Ritlecitinib

Highest phase reached
Drug type
Small molecule
First approval year

First approval year
Listing at source
Listed
Highest phase reached

Drug type
Small molecule
Drug name
Ritlecitinib
Molecular weight
Structure (SMILES)
C=CC(=O)N1C[C@H](Nc2ncnc3[nH]ccc23)CC[C@@H]1C

  • 2 propen 1 one 1 2s 5r 2 methyl 5 7h pyrrolo 2 3 d pyrimidin 4 ylamino 1 piperidinyl
  • 2-PROPEN-1-ONE, 1-((2S,5R)-2-METHYL-5-(7H-PYRROLO(2,3-D)PYRIMIDIN-4-YLAMINO)-1-PIPERIDINYL)-
  • pf 06651600
  • Pf-06651600
  • PF-06651600
  • ritlecitinib
  • Ritlecitinib
  • ritlecitinib [INN]
  • Ritlecitinib [MI]
  • Ritlecitinib [WHO-DD]
  • ritlecitinib inn
  • ritlecitinib mi
  • ritlecitinib who dd

ATC classification codes
  • L04AF08
Sources for recorded values
CAS registry numbers
  • 1792180-81-4
ChEMBL ID
CHEMBL4085457
InChIKey
CBRJPFGIXUFMTM-WDEREUQCSA-N
PubChem compound IDs
  • 118115473
RxNorm IDs (RxCUI)
  • 2641595
FDA ingredient codes (UNII)
  • 2OYE00PC25

Applicant
PFIZER
Approval date
23 Jun 2023
Application number
NDA215830

Status
Authorised
Status date
15 Sept 2023
Authorisation date
15 Sept 2023
Approved indications
Litfulo is indicated for the treatment of severe alopecia areata in adults and adolescents 12 years of age and older.
Product number
EMEA/H/C/006025
Authorisation holder
Pfizer Europe MA EEIG
Priority medicines scheme
No
Generic
No
Biosimilar
No
Generic medicines
0
Biosimilar medicines
0
Advanced therapy
No
Conditional approval
No
Additional monitoring
Yes
Accelerated assessment
No
Exceptional circumstances
No

Therapeutic areas

  • Alopecia Areata
European medicines record

Patents
0
Designations
2
First in class
No
Fast track
No
Breakthrough designation
Yes
Orphan designation
No
Priority review
No
Orphan exclusivity
No
Accelerated approval
No
Availability
Prescription only
Boxed warning
Yes

Pharmacology name
ritlecitinib
Type
Synthetic organic
Drug name stem
-tinib
Approval recorded by Guide to Pharmacology
Yes

Administration routes

  • Oral

  • Action
    Inhibition
    Action type
    Inhibitor
    Target
    Janus kinase 1
    Gene symbol
    JAK1
    Protein identifier
    P23458
    Median affinity
    5.79
    Affinity units
    pIC50
  • Action
    Inhibition
    Action type
    Inhibitor
    Target
    Janus kinase 3
    Gene symbol
    JAK3
    Protein identifier
    P52333
    Median affinity
    9.52
    Affinity units
    pIC50
    Primary target
    Yes
  • Mechanism
    TEC family kinase inhibitor
    Action type
    Inhibitor
    Target
    TEC family kinase
    Protein identifier
    P42680
  • Mechanism
    TEC family kinase inhibitor
    Action type
    Inhibitor
    Target
    TEC family kinase
    Protein identifier
    P42681
  • Mechanism
    TEC family kinase inhibitor
    Action type
    Inhibitor
    Target
    TEC family kinase
    Protein identifier
    P51813
  • Mechanism
    TEC family kinase inhibitor
    Action type
    Inhibitor
    Target
    TEC family kinase
    Protein identifier
    Q06187
  • Mechanism
    TEC family kinase inhibitor
    Action type
    Inhibitor
    Target
    TEC family kinase
    Protein identifier
    Q08881
  • Mechanism
    Tyrosine-protein kinase JAK3 inhibitor
    Action type
    Inhibitor
    Target
    Tyrosine-protein kinase JAK3
    Protein identifier
    P52333

  • Mechanism
    TEC family kinase inhibitor
    Action type
    Inhibitor
    Target
    TEC family kinase
  • Mechanism
    Tyrosine-protein kinase JAK3 inhibitor
    Action type
    Inhibitor
    Target
    Tyrosine-protein kinase JAK3

