Tuesday, May 22, 2018

Merck Data at ASCO 2018 to Showcase Progress and Further Optionality of Oncology Pipeline

          DARMSTADT, Germany--17 May--PRNewswire/InfoQuest

          Not intended for UK- or US-based media

          ASCO Abstract # ERBITUX(R) (cetuximab): 3521, 3534, e15711; avelumab: 9507, 9537, 9090, 9008, 8563, 3057, 4544, e21531, e13603, e18932, e21623, e21620, e21544; tepotinib (c-Met kinase inhibitor): 9082, 9016; M6620 (ATR inhibitor): 2549, e21048; M3814 (DNA-PK): 2518 M7824 (TGF-ss trap/anti-PD-L1): 3007, 9017, 2566; M2698 (dual p70S6k/Akt inhibitor): 2584

          - Two-year safety and efficacy data in mMCC for avelumab from pivotal JAVELIN Merkel 200 trial
          - Further data reinforcing commitment to precision medicine and position of ERBITUX(R) (cetuximab) as a standard of care in mCRC
          - Early clinical activity in advanced NSCLC and HPV-associated cancers for investigational bifunctional immunotherapy, M7824
          - Encouraging interim analysis of Phase II data in NSCLC sub-population for c-Met inhibitor, tepotinib
          - Record number of abstracts accepted across oncology, immuno-oncology and DNA Damage Response (DDR)

          Merck, a leading science and technology company, today announced new data from a number of high priority clinical development programs across its oncology portfolio to be presented at this year's American Society of Clinical Oncology Annual Meeting (ASCO), June 1-5, 2018, Chicago, IL. Abstracts representing seven therapeutic agents and eight tumor types will highlight Merck's position as a key emerging player in oncology.

          (Logo: http://photos.prnewswire.com/prnh/20151207/293543LOGO )

          "This year's data at ASCO demonstrate the potential of our pipeline to really deliver transformative advancements in cancer care," said Luciano Rossetti, Executive Vice President, Head of Global Research & Development at the biopharma business of Merck. "With our strong commitment and focus on the areas we believe in most, Merck's oncology and immuno-oncology pipeline is demonstrating significant potential in the near term with our later-stage priority programs and, in parallel, our early pipeline includes truly innovative programs that could make a real difference for patients."

          Data for the legacy brand ERBITUX(R) continue to build on Merck's heritage in oncology reinforcing its role as a standard of care in RAS wild-type metastatic colorectal cancer (mCRC), the standard of care in first-line recurrent or metastatic squamous cell carcinoma of the head and neck (R/M SCCHN), and a standard of care for patients with locally advanced SCCHN (LA SCCHN), who may not be able to tolerate cisplatin-based regimens in full.

          New data for avelumab* (BAVENCIO(R)), which is being jointly developed and commercialized with Pfizer, include an oral presentation on two-year results from the pivotal JAVELIN Merkel 200 trial. These long-term results include data on avelumab's duration of response and represent the first study to report long-term survival data for an immunotherapy in metastatic Merkel cell carcinoma (mMCC).

          The company will also present further evidence for M7824, an investigational TGF-ss trap/anti-PD-L1 bi-functional immunotherapy fusion protein, from expansion cohorts of the ongoing M7824 Phase I clinical trial (NCT02517398) program. TGF-?, a cytokine released by cells (including tumor cells), suppresses anti-tumor immune responses through a vast number of mechanisms leading to uninhibited tumor growth and metastasis. These data include results in patients with human papillomavirus (HPV)-associated cancers (presented in collaboration with the National Cancer Institute) and data in patients with advanced non-small cell lung cancer (NSCLC). In second-line (2L) NSCLC, signs of clinical activity were seen across PD-L1 expression levels. At the recommended Phase II dose, a confirmed overall response rate (ORR) of 40.7% (11/27) was observed in PD-L1+ patients (?1%), and in patients with high PD-L1 expression (80%; Ab clone 73-10 [>80%=>50% with 22C3]), the ORR was 71.4% (5/7). These data signal the potential of M7824 and provide evidence that combining a transforming growth factor-? (TGF-?) trap with the anti-PD-L1 mechanism in one molecule may generate anti-tumor activity in these patient groups with significant medical need. Treatment with M7824 was well tolerated in both studies and safety data were consistent with that observed in the overall Phase I clinical program. No new safety signals were identified.

