Darmstadt, Germany, May 17, 2017 – Merck, KGaA, Darmstadt, Germany, a leading science and technology company, today announced that new research from its growing broad oncology portfolio, from immuno-oncology (IO) to DNA damage response (DDR) approaches, will be presented across a broad range of hard-to-treat cancers at this year’s American Society of Clinical Oncology annual meeting (ASCO; June 2-6, Chicago). Over 40 abstracts showcase the impact of Merck, KGaA, Darmstadt, Germany’s commitment to shaping cancer care today and tomorrow, including data for avelumab*, which is being developed in collaboration with Pfizer, Erbitux« (cetuximab), and pipeline updates on the anti-PD-L1/TGF-▀ trap M7824, the DNA-PK inhibitor M3814, the BTK inhibitor M7583, and the c-Met inhibitor tepotinib**. In the U.S. and Canada, Merck KGaA, Darmstadt, Germany, operates its biopharmaceutical business as EMD Serono.

“We are focused on delivering innovation that matters to patients, as shown in our ASCO data that spans across IO and DDR approaches to tackle some of the hardest-to-treat cancers,” said Luciano Rossetti, Executive Vice President, Head of Global Research & Development at the biopharma business of Merck, KGaA, Darmstadt, Germany. “Merck, KGaA, Darmstadt, Germany, was among the first to leverage the potential of the PD1/PDL1 pathway for patients, and we continue to build on that progress with our ASCO presence and the two recent FDA accelerated approvals for avelumab.”

Multiple avelumab presentations at ASCO include data in first-line metastatic Merkel cell carcinoma (mMCC) and previously treated metastatic urothelial carcinoma (UC), as well as results from the Phase Ib trial from the avelumab combination trial with axitinib in renal cell carcinoma (RCC). Recently, the U.S. Food and Drug Administration (FDA) granted accelerated approval*** for avelumab for the treatment of mMCC and pretreated patients with locally advanced or metastatic UC. Avelumab is currently being evaluated as both monotherapy and combination therapy in an extensive clinical development program. Beyond mMCC, locally advanced or metastatic UC and RCC, further avelumab abstracts in non-small cell lung cancer and metastatic castrate-resistant prostate cancer, locally advanced squamous cell carcinoma of the head and neck, relapsed or refractory diffuse large B-cell lymphoma will be showcased.

In addition to avelumab data, Merck, KGaA, Darmstadt, Germany, will also feature new research at ASCO on its investigational bifunctional immunotherapy anti-PD-L1/TGF-▀ trap (M7824), which is thought to simultaneously block both PD-L1 and TGF-▀. An oral presentation will showcase dose escalation Phase I clinical data exploring the potential of M7824 in advanced solid tumors.

Pipeline updates at ASCO also include early clinical results for both Tepotinib, an investigational small-molecule inhibitor of the c-Met receptor tyrosine kinase, M7583, an oral, highly selective, covalent inhibitor of Bruton’s tyrosine kinase (BTK), and the first clinical data for M3814, an investigational DNA-dependent protein kinase (DNA-PK) inhibitor. Merck, KGaA, Darmstadt, Germany, is investing significant resources in the promising area of DDR to be a leader in this field. Merck, KGaA, Darmstadt, Germany, has recently in-licensed two promising clinical-stage programs from Vertex.

This highly focused approach to research and development channels Merck, KGaA, Darmstadt, Germany’s scientific expertise in areas of high unmet need, a legacy started with Erbitux. Multiple presentations at ASCO reinforce Erbitux as a standard-of-care treatment in squamous cell carcinoma of the head and neck (SCCHN) and metastatic colorectal cancer (mCRC), providing valuable information about biomarkers, disease response, and the importance of tumor location in mCRC, to best target treatment to the right patients.

*Avelumab is under clinical investigation for treatment of NSCLC, RCC, DLBCL, SSCHN and mCRPC and has not been demonstrated to be safe and effective for these indications. There is no guarantee that avelumab will be approved for NSCLC, RCC, DLBCL, SSCHN and mCRPC by any health authority worldwide.

**Tepotinib is the proposed nonproprietary name for the c-Met kinase inhibitor (also known as MSC2156119J).

Tepotinib, M7824 and M3814 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, KGaA, Darmstadt, Germany-supported key abstracts slated for presentation are listed below. In addition, a number of investigator-sponsored studies have been accepted, including multiple abstracts related to Erbitux and avelumab (not listed).

