On September 6, 2016 Valeant Pharmaceuticals International, Inc. (NYSE: VRX and TSX: VRX) ("Valeant") and Progenics Pharmaceuticals, Inc. (Nasdaq: PGNX) ("Progenics") reported the U.S. commercial launch of RELISTOR (methylnaltrexone bromide) Tablets, which is now available for prescribing. RELISTOR Tablets (450 mg once daily) were approved by the U.S. Food and Drug Administration (FDA) for the treatment of opioid-induced constipation (OIC) in adults with chronic non-cancer pain on July 19, 2016.

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"We are very pleased to launch RELISTOR Tablets in the U.S. and provide an exceptional new treatment option for the millions of patients who suffer from extreme discomfort due to OIC," said Joseph C. Papa, Chief Executive Officer of Valeant. "This new method of delivery for RELISTOR offers healthcare professionals a novel alternative to address the treatment of OIC – a growing need in pain management – and demonstrates Valeant’s continued commitment to delivering innovative products that improve people’s lives."

In addition, RELISTOR Tablets will be highlighted during poster presentations at PAINWeek, the largest U.S. pain conference for frontline clinicians, in Las Vegas, Nevada, from September 6-10. The posters will include the following:
Webster LR, Harper JR, Israel RJ. "Oral methylnaltrexone is efficacious and well tolerated for the treatment of opioid-induced constipation in patients with chronic noncancer pain taking concomitant methadone." PAINWeek Poster, public viewing begins on
Thursday, September 8 at 12:30 p.m. PT.

Webster LR, Harper JR, Israel RJ. "Oral methylnaltrexone does not negatively impact analgesia in patients with opioid-induced constipation and chronic noncancer pain." PAINWeek Poster, public viewing begins on Thursday, September 8 at 12:30 p.m. PT.
The RELISTOR Tablets data will also be presented by Steven Simon, M.D., Professor of Pathology, University of Miami Health System, during a product theatre, "Opioid-Induced Constipation When Reliable and Rapid Relief Matters," on Friday, September 9 at 8 a.m. PT.

Important Safety Information about RELISTOR
RELISTOR (methylnaltrexone bromide) Tablets are contraindicated in patients with known or suspected gastrointestinal obstruction and patients at increased risk of recurrent obstruction, due to the potential for gastrointestinal perforation.
Cases of gastrointestinal perforation have been reported in adult patients with OIC and advanced illness with conditions that may be associated with localized or diffuse reduction of structural integrity in the wall of the gastrointestinal tract (e.g., peptic ulcer disease, Ogilvie’s syndrome, diverticular disease, infiltrative gastrointestinal tract malignancies or peritoneal metastases). Take into account the overall risk-benefit profile when using RELISTOR in patients with these conditions or other conditions which might result in impaired integrity of the gastrointestinal tract wall (e.g., Crohn’s disease). Monitor for the development of severe, persistent, or worsening abdominal pain; discontinue RELISTOR in patients who develop this symptom.

If severe or persistent diarrhea occurs during treatment, advise patients to discontinue therapy with RELISTOR and consult their healthcare provider.

Symptoms consistent with opioid withdrawal, including hyperhidrosis, chills, diarrhea, abdominal pain, anxiety, and yawning have occurred in patients treated with RELISTOR.

Patients having disruptions to the blood-brain barrier may be at increased risk for opioid withdrawal and/or reduced analgesia. Take into account the overall risk-benefit profile when using RELISTOR in such patients. Monitor for adequacy of analgesia and symptoms of opioid withdrawal in such patients.

Avoid concomitant use of RELISTOR with other opioid antagonists because of the potential for additive effects of opioid receptor antagonism and increased risk of opioid withdrawal.

The most common adverse reactions (≥ 12%) in adult patients with opioid-induced constipation and chronic non-cancer pain receiving RELISTOR tablets were abdominal pain, diarrhea, headaches, abdominal distention, hyperhidrosis, anxiety, muscle spasms, rhinorrhea, and chills. Adverse reactions of abdominal pain, diarrhea, hyperhidrosis, anxiety, rhinorrhea, and chills may reflect symptoms of opioid withdrawal.

Please see complete Prescribing Information for RELISTOR at www.valeant.com. For more information about RELISTOR, please visit www.relistor.com.