          For tepotinib**, an investigational highly selective small molecule inhibitor of the c-Met receptor tyrosine kinase, new data to be presented include promising initial results from an ongoing Phase II VISION study providing further indication for the potential of tepotinib in patients living with advanced NSCLC harboring MET exon 14 skipping mutations. Alterations of the c-Met signaling pathway are found in various cancer types and correlate with aggressive tumor behavior and poor clinical prognosis. Based on investigator assessment of data from 15 patients in the study, 60% (9/15) had a confirmed partial response (PR) and 20% (3/15) had stable disease (SD). In addition, independent assessment of 13 patients demonstrated treatment with tepotinib led to a confirmed PR in 46.2% (6/13) and SD in 7.7% (1/13) of patients. In this study, the safety data are consistent with that observed in previous studies and confirm that treatment with tepotinib is well tolerated; no new safety signals were identified.

          Tepotinib is an important part of Merck's strategic focus on precision medicines and these results reinforce the company's progress in delivering treatments to those patients more likely to benefit, in order to achieve the best possible outcomes. Both M7824 and tepotinib were discovered in-house at Merck.

          Further pipeline updates include Phase I dose escalation data for the investigational DNA-dependent protein kinase (DNA-PK) inhibitor M3814, Phase I triplet therapy with ATR-inhibitor, M6620 +veliparib+cisplatin in advanced solid tumors, and Phase I data for M2698, a potent and selective dual inhibitor of p70S6K and AKT1/3 in the PAM pathway (PI3K/AKT/mTOR pathway). The PAM pathway regulates cell survival and growth and this pathway often displays unusual activity in many human cancers.

          *Avelumab is under clinical investigation for treatment of NSCLC, metastatic urothelial carcinoma (mUC) and mesothelioma and has not been demonstrated to be safe and effective for these indications. There is no guarantee that avelumab will be approved for NSCLC, mUC and mesothelioma by any health authority worldwide.

          **Tepotinib is the recommended International Nonproprietary Name (INN) for the c-Met kinase inhibitor (MSC2156119J). Tepotinib is currently under clinical investigation and not approved for any use anywhere in the world.

          Tepotinib, M7824, M3814, M2698 and M6620 are under clinical investigation and have not been proven to be safe and effective. There is no guarantee any product will be approved in the sought-after indication by any health authority worldwide.

          Notes to Editors

          Accepted Merck-supported key abstracts slated for presentation are listed below. In addition, a number of investigator-sponsored studies have been accepted (not listed).

                                                       Presentation

                                                       Date / Time

    Title                 Lead Author     Abstract #   (CDT)             Location

    Erbitux (cetuximab)

    Poster Sessions

    Impact of primary

    tumor side on

    outcomes of

    every-2-weeks

    (q2w) cetuximab +

    first-line FOLFOX

    or FOLFIRI in

    patients with RAS

    wild-type (wt)

    metastatic

    colorectal cancer

    (mCRC) in the         Timothy Jay                  Sun, Jun 03,

    phase 2 APEC          Price, MBBS,                 8:00 AM - 11:30

    trial.                FRACP, D.H.Sc   3534         AM                Hall A

    Final overall

    survival (OS)

    analysis of

    first-line (1L)

    FOLFOX-4 plus or

    minus cetuximab

    (cet) in patients

    (pts) with RAS

    wild-type (wt)

    metastatic

    colorectal cancer

    (mCRC) in the                                      Sun, Jun 03,

    phase 3 TAILOR        Shukui Qin,                  8:00 AM - 11:30

    trial.                MD, BA          3521         AM                Hall A

    Publication

    Cost-effectiveness

    (CE) of FOLFIRI

    (F) + cetuximab vs

    F + bevacizumab in

    the first-line

    treatment of RAS

    wild-type (wt)

    metastatic

    colorectal cancer

    (mCRC) in Germany:    Stintzing S,

    data from the         van Oostrum

    FIRE-3 (AIO           I, Pescott

    KRK-0306) study       CP, et al.      e15711

                                                       Presentation

                                                       Date / Time

    Title                 Lead Author     Abstract #   (CDT)             Location

    Avelumab

    Oral Presentations

    Two-year efficacy

    and safety update

    from JAVELIN

    Merkel 200 part A:

