Peficitinib
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Also known as Asp-015kASP015KJNJ-54781532
Summary
Peficitinib (CHEMBL3137308) is an approved small molecule (ATC L04AF06) targeting JAK1, JAK2, and JAK3; indicated across 5 conditions including rheumatoid arthritis and psoriasis.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: L04AF06
- Targets: 4 (JAK1, JAK2, JAK3…)
- Indications: 5 conditions
- Clinical trials: 31
- Chemistry: 326.4 Da · C18H22N4O2
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL3137308 |
| Name | Peficitinib |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | no |
| PubChem CID | 57928403 |
| ATC | L04AF06 |
| Molecular formula | C18H22N4O2 |
| Molecular weight | 326.4 |
| InChIKey | DREIJXJRTLTGJC-JQCLMNFQSA-N |
SMILES: C1[C@@H]2CC3(C[C@@H](C2NC4=C5C=CNC5=NC=C4C(=O)N)CC1C3)O
IUPAC name: 4-[[(1R,3S)-5-hydroxy-2-adamantyl]amino]-1H-pyrrolo[2,3-b]pyridine-5-carboxamide
Also known as: Asp-015k, ASP-015K, ASP015K, JNJ-54781532, Peficitinib, PEFICITINIB, peficitinib
Parent form; salt/anhydrous children: CHEMBL3137329
Patent coverage: 651 distinct patent families (1,722 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 1,714 (100%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.
Targets
Targets
Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).
| Gene | Target | Action | pAffinity | Cancer dependency | UniProt |
|---|---|---|---|---|---|
| JAK1 | Janus kinase 1 | Inhibition | 8.4 | 2.8% | P23458 |
| JAK2 | Janus kinase 2 | Inhibition | 8.3 | 0.7% | O60674 |
| JAK3 | Janus kinase 3 | Inhibition | 0.6% | P52333 | |
| TYK2 | tyrosine kinase 2 | Inhibition | 8.3 | 0.8% | P29597 |
Broader ChEMBL bioactivity targets: 4 (assay-derived). Sample: Tyrosine-protein kinase JAK3, Tyrosine-protein kinase JAK1, Tyrosine-protein kinase JAK2, Non-receptor tyrosine-protein kinase TYK2.
Bioactivity
ChEMBL activities: 20 potent at pChembl ≥ 5 of 20 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| JAK3 | 9.15 | IC50 | 0.71 | nM | CHEMBL_ACT_15747164 |
| JAK3 | 9.15 | IC50 | 0.7 | nM | CHEMBL_ACT_24861796 |
| JAK3 | 9.15 | IC50 | 0.7 | nM | CHEMBL_ACT_25555162 |
| JAK3 | 9.15 | IC50 | 0.7 | nM | CHEMBL_ACT_25851506 |
| JAK1 | 8.41 | IC50 | 3.9 | nM | CHEMBL_ACT_15747172 |
| JAK1 | 8.41 | IC50 | 3.9 | nM | CHEMBL_ACT_24861786 |
| JAK1 | 8.41 | IC50 | 3.9 | nM | CHEMBL_ACT_25555160 |
| JAK1 | 8.41 | IC50 | 3.9 | nM | CHEMBL_ACT_25851504 |
| TYK2 | 8.32 | IC50 | 4.8 | nM | CHEMBL_ACT_15747160 |
| TYK2 | 8.32 | IC50 | 4.8 | nM | CHEMBL_ACT_24861798 |
| TYK2 | 8.32 | IC50 | 4.8 | nM | CHEMBL_ACT_25555163 |
| TYK2 | 8.32 | IC50 | 4.8 | nM | CHEMBL_ACT_25851507 |
| JAK2 | 8.3 | IC50 | 5 | nM | CHEMBL_ACT_15747168 |
| JAK2 | 8.3 | IC50 | 5 | nM | CHEMBL_ACT_24861791 |
| JAK2 | 8.3 | IC50 | 5 | nM | CHEMBL_ACT_25555161 |
| JAK2 | 8.3 | IC50 | 5 | nM | CHEMBL_ACT_25851505 |
| JAK3 | 7.7 | IC50 | 20.1 | nM | CHEMBL_ACT_25851289 |
| JAK1 | 7.31 | IC50 | 49.1 | nM | CHEMBL_ACT_25851243 |
| JAK2 | 7.25 | IC50 | 56.4 | nM | CHEMBL_ACT_25851266 |
| TYK2 | 6.86 | IC50 | 137 | nM | CHEMBL_ACT_25851312 |
Target pathways
Aggregated over 4 target gene(s): JAK1, JAK2, JAK3, TYK2.
