> Trialight public data. Index of pages: https://trialight.com/llms.txt
> Web page: https://trialight.com/data/asset/orelabrutinib-f8934fae-2fe2-4ce8-a944-a872e27bfa47
> Record changed: 2026-10-13

# Orelabrutinib

Highest phase reached

Phase 3

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4650321)

Drug type

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4650321)

## Development status

**Listing at source**

Listed

**Highest phase reached**

Phase 3

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4650321)

## Names and chemistry

**Drug type**

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4650321)

**Drug name**

Orelabrutinib

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4650321)

**Molecular weight**

427.5

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4650321)

**Structure (SMILES)**

C=CC(=O)N1CCC(c2ccc(C(N)=O)c(-c3ccc(Oc4ccccc4)cc3)n2)CC1

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4650321)

### Brand names (2)

- innobruka
- Innobruka

### Other names (23)

- icp 022
- Icp-022
- ICP-022
- icp022
- ICP022
- orelabrutinib
- Orelabrutinib
- Orelabrutinib (High Dose)
- Orelabrutinib (ICP-022)
- Orelabrutinib (Low Dose)
- orelabrutinib \[INN\]
- ORELABRUTINIB \[USAN\]
- Orelabrutinib \[WHO-DD\]
- Orelabrutinib High dose
- orelabrutinib inn
- Orelabrutinib Low dose
- Orelabrutinib Oral Tablet
- Orelabrutinib tablet
- Orelabrutinib Tablets
- orelabrutinib usan
- orelabrutinib who dd
- Orelabrutinib( higher dose)
- Orelabrutinib( lower dose)

## Identifiers

**ATC classification codes**

- L01EL04

Sources for recorded values

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4650321)

**CAS registry numbers**

- 1655504-04-3

**ChEMBL ID**

CHEMBL4650321

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4650321)

**InChIKey**

MZPVEMOYADUARK-UHFFFAOYSA-N

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4650321)

