Ritlecitinib
Highest phase reached
Approved
Drug type
Small molecule
First approval year
2023
- First approval year
- 2023
- Listing at source
- Listed
- Highest phase reached
- Approved
- Drug type
- Small molecule
- Drug name
- Ritlecitinib
- Molecular weight
- 285.35
- 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
- NCT02958865
- NCT02969044
- NCT04413617
- NCT02974868
- NCT03732807
- NCT04006457
- NCT04517864
- NCT05650333
- NCT03395184
- NCT03715829
- NCT05583526
- NCT06072183
- NCT06163326
- NCT04016077
- NCT04037865
- NCT05549934
- NCT05636293
- NCT05743244
- NCT05879458
- NCT06373458
- 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
- Janus Kinase Inhibitors
- Tyrosine Kinase Inhibitors
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)
- A 104-Week Study of Ritlecitinib Oral Capsules in Adults With Nonsegmental Vitiligo (Active and Stable) Tranquillo 2
- A 16-Week Study to Learn About the Study Medicine Called Ritlecitinib in Adults With Long Lasting Painful Red Skin Lumps, Known by the Medical Term, Hidradenitis Suppurativa, or HS.
- A 52-Week Study of Ritlecitinib Oral Capsules in Adults and Adolescents With Nonsegmental Vitiligo (Active and Stable) Tranquillo
- A 52-Week Study to Learn About the Safety and Effects of Ritlecitinib in Participants With Nonsegmental Vitiligo
- A DRUG-DRUG INTERACTION STUDY BETWEEN PF-06650833 AND PF-06651600 FOLLOWING MULTIPLE DOSES IN HEALTHY PARTICIPANTS
- A Long-Term Study to Learn About The Study Medicine Called Ritlecitinib in Children With Severe Alopecia Areata.
- A Phase 2b Study To Evaluate The Efficacy And Safety Profile Of PF-06651600 And PF-06700841 In Active Non-segmental Vitiligo Subjects
- A Renal Impairment Study for PF-06651600
- A Single Dose Study To Test Two Pediatric Forms Of Ritlecitinib Compared With Adult Ritlecitinib In Healthy Adults
- A Study in Young People and Adults to Learn About the Medicine Ritlecitinib for Treatment of Patchy Hair Loss, Known by the Medical Term as Moderate Alopecia Areata
- A Study of 2 Doses of Ritlecitinib in People 12 Years of Age and Older With Alopecia Areata
- A Study of PF-06651600 Effect on Rosuvastatin Pharmacokinetics in Healthy Participants
- A Study to Assess Two Forms of The Study Medicine (Ritlecitinib) in Healthy Adult Participants
- A STUDY TO ESTIMATE THE EFFECT OF PF-06651600 ON THE PHARMACOKINETICS (PK) OF ORAL CONTRACEPTIVE (OC)
- A STUDY TO EVALUATE THE EFFECT OF PF-06651600 ON PHARMACOKINETICS OF SINGLE DOSE SUMATRIPTAN IN HEALTHY PARTICIPANTS.
- A Study to Evaluate the Pharmacokinetics, Safety and Tolerability of PF-06651600 in Subjects With Hepatic Impairment and Healthy Volunteers
- A Study to Learn About How Different Forms of the Study Medicine Called Ritlecitinib Pass the Intestines of Healthy Male Adults When Taken With or Without Food
- A Study to Learn About Medicine Called Ritlecitinib in Children Aged Between 6 to 12 Years With Severe Alopecia Areata
- A Study to Learn About Ritlecitinib for the Potential Treatment of Chronic Spontaneous Urticaria in Adults.
- A Study to Learn About the Medicine Called Ritlecitinib in Adults With Severe Alopecia Areata in Real-world Settings
In development for (15)
- Alopecia areata Phase 3
- Asthma Phase 2
- Celiac disease Phase 2
- Crohn disease Phase 2
- Hidradenitis suppurativa Phase 2
- Keloid Phase 2
- Kidney disorder Phase 1
- Liver disorder Phase 1
- Mycosis fungoides Phase 2
- Pseudopelade of Brocq Phase 2
- Rheumatoid arthritis Phase 2
- Sezary syndrome Phase 2
- Type 1 diabetes mellitus Phase 2
- Ulcerative colitis Phase 2
- Vitiligo Phase 3