Constellation Pharmaceuticals Announces First Patient Dosed in Phase 1b/2 PROSTAR Combination Study of CPI-1205 in Advanced Form of Prostate Cancer

On December 12, 2017 Constellation Pharmaceuticals, Inc., a clinical-stage biopharmaceutical company developing tumor-targeted and immuno-oncology therapies based on its pioneering research in cancer epigenetics, reported that the first patient has been dosed in its Phase 1b/2 PROSTAR study of CPI-1205, a small-molecule inhibitor of EZH2, combined with enzalutamide or abiraterone/prednisone in patients with metastatic castration-resistant prostate cancer (mCRPC) (Press release, Constellation Pharmaceuticals, DEC 12, 2017, View Source [SID1234522670]).

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"The initiation of this combination study marks a significant milestone for the company as we execute on our goal to rapidly advance our pipeline of epigenetic therapeutics that have the potential to address difficult-to-treat cancers," said Adrian Senderowicz, M.D., senior vice president and chief medical officer of Constellation Pharmaceuticals. "Today’s announcement marks the first evaluation of CPI-1205 in solid tumors. We anticipate advancing CPI-1205 and other therapies from our EZH2 portfolio in additional solid tumor clinical trials in the future."

CPI-1205 is a potent, highly selective, first-generation small-molecule inhibitor of EZH2, a clinically-validated target in cancer. In multiple types of cancer, including mCRPC, EZH2 contributes to drug resistance over time by enhancing pro-tumor pathways, such as androgen receptor signaling. CPI-1205 has shown single-agent activity and synergistic activity with small-molecule androgen inhibitors in preclinical studies. CPI-1205 has also demonstrated single-agent clinical activity and a dose-dependent increase in exposure correlated to pharmacodynamic biomarkers during a clinical trial of CPI-1205 in selected lymphoma patients.

"There is a tremendous need for new, safe and effective medicines for advanced prostate cancer, especially for men with progressive mCRPC," said Mary-Ellen Taplin, M.D., Dana-Farber Cancer Institute and an investigator in the trial. "We look forward to learning how CPI-1205 may help overcome resistance mechanisms in mCRPC and extend response to therapy."

The Phase 1b portion of the PROSTAR study is designed to assess safety, pharmacokinetics, pharmacodynamics, as well as a recommended Phase 2 dose (RP2D) of CPI-1205 in combination with either enzalutamide (marketed as Xtandi by Astellas and Pfizer) or abiraterone acetate (marketed as Zytiga by Janssen), which are FDA-approved second-generation androgen inhibitors. The Phase 2 portion of the PROSTAR study will assess clinical activity and potential biomarkers to identify patient populations with higher clinical anti-tumor activity to CPI-1205.

About mCRPC

mCRPC is an advanced form of prostate cancer and is defined by disease progression despite treatment with androgen depletion therapy (ADT). mCRPC may present as one, or any combination of, a continuous rise in serum levels of prostate-specific antigen (PSA), progression of known metastases, or appearance of new metastases. Prognosis is associated with several factors, including the ability to perform certain daily activities and the presence of bone pain. Additional symptoms commonly include anemia (low healthy red blood cell levels), weight loss, fatigue, hypercoagulability (abnormal blood coagulation) and increased susceptibility to infection. mCRPC presents as a spectrum of disease ranging from patients without symptoms but rising PSA levels despite ADT, to patients with metastases and significant debilitation.

About CPI-1205

CPI-1205 is a therapeutic candidate from Constellation Pharmaceuticals’ EZH2 portfolio and is an inhibitor of Enhancer of Zeste Homolog 2 (EZH2). The function of EZH2 is to selectively suppress gene expression of several pro-cancer pathways that contribute to drug resistance.

