Remibrutinib
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Summary
Remibrutinib (CHEMBL4483575) is a phase-3 clinical-stage small molecule (ATC L04AA60) targeting BTK; indicated across 6 conditions including multiple sclerosis and immune system disorder.
At a glance
- Status: Max clinical phase 3 (not approved)
- Modality: Small molecule
- ATC class: L04AA60
- Targets: 1 (BTK)
- Indications: 6 conditions
- Clinical trials: 14
- Chemistry: 507.5 Da · C27H27F2N5O3
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL4483575 |
| Name | Remibrutinib |
| Type | Small molecule |
| Max phase | 3 |
| FDA approved | no |
| PubChem CID | 118107483 |
| ATC | L04AA60 |
| Molecular formula | C27H27F2N5O3 |
| Molecular weight | 507.5 |
| InChIKey | CUABMPOJOBCXJI-UHFFFAOYSA-N |
SMILES: CC1=C(C=C(C=C1NC(=O)C2=C(C=C(C=C2)C3CC3)F)F)C4=C(C(=NC=N4)N)OCCN(C)C(=O)C=C
IUPAC name: N-[3-[6-amino-5-[2-[methyl(prop-2-enoyl)amino]ethoxy]pyrimidin-4-yl]-5-fluoro-2-methylphenyl]-4-cyclopropyl-2-fluorobenzamide
Also known as: Remibrutinib, REMIBRUTINIB
Patent coverage: 219 distinct patent families (569 SureChEMBL compound mentions), from 4 matched compound structure(s). 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 |
|---|---|---|---|---|---|
| BTK | Bruton tyrosine kinase | Inhibition | 9 | 0.7% | Q06187 |
Broader ChEMBL bioactivity targets: 13 (assay-derived). Sample: Receptor tyrosine-protein kinase erbB-2, Epidermal growth factor receptor, Tyrosine-protein kinase JAK3, Tyrosine-protein kinase Blk, Voltage-gated inwardly rectifying potassium channel KCNH2, Tyrosine-protein kinase ITK/TSK, Receptor tyrosine-protein kinase erbB-4, Phosphatidylinositol 4-kinase beta, Cytoplasmic tyrosine-protein kinase BMX, Tyrosine-protein kinase Tec.
Bioactivity
ChEMBL activities: 18 potent at pChembl ≥ 5 of 25 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| BTK | 9.62 | Kd | 0.24 | nM | CHEMBL_ACT_24797372 |
| BTK | 9.2 | Kd | 0.63 | nM | CHEMBL_ACT_19061180 |
| BTK | 9 | IC50 | 1 | nM | CHEMBL_ACT_26665913 |
| BTK | 9 | IC50 | 1 | nM | CHEMBL_ACT_27777620 |
| BTK | 9 | IC50 | 1 | nM | CHEMBL_ACT_28555112 |
| BTK | 9 | IC50 | 1 | nM | CHEMBL_ACT_29021183 |
| BTK | 8.92 | IC50 | 1.2 | nM | CHEMBL_ACT_24797235 |
| BTK | 8.89 | IC50 | 1.3 | nM | CHEMBL_ACT_19061016 |
| BTK | 8.6 | IC50 | 2.5 | nM | CHEMBL_ACT_19061046 |
| BTK | 7.75 | IC50 | 18 | nM | CHEMBL_ACT_19061074 |
| BTK | 7.17 | IC50 | 67 | nM | CHEMBL_ACT_19061320 |
| TEC | 7.11 | Kd | 77 | nM | CHEMBL_ACT_24797396 |
| TEC | 6.96 | Kd | 110 | nM | CHEMBL_ACT_19061192 |
| BMX | 6.27 | Kd | 540 | nM | CHEMBL_ACT_19061186 |
| BMX | 5.96 | Kd | 1100 | nM | CHEMBL_ACT_24797366 |
| KCNH2 | 5.85 | IC50 | 1400 | nM | CHEMBL_ACT_19061276 |
| PI4KB | 5.51 | IC50 | 3100 | nM | CHEMBL_ACT_19061426 |
| ABCB11 | 5.18 | IC50 | 6600 | nM | CHEMBL_ACT_19061427 |
Target pathways
Aggregated over 1 target gene(s): BTK.
