On September 15, 2016 ArQule, Inc. (Nasdaq: ARQL) reported the publication of a paper detailing the preclinical profile of ARQ 087, an orally available fibroblast growth factor receptor (FGFR) inhibitor (Press release, ArQule, SEP 15, 2016, View Source [SID:SID1234515151]). The findings, published on-line by PLOS ONE, View Source, demonstrate that ARQ 087 has anti-proliferative activity in cell lines driven by FGFR dysregulation, including amplifications, fusions, and mutations.

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ARQ 087 is being dosed in intrahepatic cholangiocarcinoma (iCCA) patients with FGFR2 genetic alterations as part of the phase 2 portion of a biomarker driven phase 1/2 trial. The company has been granted orphan drug designation by the U.S. Food and Drug Administration and European Medicines Agency for ARQ 087 in this indication.

About Intrahepatic Cholangiocarcinoma

Cholangiocarcinoma (CCA) is the most common biliary malignancy and the second most common hepatic malignancy after hepatocellular carcinoma (HCC)1. Depending on the anatomic location, CCA is classified as intrahepatic (iCCA), perihilar (pCCA), and extrahepatic (eCCA). iCCA originates from the intrahepatic biliary ductal system and forms an intrahepatic mass. The average age adjusted incidence rate for iCCA is approximately one in 100,000 per year in the United States and Europe2,3.

About FGFR and ARQ 087

ARQ 087 is a multi-kinase inhibitor designed to preferentially inhibit the fibroblast growth factor receptor ("FGFR") family with demonstrated activity in FGFR2 genetic alterations. The FGFR pathway is disrupted in several ways in human cancer, thus providing numerous therapeutic targets for an inhibitor of this pathway. ARQ 087 has demonstrated in vivo inhibition of tumor growth and downstream signaling in tumors whose growth is driven by FGFR targets.

Signals of single agent activity with this drug were observed in phase 1a testing. Phase 1b expansion cohorts with ARQ 087 include patients with cholangiocarcinoma and adrenocortical tumors, as well as those with FGFR translocations, amplifications and mutations. Clinical development of ARQ 087 has advanced into phase 2 for intrahepatic cholangiocarcinoma (iCCA) following the observation of two confirmed responses in this patient population in the phase 1 portion of the program.

Champions Oncology has filed a 10-Q – Quarterly report [Sections 13 or 15(d)] with the U.S. Securities and Exchange Commission .

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On September 14, 2016 – Third Rock Ventures, LLC reported the formation
of Relay Therapeutics with $57 million in Series A financing, including participation from an affiliate of
D. E. Shaw Research, LLC (Press release, Relay Therapeutics, SEP 14, 2016, View Source [SID1234520734]).

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Relay Therapeutics is building the world’s first dedicated drug discovery
platform centered on protein motion, with the aim of designing and developing new medicines that will
make a transformative difference for patients. Relay’s novel approach will build on recent scientific and
technological advances in structural biology, biophysics, computation, chemistry and biology to create
an integrated drug discovery engine fueled by a detailed understanding of the dynamic structural
changes undergone by protein molecules within the body. The company’s groundbreaking activities are
being spearheaded by a team that includes some of the world’s leaders in these emerging areas.
"Our integration of protein motion into the heart of the drug discovery process represents both a
philosophical and technological once-in-a-generation paradigm shift," said Alexis Borisy, Executive
Chairman and interim CEO of Relay Therapeutics, and Partner at Third Rock Ventures. "At Relay, we
have assembled the team and tools to build the first company with a dedicated drug discovery pipeline
centered around protein motion. This advancement in drug discovery – from static to dynamic – creates
opportunities to develop more effective therapies that we believe will improve and extend the lives of
millions of patients."