Top Reactome pathways
86 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| Interleukin-4 and Interleukin-13 signaling | 4 | JAK1, JAK2, JAK3, TYK2 |
| Interleukin-20 family signaling | 4 | JAK1, JAK2, JAK3, TYK2 |
| Potential therapeutics for SARS | 4 | JAK1, JAK2, JAK3, TYK2 |
| Interleukin-6 signaling | 3 | JAK1, JAK2, TYK2 |
| MAPK3 (ERK1) activation | 3 | JAK1, JAK2, TYK2 |
| MAPK1 (ERK2) activation | 3 | JAK1, JAK2, TYK2 |
| Cytokine Signaling in Immune system | 3 | JAK1, JAK2, JAK3 |
| Signal Transduction | 3 | JAK1, JAK2, JAK3 |
| Disease | 3 | JAK1, JAK2, JAK3 |
| Immune System | 3 | JAK1, JAK2, JAK3 |
| Signaling by Interleukins | 3 | JAK1, JAK2, JAK3 |
| Interleukin-2 family signaling | 3 | JAK1, JAK2, JAK3 |
| Interleukin-3, Interleukin-5 and GM-CSF signaling | 3 | JAK1, JAK2, JAK3 |
| Infectious disease | 3 | JAK1, JAK2, JAK3 |
| RAF/MAP kinase cascade | 3 | JAK1, JAK2, JAK3 |
| MAPK family signaling cascades | 3 | JAK1, JAK2, JAK3 |
| MAPK1/MAPK3 signaling | 3 | JAK1, JAK2, JAK3 |
| IL-6-type cytokine receptor ligand interactions | 3 | JAK1, JAK2, TYK2 |
| Interleukin-35 Signalling | 3 | JAK1, JAK2, TYK2 |
| Interleukin-12 signaling | 3 | JAK1, JAK2, TYK2 |
| Interleukin-27 signaling | 3 | JAK1, JAK2, TYK2 |
| Interleukin receptor SHC signaling | 3 | JAK1, JAK2, JAK3 |
| Signaling by CSF3 (G-CSF) | 3 | JAK1, JAK2, TYK2 |
| SARS-CoV Infections | 3 | JAK1, JAK2, JAK3 |
| Inactivation of CSF3 (G-CSF) signaling | 3 | JAK1, JAK2, TYK2 |
| Viral Infection Pathways | 3 | JAK1, JAK2, JAK3 |
| Activation of STAT3 by cadherin engagement | 3 | JAK1, JAK2, TYK2 |
| RAF-independent MAPK1/3 activation | 2 | JAK1, JAK2 |
| Interleukin-7 signaling | 2 | JAK1, JAK3 |
| Interleukin-12 family signaling | 2 | JAK1, JAK2 |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| protein phosphorylation | 4 |
| cell surface receptor signaling pathway via JAK-STAT | 4 |
| cytokine-mediated signaling pathway | 4 |
| cell differentiation | 4 |
| intracellular signal transduction | 4 |
| growth hormone receptor signaling pathway via JAK-STAT | 4 |
| regulation of cell-cell adhesion | 4 |
| type II interferon-mediated signaling pathway | 3 |
| cellular response to virus | 3 |
| regulation of receptor signaling pathway via JAK-STAT | 3 |
| regulation of alpha-beta T cell activation | 3 |
| interleukin-15-mediated signaling pathway | 2 |
| interleukin-4-mediated signaling pathway | 2 |
| interleukin-2-mediated signaling pathway | 2 |
| interleukin-7-mediated signaling pathway | 2 |
Indications & clinical
Indications
5 indications (0 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).