Top Reactome pathways
45 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| ER-Phagosome pathway | 1 | BTK |
| Antigen processing-Cross presentation | 1 | BTK |
| Adaptive Immune System | 1 | BTK |
| Signal Transduction | 1 | BTK |
| Disease | 1 | BTK |
| Toll Like Receptor 4 (TLR4) Cascade | 1 | BTK |
| MyD88:MAL(TIRAP) cascade initiated on plasma membrane | 1 | BTK |
| Toll Like Receptor TLR1:TLR2 Cascade | 1 | BTK |
| Toll Like Receptor TLR6:TLR2 Cascade | 1 | BTK |
| Innate Immune System | 1 | BTK |
| Immune System | 1 | BTK |
| Toll-like Receptor Cascades | 1 | BTK |
| Toll Like Receptor 2 (TLR2) Cascade | 1 | BTK |
| Signaling by Rho GTPases | 1 | BTK |
| RHO GTPase Effectors | 1 | BTK |
| Fcgamma receptor (FCGR) dependent phagocytosis | 1 | BTK |
| Regulation of actin dynamics for phagocytic cup formation | 1 | BTK |
| DAP12 interactions | 1 | BTK |
| DAP12 signaling | 1 | BTK |
| Fc epsilon receptor (FCERI) signaling | 1 | BTK |
| FCERI mediated Ca+2 mobilization | 1 | BTK |
| Signaling by GPCR | 1 | BTK |
| GPCR downstream signalling | 1 | BTK |
| G-protein beta:gamma signalling | 1 | BTK |
| G alpha (q) signalling events | 1 | BTK |
| G alpha (12/13) signalling events | 1 | BTK |
| Diseases of Immune System | 1 | BTK |
| Diseases associated with the TLR signaling cascade | 1 | BTK |
| MyD88 deficiency (TLR2/4) | 1 | BTK |
| IRAK4 deficiency (TLR2/4) | 1 | BTK |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| neutrophil homeostasis | 1 |
| positive regulation of type III hypersensitivity | 1 |
| positive regulation of type I hypersensitivity | 1 |
| adaptive immune response | 1 |
| B cell affinity maturation | 1 |
| histamine secretion by mast cell | 1 |
| positive regulation of immunoglobulin production | 1 |
| regulation of B cell cytokine production | 1 |
| MyD88-dependent toll-like receptor signaling pathway | 1 |
| regulation of B cell apoptotic process | 1 |
| mesoderm development | 1 |
| peptidyl-tyrosine phosphorylation | 1 |
| calcium-mediated signaling | 1 |
| proteoglycan catabolic process | 1 |
| negative regulation of B cell proliferation | 1 |
Indications & clinical
Indications
6 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 |
|---|---|---|---|
| multiple sclerosis | 3 | MONDO:0005301 | MONDO:0005301 |
| immune system disorder | 3 | MONDO:0005046 | EFO:0000540 |
| allergic disease | 2 | MONDO:0005271 | MONDO:0005271 |
| Sjogren syndrome | 2 | MONDO:0010030 | EFO:0000699 |
| liver disorder | 1 | MONDO:0005154 | EFO:0001421 |
1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 14.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE3 | 9 |
| PHASE2 | 3 |
| PHASE1 | 1 |
| Not specified | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT05147220 | PHASE3 | ACTIVE_NOT_RECRUITING | Efficacy and Safety of Remibrutinib Compared to Teriflunomide in Participants With Relapsing Multiple Sclerosis (RMS) |
