On April 15, 2016 Incyte Corporation (Nasdaq: INCY) reported that it will highlight the productivity of its drug discovery and development organization and aspects of its development portfolio at an investor event on Sunday, April 17, 2016 at the American Association for Cancer Research (AACR) (Free AACR Whitepaper) Annual Meeting 2016 in New Orleans, Louisiana (Press release, Incyte, APR 15, 2016, View Source;p=RssLanding&cat=news&id=2157635 [SID:1234510922]).

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The event will include a discussion of Incyte’s second-generation PI3Kδ inhibitor, INCB50465; the Company’s immuno-oncology portfolio, including its anti-GITR antibody, INCAGN1876, anti-OX40 antibody, INCAGN1949, and emerging data with its small molecule BRD inhibitor, INCB54329; as well as its targeted epigenetic therapies, including a novel LSD1 inhibitor entering Phase 1 development, INCB59872 .

"Incyte operates with the conviction that investment in basic research can translate into innovative therapies that can address important unmet medical needs. To that end, we are pleased to be able to highlight such a broad collection of abstracts from our emerging development portfolio at this year’s AACR (Free AACR Whitepaper) Annual Meeting," stated Reid Huber, Ph.D., Incyte’s Chief Scientific Officer. "The research team’s productivity is a result of the quality of our scientific organization and the efficiency of our R&D model."

As part of its succession plan, Incyte also announced that after almost 13 years at the Company, Dr. Richard Levy, Chief Drug Development Officer, is retiring effective April 30, 2016. Dr. Steven Stein, Incyte’s Chief Medical Officer, will now assume all of Dr. Levy’s responsibilities. Dr. Levy was instrumental in building the broad and diverse portfolio Incyte has today, and developing Jakafi (ruxolitinib), the Company’s proprietary JAK 1/JAK 2 inhibitor

Chronic obstructive pulmonary disease (COPD) is associated with exercise limitation and physical inactivity, which are believed to have significant long-term negative health consequences for patients. While a number of COPD treatments and exercise training programmes increase exercise capacity, there is limited evidence for their effects on physical activity levels, with no clear association between exercise capacity and physical activity in clinical trials. Physical activity depends on a number of behaviour, environmental and physiological factors. We describe the design of the PHYSACTO trial, which is investigating the effects of bronchodilators, either alone or with exercise training, in combination with a standardised behaviour-change self-management programme, on exercise capacity and physical activity in patients with COPD. It is hypothesised that bronchodilators in conjunction with a behaviour-change self-management programme will improve physical activity and that this effect will be amplified by the addition of exercise training.
Patients are being recruited from 34 sites in Australia, New Zealand, the USA, Canada and Europe. Patients receiving a multicomponent intervention designed to support behaviour change related to physical activity are randomised to four treatment arms: placebo, tiotropium, tiotropium+olodaterol, and tiotropium+olodaterol+exercise training. The primary outcome is improvement in exercise capacity after 8 weeks, measured by endurance time during a shuttle walk test. The secondary outcome is improvement in physical activity, including objective accelerometer assessment and patient-reported functioning using the Functional Performance Inventory-Short Form and the novel hybrid PROactive instrument. Additionally, the influence of moderating variables (ie, factors influencing a patient’s choice to be physically active) on increases in physical activity is also explored.
The study has been approved by the relevant Institutional Review Boards, Independent Ethics Committee and Competent Authority according to national and international regulations. The findings of the trial will be disseminated through relevant peer-reviewed journals and international conference presentations.
NCT02085161.
Published by the BMJ Publishing Group Limited. For permission to use (where not already granted under a licence) please go to View Source

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A simplified method for monitoring the incorporation of radiolabeled acetate into lipids in a cellular system is described. The assay eliminates the commonly employed labor-intensive organic extraction step by plating the cells in 96-well tissue culture-treated ScintiPlates() that enable direct measurement of radiolabeled cell membrane-embedded lipids. Since the scintillant is entrenched in the plates, radioactivity in close proximity to the scintillant is measured without the need for liquid scintillation cocktail. The utility of this method for evaluating inhibitors of the de novo fatty acid synthetic pathway is demonstrated here with fatty acid synthase (FASN). Due to the upregulation of FASN activity in many tumor types, development of inhibitors to block the FASN activity in cells shows promise as an attractive and tractable approach for therapeutic intervention.

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c-KIT kinase is a validated drug discovery target for gastrointestinal stromal tumors (GISTs). Clinically used c-KIT kinase inhibitors, i.e., Imatinib and Sunitinib, bear other important targets such as ABL or FLT3 kinases. Here we report our discovery of a more selective c-KIT inhibitor, compound 13 (CHMFL-KIT-110), which completely abolished ABL and FLT3 kinase activity. KinomeScan selectivity profiling (468 kinases) of 13 exhibited a high selectivity (S score (1) = 0.01). 13 displayed great antiproliferative efficacy against GISTs cell lines GIST-T1 and GIST-882 (GI50: 0.021 and 0.043 μM, respectively). In the cellular context, it effectively affected c-KIT-mediated signaling pathways and induced apoptosis as well as cell cycle arrest. In addition, 13 possessed acceptable bioavailability (36%) and effectively suppressed the tumor growth in GIST-T1 cell inoculated xenograft model without apparent toxicity. 13 currently is undergoing extensive preclinical evaluation and might be a potential drug candidate for GISTs.

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To evaluate the safety and efficacy of the combination therapy of fluorouracil, leucovorin and irinotecan (FOLFIRI) and aflibercept in Asian patients with metastatic colorectal cancer (mCRC), who had progressed after oxaliplatin-based chemotherapy.
This is a retrospective analysis of 19 mCRC patients who received FOLFIRI and aflibercept (4 mg/kg intravenously) every 2 weeks via a Named Patient Program (supported by Sanofi Aventis) in Singapore. Treatment was administered until disease progression or unacceptable toxicities. Kaplan-Meier method was used to estimate progression-free survival (PFS) and overall survival (OS). Efficacy and toxicities were summarized using descriptive statistics. Statistical analysis was performed using STATA 12.0 software.
The majority (84%) of the patients were of chinese ethnicity. The median age was 59 years, with 63.2% of the patients having an Eastern Cooperative Oncology Group status of 1. Four patients (21.1%) achieved partial response and 8 patients (42.1%) achieved stable disease. After a median follow-up of 9.6 months [95% confidence interval (CI), 2.2-13.1 months], the median OS was 11.6 months (95% CI, 6.1 to not-estimable), and median PFS was 4.1 months (95% CI, 2.2-5.9). Majority of the toxicities were grade 1-2, and include leucopenia (84.2%), anemia (73.7%), liver enzyme elevation (68.4%) and fatigue (68.4%). The most frequently reported grade 3 toxicities were neutropenia and neutropenic complications (both 15.8%). All adverse events resolved with supportive management.
The clinical benefit and safety profile of the combination of FOLFIRI/aflibercept in Asian patients with mCRC are consistent with that of Western population. FOLFIRI/aflibercept may be an appropriate therapeutic option in Asian patients with mCRC previously treated with an oxaliplatin-based regimen.
© 2016 John Wiley & Sons Australia, Ltd.

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