Avila Therapeutics Presents Data Demonstrating The Relevance Of Its Btk Inhibitor, AVL-292, In B Cell Malignancies Such As CLL

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BlankAvila Therapeutics Presents Data Demonstrating The Relevance Of Its Btk

Inhibitor, AVL-292, In B Cell Malignancies Such As CLL

13 Jun 2011

Avila Therapeutics™, Inc., a biotechnology company developing novel targeted

covalent drugs, today announced the presentation of data on AVL-292, a

clinical-stage inhibitor of Bruton's tyrosine kinase (Btk), at the 16th Congress

of the European Hematology Association (EHA).

In the studies presented, AVL-292 inhibited both the growth of B cell lymphoma

cell lines in vitro and the survival of primary chronic lymphocytic leukemia

cells ex vivo. The data reinforce the potential of AVL-292 to treat B cell

malignancies such as chronic lymphocytic leukemia (CLL) through potent and

selective inhibition of Btk.

" Bruton's tyrosine kinase (Btk) plays a crucial role in promoting proliferation

and survival of B cell malignancies, representing a promising new drug target

for novel therapies such as AVL-292, " said Jan A. Burger, M.D., Ph.D., Assistant

Professor, Department of Leukemia, The University of Texas MD Cancer

Center, Houston, TX, and contributing author on the presentation. " These data

show that the covalent inhibition of Btk has an effect not only on B lymphoma

cells, but also on the interaction of these cancer cells with their

microenvironment, suggesting that Btk inhibition has the potential to mediate a

robust therapeutic effect. "

In a poster presentation titled " A Targeted Therapy (AVL-292) For Bruton's

Tyrosine Kinase In B-Cell Malignancies " , Juswinder Singh, Ph.D., Co-Founder and

Chief Scientific Officer at Avila Therapeutics, presented data demonstrating

that:

- AVL-292 is a potent, selective, covalent inhibitor of Btk.

- AVL-292 completely abrogates anti-IgM induced viability of primary CLL cells,

and completely blocks B cell receptor activation.

- AVL-292 reduces expression of the chemokines, CCL3 and CCL4, in primary CLL

cells cultured with Nurse-like Cells (NLCs).

- AVL-292 reduces migration of CLL cells towards CXCL12 and CXCL13

- In a Phase 1a clinical trial in healthy volunteers, AVL-292 was safe and

well-tolerated with dose-proportional exposure to drug at doses from 0.5 mg/kg

to 7.0 mg/kg. Further, Btk target occupancy was detected at all dose levels

tested, and complete target engagement was demonstrated at dose levels =1 mg/kg.