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

Stem definitionDrug idCAS RN
Janus kinase inhibitors, antineoplastics 5728 1792180-81-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • ritlecitinib
  • ritlecitinib tosylate
  • PF-06651600
  • litfulo
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.
  • Molecular weight: 285.35
  • Formula: C15H19N5O
  • CLOGP: 1.94
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 2
  • TPSA: 73.91
  • ALOGS:
  • ROTB: 3
  • Status: ONP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
50 mg O

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2B,AURKA,BLK,BMX,BTK,CAMK2D,CHEK2,CSNK1G2,DDR1,DYRK1B,EGFR,EIF2AK3,ERBB2,ERBB4,GRK2,ITK,JAK3,MAP3K10,MAP3K21,MAPK3,MARK4,PDK1,PDK2,PDK4,RIPK3,STK33 26
kinase-selectivity-class AURKA,BLK,BMX,BTK,CLK2,EGFR,ERBB2,ERBB4,JAK3,MAP3K10,MAP3K21,PDK1 12
mdck-mdr1-bcrp-efflux MDCK-MDR1-BCRP efflux ratio 8.933 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
rat-kpuu-brain Rat brain Kpuu 0.039 % High 1

Approvals:

DateAgencyCompanyOrphan
June 23, 2023 FDA PFIZER INC
Sept. 15, 2023 EMA PFIZER EUROPE MA EEIG
June 26, 2023 PMDA Pfizer Japan Inc.

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
Drug ineffective 157.50 44.91 116 735 1384182 89243414
Therapeutic product effect incomplete 142.95 44.91 57 794 193839 90433757
Condition aggravated 75.46 44.91 54 797 595491 90032105
Acne 66.77 44.91 20 831 28487 90599109
Product dose omission issue 44.99 44.91 30 821 291657 90335939

FDA Adverse Event Reporting System (Male)

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
Therapeutic product effect incomplete 161.99 67.62 49 378 70890 42550018
Drug ineffective 147.38 67.62 84 343 630113 41990795

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
Therapeutic product effect incomplete 256.64 48.79 92 1005 223713 110364489
Drug ineffective 250.66 48.79 163 934 1520377 109067825
Condition aggravated 104.51 48.79 73 1024 734763 109853439
Product dose omission issue 75.40 48.79 44 1053 321738 110266464
Acne 75.01 48.79 23 1074 33497 110554705

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L04AF08 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
IMMUNOSUPPRESSANTS
IMMUNOSUPPRESSANTS
Janus-associated kinase (JAK) inhibitors
MeSH PA D000075242 Janus Kinase Inhibitors
MeSH PA D000092004 Tyrosine Kinase Inhibitors
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D047428 Protein Kinase Inhibitors
CHEBI has role CHEBI:35472 anti-inflammatory drug
CHEBI has role CHEBI:35526 hypoglycemic agent
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:35705 immunosuppressive agent
CHEBI has role CHEBI:35842 antirheumatic drug
CHEBI has role CHEBI:50177 dermatologic drug
CHEBI has role CHEBI:67079 anti-inflammatory agent
CHEBI has role CHEBI:76617 EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor
CHEBI has role CHEBI:231911 renoprotective agent

Related Drugs by ATC class:

L04AF Janus-associated kinase (JAK) inhibitors 7 drugs
baricitinibdeucravacitinibdeuruxolitinibfilgotinibpeficitinibtofacitinibupadacitinib

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

DiseaseRelationSNOMED_IDDOID
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)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 50MG BASE LITFULO PFIZER N215830 June 23, 2023 RX CAPSULE ORAL 12077533 Dec. 3, 2034 METHOD OF TREATING SEVERE ALOPECIA AREATA IN ADULTS AND ADOLESCENTS 12 YEARS AND OLDER BY ADMINISTERING RITLECTINIB

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 50MG BASE LITFULO PFIZER N215830 June 23, 2023 RX CAPSULE ORAL June 23, 2028 NEW CHEMICAL ENTITY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA 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:

IDSource
CHEBI:229233 CHEBI
CHEMBL4085457 ChEMBL_ID
C000614924 MESH_SUPPLEMENTAL_RECORD_UI
9559 IUPHAR_LIGAND_ID
DB14924 DRUGBANK_ID
2054121000122104 SNOMEDCT_US
42476811000001107 SNOMEDCT_US
4042382 VANDF
C5418278 UMLSCUI
CHEMBL5314649 ChEMBL_ID
11170 INN_ID
2192215-81-7 SECONDARY_CAS_RN
118115473 PUBCHEM_CID
368615 MMSL
41733 MMSL
d10074 MMSL
019479 NDDF
019480 NDDF
D11970 KEGG_DRUG
2OYE00PC25 UNII
2641595 RXNORM
2OYE00PC25 INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Litfulo HUMAN PRESCRIPTION DRUG LABEL 1 0069-0334 CAPSULE 50 mg ORAL NDA 32 sections
Litfulo HUMAN PRESCRIPTION DRUG LABEL 1 63539-334 CAPSULE 50 mg ORAL NDA 32 sections