About RELISTOR
Progenics has exclusively licensed development and commercialization rights for its first commercial product, RELISTOR, to Valeant. RELISTOR Tablets (450 mg once daily) is approved in the United States for the treatment of OIC in patients with chronic non-cancer pain. RELISTOR Subcutaneous Injection (12 mg and 8 mg) is a treatment for opioid-induced constipation approved in the United States and worldwide for patients with advanced illness and chronic non-cancer pain.

On September 6, 2016 TESARO, Inc. (NASDAQ:TSRO), an oncology-focused biopharmaceutical company, reported that data from six abstracts will be presented at the 2016 European Society for Medical Oncology (ESMO) (Free ESMO Whitepaper) annual meeting, October 7 to October 11, 2016, in Copenhagen (Press release, TESARO, SEP 6, 2016, View Source [SID:1234514953]). In addition, TESARO will webcast an investor and analyst briefing from Copenhagen on Saturday, October 8 at 7:00 PM local time in conjunction with the ESMO (Free ESMO Whitepaper) annual meeting.

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Please plan to visit TESARO at Booth #415 for information about our pipeline.

Presentation Details (all times local):

Niraparib

Saturday, October 8, 2016, 4:30 PM to 6:00 PM — Presidential Symposium 1
A randomized, double-blind phase 3 trial of maintenance therapy with niraparib vs placebo in patients with platinum-sensitive recurrent ovarian cancer (ENGOT-OV16/NOVA trial)
Presentation: LBA3_PR, Presidential Symposium 1, Location: Copenhagen Room, Time: 5:30 PM
Results selected for inclusion in the ESMO (Free ESMO Whitepaper) Press Programme

Sunday, October 9, 2016, 1:00 PM to 2:00 PM
Modeling maintenance therapy in ovarian cancer
Poster: 1043P, Location: Hall E

Niraparib is an investigational product candidate that has not been approved by any regulatory agencies.

Rolapitant

Sunday, October 9, 2016, 1:00 PM to 2:00 PM
Efficacy and safety of rolapitant in the prevention of chemotherapy-induced nausea and vomiting (CINV) in elderly patients
Poster: 1441P, Location: Hall E

Sunday, October 9, 2016, 1:00 PM to 2:00 PM
Efficacy of rolapitant for prevention of chemotherapy-induced nausea and vomiting (CINV) in patients with gastrointestinal and colorectal cancers
Poster: 1440P, Location: Hall E

Sunday, October 9, 2016, 1:00 PM to 2:00 PM
Safety of rolapitant for prevention of chemotherapy-induced nausea and vomiting (CINV) in patients receiving Breast Cancer Resistant Protein (BCRP) substrate chemotherapy agents
Poster: 1442P, Location: Hall E

Sunday, October 9, 2016, 1:00 PM to 2:00 PM
Systematic review of the efficacy and safety of neurokinin-1 receptor antagonists for chemotherapy-induced nausea and vomiting: identification of the relevant clinical trials
Poster: 1443P, Location: Hall E

Rolapitant is marketed in the United States under trade name VARUBI. Rolapitant has not been approved by any regulatory agencies outside of the United States.

Investor Briefing and Webcast
TESARO will webcast an investor and analyst briefing in Copenhagen on Saturday, October 8 at 7:00 PM local time in conjunction with the ESMO (Free ESMO Whitepaper) annual meeting. At this briefing, TESARO management will review the niraparib development program and data presented at ESMO (Free ESMO Whitepaper) and answer questions from investors and analysts. This event will be webcast live and archived for 30 days, and may be accessed from the TESARO Investor Events and Presentations webpage at www.tesarobio.com.

About Niraparib
Niraparib is an oral, once-daily PARP inhibitor that is currently being evaluated in four ongoing pivotal trials. TESARO is building a robust niraparib franchise by assessing activity across multiple tumor types and by evaluating several potential combinations of niraparib with other therapeutics. The ongoing development program for niraparib includes the Phase 3 trial in patients with recurrent ovarian cancer (the NOVA trial); a registrational Phase 2 treatment trial in patients with ovarian cancer (the QUADRA trial); a Phase 3 trial for the treatment of patients with BRCA-positive breast cancer (the BRAVO trial); and a Phase 3 trial in patients with first-line ovarian cancer (the PRIMA trial). Several collaborator-sponsored studies are also underway, including combination trials of niraparib plus pembrolizumab and bevacizumab. Janssen Biotech has licensed rights to develop and commercialize niraparib specifically for patients with prostate cancer worldwide, except in Japan.

