Ibrutinib

Generic Name: Ibrutinib

Brand Names: Imbruvica

Drug Type: Small Molecule

Chemical Formula: C_₂₅H_₂₄N_₆O_₂

CAS Number: 936563-96-1

Unique Ingredient Identifier: 1X70OSD4VX

Background: Ibrutinib is a small molecule that acts as an irreversible potent inhibitor of Burton's tyrosine kinase. It is designated as a targeted covalent drug and presented as a promising activity in B-cell malignancies in clinical trials. Ibrutinib was developed by Pharmacyclics Inc and was first approved by the FDA in November 2013 for the treatment of mantle cell lymphoma (MCL) under accelerated approval; however, in April 2023, the drug manufacturer withdrew the accelerated approvals for ibrutinib in the US.

Ibrutinib was approved by the EMA in October 2014 and by Health Canada in November 2014. It is currently approved for the treatment of various conditions, such as chronic lymphocytic leukemia (CLL), Waldenström's Macroglobulinemia, and chronic graft versus host disease (cGVHD) in August 2017. Notably, ibrutinib became the first FDA-approved cGVHD treatment for children in August 2017.

Indication: Ibrutinib is indicated for the treatment of the following conditions.

Chronic lymphocytic leukemia (CLL)/small lymphocytic lymphoma (SLL)

Waldenström's macroglobulinemia

Chronic graft-versus-host disease (cGVHD)

Mantle cell lymphoma (MCL)

Marginal zone lymphoma (MZL)

Associated Conditions: Chronic Graft-Versus-Host Disease, Chronic Lymphocytic Leukemia, Marginal Zone Lymphoma (MZL), Refractory Mantle Cell Lymphoma, Relapsed Mantle Cell Lymphoma, Small Lymphocytic Lymphoma, Steroid-dependent chronic graft-versus-host disease, Waldenström's Macroglobulinemia (WM), Steroid refractory Chronic graft versus host disease

Clinical Trials

Rituximab and Ibrutinib (RI) Versus Dexamethasone, Rituximab and Cyclophosphamide (DRC) as Initial Therapy for Waldenström's Macroglobulinaemia

Phase 2

Recruiting

Conditions: Waldenstrom Macroglobulinemia

Interventions: Drug: Rituximab, ibrutinib
Drug: Dexamethasone, cyclophosphamide, rituximab

First Posted Date: 2019-08-19

Last Posted Date: 2024-05-10

Lead Sponsor: University College, London

Target Recruit Count: 148

Registration Number: NCT04061512

Locations: 🇬🇧
The Royal Bournemouth and Christchurch Hospitals NHS Foundation Trust, Bournemouth, United Kingdom
🇬🇧
University Hospital of Wales, Cardiff, United Kingdom
🇬🇧
Royal United Hospital, Bath, Bath, United Kingdom

and more 22 locations

ERK 1/2 Signaling in Ibrutinib Resistant B-cell Malignancies

Phase 1

Withdrawn

Conditions: Marginal Zone Lymphoma
Chronic Lymphocytic Leukemia
Waldenstrom Macroglobulinemia
Mantle Cell Lymphoma

Interventions: Drug: Ibrutinib
Drug: LY3214996

First Posted Date: 2019-08-02

Last Posted Date: 2020-02-05

Lead Sponsor: Dana-Farber Cancer Institute

Registration Number: NCT04043845

A Study of Ibrutinib (PCI-32765) in Chinese Participants With Relapse or Refractory Waldenstrom's Macroglobulinemia (WM)

Phase 4

Completed

Conditions: Waldenstrom Macroglobulinemia

Interventions: Drug: Ibrutinib

First Posted Date: 2019-08-01

Last Posted Date: 2025-04-27

Lead Sponsor: Janssen Research & Development, LLC

Target Recruit Count: 17

Registration Number: NCT04042376

Locations: 🇨🇳
Wuhan Union Hospital, Wuhan, China
🇨🇳
The Second Affiliated Hospital of Xi'an Jiaotong University, Xi'an, China
🇨🇳
Henan Cancer Hospital, Zhengzhou, China

and more 3 locations

Biomarker Guided Treatment in DLBCL

Phase 2

Conditions: Diffuse Large B Cell Lymphoma

Interventions: Drug: Cyclophosphamide
Drug: Rituximab
Drug: Doxorubicin
Drug: Vincristine
Drug: Prednisone
Drug: Ibrutinib
Drug: Lenalidomide
Drug: chidamide
Drug: decitabine