| Indication | Trial phase | MONDO | EFO |
|---|---|---|---|
| rheumatoid arthritis | 3 | MONDO:0008383 | EFO:0000685 |
| psoriasis | 2 | MONDO:0005083 | EFO:0000676 |
| ulcerative colitis | 2 | MONDO:0005101 | EFO:0000729 |
| liver disorder | 1 | MONDO:0005154 | EFO:0001421 |
| kidney disorder | 1 | MONDO:0005240 | EFO:0003086 |
Clinical trials
Total trials: 31.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE1 | 21 |
| PHASE2 | 5 |
| PHASE3 | 4 |
| Not specified | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT01638013 | PHASE3 | COMPLETED | A Study to Continue ASP015K Treatment to Rheumatoid Arthritis Patients Who Completed Phase IIb Study or Phase III Study of ASP015K |
| NCT02305849 | PHASE3 | COMPLETED | A Study to Evaluate Efficacy and Safety of ASP015K in Patients With Rheumatoid Arthritis (RA) Who Had an Inadequate Response to Methotrexate (MTX) Treatment |
| NCT02308163 | PHASE3 | COMPLETED | A Study to Evaluate Safety and Efficacy of ASP015K in Patients With Rheumatoid Arthritis (RA) Who Had an Inadequate Response to DMARDs |
| NCT03660059 | PHASE3 | COMPLETED | A Study to Assess Safety and Efficacy of ASP015K in Participants With Rheumatoid Arthritis (RA) Who Had an Inadequate Response or Intolerance to Methotrexate (MTX) |
| NCT01096862 | PHASE2 | COMPLETED | A Study to Explore Efficacy and Safety of ASP015K in Subjects With Moderate to Severe Psoriasis |
| NCT01554696 | PHASE2 | COMPLETED | A Study to Evaluate the Safety and Efficacy of ASP015K in Moderate to Severe Rheumatoid Arthritis Subjects Who Have Had an Inadequate Response to Methotrexate |
| NCT01565655 | PHASE2 | COMPLETED | A Study to Evaluate the Safety and Efficacy of ASP015K in Moderate to Severe Rheumatoid Arthritis |
| NCT01649999 | PHASE2 | COMPLETED | A Study to Evaluate the Efficacy and Safety of ASP015K in Moderate to Severe Rheumatoid Arthritis Subjects |
| NCT01711814 | PHASE2 | COMPLETED | A Study to Evaluate the Long-term Safety and Efficacy of ASP015K in Subjects Previously Enrolled in a Phase 2 ASP015K Rheumatoid Arthritis Study |
| NCT01182077 | PHASE1 | COMPLETED | A Study to Assess Drug Interaction of ASP015K and Midazolam |
| NCT01190670 | PHASE1 | COMPLETED | A Study to Evaluate the Drug Interaction of ASP015K and Tacrolimus |
| NCT01225224 | PHASE1 | COMPLETED | Single and Multiple Oral Administration Study of ASP015K in Healthy Nonelderly Volunteers |
| NCT01364974 | PHASE1 | COMPLETED | A Study to Assess the Safety, Tolerability and Pharmacokinetics of ASP015K |
| NCT01364987 | PHASE1 | COMPLETED | Pharmacokinetic Interaction Study to Assess the Effect of ASP015K on Mycophenolate Mofetil in Healthy Volunteers |
| NCT01387087 | PHASE1 | COMPLETED | A Study to Assess the Safety, Tolerability and Pharmacokinetics of ASP015K |
| NCT01406132 | PHASE1 | COMPLETED | A Study to Assess the Pharmacokinetics of ASP015K in Healthy Male Subjects |
| NCT01430065 | PHASE1 | COMPLETED | Pharmacokinetic Interaction Study to Assess the Effect of ASP015K on Tacrolimus in Healthy Volunteers |
| NCT01430078 | PHASE1 | COMPLETED | A Study to Assess the Bioavailability of ASP015K |
| NCT01484964 | PHASE1 | COMPLETED | A Single Oral Dose Study to Compare the Bioavailability Between Two Different Tablet Formulations and Assess if There is a Food Effect With the New Formulation |
| NCT01486017 | PHASE1 | COMPLETED | A Single Oral Dose Study of ASP015K in Healthy Volunteers Assessing the Relative Bioavailability Across Three Tablet Strengths From a New Formulation of ASP015K |
| NCT01754805 | PHASE1 | COMPLETED | A Drug Interaction Study to Evaluate the Pharmacokinetics of ASP015K and Methotrexate in Patients With Rheumatoid Arthritis |
| NCT01929577 | PHASE1 | COMPLETED | A Study to Assess the Relative Bioavailability Between Two ASP015K Tablets and the Food Effect of a New Tablet in Healthy Adult Subjects |
| NCT01959399 | PHASE1 | COMPLETED | Drug-Drug Interaction Study Evaluating Effects of ASP015K on Rosuvastatin |
| NCT02111317 | PHASE1 | COMPLETED | A Study to Evaluate the Effect of Verapamil on the Pharmacokinetics of ASP015K in Healthy Adult Subjects |
| NCT02141425 | PHASE1 | COMPLETED | A Study to Assess the Safety, Tolerability and Pharmacokinetics of ASP015K in Healthy Subjects |
| NCT02531191 | PHASE1 | COMPLETED | Bioequivalence Evaluation of a New and Current Tablet of ASP015K |
| NCT02586194 | PHASE1 | COMPLETED | Pharmacokinetics Study in Patients With Impaired Hepatic Function |
| NCT02603497 | PHASE1 | COMPLETED | Pharmacokinetics Study in Patients With Impaired Renal Function and Subjects With Normal Renal Function |
| NCT02760342 | PHASE1 | COMPLETED | A Drug Interaction Study to Evaluate the Pharmacokinetics of ASP015K and Metformin |
| NCT04143477 | PHASE1 | COMPLETED | A Study to Evaluate the Pharmacokinetics and Safety of ASP015K in Healthy Chinese Subjects |
| NCT03971253 | Not specified | RECRUITING | Japan Post-Marketing Surveillance for Peficitinib to Assess Safety and Effectiveness in the Patients With Rheumatoid Arthritis |
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
No PharmGKB pharmacogenomic data curated for this drug.