  • Condition
    Crohn Disease
    Highest recorded phase
    2
    Condition identifier
    EFO:0000384
    Subject identifier
    D003424
  • Condition
    Arthritis, Rheumatoid
    Highest recorded phase
    2
    Condition identifier
    EFO:0000685
    Subject identifier
    D001172
  • Condition
    Colitis, Ulcerative
    Highest recorded phase
    2
    Condition identifier
    EFO:0000729
    Subject identifier
    D003093
  • Condition
    Celiac Disease
    Highest recorded phase
    2
    Condition identifier
    EFO:0001060
    Subject identifier
    D002446
  • Condition
    Liver Diseases
    Highest recorded phase
    1
    Condition identifier
    EFO:0001421
    Subject identifier
    D008107
  • Condition
    Kidney Diseases
    Highest recorded phase
    1
    Condition identifier
    EFO:0003086
    Subject identifier
    D007674
  • Condition
    Alopecia Areata
    Highest recorded phase
    3
    Condition identifier
    EFO:0004192
    Subject identifier
    D000506
  • Condition
    Vitiligo
    Highest recorded phase
    3
    Condition identifier
    EFO:0004208
    Subject identifier
    D014820
  • Condition
    Keloid
    Highest recorded phase
    2
    Condition identifier
    EFO:0004212
    Subject identifier
    D007627
  • Condition
    Sezary Syndrome
    Highest recorded phase
    2
    Condition identifier
    EFO:1000785
    Subject identifier
    D012751
  • Condition
    Mycosis Fungoides
    Highest recorded phase
    2
    Condition identifier
    EFO:1001051
    Subject identifier
    D009182
  • Condition
    Alopecia
    Highest recorded phase
    2
    Condition identifier
    EFO:1002028
    Subject identifier
    D000505
  • Condition
    Diabetes Mellitus, Type 1
    Highest recorded phase
    2
    Condition identifier
    MONDO:0005147
    Subject identifier
    D003922

  • Condition identifier
    EFO_0000384
    Highest recorded phase
    2
  • Condition identifier
    EFO_0000685
    Highest recorded phase
    2
  • Condition identifier
    EFO_0000729
    Highest recorded phase
    2
  • Condition identifier
    EFO_0001060
    Highest recorded phase
    2
  • Condition identifier
    EFO_0001421
    Highest recorded phase
    1
  • Condition identifier
    EFO_0003086
    Highest recorded phase
    1
  • Condition identifier
    EFO_0004192
  • Condition identifier
    EFO_0004208
    Highest recorded phase
    3
  • Condition identifier
    EFO_0004212
    Highest recorded phase
    2
  • Condition identifier
    EFO_1000710
    Highest recorded phase
    2
  • Condition identifier
    EFO_1002028
    Highest recorded phase
    2
  • Condition identifier
    MONDO_0000607
    Highest recorded phase
    2
  • Condition identifier
    MONDO_0004907
  • Condition identifier
    MONDO_0004907
    Highest recorded phase
    2
  • Condition identifier
    MONDO_0004979
    Highest recorded phase
    2
  • Condition identifier
    MONDO_0005011
    Highest recorded phase
    2
  • Condition identifier
    MONDO_0005101
    Highest recorded phase
    2
  • Condition identifier
    MONDO_0005147
    Highest recorded phase
    2
  • Condition identifier
    MONDO_0005340
    Highest recorded phase
    4
  • Condition identifier
    MONDO_0005348
    Highest recorded phase
    2
  • Condition identifier
    MONDO_0006559
    Highest recorded phase
    2
  • Condition identifier
    MONDO_0008383
    Highest recorded phase
    2
  • Condition identifier
    MONDO_0008661
    Highest recorded phase
    3
  • Condition identifier
    MONDO_0044212
    Highest recorded phase
    2

  • Warning
    Black Box Warning
    Effect
    carcinogenicity
    Country
    United States
  • Warning
    Black Box Warning
    Effect
    cardiotoxicity
    Country
    United States
  • Warning
    Black Box Warning
    Effect
    infectious disease
    Country
    United States
  • Warning
    Black Box Warning
    Effect
    vascular toxicity
    Country
    United States

Dose
50 mg
Route
Oral
How often
Once daily

  • Do not crush, split, or chew capsules
  • Swallow capsules whole

Hydrogen bond acceptors
4
Hydrogen bond donors
2
Polar surface area
73.91
Calculated partition coefficient (ALogP)
1.94
Calculated partition coefficient (XLogP)
2.1
Prodrug
No
Chirality
Single enantiomer
Inorganic
No
Rule-of-five violations
0
Rotatable bonds
3
Heavy atoms
21
Molecular formula
C15H19N5O
Monoisotopic mass
285.15896025
Natural product
No

Recorded assays
229
Active assays
65

  • Confirmatory
  • Other

Oral bioavailability

Median
64
Mean
75.2
Minimum
56
Maximum
109
Unit
%
Assays
5
Standard deviation
21.8335
Summary method
median
Censored results excluded
0
Other units excluded
0
Unknown units excluded
0

Measurement types

  • F

Related records

Trials (53)

In development for (15)

Other linked conditions (1)

Targets (6)