Geron Reports Imetelstat Presentations at American Society of Hematology Annual Meeting

On December 12, 2017 Geron Corporation (Nasdaq:GERN) reported four presentations related to imetelstat at the 59th American Society of Hematology (ASH) (Free ASH Whitepaper) Annual Meeting and Exposition held in Atlanta, Georgia from December 9-12, 2017 (Press release, Geron, DEC 12, 2017, View Source;p=RssLanding&cat=news&id=2322273 [SID1234522575]). Imetelstat is a telomerase inhibitor initially developed by Geron and exclusively licensed to Janssen Biotech, Inc. (Janssen) on a worldwide basis. The presentations are available on Geron’s website at www.geron.com/presentations.

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"We and our partner are pleased to have this first presentation of data from IMerge displaying an 8-week transfusion independence rate of 54% among the subset of patients who were naïve to lenalidomide and HMAs and who lacked del(5q), which suggests that imetelstat could offer lower risk MDS patients a much-needed treatment option," said John A. Scarlett, M.D., Geron’s President and Chief Executive Officer. "In addition, the non-clinical data presentations continue to support the potential use of imetelstat in multiple hematologic malignancies. We continue to be encouraged by the consistent interest in imetelstat by collaborators around the world."

Clinical Data Presentation

Title: Efficacy and Safety of Imetelstat in RBC Transfusion-Dependent (TD) IPSS Low/Int-1 MDS Relapsed/Refractory to Erythropoiesis-Stimulating Agents (ESA) (IMerge) (Abstract #4256)

This poster presentation described data from the first 32 patients enrolled in Part 1 of IMerge, the ongoing Phase 2/3 clinical trial of imetelstat in red blood cell (RBC) transfusion-dependent (TD) patients with lower risk MDS. TD is defined as an RBC transfusion requirement of ≥4 units over 8 weeks prior to entry into the trial. The primary efficacy endpoint is the rate of RBC transfusion-independence (TI) lasting at least 8 weeks, defined as the proportion of patients without any RBC transfusion during any consecutive 8 weeks since entry to the trial. Key secondary endpoints are the rate of 24-week TI and the rate of hematologic improvement-erythroid (HI-E), defined as a rise in hemoglobin of at least 1.5 g/dL above the pretreatment level for at least 8 weeks or a reduction of at least 4 units of RBC transfusions over 8 weeks compared with the prior RBC transfusion burden. IMerge is designed in two parts: Part 1 is a Phase 2, open-label, single-arm trial of imetelstat administered as a single agent by intravenous infusion, and Part 2 is designed to be a Phase 3, randomized, controlled trial.

Data as of October 2017 with a median follow-up of 66.1 weeks in Part 1 were presented. Part 2 has not yet begun.

Efficacy in the Overall Trial Population (n=32):

38% (12/32) of patients achieved ≥8-week RBC TI
Mean relative reduction in transfusion burden from baseline was 64%
16% (5/32) of patients achieved ≥24-week RBC TI, with the median TI duration exceeding one year in these patients
63% (20/32) of patients achieved an erythroid hematologic improvement (HI-E)
Efficacy in the Lenalidomide and HMA Naïve and Non-Del(5q) Subset (n=13):

54% (7/13) of patients achieved ≥8-week RBC TI
Mean relative reduction in transfusion burden from baseline was 71%
31% (4/13) of patients achieved ≥24-week RBC TI
69% (9/13) of patients achieved an HI-E
Safety Summary:

Cytopenias, particularly neutropenia and thrombocytopenia, were the most frequently reported adverse events which were predictable, manageable and reversible
Link to IMerge poster: Fenaux P, et al. ASH (Free ASH Whitepaper) 2017

Based on these data, Part 1 of IMerge is being expanded to enroll approximately 20 additional patients who are naïve to lenalidomide and HMA treatment and are non-del(5q) to increase the experience and confirm the benefit-risk profile of imetelstat in this refined target patient population. For more information about IMerge, please visit View Source

Non-Clinical Data Presentations

Data were presented from three non-clinical studies by academic scientists in collaboration with Janssen.