Related molecules
Related molecules
Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.
126 molecules share ≥1 primary target. Top 60 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| CRIZOTINIB | ChEMBL + PubChem | Phase 4 (approved) | JAK1, JAK2, JAK3, TYK2 |
| DEUCRAVACITINIB | ChEMBL + PubChem | Phase 4 (approved) | JAK1, JAK2, JAK3, TYK2 |
| Pazopanib | ChEMBL + PubChem | Phase 4 (approved) | JAK1, JAK2, JAK3, TYK2 |
| RITLECITINIB | ChEMBL + PubChem | Phase 4 (approved) | JAK1, JAK2, JAK3, TYK2 |
| ABROCITINIB | ChEMBL | Phase 4 (approved) | JAK1, JAK2, JAK3, TYK2 |
| BARICITINIB | ChEMBL | Phase 4 (approved) | JAK1, JAK2, JAK3, TYK2 |
| FEDRATINIB | ChEMBL | Phase 4 (approved) | JAK1, JAK2, JAK3, TYK2 |
| FILGOTINIB | ChEMBL | Phase 4 (approved) | JAK1, JAK2, JAK3, TYK2 |
| MIDOSTAURIN | ChEMBL | Phase 4 (approved) | JAK1, JAK2, JAK3, TYK2 |
| MOMELOTINIB | ChEMBL | Phase 4 (approved) | JAK1, JAK2, JAK3, TYK2 |
| NINTEDANIB | ChEMBL | Phase 4 (approved) | JAK1, JAK2, JAK3, TYK2 |
| PACRITINIB | ChEMBL | Phase 4 (approved) | JAK1, JAK2, JAK3, TYK2 |
| RUXOLITINIB | ChEMBL | Phase 4 (approved) | JAK1, JAK2, JAK3, TYK2 |
| SUNITINIB | ChEMBL | Phase 4 (approved) | JAK1, JAK2, JAK3, TYK2 |
| TOFACITINIB | ChEMBL | Phase 4 (approved) | JAK1, JAK2, JAK3, TYK2 |
| UPADACITINIB | ChEMBL | Phase 4 (approved) | JAK1, JAK2, JAK3, TYK2 |
| BREPOCITINIB | ChEMBL | Phase 3 | JAK1, JAK2, JAK3, TYK2 |
| DELGOCITINIB | ChEMBL | Phase 3 | JAK1, JAK2, JAK3, TYK2 |
| DOVITINIB | ChEMBL | Phase 3 | JAK1, JAK2, JAK3, TYK2 |
| ITACITINIB | ChEMBL | Phase 3 | JAK1, JAK2, JAK3, TYK2 |
| LESTAURTINIB | ChEMBL | Phase 3 | JAK1, JAK2, JAK3, TYK2 |
| AT-9283 | ChEMBL | Phase 2 | JAK1, JAK2, JAK3, TYK2 |
| ATINVICITINIB | ChEMBL | Phase 2 | JAK1, JAK2, JAK3, TYK2 |
| AZD-1480 | ChEMBL | Phase 2 | JAK1, JAK2, JAK3, TYK2 |
| BMS-911543 | ChEMBL | Phase 2 | JAK1, JAK2, JAK3, TYK2 |
| CC-401 | ChEMBL | Phase 2 | JAK1, JAK2, JAK3, TYK2 |
| CERDULATINIB | ChEMBL | Phase 2 | JAK1, JAK2, JAK3, TYK2 |
| DECERNOTINIB | ChEMBL | Phase 2 | JAK1, JAK2, JAK3, TYK2 |
| GANDOTINIB | ChEMBL | Phase 2 | JAK1, JAK2, JAK3, TYK2 |
| GOLIDOCITINIB | ChEMBL | Phase 2 | JAK1, JAK2, JAK3, TYK2 |
| GUSACITINIB | ChEMBL | Phase 2 | JAK1, JAK2, JAK3, TYK2 |