| NCT05156281 | PHASE3 | ACTIVE_NOT_RECRUITING | Efficacy and Safety of Remibrutinib Compared to Teriflunomide in Participants With Relapsing Multiple Sclerosis (RMS) |
| NCT05976243 | PHASE3 | ACTIVE_NOT_RECRUITING | A Study to Investigate Efficacy, Safety, and Tolerability of Remibrutinib Compared With Placebo in Adults With CINDU Inadequately Controlled by H1-antihistamines |
| NCT06042478 | PHASE3 | ACTIVE_NOT_RECRUITING | Phase 3b Study to Assess the Efficacy, Safety, and Tolerability of Remibrutinib in Comparison to Placebo, With Omalizumab as Active Control, in Adult CSU Patients, Followed by an Open-label 52-week Optional Extension. |
| NCT06744920 | PHASE3 | RECRUITING | A Study to Investigate the Efficacy, Safety and Tolerability of Remibrutinib Versus Placebo in Adult Patients With Generalized Myasthenia Gravis |
| NCT06846281 | PHASE3 | RECRUITING | Efficacy and Safety of Remibrutinib After Switching From Ocrelizumab in Participants Living With Relapsing Multiple Sclerosis. |
| NCT06868212 | PHASE3 | RECRUITING | A Study to Evaluate Efficacy of Remibrutinib Compared to Dupilumab at Early Timepoints in Adults With Chronic Spontaneous Urticaria Inadequately Controlled by Second Generation H1-antihistamines |
| NCT07225504 | PHASE3 | RECRUITING | A Study to Evaluate the Efficacy and Safety of Remibrutinib in Secondary Progressive Multiple Sclerosis |
| NCT07456891 | PHASE3 | RECRUITING | Remibrutinib Open Label Roll-over Post-trial Access Protocol |
| NCT06865651 | PHASE2 | RECRUITING | Study of Remibrutinib (LOU064) Efficacy and Safety and Exploration of Its Mechanism of Action in Participants With Chronic Urticaria |
| NCT04035668 | PHASE2 | TERMINATED | A Phase 2 Study to Evaluate the Safety and Efficacy of LOU064 in Patients With Moderate to Severe Sjögren’s Syndrome |
| NCT05432388 | PHASE2 | COMPLETED | Study of Efficacy, Safety and Tolerability of Remibrutinib in Adult Participants With an Allergy to Peanuts |
| NCT07032272 | PHASE1 | COMPLETED | A Study to Investigate the Pharmacokinetics and Safety of Remibrutinib in Participants With Severe Renal Impairment Compared to Matched Healthy Participants. |
| NCT05170724 | Not specified | AVAILABLE | Global Managed Access Program Cohort for Remibrutinib in Adult Patients With Chronic Spontaneous Urticaria |
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.
80 molecules share ≥1 primary target. Top 60 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| CRIZOTINIB | ChEMBL + PubChem | Phase 4 (approved) | BTK |
| RITLECITINIB | ChEMBL + PubChem | Phase 4 (approved) | BTK |
| ACALABRUTINIB | ChEMBL | Phase 4 (approved) | BTK |
| BOSUTINIB | ChEMBL | Phase 4 (approved) | BTK |
| BRIGATINIB | ChEMBL | Phase 4 (approved) | BTK |
| CERITINIB | ChEMBL | Phase 4 (approved) | BTK |
| DASATINIB | ChEMBL | Phase 4 (approved) | BTK |
| ENTRECTINIB | ChEMBL | Phase 4 (approved) | BTK |