    A registrational

    study of avelumab

    in metastatic

    Merkel cell

    carcinoma                                          Mon, Jun 04,

    progressed on         Paul Nghiem,                 10:12 AM -        Arie Crown

    chemotherapy.         MD, PhD         9507         10:24 AM          Theater

    Avelumab

    (anti-PD-L1) in

    combination with

    crizotinib or

    lorlatinib in

    patients with

    previously treated

    advanced NSCLC:

    Phase 1b results                                   Fri, Jun 01,

    from JAVELIN Lung     Alice Tsang                  4:30 PM - 4:42

    101.                  Shaw, MD, PhD   9008         PM                Hall D1

    Poster Sessions

    Avelumab

    (anti-PD-L1) in

    patients with

    platinum-treated

    advanced NSCLC:

    2.5-year follow-up                                 Sun, Jun 03,

    from the JAVELIN      Arun Rajan,                  8:00 AM - 11:30

    Solid Tumor trial.    MD              9090         AM                Hall A

    Phase 1b study of

    avelumab in

    advanced

    previously treated

    mesothelioma:

    long-term

    follow-up from                                     Sun, Jun 03,

    JAVELIN Solid         Raffit                       8:00 AM - 11:30

    Tumor.                Hassan, MD      8563         AM                Hall A

    Second-line

    avelumab treatment

    of patients (pts)

    with metastatic

    Merkel cell

    carcinoma (mMCC):

    Experience from a

    global expanded       John WT                      Mon, Jun 04,

    access program        Walker, MD,                  1:15 PM - 4:45

    (EAP).                PhD             9537         PM                Hall A

    Association of

    efficacy and

    adverse events of     Karen Kelly,

    special interest      MD, FASCO

    of avelumab in the

    JAVELIN solid                                      Mon, Jun 04,

    tumor and JAVELIN                                  8:00 AM - 11:30

    Merkel 200 trials.                    3057         AM                Hall A

    SPEAR-bladder

    (study informing

    treatment pathway

    decision in

    bladder cancer):

    First- through

    third-line time to                                 Sat, Jun 02,

    treatment failure     Gurjyot K.                   8:00 AM - 11:30

    in the US.            Doshi, MD       4544         AM                Hall A

    Publication

    Avelumab in

    patients with

    previously treated

    metastatic

    melanoma: phase 1b    Keilholz U,

    results from the      Mehnert J,

    JAVELIN Solid         Bauer S, et

    Tumor trial           al.             e21531

    Characteristics,

    treatment patterns

    and safety events

    from 4 cohorts of

    advanced or

    metastatic cancer     Russo L,

    patients based on     Esposito D,

    healthcare claims     Lamy FX, et

    data                  al.             e13603

    Healthcare

    resource use and

    expenditures among

    patients with         Kearney M,

    Merkel cell           Thokagevistk

    carcinoma by level    K, Boutmy E,

    of comorbidity        et al.          e18932

    Projecting

    long-term survival

    for avelumab in       Phatak H,

    patients with         Proskorovsky

    refractory Merkel     I, Lanitis T,

    cell carcinoma        et al.          e21623

    Predicting overall

    survival in

    patients (Pts)

    with

    treatment-naive

    metastatic Merkel     Bullement A,

    Cell carcinoma        D'Angelo SP,

    (mMCC) treated        Amin A, et

    with avelumab         al.             e21620

    A novel,

    open-access data

    commons for

    improved disease      Murphy M,

    management in         Sartor O,

    Merkel cell           Bertagnolli

    carcinoma patients    M, et al.       e21544

                                                       Presentation

                                                       Date / Time

    Title                 Lead Author     Abstract #   (CDT)           Location

    M7824 (beta-trap)

    Oral Presentation

    Safety and

    activity of M7824,

    a bifunctional

    fusion protein

    targeting PD-L1

    and TGF-beta, in

    patients with HPV                                  Sat, Jun 02,

    associated            Julius                       5:12 PM - 5:24

    cancers.              Strauss, MD     3007         PM              Hall B1

    Poster Discussion

    Results from a

    second-line (2L)