| IFIDANCITINIB | ChEMBL | Phase 2 | JAK1, JAK2, JAK3, TYK2 |
| IZENCITINIB | ChEMBL | Phase 2 | JAK1, JAK2, JAK3, TYK2 |
| NEZULCITINIB | ChEMBL | Phase 2 | JAK1, JAK2, JAK3, TYK2 |
| NS-018 | ChEMBL | Phase 2 | JAK1, JAK2, JAK3, TYK2 |
| OCLACITINIB | ChEMBL | Phase 2 | JAK1, JAK2, JAK3, TYK2 |
| R-406 | ChEMBL | Phase 2 | JAK1, JAK2, JAK3, TYK2 |
| ROPSACITINIB | ChEMBL | Phase 2 | JAK1, JAK2, JAK3, TYK2 |
| SOLCITINIB | ChEMBL | Phase 2 | JAK1, JAK2, JAK3, TYK2 |
| SU-014813 | ChEMBL | Phase 2 | JAK1, JAK2, JAK3, TYK2 |
| TOZASERTIB | ChEMBL | Phase 2 | JAK1, JAK2, JAK3, TYK2 |
| Afatinib | PubChem | Approved | JAK1, JAK2, JAK3, TYK2 |
| Gefitinib | PubChem | Approved | JAK1, JAK2, JAK3, TYK2 |
| Idelalisib | PubChem | Approved | JAK1, JAK2, JAK3, TYK2 |
| Selumetinib | PubChem | Approved | JAK1, JAK2, JAK3, TYK2 |
| dacomitinib | ChEMBL + PubChem | Phase 4 (approved) | JAK1, JAK3, TYK2 |
| IMATINIB | ChEMBL + PubChem | Phase 4 (approved) | JAK1, JAK2, TYK2 |
| AXITINIB | ChEMBL | Phase 4 (approved) | JAK2, JAK3, TYK2 |
| BOSUTINIB | ChEMBL | Phase 4 (approved) | JAK2, JAK3, TYK2 |
| CERITINIB | ChEMBL | Phase 4 (approved) | JAK1, JAK2, JAK3 |
| DASATINIB | ChEMBL | Phase 4 (approved) | JAK2, JAK3, TYK2 |
| ENTRECTINIB | ChEMBL | Phase 4 (approved) | JAK1, JAK2, JAK3 |
| ERLOTINIB | ChEMBL | Phase 4 (approved) | JAK2, JAK3, TYK2 |
| ABIVERTINIB | ChEMBL | Phase 3 | JAK1, JAK2, JAK3 |
| ALVOCIDIB | ChEMBL | Phase 3 | JAK2, JAK3, TYK2 |
| DEFACTINIB | ChEMBL | Phase 3 | JAK2, JAK3, TYK2 |
| BMS-919373 | ChEMBL | Phase 2 | JAK2, JAK3, TYK2 |
| CENISERTIB | ChEMBL | Phase 2 | JAK2, JAK3, TYK2 |
| LONDAMOCITINIB | ChEMBL | Phase 2 | JAK1, JAK2, TYK2 |
| belumosudil | PubChem | Approved | JAK2, JAK3, TYK2 |
Related Atlas pages
- Genes: JAK1, JAK2, JAK3, TYK2
- Diseases: rheumatoid arthritis
- Drugs: Crizotinib, Deucravacitinib, Pazopanib, Ritlecitinib, Abrocitinib, Baricitinib, Fedratinib, Filgotinib, Midostaurin, Momelotinib, Nintedanib, Pacritinib, Ruxolitinib, Sunitinib, Tofacitinib, Upadacitinib, Brepocitinib, Delgocitinib, Dovitinib, Itacitinib, Lestaurtinib, Afatinib, Gefitinib, Idelalisib, Selumetinib, dacomitinib, Imatinib, Axitinib, Bosutinib, Ceritinib, Dasatinib, Entrectinib, Erlotinib, Abivertinib, Alvocidib, Defactinib, belumosudil