IBRUTINIB 依鲁替尼 A Btk protein inhibitor. « New Drug Approvals

IBRUTINIB 依鲁替尼 A Btk protein inhibitor. « New Drug Approvals:



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U.S. Food and Drug Administration Approves IMBRUVICA™ (ibrutinib) as a Single Agent for Patients with Mantle Cell Lymphoma « New Drug Approvals

U.S. Food and Drug Administration Approves IMBRUVICA™ (ibrutinib) as a Single Agent for Patients with Mantle Cell Lymphoma « New Drug Approvals:

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Ibrutinib Phase 2 Data: Analyses Show Efficacy with Ibrutinib Monotherapy in Patients with Relapsed or Refractory Mantle Cell or Diffuse Large B-cell Lymphoma

ibrutinib

June 16, 2013 

Janssen Research & Development, LLC (Janssen), today announced the results of two separate Phase 2 studies suggesting that ibrutinib, an investigational oral Bruton's tyrosine kinase (BTK) inhibitor, shows efficacy when used as a monotherapy in patients with relapsed/refractory mantle cell lymphoma (MCL) or diffuse large B-cell lymphoma (DLBCL). The studies were presented today at the European Hematology Association (EHA) 18^th Annual Congress in Stockholm, Sweden. Ibrutinib is being jointly developed by Janssen and Pharmacyclics, Inc.

Ibrutinib (USAN), also known as PCI-32765, is an experimental drug candidate for the treatment of various types of cancer. It is an orally-administered, selective and covalent inhibitor of the enzyme Bruton tyrosine kinase (Btk).

Ibrutinib is currently under development by Pharmacyclics, Inc and Johnson & Johnson's Janssen Pharmaceutical division for B-cell malignancies including chronic lymphocytic leukemia, mantle cell lymphoma, diffuse large B-cell lymphoma, and multiple myeloma.

Ibrutinib was first designed and synthesized at Celera Genomics by Zhengying Pan, who along with a team of chemists and biologists reported in 2007 a structure-based approach for creating a series of small molecules that inactivate BTK through covalent binding to cysteine-481 near the ATP binding domain of BTK[2]. 

These small molecules irreversibly inhibited BTK by using a Michael acceptor for binding to the target cysteine. 

In April 2006, Pharmacyclics acquired Celera’s small molecule BTK inhibitor discovery program, which included a compound, PCI-32765 (known as compound 13 in the Pan et al paper) that was subsequently chosen for further preclinical development based on the discovery of anti-lymphoma properties in vivo . 

Since 2006, Pharmacyclics’ scientists have advanced the molecule into clinical trials and identified specific clinical indications for the drug.  It also has potential effects against autoimmune arthritis.