Litfulo | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63539-334 | CAPSULE | 50 mg | ORAL | NDA | 30 sections |