**PubChem compound IDs**

- 91667513

**FDA ingredient codes (UNII)**

- WJA5UO9E10

## Regulatory information

### Other regulatory facts

**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

## Pharmacology

### Drug classification

**Pharmacology name**

orelabrutinib

**Type**

Synthetic organic

**Drug name stem**

\-tinib

**Approval recorded by Guide to Pharmacology**

Yes

### Mechanisms of action (2)

- **Action**  
Inhibition

**Action type**  
Inhibitor

**Target**  
Bruton tyrosine kinase

**Gene symbol**  
BTK

**Protein identifier**  
Q06187

**Median affinity**

8.36

**Affinity units**  
pIC50
- **Mechanism**  
Tyrosine-protein kinase BTK inhibitor

**Action type**  
Inhibitor

**Target**  
Tyrosine-protein kinase BTK

**Protein identifier**  
Q06187

### Open Targets mechanisms

- **Mechanism**  
Tyrosine-protein kinase BTK inhibitor

**Action type**  
Inhibitor

**Target**  
Tyrosine-protein kinase BTK

### Investigated indications (15)

- **Condition**  
Leukemia, Lymphocytic, Chronic, B-Cell

**Highest recorded phase**  
3

**Condition identifier**  
EFO:0000095

**Subject identifier**  
D015451
- **Condition**  
Lymphoma, Follicular

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0000096

**Subject identifier**  
D008224
- **Condition**  
Hodgkin Disease

**Highest recorded phase**  
1

**Condition identifier**  
EFO:0000183

**Subject identifier**  
D006689
- **Condition**  
Lymphoma, Large B-Cell, Diffuse

**Highest recorded phase**  
3

**Condition identifier**  
EFO:0000403

**Subject identifier**  
D016403
- **Condition**  
Lymphoma

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0000574

**Subject identifier**  
D008223
- **Condition**  
Neoplasms

**Highest recorded phase**  
3

**Condition identifier**  
EFO:0000616

**Subject identifier**  
D009369
- **Condition**  
Liver Diseases

**Highest recorded phase**  
1

**Condition identifier**  
EFO:0001421

**Subject identifier**  
D008107
- **Condition**  
Multiple Sclerosis, Relapsing-Remitting

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0003929

**Subject identifier**  
D020529
- **Condition**  
Purpura, Thrombocytopenic, Idiopathic

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0007160

**Subject identifier**  
D016553
- **Condition**  
Waldenstrom Macroglobulinemia

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0009441

**Subject identifier**  
D008258
- **Condition**  
Lymphoma, B-Cell, Marginal Zone

**Highest recorded phase**  
3

**Condition identifier**  
EFO:1000630

**Subject identifier**  
D018442
- **Condition**  
Lymphoma, Mantle-Cell

**Highest recorded phase**  
3

**Condition identifier**  
EFO:1001469

**Subject identifier**  
D020522
- **Condition**  
Neoplasms

**Highest recorded phase**  
3

**Condition identifier**  
MONDO:0004992

**Subject identifier**  
D009369
- **Condition**  
Lupus Erythematosus, Systemic

**Highest recorded phase**  
2

**Condition identifier**  
MONDO:0007915

**Subject identifier**  
D008180
- **Condition**  
Lymphoma, Follicular

**Highest recorded phase**  
2

**Condition identifier**  
MONDO:0018906

**Subject identifier**  
D008224

### Open Targets indications (38)

- **Condition identifier**  
EFO\_0000095

**Highest recorded phase**  
3
- **Condition identifier**  
EFO\_0000096

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_0000191

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_0000403

**Highest recorded phase**  
3
- **Condition identifier**  
EFO\_0000574

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_0000616
- **Condition identifier**  
EFO\_0001421

**Highest recorded phase**  
1
- **Condition identifier**  
EFO\_0003929

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_0004256
- **Condition identifier**  
EFO\_0007160

**Highest recorded phase**  
3
- **Condition identifier**  
EFO\_0008522

**Highest recorded phase**  
3
- **Condition identifier**  
EFO\_0009441

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_1000157

**Highest recorded phase**  
3
- **Condition identifier**  
EFO\_1000630

**Highest recorded phase**  
3
- **Condition identifier**  
EFO\_1001469

**Highest recorded phase**  
3
- **Condition identifier**  
EFO\_1001938
- **Condition identifier**  
MONDO\_0002083

**Highest recorded phase**  
1
- **Condition identifier**  
MONDO\_0002571

**Highest recorded phase**  
3
- **Condition identifier**  
MONDO\_0003864
- **Condition identifier**  
MONDO\_0004948

**Highest recorded phase**  
3
- **Condition identifier**  
MONDO\_0004949

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0004992
- **Condition identifier**  
MONDO\_0005070

**Highest recorded phase**  
4
- **Condition identifier**  
MONDO\_0005301

**Highest recorded phase**  
3
- **Condition identifier**  
MONDO\_0007650

**Highest recorded phase**  
2

And 13 more, listed on the interactive page.