Scientific Approach
While much of biology is controlled by the three-dimensional motion of proteins, this reality is not
reflected in today’s drug discovery process. Relay Therapeutics is using emerging technologies and
insights to move from a static perspective to a moving one, allowing for the rational discovery and
design of medicines for diseases where effective therapies do not currently exist. The company’s drug
discovery engine illuminates the full mobility of a protein and the ways in which protein motion
regulates function. By applying these technologies as an integrated team focused on disease-causing
targets, Relay Therapeutics aims to develop breakthrough medicines for patients in need. The
company’s initial programs are focused on oncology.
"Relay’s novel approach enables us to observe large-scale and subtle protein motions, identifying new
opportunities for the drug design process," said Mark Murcko, Ph.D., Chief Scientific Officer of Relay
Therapeutics. "This innovative and integrated approach allows us to pursue novel medicines against a
wide array of compelling drug targets that, until now, have been challenging or even inaccessible."
History of Protein Motion in Drug Discovery
Sixty years ago, scientists acquired the ability to generate detailed static images of the molecular
machines that operate within our bodies, yielding an improved understanding of the molecular
underpinnings of certain diseases. By the late 1980s, after a generation of technological improvements,
the adoption of these stationary molecular snapshots into the drug discovery process marked a turning
point in the history of the pharmaceutical industry, accelerating the design of more effective drugs. In
recent years, however, it has become clear that such static images tell only part of the story, and that the
emerging ability to observe how these machines move, function, and interact has the potential to once
again transform the process of drug design. Today – two generations after the first static pictures of
molecular structures, and one generation after they were first incorporated into drug discovery – Relay
Therapeutics is drawing on new computational and experimental advances to move beyond the era of
static snapshots into one in which movies of the body’s molecular machines become central to drug
discovery.
Founders
Relay Therapeutics was founded by a group of experts in structural biology, biophysics and
biomolecular simulation who have played a pioneering role in the development of technologies that are
central to the company’s approach. The founding team is applying this expertise to Relay’s drug
discovery efforts, focusing on achieving a deeper understanding of the relationship between protein
motion and drug action. The company founders are:
• Matthew Jacobson, Ph.D., Professor and Pharmaceutical Chemistry Department Chair,
University of California, San Francisco (UCSF)
• Dorothee Kern, Ph.D., Professor, Brandeis University; Investigator, Howard Hughes Medical
Institute
• Mark Murcko, Ph.D., Chief Scientific Officer and Co-Founder, Relay Therapeutics; Senior
Lecturer, Massachusetts Institute of Technology (MIT)
• D. E. Shaw Research (David E. Shaw, Ph.D., Chief Scientist)
About Relay Therapeutics
Relay Therapeutics is committed to discovering and developing medicines that will make a
transformative difference for patients by building the first dedicated drug discovery pipeline centered on
protein motion. Bringing together the latest scientific advances in structural biology, biophysics,
computation, chemistry and biology, Relay’s drug discovery engine illuminates the full mobility of a
protein and the ways in which protein motion regulates function. By applying this approach as an
integrated team focused on disease-causing targets, Relay aims to develop breakthrough medicines for
patients in need. The company’s initial programs are focused on developing therapeutics in oncology.
Headquartered in Cambridge, Massachusetts, Relay Therapeutics is a private company launched in 2016
with $57 million in Series A financing from Third Rock Ventures and an affiliate of D. E. Shaw
Research.

On September 14, 2016 Varian Medical Systems (NYSE: VAR), reported it has been selected by Proton Therapy Pte., Ltd. (View Source) to install and service a Varian ProBeam Compact single-room proton therapy system for a new oncology center in Singapore. Construction of the new center is expected to begin by the end of 2016 (Press release, InfiMed, SEP 14, 2016, View Source [SID:SID1234515137]). In addition to a 10 year service agreement, Varian will also provide its Eclipse treatment planning system training environment for use by Proton Therapy Pte., Ltd. at its new Advanced Medicine Training Centre. Varian booked the order for the equipment in the fourth quarter of its fiscal year 2016.

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The Varian ProBeam Compact system is the only single room system capable of fully rotational intensity modulated proton therapy (IMPT). Treatments can be delivered with an unmatched combination of speed, flexibility and cost efficiency. The full-featured ProBeam Compact includes a cyclotron, Varian’s unique Dynamic Peak scanning technology for IMPT, a fully rotational gantry, robotic patient positioning tools, and a comprehensive suite of motion management tools. It incorporates cone beam CT imaging for positioning the patient based on high quality anatomical images with excellent soft tissue resolution, and Varian’s world-class Eclipse and ARIA software systems for the planning and managing of treatments.

"We selected the Varian ProBeam Compact system because it is the only system suitable to fit within the existing building constraints and for its many technical advantages, the full system integration with ARIA and Eclipse, and Varian’s history of innovation and providing its customers access to new technology for the life of the platform," said Dr. Djeng Shih Kien, chairman, Proton Therapy Pte., Ltd. "We look forward to working closely with the Varian team on this important cancer-fighting technology in Singapore."