Title: Imetelstat, a Telomerase Inhibitor, Is Capable of Depleting Myelofibrosis Hematopoietic Stem Cells and Progenitor Cells (Abstract #1654)

This poster presentation described the effects of imetelstat on normal and myelofibrosis (MF) stem and progenitor cells in non-clinical models. The data showed that imetelstat inhibited the proliferation and differentiation of MF progenitor and stem cells in hematopoietic colony assays and xenograft models, but had minimal effects on normal hematopoietic stem and progenitor cells in such experiments. Imetelstat treatment of MF stem and progenitor cells reduced telomerase activity and induced apoptosis. These data provide further support that imetelstat may selectively inhibit the proliferation of and promote apoptosis in MF progenitor and stem cells, suppressing the malignant clones that drive the disease in patients.

Title: Telomerase Inhibition Impairs Self-Renewal of b-Catenin Activated Myeloproliferative Neoplasm Progenitors (Abstract #2860)

This poster presentation described the potential impact of imetelstat on leukemia stem cells in non-clinical models of chronic myeloid leukemia (CML) in blast crisis. The data suggest that imetelstat plus dasatinib, a standard treatment for CML, may inhibit self-renewal of blast crisis cells in vitro compared with normal bone marrow progenitors. In mouse xenograft models of blast crisis CML, imetelstat treatment reduced the number of leukemia progenitor cells detected in bone marrow and spleen, decreased spleen size, inhibited the self-renewal capacity and prolonged survival compared to controls. These data suggest that imetelstat may inhibit proliferation of malignant progenitors in CML.

Title: Integrated Molecular Analysis Identifies Replicative Stress as Sensitizer to Imetelstat Therapy in AML (Abstract #798)

This oral presentation described imetelstat’s activity in human acute myeloid leukemia (AML) patient-derived xenograft models. The preclinical data demonstrated that imetelstat prolonged overall survival of AML xenografts derived from 17 out of 30 individual patient samples compared to saline-treated controls. Molecular analysis showed that sustained responders were associated with gene signatures of replicative stress at baseline. The data also suggest that inducing replicative stress with standard induction chemotherapy may sensitize poorly responding samples to imetelstat. These data build on previously published preclinical work and further support potential application of imetelstat in the treatment of AML.

Webcast Investor Event

Management will be hosting a live webcast of an analyst and investor meeting on December 19, 2017 at 8:30 a.m. ET to discuss the imetelstat clinical data in MDS presented at ASH (Free ASH Whitepaper). The audio and slide presentation webcast will be accessible at www.geron.com on the Investor Relations pages, under Events. Following the live presentation, the webcast will be archived and available for replay at the same address for a period of 30 days.

About Imetelstat

Imetelstat (GRN163L; JNJ-63935937) is a potent and specific inhibitor of telomerase that is administered by intravenous infusion. This first-in-class compound, discovered by Geron, is a specially designed and modified short oligonucleotide, which targets and binds directly with high affinity to the active site of telomerase. Preliminary clinical data suggest imetelstat might have disease-modifying activity by inhibiting the progenitor cells of the malignant clones associated with hematologic malignancies in a relatively select manner. Most commonly reported adverse events in imetelstat clinical studies include fatigue, gastrointestinal symptoms and cytopenias. Imetelstat has not been approved for marketing by any regulatory authority.

About the Collaboration with Janssen

On November 13, 2014, Geron entered into an exclusive worldwide license and collaboration agreement with Janssen Biotech, Inc., to develop and commercialize imetelstat for oncology, including hematologic myeloid malignancies, and all other human therapeutics uses. Under the terms of the agreement, Geron received an upfront payment of $35 million and is eligible to receive additional payments up to a potential total of $900 million for the achievement of development, regulatory and commercial milestones, as well as royalties on worldwide net sales. All regulatory, development, manufacturing and promotional activities related to imetelstat are being managed through a joint governance structure, with Janssen responsible for these activities.

