Avila Therapeutics
(Private) Drug Development

Katrine S. Bosley, CEO Juswinder Singh, PhD, Co-Founder and CSO Nagesh Mahanthappa, PhD, VP-Corporate Development and Operations Russell C. Petter, PhD, VP-Drug Discovery William Westlin, PhD, VP-Preclinical Research
100 Beaver Street
Waltham, MA 02453 USA
Tel: (781) 891-0086 Fax: (781) 891-0069
Website: http://www.avilatx.com/

Technology
Using its Avilomics platform, Avila Therapeutics generates covalent drugs that strongly and resiliently bond to specific disease-causing proteins, thereby silencing them to eradicate the corresponding disease. Avila’s novel covalent drugs may improve patient outcomes in a fundamentally new way. Avila is developing these therapies for a number of diseases, including viral infections, cancer and autoimmune diseases. Avila’s Avilomics platform with its broad applicability across multiple disease areas, is a powerful approach to the design and development of selective drugs with superior pharmacology. The main components of Avilomics are proprietary informatics technologies that uniquely identify sites amenable to selective covalent modification and target silencing; a unique library of highly selective chemistries for target silencing; and design tools that integrate target analysis and covalent chemistry to create novel medicines.

Avila Therapeutics is developing orally available small molecule drugs that form covalent bonds with their cellular targets to completely shut down the targeted receptor's activity. This covalent bonding mechanism that leads to protein silencing has increased selectivity. Covalent drugs are highly selective because of their ability to form bonds with sites that are unique to disease-causing proteins, therefore, are expected to be more efficaceous and less toxic. In addition, these drugs silence their target, and these targets remain silenced until a new protein is synthesized. Thus, Avila’s drugs lead to a prolonged duration of action, in contrast to most current drugs which need to maintain high exposure as the protein-drug interaction is transient. The benefits of this include the potential for better efficacy, less frequent dosing and less overall drug exposure that should improve safety. Because disease-causing proteins often mutate, the effectiveness of transiently binding agents decreases as the binding sites changes size and shape. However, because covalent drugs only must engage with the protein once to form a resilient bond, they do not readily disengage from a mutated protein and, therefore retain their efficacy in this setting. These covalent drugs are particularly well suited to the treatment of cancer and infectious diseases where mutations present an important challenge to patients and physicians. The company is developing covalently binding agents such as pan-ErbB, Btk, c-kit, VEGFr, PDGFr, and FLT3 inhibitors for the treatment of cancer.

In July 2009, Avila Therapeutics entered into an option agreement with the Novartis Option Fund focused on Avila’s advancement of a novel covalent drug program from Avila’s research pipeline in conjunction with an equity investment. The agreement includes upfront and potential milestones payments to Avila totaling over $200 million plus royalties. Avila’s covalent drugs offer the potential to treat many serious diseases through protein silencing.

Current as of June 19, 2010