### Reported adverse events (8)

- **Event**  
anaemia

**Reports**  
9

**Reporting signal score**

22.2936
- **Event**  
hypoalbuminaemia

**Reports**  
2

**Reporting signal score**

7.95082
- **Event**  
hypokalaemia

**Reports**  
8

**Reporting signal score**

29.4367
- **Event**  
myelosuppression

**Reports**  
4

**Reporting signal score**

17.2044
- **Event**  
neutropenia

**Reports**  
7

**Reporting signal score**

17.2305
- **Event**  
neutrophil count decreased

**Reports**  
5

**Reporting signal score**

16.6713
- **Event**  
pneumonia

**Reports**  
7

**Reporting signal score**

14.3736
- **Event**  
thrombocytopenia

**Reports**  
5

**Reporting signal score**

10.9802

### Trial references (34)

- NCT03493217  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03493217)
- NCT04578613  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04578613)
- NCT05322733  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05322733)
- NCT05491044  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05491044)
- NCT05918276  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05918276)
- NCT06476899  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT06476899)
- NCT03494179  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03494179)
- NCT05051891  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05051891)
- NCT05076097  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05076097)
- NCT05978739  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05978739)
- NCT06363994  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT06363994)
- NCT03797456  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03797456)
- NCT06082102  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT06082102)
- NCT04014205  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04014205)
- NCT06378138  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT06378138)
- NCT04304040  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04304040)
- NCT05014100  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05014100)
- NCT05926427  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05926427)
- NCT04305197  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04305197)
- NCT05688696  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05688696)
- NCT04438005  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04438005)
- NCT05234684  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05234684)
- NCT05351346  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05351346)
- NCT05381506  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05381506)
- NCT05498259  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05498259)

And 9 more, listed on the interactive page.

## Chemical properties

**Hydrogen bond acceptors**

4

**Hydrogen bond donors**

1

**Polar surface area**

85.52

**Calculated partition coefficient (ALogP)**

4.53

**Calculated partition coefficient (XLogP)**

3.6

**Prodrug**

No

**Chirality**

Achiral

**Inorganic**

No

**Rule-of-five violations**

0

**Rotatable bonds**

6

**Heavy atoms**

32

**Molecular formula**

C26H25N3O3

**Monoisotopic mass**

427.18959167

**Natural product**

No

## Evidence counts

**Recorded assays**

128

**Active assays**

9

### Active assay types

- Confirmatory

## Related records

### Trials (139)

- A Clinical Study on the Efficacy and Safety of Methotrexate (MTX) or Thiotepa (for MTX Intolerance) or Temozolomide (TMZ) Combined With Orelabrutinib and Selinexor in Relapsed/Refractory Primary or Secondary Central Nervous System Lymphoma（SELINA）
- A Clinical Trial of the Orelabrutinib in the Management of Refractory ITP
- A Dose-escalating Pilot Study of Orelabrutinib for Newly-diagnosed PCNSL
- A Exploratory Study on Untreated Follicular Lymphoma With Orelabrutinib, Tafasitamab, and Lenalidomide
- A Global Phase 3 Study of Orelabrutinib+BR Vs.BR in Pts with TN MCL
- A Lassa Fever Vaccine Trial in Adults and Children Residing in West Africa
- A Multicenter, Prospective, Open-Label, Randomized Controlled Clinical Study of Orelabrutinib Combined With Obinutuzumab and Lenalidomide Versus Obinutuzumab Plus Chemotherapy for Treatment-Naive Follicular Lymphoma
- A Phase 2 Study of Orelabrutinib in Patients With Relapsing-Remitting Multiple Sclerosis
- A Phase 3 Study to Compare the Efficacy of ICP-248 in Combination With Orelabrutinib Versus Pirtobrutinib in Participants With Relapsed or Refractory Mantle Cell Lymphoma (r/r MCL).
- A Phase I Study of ICP-022 in Healthy Subjects
- A Phase III Clinical Study of the Efficacy and Safety of Two Low-concentration Atropine Sulfate Eye Drops
- A Practical Clinical Study Comparing the Fixed-cycle Regimen Containing Orelabrutinib With BTKi Monotherapy
- A Prospective, Single-Center Study Evaluating the Efficacy and Safety of Glofitamab Combined With Orelabrutinib and Bortezomib in Patients With High-Risk Mantle Cell Lymphoma
- A Randomized, Open-label, Multi-center, Phase III Study of Orelabrutinib in Combination With Rituximab, Cyclophosphamide, Doxorubicin, Vincristine, and Prednisone (R-CHOP) vs. R-CHOP Alone in Patients With Treatment-naїve Mantle Cell Lymphoma
- A Study Comparing the Efficacy and Safety of Pola-RCHP-X Versus RCHOP-X and Pola-RCHP in Previously Untreated Patients With DLBCL
- A Study of ICP-022 in Patients With R/R DLBCL
- A Study of ICP-022 in Patients With Systemic Lupus Erythematosus (SLE)
- A Study of ICP-022 in the Treatment of Recurrent or Refractory Waldenstrom Macroglobulinemia
- A Study of MIL62 Combined With Orelabrutinib for the Treatment of R/R CD20+B Cell Lymphoma
- A Study of OLR in First-line Treatment of Mantle Cell Lymphoma