About VARUBI (Rolapitant)
Rolapitant is marketed in the United States under trade name VARUBI. VARUBI is a substance P/neurokinin-1 (NK-1) receptor antagonist indicated in the U.S. in combination with other antiemetic agents in adults for the prevention of delayed nausea and vomiting associated with initial and repeat courses of emetogenic cancer chemotherapy, including, but not limited to, highly emetogenic chemotherapy. VARUBI is contraindicated in patients receiving thioridazine, a CYP2D6 substrate. The inhibitory effect of a single dose of VARUBI on CYP2D6 lasts at least seven days and may last longer. Avoid use of pimozide; monitor for adverse events if concomitant use with other CYP2D6 substrates with a narrow therapeutic index cannot be avoided. Please see full prescribing information, including additional important safety information, available at www.varubirx.com.

An intravenous formulation of rolapitant is also being developed. TESARO licensed exclusive rights for the development, manufacture, commercialization, and distribution of VARUBI (rolapitant) from OPKO Health, Inc.

On September 6, 2016 Infinity Pharmaceuticals, Inc. (NASDAQ: INFI) reported that new preclinical data as well as early clinical data from an ongoing Phase 1 study will be presented for IPI-549, an immuno-oncology development candidate that selectively inhibits PI3K-gamma, during the Second CRI-CIMT-EATI-AACR International Cancer Immunotherapy Conference (CIMT) (Free CIMT Whitepaper): Translating Science into Survival taking place September 25-28, 2016, in New York City (Press release, Infinity Pharmaceuticals, SEP 6, 2016, View Source;p=RssLanding&cat=news&id=2199662 [SID:1234514950]).

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The following two presentations will take place during the poster session being held on Monday, September 26, from 5:15 p.m. – 7:45 p.m. ET:

Title: IPI-549-01: A Phase 1/1b first-in-human study of IPI-549, a PI3K-gamma inhibitor, as monotherapy and in combination with an anti-PD1 antibody in subjects with advanced solid tumors
Poster Board: B070
Presentation Time: Monday, September 26, 6:15 p.m. – 7:15 p.m. ET

Title: The PI3K-gamma inhibitor, IPI-549, increases antitumor immunity by targeting tumor-associated myeloid cells and remodeling the immune-suppressive tumor microenvironment
Poster Board: B032
Presentation Time: Monday, September 26, 6:15 p.m. – 7:15 p.m. ET

About IPI-549
IPI-549 is an orally administered immuno-oncology development candidate that selectively inhibits PI3K-gamma. In preclinical studies, IPI-549 inhibits immune-suppressive macrophages within the tumor microenvironment, whereas other immunotherapies such as checkpoint modulators more directly target immune effector cell function. As such, IPI-549 may have the potential to treat a broad range of solid tumors and represents a potentially complementary approach to restoring anti-tumor immunity in combination with other immunotherapies such as checkpoint inhibitors.

IPI-549 is an investigational compound and its safety and efficacy has not been evaluated by the U.S. Food and Drug Administration or any other health authority.

On September 6, 2016 (GLOBE NEWSWIRE) Cyclacel Pharmaceuticals, Inc. (Nasdaq:CYCC) (Nasdaq:CYCCP) ("Cyclacel" or the "Company"), a biopharmaceutical company developing oral therapies that target various phases of cell cycle control for the treatment of cancer and other serious disorders, reported the presentation of preclinical data demonstrating that both Cyclacel’s CYC065, a clinical stage, second generation, cyclin-dependent kinase CDK2/9 inhibitor, and CCT68127, a preclinical stage CDK2/9 inhibitor, prolong survival in MYCN-addicted neuroblastoma models (Press release, Cyclacel, SEP 6, 2016, View Source [SID:1234514936]). The data were presented at the Childhood Cancer Meeting, September 5 — 7th in London, UK.

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"This study adds to the growing evidence of the value of CDK inhibition as an approach to treating cancer. MYCN is an important therapeutic target in oncology and a major oncogenic driver of neuroblastoma, a childhood cancer. There are no approved drugs that act against MYCN or MYC proteins," said Spiro Rombotis, President and Chief Executive Officer of Cyclacel. "We are encouraged by the preclinical data, which extend and support earlier findings, showing that CYC065 and CCT68127 reduce MYCN transcription and protein levels and have antitumor activity in neuroblastoma models. Additionally, we have demonstrated in other preclinical studies, that our transcriptional CDK2/9 inhibitors target key molecular features of cancers with poor prognosis, such as MLL-r leukemias or MYC-driven lymphomas. Furthermore, evidence from early clinical trials show that CDK2/9 inhibitors can have a synergistic effect with other anticancer agents. We look forward to reporting data from our ongoing Phase 1 study of CYC065 in patients with solid tumors."

