TG Therapeutics and Jiangsu Hengrui Medicine Announce Global License Agreement for Development and Commercialization of Novel BTK Inhibitor Program for the Treatment of Hematologic Malignancies

US IND Filing Expected in the First Half of 2018

Hengrui is Eligible to Receive Collaboration and Licensing Payments of Approximately $350MM, in Addition to Royalties on Future Sales

NEW YORK and SHANGHAI, China, Jan. 08, 2018 -- TG Therapeutics, Inc. (NASDAQ:TGTX) (or “TG”) and Jiangsu Hengrui Medicine Co., Ltd. (SSE:600276) (or “Hengrui”) today announced that the companies have entered into an exclusive global license agreement pursuant to which TG Therapeutics will obtain worldwide rights, excluding Asia but including Japan, for the development of Hengrui’s Bruton’s Tyrosine Kinase (BTK) inhibitor program, including lead candidate TG-1701 (known in China as SHR-1459), as monotherapy and in combination with ublituximab (TG-1101), TG’s glycoengineered anti-CD20 monoclonal antibody, and umbralisib (TGR-1202), TG’s next generation PI3K-delta inhibitor.  In addition to TG-1701, the global license agreement covers TG-1702 (SHR-1266), another BTK inhibitor in pre-clinical development. 

Under the terms of the agreement, Hengrui will receive an up-front licensing fee and near-term milestones, payable in TG common stock, and will be eligible to receive additional payments contingent on certain clinical, regulatory, and commercial milestones, totaling approximately $350MM, as well as tiered royalties on net sales.

TG-1701 (SHR-1459) and TG-1702 (SHR-1266) are orally available, covalently-bound BTK inhibitors that exhibit superior selectivity to BTK compared to ibrutinib in in vitro kinase screening.  Hengrui commenced a Phase 1 clinical trial for TG-1701 (SHR-1459) in China in December 2017 while TG-1702 (SHR-1266) is in pre-clinical development.

Previously, TG reported that the triple combination of ublituximab, umbralisib, and the BTK inhibitor ibrutinib, resulted in a 100% Overall Response Rate (ORR) among 19 treated patients with Chronic Lymphocytic Leukemia (CLL)/Small Lymphocytic Lymphoma (SLL), an 86% ORR among 7 treated patients with iNHL (Follicular Lymphoma and Marginal Zone Lymphoma) and 100% ORR in the 4 treated patients with Mantle Cell Lymphoma (MCL).    

Michael S. Weiss, Executive Chairman and Chief Executive Officer of TG Therapeutics stated, "We are pleased to be partnering with one of the leading Chinese biopharmaceutical companies.  We have been evaluating potential BTK inhibitors for quite some time and we were really impressed with Hengrui’s research that led to the development of these two highly selective BTK inhibitors.  We believe TG-1701 could be comparable to the best-in-class BTK inhibitors and in combination with ublituximab and umbralisib, could represent a truly unique triple combination treatment option across CLL and NHL.”  Mr. Weiss continued, “With our UNITY program, we have pivotal and registration directed trials either already fully enrolled or enrolling across CLL and NHL for our U2 combination of umbralisib + ublituximab, and for umbralisib as a single agent.  With this license, we have taken a major step toward the development of a next generation, wholly-owned, proprietary, triplet therapy.  Our goal is to advance TG-1701 into the clinic as quickly as possible in the first half of this year." 

“TG Therapeutics has a distinctive strategy towards addressing B-cell lymphomas, employing unique combination strategies to harness key drivers of oncogenesis based on a portfolio of differentiated assets,” said Lianshan Zhang, Ph.D., President of Global R&D of Hengrui. “We have been very impressed by the leadership at TG Therapeutics and their vision in re-defining the treatment landscape for lymphoma patients.”