### In development for (18)

- [Autoimmune thrombocytopenic purpura](https://trialight.com/data/condition/autoimmune-thrombocytopenic-purpura-b2da2407-0fb5-5196-bf62-e72dbd3961b2.md) Phase 2
- [B-cell chronic lymphocytic leukemia](https://trialight.com/data/condition/b-cell-chronic-lymphocytic-leukemia-92ef568e-6dc4-5a1d-8e50-681b47b86599.md) Phase 3
- [Cancer](https://trialight.com/data/condition/cancer-703b1dfc-4812-50eb-83f4-d7a205d16bdb.md) Phase 3
- [Diffuse large B-cell lymphoma](https://trialight.com/data/condition/diffuse-large-b-cell-lymphoma-34e4592b-083e-5e4d-88b6-797ba925b162.md) Phase 3
- [Follicular lymphoma](https://trialight.com/data/condition/follicular-lymphoma-88de1ce9-ab0e-5d65-85c4-45a681fa2931.md) Phase 2
- Hodgkins lymphoma Phase 1
- [Liver disorder](https://trialight.com/data/condition/liver-disorder-8388d30a-2581-5015-9ddf-adc5f6a331d7.md) Phase 1
- [Lymphoma](https://trialight.com/data/condition/lymphoma-de4db685-7419-5e0e-b958-4591ffd69d43.md) Phase 2
- MALT lymphoma Phase 2
- [Mantle cell lymphoma](https://trialight.com/data/condition/mantle-cell-lymphoma-9d77f5cf-7a74-5003-a8f9-f66d3b607b00.md) Phase 3
- [Marginal zone lymphoma](https://trialight.com/data/condition/marginal-zone-lymphoma-e01375fa-199e-506d-9b41-a0427d6844a7.md) Phase 3
- Neoplasm Phase 3
- Neoplasm of mature B-cells Phase 2
- [Primary central nervous system lymphoma](https://trialight.com/data/condition/primary-central-nervous-system-lymphoma-0f3f2051-d8a7-5ab2-bc09-6bacfa58c99a.md) Phase 3
- [Relapsing-remitting multiple sclerosis](https://trialight.com/data/condition/relapsing-remitting-multiple-sclerosis-dbe6fc02-bfff-56b7-8299-64be5abdf415.md) Phase 2
- [Secondary progressive multiple sclerosis](https://trialight.com/data/condition/secondary-progressive-multiple-sclerosis-c559b49a-e39f-545b-aab5-dd41263dd2f6.md) Phase 3
- [Systemic lupus erythematosus](https://trialight.com/data/condition/systemic-lupus-erythematosus-6c9d074f-cc5f-588b-bf0c-6338d30c6eac.md) Phase 2
- [Waldenstrom macroglobulinemia](https://trialight.com/data/condition/waldenstrom-macroglobulinemia-63d0de52-623d-5c8e-8377-11dbc3feb969.md) Phase 2

### Other linked conditions (3)

- [B-cell non-Hodgkin lymphoma](https://trialight.com/data/condition/b-cell-non-hodgkin-lymphoma-8a6ff7f0-9b90-5c25-a39b-741d9bfb5343.md)
- [Chronic lymphocytic leukemia/small lymphocytic lymphoma](https://trialight.com/data/condition/chronic-lymphocytic-leukemia-small-lymphocytic-lymphoma-d0c3b47f-2179-530d-bb5f-1b02ebb91c98.md)
- Neuromyelitis optica

### Targets (1)

- [BTK](https://trialight.com/data/target/btk-0715d96c-6e26-5c6e-a6e0-2a745512051d.md) Tyrosine-protein kinase BTK inhibitor

---

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