In this preclinical study, an international group of researchers led by Prof. Louis Chesler from The Institute of Cancer Research, London, explored in vitro and in vivo the sensitivity of neuroblastoma cells to CYC065 and CCT68127. Neuroblastoma cells with MYCN amplification and overexpression were found to be particularly sensitive to both CDK2/9 inhibitors. The mechanism of action of CYC065 and CCT68127 included inhibition of MYCN transcription, downregulation of N-MYC protein, blocking neuroblastoma cell proliferation and induction of apoptosis. Treatment with either CYC065 or CCT68127 significantly reduced tumor burden and prolonged survival in several neuroblastoma models in vivo.

Citation

Poon E, Jamin Y, Walz S, Hakkert S, Kwok C, Hallsworth A, Thway K, Barker K, Sbirkov Y, Pickard L, Urban Z, Tardif N, Webber H, Box G, Valenti M, De Haven Brandon A, Petrie K, Ebus M, Molenaar J, Eccles S, Robinson SP, Zheleva D, Eilers M, Workman P, Chesler L. The small molecule CDK2 and CDK9 inhibitors CYC065 and CCT68127 are potent inhibitors of MYCN via transcriptional repression. Childhood Cancer Meeting 2016, September 5 — 7th, London, UK, Abs. 1-19.

About MYCN

The MYCN gene encodes a transcription factor that is expressed in fetal brain and neural crest and is critical for normal development of the brain and nerves. The MYCN oncogene is over-expressed in a number of different types of cancer, most notably neuroblastoma, and also rhabdomyosarcoma, medulloblastoma, astrocytoma, Wilms’ tumor and small cell lung cancer. Amplification of the MYCN oncogene is the most common genomic alteration in aggressive neuroblastomas and is associated with poor clinical outcome. There are no approved drugs that directly target MYCN prompting the investigation of indirect approaches such as exploitation of a synthetic lethal relationship between MYCN amplification/overexpression and inhibition of CDK2.

About Neuroblastoma

According to the American Cancer Society, neuroblastoma is the most common cancer in infants less than one year old and it accounts for about six percent of all pediatric cancers or about 700 cases per year. The disease has a fatal outcome in one out of every seven children diagnosed with it. Preclinical data from an international investigator group demonstrated that Cyclacel’s CYC065 and CCT68127 target MYCN gene expression and have potent in vitro and in vivo anti-tumor activities, suggesting therapeutic potential in neuroblastoma, including high-risk patients with MYCN amplification.

About CYC065

CYC065 is a highly-selective, orally- and intravenously-available, second generation inhibitor of CDK2 and CDK9 and causes apoptotic death of cancer cells at sub-micromolar concentrations. Antitumor efficacy has been achieved in vivo with once a day oral dosing at well tolerated doses. Evidence from published nonclinical studies show that CYC065 may benefit patients with adult and pediatric hematological malignancies, including certain Acute Myeloid Leukemias (AML), Acute Lymphocytic Leukemias (ALL), Chronic Lymphocytic Leukemias (CLL), B-cell lymphomas, multiple myelomas, and certain solid tumors, including breast and uterine cancers. Independent investigators published nonclinical evidence that CYC065 induced regression or tumor growth inhibition in a model of HER2-positive breast cancer addicted to cyclin E that is resistant to trastuzumab, reduced tumor growth in models of CCNE1-amplified uterine serous carcinoma and reduced tumor burden and prolonged survival in several neuroblastoma models in vivo.

CYC065 is mechanistically similar but has much higher dose potency, in vitro and in vivo, improved metabolic stability and longer patent protection than seliciclib, Cyclacel’s first generation CDK inhibitor. Translational biology data support development of CYC065 as a stratified medicine for solid and liquid cancers. CYC065 has been shown to reverse drug resistance associated with the addiction of cancer cells to cyclin E and may inhibit CDK9-dependent oncogenic and leukemogenic pathways, including malignancies driven by certain oncogenes and mixed lineage leukemia rearrangements (MLL-r). CYC065 causes prolonged down regulation of the Mcl-1-mediated pro-survival pathway in cancer cells.