"We have given our Compact system all the technical capabilities of our multi-room ProBeam systems so that clinics can offer the best possible treatment without having to make any sacrifices in performance," said Dr. Moataz Karmalawy, general manager of Varian’s Particle Therapy division. "By working closely with Proton Therapy Pte., Ltd. on the adoption of precision proton treatments, we are providing the opportunity for increased access to this technology for cancer patients across Southeast Asia and Australasia."

On September 14, 2016 Allergan plc (NYSE: AGN), a leading global pharmaceutical company, and Vitae Pharmaceuticals, Inc. (NASDAQ: VTAE), a clinical-stage biotechnology company, reported that they have entered into a definitive agreement under which Allergan will acquire Vitae for $21.00 per share, in cash, for a total transaction value of approximately $639 million (Press release, Allergan, SEP 14, 2016, View Source [SID1234523885]). The Boards of Directors of both companies have unanimously approved the transaction.

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The acquisition will strengthen Allergan’s dermatology product pipeline, with the addition of VTP-43742, a Phase 2 first-in-class, orally active RORγt (retinoic acid receptor-related orphan receptor gamma) inhibitor for the potential treatment of psoriasis and other autoimmune disorders. VTP-43742 acts through the potent inhibition of IL-17 activity. In preclinical studies, VTP-43742 has been observed to inhibit RORγt activity, is highly selective versus other ROR isotypes and may provide a treatment that could be administered as a once-daily oral dose. The compound recently completed a Phase 2 proof-of-concept multiple ascending dose trial in patients with moderate to severe psoriasis.

The acquisition also adds VTP-38543, a topical LXRβ (Liver X Receptor beta) selective agonist for the potential treatment of atopic dermatitis. It is believed that VTP-38543 works by decreasing inflammation in damaged skin tissue and repairing the damaged outer layer of skin. VTP-38543 is currently in a Phase 2a proof-of-concept clinical trial assessing the safety, tolerability and efficacy in patients with mild to moderate atopic dermatitis.

Vitae has developed and utilizes its Contour structure-based drug design platform to discover product candidates for validated therapeutic targets where biopharmaceutical research and development has traditionally struggled to develop drugs due to challenges related to potency, selectivity and pharmacokinetics. This has provided Vitae’s R&D team the ability to create first-in-class product candidates for challenging therapeutic targets.

"The acquisition of Vitae is a strategic investment for Allergan that adds strength and depth to our innovative medical dermatology franchise," said Brent Saunders, CEO and President of Allergan. "Vitae has pioneered the discovery and development of highly differentiated first-in-class compounds in atopic dermatitis, psoriasis and autoimmune diseases, areas of medicine where innovation is needed for patients."

"The Vitae team has been tremendously successful in discovering and conducting early development work in areas of medicine that can benefit from significant innovation," said Jeff Hatfield, President and Chief Executive Officer of Vitae. "Allergan has a long track record in developing and commercializing innovative dermatologic treatments. I believe our programs will be poised for successful development as part of Allergan’s portfolio. I am very proud of the tremendous contributions of our research teams and the clinical community who have led the discovery and development of our pipeline programs, and I thank them for their dedication to this science that may one day help many patients with dermatologic conditions, autoimmune disorders and potentially other conditions."

"Both the VTP-43742 and VTP-38543 programs offer the potential for highly differentiated mechanisms of action for the treatment of dermatologic conditions where patients are underserved by currently approved treatments," said David Nicholson, Chief Research & Development Officer, Allergan. "In addition, Vitae’s novel Contour drug discovery platform and its team, which have been instrumental in the discovery of novel ‘difficult to drug’ compounds, will be highly complementary to Allergan’s existing R&D discovery efforts in key therapeutic areas."

Under the terms of the merger agreement, a subsidiary of Allergan will commence a cash tender offer to purchase all of the outstanding shares of Vitae common stock for $21.00 per share. The closing of the tender offer is subject to customary closing conditions, including U.S. antitrust clearance and the tender of a majority of the outstanding shares of Vitae common stock. The merger agreement contemplates that Allergan will acquire any shares of Vitae that are not tendered into the offer through a second-step merger, which will be completed promptly following the closing of the tender offer. Pending approvals, Allergan anticipates closing the transaction by the end of 2016.

Additional information about Vitae, VTP-43742 and VTP-38543, as well as the unmet medical need in the treatment of psoriasis and atopic dermatitis, is available as a slide presentation on the Allergan web site at View Source

Debevoise & Plimpton LLP is serving as Allergan’s legal counsel. J.P. Morgan is serving as financial advisor to Vitae and Gunderson Dettmer Stough Villeneuve Franklin & Hachigian, LLP is serving as Vitae’s legal counsel.