GlycoMimetics Reports Improvements in Median Overall Survival Versus Historical Matched Controls for Two AML Patient Subgroups in Phase 1/2 Trial for GMI-1271

On December 12, 2017 GlycoMimetics, Inc. (NASDAQ: GLYC) reported updated data from the Phase 1/2 trial evaluating the safety, tolerability and efficacy of GMI-1271 in patients with relapsed/refractory (R/R) acute myeloid leukemia (AML) and in older adults with newly diagnosed AML, including the following conclusions (Press release, GlycoMimetics, DEC 12, 2017, View Source [SID1234522581]):

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For patients with R/R AML treated at the Phase 2 dose (n = 54) and for whom median follow up was 6.6 months:

Clinical remission (CR+CRi) was 43%.
Median overall survival was 9.4 months (95% CI: 5.7 – 15.1 months; calculated by Kaplan Meier method). This compares favorably to a median overall survival of up to 5.4 months reported for historical, matched controls treated with mitoxantrone, etoposide and cytarabine (MEC) alone. 1,2
Median duration of remission was 11.1 months (95% CI: 5.8-NA; calculated by Kaplan Meier method).
For older patients with newly diagnosed disease (n=25) and for whom median follow up was 10.5 months:

Clinical remission rate was 68%.
Median overall survival was 15.8 months (95% CI: 10.3 – NA; calculated by Kaplan Meier method). This compares favorably to a historical median overall survival of approximately 12 months in matched controls treated with 7+3 chemotherapy alone. 3,4
Median duration of remission was 14.8 months (95% CI: 8.3 – NA; calculated by Kaplan Meier method).
Median event free survival was 11.3 months.
The data were presented yesterday during an oral scientific session at the 59th American Society of Hematology (ASH) (Free ASH Whitepaper) Annual Meeting and Expo in Atlanta.

Across both populations, GMI-1271 was well tolerated with no obvious incremental toxicity observed and lower than expected rates of severe, debilitating, grade 3-4 mucositis reported (e.g., 3% incidence reported vs. historical 20-25% incidence with MEC alone).

"These new data from our Phase 1/2 clinical trial demonstrate that encouraging clinical outcomes are possible for both duration of remission and survival endpoints when GMI-1271 is added to chemotherapy in two distinct AML patient populations," noted Helen Thackray, M.D., FAAP, GlycoMimetics Senior Vice-President, Clinical Development and Chief Medical Officer. "Beyond the high response rates previously reported with GMI-1271, we can now point to additional long-term endpoints that further support our plan to move the drug candidate into a Phase 3 clinical trial scheduled to begin in mid-2018. Importantly, with respect to safety, the low mucositis rate in relapsed and refractory patients receiving MEC induction chemotherapy — where you would expect around 25% severe mucositis — is quite striking. This was predicted and explained by preclinical models in which GMI-1271 blocked inflammatory macrophages trafficking to the gut and thus prevented mucosal injury."

"These results continue to show that AML patients treated with GMI-1271 consistently perform better than expected," said Daniel J. DeAngelo, M.D., Ph.D., the trial’s lead investigator and Director of Clinical and Translational Research, Adult Leukemia Program, at the Dana-Farber Cancer Institute and Brigham and Women’s Hospital, who presented the data at the ASH (Free ASH Whitepaper) Annual Meeting. "Our Phase 2 population consists of very high-risk patients based on age, disease status, and cytogenetic risk factors. The updated data continue to support the concept that disrupting the relationship between leukemic cells and the protective bone marrow microenvironment, when combined with chemotherapy, could improve the outlook and prognosis for these patients."