“Our steadfast commitment towards providing better and safer medicines for patients has propelled Hengrui to be a leading biopharmaceutical company in China,” said Piaoyang Sun, Ph.D., Chairman of Hengrui. “In recent years we have worked hard to generate and develop novel, potentially high impact oncology assets across modalities including immuno-oncology, targeted therapies, hormonal therapies, antibody-drug conjugates, oncolytic viruses, and epigenetics, among others. Hengrui is absolutely delighted to be a partner of TG Therapeutics to jointly make a difference for patients who suffer hematology malignancies around the world.”

ABOUT BTK INHIBITORS

Bruton’s tyrosine kinase (BTK) is an essential component of the B-cell receptor signaling pathways that regulate the survival, activation, proliferation, and differentiation of B lymphocytes. Targeting BTK with small molecule inhibitors has been demonstrated to be an effective treatment option for B-cell lymphomas and autoimmune diseases.  

About Jiangsu Hengrui Medicine Co., Ltd.

Jiangsu Hengrui Medicine Co., Ltd., established in 1970, is a leading biopharmaceutical company based in China with annual net sales of over $1.6 billion in 2016. Hengrui is devoted to empowering healthier lives through research, and currently has 3 programs under China NDA as well as 21 new molecular entities in clinical development in China, U.S., and Australia, across oncology, anesthesiology & pain management, immunology & inflammation, and cardiovascular & metabolic diseases.

ABOUT TG THERAPEUTICS, INC.

TG Therapeutics is a biopharmaceutical company focused on the acquisition, development and commercialization of novel treatments for B-cell malignancies and autoimmune diseases. Currently, the company is developing two therapies targeting hematological malignancies and autoimmune diseases. Ublituximab (TG-1101) is a novel, glycoengineered monoclonal antibody that targets a specific and unique epitope on the CD20 antigen found on mature B-lymphocytes. TG Therapeutics is also developing umbralisib (TGR-1202), an orally available PI3K delta inhibitor. The delta isoform of PI3K is strongly expressed in cells of hematopoietic origin and is believed to be important in the proliferation and survival of B‐lymphocytes. Both ublituximab and umbralisib, or the combination of which is referred to as "U2", are in Phase 3 clinical development for patients with hematologic malignancies, with ublituximab also in Phase 3 clinical development for Multiple Sclerosis. Additionally, the Company has recently brought its anti-PD-L1 monoclonal antibody into Phase 1 development and aims to bring additional pipeline assets into the clinic in the future.  TG Therapeutics is headquartered in New York City.

Cautionary Statement

Some of the statements included in this press release may be forward-looking statements that involve a number of risks and uncertainties.  For those statements, we claim the protection of the safe harbor for forward-looking statements contained in the Private Securities Litigation Reform Act of 1995.  In addition to the risk factors identified from time to time in our reports filed with the Securities and Exchange Commission, factors that could cause our actual results to differ materially are the following: our ability to successfully and cost effectively complete preclinical and clinical trials; the risk that early clinical trial results, that may have  influenced our decision to proceed with additional clinical trials, will not be reproduced in future studies; the risk that the combination of ublituximab (TG-1101) and umbralisib (TGR-1202), referred to as ‘U2’ or TG-1303 and being studied in the UNITY clinical trials, will not prove to be a safe and efficacious combination or backbone for future triple or quad combination therapies; the risk that the company will not move forward with the development of TG-1701 or any inhibitor in the BTK inhibitor program licensed from Hengrui  Any forward-looking statements set forth in this press release speak only as of the date of this press release. We do not undertake to update any of these forward-looking statements to reflect events or circumstances that occur after the date hereof. This press release and prior releases are available at www.tgtherapeutics.com. The information found on our website is not incorporated by reference into this press release and is included for reference purposes only.

Contacts

For TG Therapeutics:

Investor Relations:
Jenna Bosco
Vice President, Investor Relations
TG Therapeutics, Inc.
Telephone: 212.554.4351
Email: [email protected] 

For Hengrui Medicine:
Paul Lu, Ph.D.
Global Business Development
+1.609.423.2155

Investor Relations:
Eric Laub
Senior Vice President/ICR
+1.617.956.6733
[email protected] 

Media:
James Heins
Senior Vice President/ICR
+1.203.682.8251
[email protected]