| FEDRATINIB | ChEMBL | Phase 4 (approved) | BTK |
| FUTIBATINIB | ChEMBL | Phase 4 (approved) | BTK |
| IBRUTINIB | ChEMBL | Phase 4 (approved) | BTK |
| MITOXANTRONE | ChEMBL | Phase 4 (approved) | BTK |
| NERATINIB | ChEMBL | Phase 4 (approved) | BTK |
| NINTEDANIB | ChEMBL | Phase 4 (approved) | BTK |
| OLMUTINIB | ChEMBL | Phase 4 (approved) | BTK |
| OSIMERTINIB | ChEMBL | Phase 4 (approved) | BTK |
| PIRTOBRUTINIB | ChEMBL | Phase 4 (approved) | BTK |
| PONATINIB | ChEMBL | Phase 4 (approved) | BTK |
| SUNITINIB | ChEMBL | Phase 4 (approved) | BTK |
| TIRABRUTINIB | ChEMBL | Phase 4 (approved) | BTK |
| VANDETANIB | ChEMBL | Phase 4 (approved) | BTK |
| ZANUBRUTINIB | ChEMBL | Phase 4 (approved) | BTK |
| ABIVERTINIB | ChEMBL | Phase 3 | BTK |
| ALISERTIB | ChEMBL | Phase 3 | BTK |
| CANERTINIB | ChEMBL | Phase 3 | BTK |
| CEDIRANIB | ChEMBL | Phase 3 | BTK |
| DOVITINIB | ChEMBL | Phase 3 | BTK |
| ENTOSPLETINIB | ChEMBL | Phase 3 | BTK |
| EVOBRUTINIB | ChEMBL | Phase 3 | BTK |
| FENEBRUTINIB | ChEMBL | Phase 3 | BTK |
| LESTAURTINIB | ChEMBL | Phase 3 | BTK |
| NEMTABRUTINIB | ChEMBL | Phase 3 | BTK |
| ORELABRUTINIB | ChEMBL | Phase 3 | BTK |
| POZIOTINIB | ChEMBL | Phase 3 | BTK |
| PYROTINIB | ChEMBL | Phase 3 | BTK |
| RILZABRUTINIB | ChEMBL | Phase 3 | BTK |
| ROCILETINIB | ChEMBL | Phase 3 | BTK |
| SARACATINIB | ChEMBL | Phase 3 | BTK |
| TESEVATINIB | ChEMBL | Phase 3 | BTK |
| TOLEBRUTINIB | ChEMBL | Phase 3 | BTK |
| APITOLISIB | ChEMBL | Phase 2 | BTK |
| AT-9283 | ChEMBL | Phase 2 | BTK |
| ATUZABRUTINIB | ChEMBL | Phase 2 | BTK |
| BIIB-091 | ChEMBL | Phase 2 | BTK |
| BMS-754807 | ChEMBL | Phase 2 | BTK |
| BMS-919373 | ChEMBL | Phase 2 | BTK |
| BMS-986142 | ChEMBL | Phase 2 | BTK |
| BRANEBRUTINIB | ChEMBL | Phase 2 | BTK |
| CENISERTIB | ChEMBL | Phase 2 | BTK |
| CEP-11981 | ChEMBL | Phase 2 | BTK |
| DANUSERTIB | ChEMBL | Phase 2 | BTK |
| DEFOSBARASERTIB | ChEMBL | Phase 2 | BTK |
| EDRALBRUTINIB | ChEMBL | Phase 2 | BTK |
| ELSUBRUTINIB | ChEMBL | Phase 2 | BTK |
| FORETINIB | ChEMBL | Phase 2 | BTK |
| ILORASERTIB | ChEMBL | Phase 2 | BTK |
| MILREBRUTINIB | ChEMBL | Phase 2 | BTK |
| PELITINIB | ChEMBL | Phase 2 | BTK |
| POSELTINIB | ChEMBL | Phase 2 | BTK |
| R-406 | ChEMBL | Phase 2 | BTK |
Related Atlas pages
- Genes: BTK
- Diseases: multiple sclerosis, immune system disorder
- Drugs: Crizotinib, Ritlecitinib, Acalabrutinib, Bosutinib, Brigatinib, Ceritinib, Dasatinib, Entrectinib, Fedratinib, Futibatinib, Ibrutinib, Mitoxantrone, Neratinib, Nintedanib, Olmutinib, Osimertinib, Pirtobrutinib, Ponatinib, Sunitinib, Tirabrutinib, Vandetanib, Zanubrutinib, Abivertinib, Alisertib, Canertinib, Cediranib, Dovitinib, Entospletinib, Evobrutinib, Fenebrutinib, Lestaurtinib, Nemtabrutinib, Orelabrutinib, Poziotinib, Pyrotinib, Rilzabrutinib, Rociletinib, Saracatinib, Tesevatinib, Tolebrutinib