– Wholly-owned BTK inhibitor will be tested in dose escalation cohorts in indolent B-cell malignancies to establish single-agent properties and preliminary anti-tumor activity –
– Third oncology candidate to enter clinic within last 9 months –

BEIJING, China I August 26, 2014 I BeiGene (Beijing), Co., Ltd., an innovative oncology company focused on developing targeted and immune-oncology therapeutics, today announced that it has dosed the first patient in a Phase 1 study of BGB-3111 for the treatment of cancer. BGB-3111 is an investigational, oral, highly selective and potent inhibitor of Bruton tyrosine kinase (BTK), a critical component of B-cell receptor (BCR) signaling which plays an important role in B-cell malignancies.

“We are excited to begin this first-in-human trial of BGB-3111, which we feel has the potential to be a best-in-class BTK inhibitor based on our preclinical results to date,” said Dr. Jason Yang, Senior Vice President and Head of Clinical Development at BeiGene. “With the strong support of our experienced team of investigators, we look forward to conducting this study and assessing dosing, PK and safety results, with the potential for early anti-tumor activity as we move toward the trial’s expansion phase later this year.”

The Phase 1a dose escalation portion of study will be conducted at 4 Australian sites, followed by a 1b expansion phase which will enroll disease-specific cohorts at the maximally-tolerated or biologically-relevant dose. BeiGene currently expects to finish the dose escalation portion in the second quarter of 2015, with data readout for the expansion stage expected by the end of 2015 or beginning of 2016.

“I am very pleased to be involved in the clinical development of this exciting new anti-cancer drug,” commented Dr. Constantine Tam, lead investigator for the trial at the Peter MacCallum Cancer Centre in Melbourne. “BTK inhibitors have demonstrated impressive clinical activity in several B-cell malignancies, and BGB-3111 shows the potential for significant advantages over previous BTK inhibitors in preclinical studies. We hope these advantages will continue to translate into a stronger activity and safety profile as BGB-3111 advances through the clinic.”

“We have continued to rapidly accelerate our research development plan, with three promising candidates against different targets entering the clinic within the past 9 months,” commented John V. Oyler, CEO of BeiGene. “As our first wholly-owned program to enter clinical studies, BGB-3111 is yet another validation of our novel translational research platform and a reflection of our ability to execute on significant clinical milestones – both on our lead partnered programs and our proprietary compounds. We look forward to advancing our additional promising preclinical candidates in the months ahead, and expect to bring up to several new small molecules/biologics into the clinic within the next year.”

BeiGene is currently investigating two other small molecule inhibitors in clinical development as part of a strategic partnership with Merck Serono: BGB-283, a second-generation B-RAF inhibitor which entered a Phase 1 study in November 2013; and BGB-290, a PARP inhibitor which entered a Phase 1 study in July 2014.

About the Study

The Phase 1 multicenter, open-label, dose escalation clinical trial of BGB-3111 is designed to assess the safety, tolerability and pharmacokinetic properties of BGB-3111 as a single agent. Key objectives in the study include determining maximum tolerated dose, pharmacokinetics, pharmacodynamics and preliminary anti-tumor activity of BGB-3111. Disease-specific expansion cohorts will be enrolled at the maximally-tolerated or biologically-relevant dose.

About BTK Proteins and Inhibitors

Bruton tyrosine kinase (BTK), a member of the TEC family of kinases, is a signaling molecule positioned within the B-cell receptor signaling cascade. BTK is predominantly expressed in B lymphocytes at various stages of development. Activation of BTK in B cells initiates a series of signaling events that leads to subsequent NF-κB activation and the expression of genes involved in proliferation and survival. Several BTK inhibitors have demonstrated sustained antitumor responses as a single agent in patients with B-cell malignancies.

About BeiGene (Beijing), Co., Ltd.

BeiGene is an innovative Chinese oncology R&D company focused on discovering, developing and commercializing targeted and immune-oncology therapeutics through a novel translational research platform that leverages our strong internal oncology biology expertise with unique access to large number of patient-derived tumor biopsies. With a team of 150 scientists and staff, its pipeline is comprised of novel oral small molecules and monoclonal antibodies for cancer. BeiGene Ltd. is a Cayman Islands exempted company that is an investor in and collaborator with BeiGene (Beijing), Co. Ltd. For more information, please visit our website at www.beigene.com.