BeiGene Enrolls First Patient in Phase 1 Study of BGB-290

– PARP inhibitor will be tested in disease-specific dose escalation cohorts to establish single-agent properties and preliminary anti-tumor activity –

BEIJING--()--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-290 for the treatment of cancer. BGB-290 is an investigational, oral, selective and potent inhibitor of poly (ADP-ribose) polymerase (PARP), an enzyme family which is involved in a number of cellular processes, including DNA repair and programmed cell death.

BGB-290 is the second compound in BeiGene’s two-asset collaboration with Merck, which was established in 2013 with the goal of leveraging Merck’s global oncology development and commercialization expertise. The first compound, BGB-283, an investigational second-generation B-RAF inhibitor, entered a Phase 1 study in November 2013.

“We are excited to begin dosing in the first-in-human trial of BGB-290, which we believe has the potential to be a new and better PARP inhibitor option for the treatment of cancer,” said John V. Oyler, CEO of BeiGene. “We continue to execute on our clinical plan through this strategic collaboration with Merck as we advance both compounds through the clinic and work toward our mission of developing life-saving cancer therapeutics to treat the unmet medical needs of cancer patients.”

“I am very pleased to be involved in the clinical development of this exciting new investigational anti-cancer drug,” commented Dr. Michael Millward, lead investigator for the trial and Cancer Council Professor of Clinical Cancer Research at the University of Western Australia. “We are hopeful that BGB-290 will demonstrate the potential to offer significant advantages over other drugs in this class, and could become an important part of the treatment options for patients with common cancers including small cell lung cancer, gastric cancer, primary brain tumors, and some ovarian and breast cancers.”

About the Study

The Phase 1 multicenter, open-label, dose escalation clinical trial of BGB-290 is designed to assess the safety, tolerability and pharmacokinetic properties of BGB-290 as a single agent. Key objectives in the study include determining maximum tolerated dose, pharmacokinetics, pharmacodynamics and preliminary anti-tumor activity of BGB-290. Disease-specific expansion cohorts will be enrolled at the maximally-tolerated or biologically-relevant dose.

About PARP Proteins and Inhibitors

PARP proteins are involved in DNA replication, transcriptional regulation and DNA damage repair. Inhibition of PARP converts common single-strand DNA breaks into double-strand breaks during DNA replication. Small-molecule inhibitors of PARP1/2 represent a class of anticancer agents that exert their cytotoxic effect by modulating the PARylation activity of PARP1/2 and trap PARP proteins on damaged DNA. A number of PARP inhibitors have demonstrated sustained antitumor responses as a single agent in patients with BRCA1- or BRCA2-mutant tumors with good safety profiles. (1)

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 combines unique access to internal patient-derived biopsies with strong oncology biology. 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.

1.   Papeo, G., Casale, E., Montagnoli, A., and Cirla, A. (2013) PARP inhibitors in cancer therapy: an update, Expert opinion on therapeutic patents 23, 503-514.

Contacts

Media/Investor:
For BeiGene (Beijing), Co., Ltd.
Jesse Baumgartner, 212-362-1200
pr@beigene.com

Release Summary

BeiGene (Beijing), Co., Ltd. today announced that it has dosed the first patient in a Phase 1 study of BGB-290 for the treatment of cancer.

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Contacts

Media/Investor:
For BeiGene (Beijing), Co., Ltd.
Jesse Baumgartner, 212-362-1200
pr@beigene.com