    NSCLC cohort

    treated with M7824

    (MSB0011359C), a

    bifunctional

    fusion protein        Luis G.                      Sun, Jun 03,

    targeting TGF-beta    Paz-Ares, MD,                11:30 AM -      Arie Crown

    and PD-L1.            PhD             9017         12:45 PM        Theater

    Poster Session

    Selection of the

    recommended phase

    2 dose (RP2D) for

    M7824

    (MSB0011359C), a

    bifunctional

    fusion protein        Yulia                        Mon, Jun 04,

    targeting TGF-beta    Vugmeyster,                  8:00 AM - 11:30

    and PD-L1.            PhD             2566         AM              Hall A

                                                       Presentation

                                                       Date / Time

    Title                 Lead Author     Abstract #   (CDT)           Location

    Tepotinib

    Poster Discussion

    Tepotinib in

    patients with

    advanced non-small

    cell lung cancer

    (NSCLC) harboring

    MET exon

    14-skipping                                        Sun, Jun 03,

    mutations: Phase      Enriqueta                    11:30 AM -      Arie Crown

    II trial.             Felip, MD       9016         12:45 PM        Theatre

    Poster Session

    Can duration of

    response be used

    as a surrogate

    endpoint for

    overall survival

    in advanced                                        Sun, Jun 03,

    non-small cell        Boris M                      8:00 AM - 11:30

    lung cancer?          Pfeiffer        9082         AM              Hall A

                                                       Presentation

                                                       Date / Time

    Title                 Lead Author     Abstract #   (CDT)           Location

    M2698

    Poster Session

    Precision

    oncology: Results

    of a phase I study

    of M2698, a

    p70S6K/AKT

    targeted agent in

    patients with

    advanced cancer

    and tumor             Apostolia

    PI3K/AKT/mTOR         Maria                        Mon, Jun 04,

    (PAM) pathway         Tsimberidou,                 8:00 AM - 11:30

    abnormalities.        MD, PhD         2584         AM              Hall A

                                                       Presentation

                                                       Date / Time

    Title                 Lead Author     Abstract #   (CDT)           Location

    M3814

    Poster Discussion

    A phase Ia/Ib

    trial of the

    DNA-PK inhibitor

    M3814 in

    combination with

    radiotherapy (RT)

    in patients (pts)

    with advanced

    solid tumors:         Baukelien Van                Mon, Jun 04,

    Dose-escalation       Triest, MD,                  3:00 PM - 4:15

    results.              PhD              2518        PM               S406

    Title                  Lead Author     Abstract #   Presentation
                                                        Date / Time
                                                        (CDT)           Location

             M6620

    Poster Discussion
    Phase I trial of the
    triplet M6620
    (formerly VX970) +
    veliparib + cisplatin  Geraldine                    Mon, Jun 04,
    in patients with       Helen O'Sullivan             8:00 AM -
    advanced solid tumors. Coyne, MD,PhD    2549        11:30 AM        Hall A
         

             Publication 

    Safety and tolerability
    of intravenous M6620
    (VX?970) administered
    with gemcitabine in     Plummer R,
    subjects with advanced  Cook N,                     Mon, Jun 04,
    non-small cell lung     Arkenau H-T,                8:00 AM -
    cancer (NSCLC)          et al.          e21048      11:30 AM        Hall A
       
          All Merck Press Releases are distributed by e-mail at the same time they become available on the Merck Website. Please go to http://www.merckgroup.com/subscribe to register online, change your selection or discontinue this service.

          About Avelumab

          Avelumab is a human anti-programmed death ligand-1 (PD-L1) antibody. Avelumab has been shown in preclinical models to engage both the adaptive and innate immune functions. By blocking the interaction of PD-L1 with PD-1 receptors, avelumab has been shown to release the suppression of the T cell-mediated antitumor immune response in preclinical models. Avelumab has also been shown to induce NK cell-mediated direct tumor cell lysis via antibody-dependent cell-mediated cytotoxicity (ADCC) in vitro In November 2014, Merck and Pfizer announced a strategic alliance to co-develop and co-commercialize avelumab.

          Approved Indications in the US

          The FDA granted accelerated approval for avelumab (BAVENCIO(R)) for the treatment of (i) adults and pediatric patients 12 years and older with metastatic Merkel cell carcinoma (mMCC) and (ii) patients with locally advanced or metastatic urothelial carcinoma (mUC) who have disease progression during or following platinum-containing chemotherapy, or have disease progression within 12 months of neoadjuvant or adjuvant treatment with platinum-containing chemotherapy. These indications are approved under accelerated approval based on tumor response rate and duration of response. Continued approval for these indications may be contingent upon verification and description of clinical benefit in confirmatory trials.

          Important Safety Information from the US FDA Approved Label

          The warnings and precautions for BAVENCIO include immune-mediated adverse reactions (such as pneumonitis, hepatitis, colitis, endocrinopathies, nephritis and renal dysfunction, and other adverse reactions), infusion-related reactions and embryo-fetal toxicity.