First Posted Date: 2019-07-19

Last Posted Date: 2020-11-19

Lead Sponsor: Ruijin Hospital

Target Recruit Count: 128

Registration Number: NCT04025593

Locations: 🇨🇳
Ruijin hospital, Shanghai, Shanghai, China

Study to Assess the Efficacy and Safety of Ublituximab and Umbralisib in Participants With Chronic Lymphocytic Leukemia (CLL) Currently Treated With Ibrutinib, Acalabrutinib or Venetoclax

Phase 2

Terminated

Conditions: Chronic Lymphocytic Leukemia

Interventions: Drug: Ublituximab
Drug: Umbralisib
Drug: Acalabrutinib Oral Capsule
Drug: Ibrutinib
Drug: Venetoclax

First Posted Date: 2019-07-11

Last Posted Date: 2023-07-24

Lead Sponsor: TG Therapeutics, Inc.

Target Recruit Count: 41

Registration Number: NCT04016805

Locations: 🇺🇸
TG Therapeutics Investigational Trial Site, New York, New York, United States

A Prospective Multicenter Phase 2 Study of FCR/BR Alternating With Ibrutinib in Treatment-naive Patients With CLL

Phase 2

Recruiting

Conditions: Chronic Lymphocytic Leukemia

Interventions: Drug: FCR and Ibrutinib
Drug: BR and Ibrutinib
Drug: Ibrutinib and Thalidomide

First Posted Date: 2019-06-10

Last Posted Date: 2019-06-10

Lead Sponsor: Institute of Hematology & Blood Diseases Hospital, China

Target Recruit Count: 50

Registration Number: NCT03980002

Locations: 🇨🇳
Institute of Hematology & Blood Diseases Hospital Chinese Academy of Medical Sciences & Peking Union Medical College, Tianjin, Tianjin, China

Temozolomide, Etoposide, Doxil, Dexamethasone, Ibrutinib, and Rituximab (TEDDI-R) in Aggressive B-cell Lymphomas With Secondary Involvement of the Central Nervous System (CNS)

Phase 2

Active, not recruiting

Conditions: Central Nervous System Lymphoma
Secondary Central Nervous System Lymphoma

Interventions: Drug: TEDD-R
Drug: TEDDI-R
Drug: Ibrutinib
Drug: Cytarabine
Drug: Isavuconazole
Drug: Methotrexate

First Posted Date: 2019-05-28

Last Posted Date: 2025-04-10

Lead Sponsor: National Cancer Institute (NCI)

Target Recruit Count: 48

Registration Number: NCT03964090

Locations: 🇺🇸
National Institutes of Health Clinical Center, Bethesda, Maryland, United States

Phase I/II Study of Rapcabtagene Autoleucel in CLL, 3L+ DLBCL, r/r ALL and 1L HR LBCL

Phase 1

Recruiting

Conditions: Diffuse Large B-cell Lymphoma
Large B-cell Lymphoma
Acute Lymphoblastic Leukemia
Chronic Lymphocytic Leukemia
Small Lymphocytic Lymphoma

Interventions: Biological: Rapcabtagene autoleucel single agent
Drug: Ibrutinib

First Posted Date: 2019-05-23

Last Posted Date: 2025-05-21

Lead Sponsor: Novartis Pharmaceuticals

Target Recruit Count: 225

Registration Number: NCT03960840

Locations: 🇺🇸
University of California LA, Los Angeles, California, United States
🇺🇸
Stanford University Medical Center, Stanford, California, United States
🇺🇸
H Lee Moffitt Cancer Center and Research Institute, Tampa, Florida, United States

and more 13 locations