The second oral presentation at the ASH (Free ASH Whitepaper) meeting highlighted a preclinical study in murine models of AML in which E-selectin was shown to be upregulated, and AML cells binding to E-selectin increased chemo-resistance by activating specific tumor cell survival signaling pathways. This effect within the bone marrow microenvironment is unique to E-selectin as compared to other vascular adhesion molecules and can be blocked by GMI-1271. This translational research provides important evidence that elucidates how treatment with GMI-1271 appears to be improving sensitivity to chemotherapy.

"Given response rates we’ve observed to date that suggest clinical benefit in combination with chemotherapy in two AML populations, this preclinical work provides important further support for the mechanism of action of GMI-1271," noted Dr. Thackray. "Together, the clinical and preclinical data we have shared at the ASH (Free ASH Whitepaper) Annual Meeting demonstrate that GMI-1271 could represent a novel and truly differentiated approach to treatment of AML," Dr. Thackray concluded.

Meeting abstracts are available on ASH (Free ASH Whitepaper)’s website.

GlycoMimetics to Hold Post-ASH Meeting Briefing in Boston on December 19

GlycoMimetics will hold a briefing for investors/analysts, which will also be available via webcast, to review the GMI-1271 program with a focus on the AML clinical data presented at the ASH (Free ASH Whitepaper) Annual Meeting, at the Langham Hotel in Boston, December 19, at 7:30 a.m. EST. Dr. DeAngelo will present the clinical data from the ASH (Free ASH Whitepaper) oral presentation and respond to questions from on-site participants.

Myriad’s BRACAnalysis CDx® Test Effectively Identified Metastatic Breast Cancer Patients with Improved Outcomes from Pfizer’s PARP Inhibitor, Talazoparib

On December 12, 2017 Myriad Genetics, Inc. (NASDAQ:MYGN), a leader in molecular diagnostics and personalized medicine, reported that data from the EMBRACA trial showed Myriad’s BRACAnalysis CDx test successfully identified patients with metastatic breast cancer (MBC) who responded to Pfizer’s investigational PARP inhibitor, talazoparib (Press release, Myriad Genetics, DEC 12, 2017, View Source [SID1234522582]).

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The EMBRACA trial (NCT01945775) data were presented last week at the 2017 San Antonio Breast Cancer Symposium (SABCS). The study included approximately 400 patients, all of whom tested positive for germline BRCA mutations as determined by Myriad’s FDA-approved BRACAnalysis CDx test. As presented at SABCS, the results demonstrated that patients with gBRCA+ locally advanced and/or MBC demonstrated superior progression-free survival (PFS) in patients treated with talazoparib, compared to patients who received physician’s choice standard-of-care chemotherapy. Additionally, the PFS benefit was consistent across metastatic BRCA-positive patients, including those with hormone receptor-positive and triple negative disease.

"BRACAnalysis CDx is the only germline companion diagnostic test approved by the FDA to identify patients with BRCA1/2 mutations, and we are excited to support Pfizer’s clinical development program and help identify patients who are most likely to benefit from talazoparib," said Mark C. Capone, president and CEO, Myriad Genetics. "As the pioneers in companion diagnostics for PARP inhibitors, we are excited that more patients may benefit from these novel drugs in the future."

It is estimated there are approximately 60,000 patients with metastatic breast cancer, two thirds of whom are not currently eligible for BRCA testing based upon family and personal history alone or current testing criteria.

Myriad first announced its collaboration to develop a novel companion diagnostic test for talazoparib on Oct. 1, 2013. Under that agreement (originally with BioMarin; now Pfizer), Myriad plans to submit a supplementary premarket approval (sPMA) application to the U.S. Food and Drug Administration (FDA) under its existing PMA for BRACAnalysis CDx to include talazoparib.

