Delving into the Latest Updates on JNJ-64264681 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

JNJ 4681, JNJ 64264681, JNJ-4681

+ [2]

Target

BTK

Action

inhibitors

Mechanism

BTK inhibitors(Tyrosine-protein kinase BTK inhibitors)

Therapeutic Areas

NeoplasmsImmune System DiseasesHemic and Lymphatic Diseases+ [1]

Active Indication

Acute Myeloid LeukemiaMetastatic castration-resistant prostate cancerMyelodysplastic Syndromes+ [4]

Inactive Indication-

Originator Organization

Janssen Research & Development LLC

Active Organization

Johnson & JohnsonJanssen Research & Development LLC

Inactive Organization-

License Organization-

Drug Highest PhasePhase 1

First Approval Date-

Regulation-

Login to view timeline

Structure/Sequence

Molecular FormulaC27H30N6O3S

InChIKeyOPLNLPWGEZNZFL-ZWKOTPCHSA-N

CAS Registry2101524-34-7

The purpose of this study is to collect long-term safety data in participants with cancers including acute myeloid leukemia, non-Hodgkin lymphoma, myelodysplastic syndrome, chronic lymphocytic leukemia (type of cancer of the blood and bone marrow in which the bone marrow makes a large number of abnormal blood cells) and advanced solid tumors and metastatic castration-resistant prostate cancer (mCRPC).

Start Date30 Dec 2024

Sponsor / Collaborator

Janssen Research & Development LLC

NCT04657224

/ CompletedPhase 1

A Phase 1b, Open-Label Study of the Safety, Pharmacokinetics, and Pharmacodynamics of JNJ-64264681 in Combination With JNJ-67856633 in Participants With Non-Hodgkin Lymphoma and Chronic Lymphocytic Leukemia

The primary purpose of this study is to determine: the recommended Phase 2 doses (RP2Ds) of JNJ-64264681 and JNJ 67856633 when administered together in participants with B cell non-Hodgkin lymphoma (NHL) and chronic lymphocytic leukemia (CLL) (Part A - Dose Escalation); and the safety of the RP2Ds for this combination in different histologies/participant populations (Part B - Cohort Expansion).

Start Date25 Feb 2021

Sponsor / Collaborator

Janssen Research & Development LLC

NCT04210219

/ Active, not recruitingPhase 1

A Phase 1, Open-Label Study of the Safety, Pharmacokinetics, and Pharmacodynamics of JNJ-64264681 in Participants With Non-Hodgkin Lymphoma and Chronic Lymphocytic Leukemia

The purpose of the study is to determine the recommended Phase 2 dose(s) (RP2D[s]) in B cell non-Hodgkin lymphoma (NHL) and chronic lymphocytic leukemia (CLL) in Part 1 and to evaluate the safety of JNJ-64264681 at the RP2D(s) in Part 2.

Start Date02 Jul 2020

Sponsor / Collaborator

Janssen Research & Development LLC

100 Clinical Results associated with JNJ-64264681

Login to view more data

100 Translational Medicine associated with JNJ-64264681

Login to view more data

100 Patents (Medical) associated with JNJ-64264681

Login to view more data

1

Literatures (Medical) associated with JNJ-64264681

10 Nov 2022·Journal of medicinal chemistryQ1 · MEDICINE

Discovery of JNJ-64264681: A Potent and Selective Covalent Inhibitor of Bruton’s Tyrosine Kinase

Q1 · MEDICINE

Article

Author: Wang, Weixue ; Sepassi, Kia ; Huber, Michael ; Xiouras, Christos ; Venable, Jennifer D. ; Wu, Jiejun ; Bacani, Genesis M. ; Hirst, Gavin ; Coe, Kevin J. ; Wiener, John J. M. ; Cornelissen, Ivo ; Milligan, Cynthia ; Rex, Elizabeth ; Alexander, Richard ; Barbay, J. Kent ; Philippar, Ulrike ; Wei, Jianmei ; Gaudiano, Marcello ; Lebsack, Alec D. ; Kreutter, Kevin D. ; Packman, Kathryn ; Seierstad, Mark ; Rao, Navin L. ; Bekkers, Mariette ; Balasubramanian, Sriram ; Bembenek, Scott D. ; Clancy, Kathleen W. ; Ahn, Kay ; Edwards, James P. ; Rui, Haopeng ; Pooley Deckhut, Charlotte ; Murrey, Heather E. ; Chang, Leon ; Tichenor, Mark S.

Bruton's tyrosine kinase (BTK) is a Tec family kinase that plays an essential role in B-cell receptor (BCR) signaling as well as Fcγ receptor signaling in leukocytes. Pharmacological inhibition of BTK has been shown to be effective in treating hematological malignancies and is hypothesized to provide an effective strategy for the treatment of autoimmune diseases such as rheumatoid arthritis and systemic lupus erythematosus. We report the discovery and preclinical properties of JNJ-64264681 (13), a covalent, irreversible BTK inhibitor with potent whole blood activity and exceptional kinome selectivity. JNJ-64264681 demonstrated excellent oral efficacy in both cancer and autoimmune models with sustained in vivo target coverage amenable to once daily dosing and has advanced into human clinical studies to investigate safety and pharmacokinetics.

100 Deals associated with JNJ-64264681

Login to view more data

R&D Status

10 top R&D records.

Login

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Acute Myeloid Leukemia	Phase 1	United States	Janssen Research & Development LLC	30 Dec 2024
Acute Myeloid Leukemia	Phase 1	Japan	Janssen Research & Development LLC	30 Dec 2024
Acute Myeloid Leukemia	Phase 1	Belgium	Janssen Research & Development LLC	30 Dec 2024
Acute Myeloid Leukemia	Phase 1	France	Janssen Research & Development LLC	30 Dec 2024
Acute Myeloid Leukemia	Phase 1	Georgia	Janssen Research & Development LLC	30 Dec 2024
Acute Myeloid Leukemia	Phase 1	Greece	Janssen Research & Development LLC	30 Dec 2024
Acute Myeloid Leukemia	Phase 1	Israel	Janssen Research & Development LLC	30 Dec 2024
Acute Myeloid Leukemia	Phase 1	Poland	Janssen Research & Development LLC	30 Dec 2024
Acute Myeloid Leukemia	Phase 1	Taiwan Province	Janssen Research & Development LLC	30 Dec 2024
Acute Myeloid Leukemia	Phase 1	Ukraine	Janssen Research & Development LLC	30 Dec 2024