          Common adverse reactions (reported in at least 20% of patients) in patients treated with BAVENCIO for mMCC and patients with locally advanced or mUC include fatigue, musculoskeletal pain, diarrhea, nausea, infusion-related reaction, peripheral edema, decreased appetite/hypophagia, urinary tract infection and rash.

          About Erbitux(R) (cetuximab)

          Erbitux(R) is a highly active IgG1 monoclonal antibody targeting the epidermal growth factor receptor (EGFR). As a monoclonal antibody, the mode of action of Erbitux is distinct from standard non-selective chemotherapy treatments in that it specifically targets and binds to the EGFR. This binding inhibits the activation of the receptor and the subsequent signal-transduction pathway, which results in reducing both the invasion of normal tissues by tumor cells and the spread of tumors to new sites. It is also believed to inhibit the ability of tumor cells to repair the damage caused by chemotherapy and radiotherapy and to inhibit the formation of new blood vessels inside tumors, which appears to lead to an overall suppression of tumor growth. Erbitux also targets cytotoxic immune effector cells towards EGFR expressing tumor cells (antibody dependent cell-mediated cytotoxicity, ADCC).

          The most commonly reported side effect with Erbitux is an acne-like skin rash. In approximately 5% of patients, hypersensitivity reactions may occur during treatment with Erbitux; about half of these reactions are severe.

          Erbitux has already obtained market authorization in over 100 countries world-wide for the treatment of RAS wild-type metastatic colorectal cancer and for the treatment of squamous cell carcinoma of the head and neck (SCCHN). Merck licensed the right to market Erbitux, a registered trademark of ImClone LLC, outside the U.S. and Canada from ImClone LLC, a wholly-owned subsidiary of Eli Lilly and Company, in 1998.

          About M3814

          M3814 is an investigational small-molecule which is thought to inhibit DNA-dependent protein kinase (DNA-PK). DNA-PK is a key enzyme for non-homologous end-joining (NHEJ), an important DNA double strand break (DSB) repair pathway. Clinical studies investigating combinations of M3814 with other commonly used DNA-damaging agents such as radiotherapy and chemotherapy are underway.

          About M7824

          M7824 is an investigational bifunctional immunotherapy that is designed to bring together a TGF-? trap and 'fuse' it with the anti-PD-L1 mechanism. M7824 is designed to simultaneously block the two immunosuppressive pathways - targeting both pathways aims to control tumor growth by potentially restoring and enhancing anti-tumor responses. M7824 is currently in Phase I studies for solid tumors.

          About M2698

          M2698 is an investigational small-molecule which is thought to inhibit p70S6K and Akt. Both targets are part of the PI3K/AKT/mTOR (PAM)pathway, which is often dysregulated in solid tumors.

          About tepotinib

          Tepotinib (MSC2156119J) is an investigational small-molecule inhibitor of the c-Met receptor tyrosine kinase. Alterations of the c-Met signaling pathway are found in various cancer types and it is thought to correlate with aggressive tumor behavior and poor clinical prognosis.

          About M6620

          M6620 (previously known as VX-970) is an investigational small-molecule thought to inhibit ataxia telangiectasia and Rad3-related protein (ATR). ATR is believed to be a key sensor for DNA damage, activating the DNA damage checkpoint and leading to cell cycle arrest. Inhibition of ATR could potentially enhance the efficacy of DNA-damaging agents, but is also being investigated as a monotherapy against tumors with high levels of replication stress induced by overexpression of oncogenes.

          About Merck

          Merck is a leading science and technology company in healthcare, life science and performance materials. Almost 53,000 employees work to further develop technologies that improve and enhance life - from biopharmaceutical therapies to treat cancer or multiple sclerosis, cutting-edge systems for scientific research and production, to liquid crystals for smartphones and LCD televisions. In 2017, Merck generated sales of EUR 15.3 billion in 66 countries.

          Founded in 1668, Merck is the world's oldest pharmaceutical and chemical company. The founding family remains the majority owner of the publicly listed corporate group. Merck holds the global rights to the Merck name and brand. The only exceptions are the United States and Canada, where the company operates as EMD Serono, MilliporeSigma and EMD Performance Materials.

          Contact: Gangolf Schrimpf, +49-6151-72-9591

          Investor relations: +49-6151-72-3321

          Source: Merck KGaA

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