About BRACAnalysis CDx
BRACAnalysis CDx is an in vitro diagnostic device intended for the qualitative detection and classification of variants in the protein coding regions and intron/exon boundaries of the BRCA1 and BRCA2 genes using genomic DNA obtained from whole blood specimens collected in EDTA. Single nucleotide variants and small insertions and deletions (indels) are identified by polymerase chain reaction (PCR) and Sanger sequencing. Large deletions and duplications in BRCA1 and BRCA2 are detected using multiplex PCR. Results of the test are used as an aid in identifying ovarian cancer patients with deleterious or suspected deleterious germline BRCA variants, who are or may become eligible for treatment with Lynparza (olaparib). Detection of deleterious or suspected deleterious germline BRCA variants by the BRACAnalysis CDx test in ovarian cancer patients is also associated with enhanced progression-free survival (PFS) from Zejula (niraparib)maintenance therapy. This assay is for professional use only and is to be performed only at Myriad Genetic Laboratories, a single laboratory site located at 320 Wakara Way, Salt Lake City, UT 84108. Learn more at: View Source

Arrowhead Pharmaceuticals Reports Fiscal 2017 Year End Results

On December 12, 2017 Arrowhead Pharmaceuticals, Inc. (NASDAQ: ARWR) reported financial results for its fiscal 2017 fourth quarter and year ended September 30, 2017 (Press release, Arrowhead Research Corporation, DEC 12, 2017, View Source [SID1234522592]). The company is hosting a conference call at 4:30 p.m. EST to discuss results.

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Conference Call and Webcast Details

Investors may access a live audio webcast on the Company’s website at View Source For analysts that wish to participate in the conference call, please dial 855-215-6159 or 315-625-6887 and provide Conference ID 6977547.

A replay of the webcast will be available on the company’s website approximately two hours after the conclusion of the call and will remain available for 90 days. An audio replay will also be available approximately two hours after the conclusion of the call and will be available for 3 days. To access the audio replay, dial 855-859-2056 or 404-537-3406 and provide Conference ID 6977547.

Selected Fiscal 2017 and Recent Events

Hosted an Analyst R&D Day in September 2017 to highlight the following:
The Targeted RNAi Molecule platform, or TRiM, which utilizes ligand-mediated delivery and is designed to enable tissue-specific targeting, while being structurally simple
The TRiM platform offers several potential competitive advantages including:
Simplified manufacturing at reduced cost
Multiple routes of administration (subcutaneous, intravenous, and inhaled)
Faster time to clinical candidates
Wide safety margins
Promise of taking RNAi to tissues beyond the liver
ARO-AAT, Arrowhead’s second generation subcutaneously administered clinical candidate for the treatment of alpha-1 antitrypsin deficiency liver disease with a planned Clinical Trial Application (CTA) filing in Q1 2018
ARO-HBV, Arrowhead’s third generation subcutaneously administered clinical candidate for the treatment of chronic hepatitis B virus infection with a planned CTA filing in Q2 2018
Arrowhead’s expanded cardiometabolic pipeline, which now includes ARO-APOC3, targeting apolipoprotein C-III, and ARO-ANG3, targeting angiopoietin-like protein 3 (ANGPTL3) with CTA filings planned around the end of 2018
The TRiM platform’s ability to target extra-hepatic tissues, including the lung and tumors, represented by the following programs:
ARO-Lung1, the first candidate against an undisclosed gene target in the lung, which achieved almost 90% target knockdown following inhaled administration in rodents
ARO-HIF2, Arrowhead’s candidate targeting renal cell carcinoma, which achieved 85% target gene knockdown in a rodent tumor model
CTA filings are planned in Q4 2018 and in 2019 for ARO-Lung1 and ARO-HIF2, respectively
Presented new clinical data at HEP DART 2017 demonstrating up to 5.0 log10 reduction in HBV s-antigen and a Sustained Host Response in 50% of hepatitis B patients following RNAi therapy, ARC-520, in the 2001 open label extension study
Made continued progress on our two-product cardiovascular collaboration with Amgen, in which one that was previously called ARO-LPA against the target lipoprotein(a) has been formally nominated as a clinical candidate and which is now referred to as AMG-890 by Amgen