TitleLead AuthorAbstract #Presentation Date / Time (CDT)Location
M7824 (TGF-▀ trap)
Oral Presentation
Solid Tumors
Preliminary results from a phase 1 trial of M7824 (MSB0011359C), a bifunctional fusion protein targeting PD-L1 and TGF-Ô, in advanced solid tumors
JL Gulley3006June 5
13:15-16:27
Hall D1
TitleLead AuthorAbstract # Presentation Date / Time (CDT)Location
Avelumab
Oral Presentation
Renal Cell Carcinoma
(JAVELIN Renal 100)
First-line avelumab + axitinib therapy in patients with advanced renal cell carcinoma: results from a phase 1b trial
TK Choueiri 4504June 5
8:00-11:00
Arie Crown Theater
Poster Sessions
Non-Small Cell Lung Cancer (JAVELIN Solid Tumor)
Exposure-response and PD-L1 expression analysis of second-line avelumab in patients with advanced NSCLC: Data from the JAVELIN Solid Tumor trial
JL Gulley9086June 3
8:00-11:30
Hall A
Merkel Cell Carcinoma (JAVELIN Merkel 200)
First-line avelumab treatment in patients with metastatic Merkel cell carcinoma: preliminary data from an ongoing study
S D’Angelo9530June 3
13:15-16:45
Hall A
Merkel Cell Carcinoma (JAVELIN Merkel 200)
Exploratory biomarker analysis in patients with chemotherapy-refractory metastatic Merkel cell carcinoma treated with avelumab
I Shapiro9557June 3
13:15-16:45
Hall A
Urothelial Carcinoma
Updated efficacy and safety of avelumab in metastatic urothelial carcinoma: pooled analysis from 2 cohorts of the phase 1b JAVELIN Solid Tumor study
AB Apolo4528June 4
8:00-11:30
Hall A
Renal Cell Carcinoma (JAVELIN Renal 101)
Avelumab plus axitinib vs sunitinib as first-line treatment of advanced renal cell carcinoma: phase 3 study (JAVELIN Renal 101)
TK Choueiri TPS4594June 4
8:00-11:30
Hall A
Pan-Tumor
(JAVELIN Solid Tumor)
Safety profile of avelumab in patients with advanced solid tumors: a JAVELIN pooled analysis of phase 1 and 2 data
K Kelly3059June 5
8:00-11:30
Hall A
Lymphoma (TiP)
(JAVELIN DLBCL)
Phase 1b/3 study of avelumab-based combination regimens in patients (pts) with relapsed or refractory diffuse large B-cell lymphoma (R/R DLBCL)
R ChenTPS7575June 5
8:00-11:30
Hall A
Prostate Cancer
(JAVELIN Solid Tumor)
Avelumab in metastatic castration-resistant prostate cancer (mCRPC)
F Fakhrejahani5037June 5
13:15-16:45
Hall A
Head and Neck Cancer (TiP)
(JAVELIN Head and Neck 100)
JAVELIN Head and Neck 100: a phase 3 trial of avelumab in combination with chemoradiotherapy (CRT) vs CRT for 1st-line treatment of locally advanced squamous cell carcinoma of the head and neck (LA SCCHN)
NY LeeTPS6093June 5
13:15-16:45
Hall A
Publications
Merkel Cell Carcinoma (JAVELIN Merkel 200)
Non-progression during avelumab treatment is associated with clinically relevant improvements in health-related quality of life in patients with Merkel cell carcinoma
M Bharmale21070N/AN/A
Merkel Cell Carcinoma (JAVELIN Merkel 200)
Patient experiences with avelumab vs chemotherapy for treating Merkel cell carcinoma: results from protocol-specified qualitative research
H Kaufmane21065

N/AN/A
Non-Small Cell Lung Cancer (JAVELIN Solid Tumor)
Comparative study of two PD-L1 expression assays in patients with non-small cell lung cancer (NSCLC)
Z Fenge20581N/AN/A
TitleLead AuthorAbstract #Presentation Date / Time (CDT)Location
Tepotinib
Poster Sessions
Hepatocellular Carcinoma
Phase Ib trial of tepotinib in Asian patients with advanced hepatocellular carcinoma (HCC): Final data including long-term outcomes
S Qin4087June 3
8:00-11:30
Hall A
Non-Small Cell Lung Cancer
Phase Ib study of tepotinib in EGFR-mutant/c-Met-positive NSCLC: final data and long-term responders
Y-L Wu8547June 3
8:00-11:30
Hall A
Publications
Hepatocellular Carcinoma
Final phase Ib data for the oral c-Met inhibitor tepotinib in patients with previously treated advanced hepatocellular carcinoma
S Faivree15676N/AN/A
Advanced Lung Adenocarcinoma
Phase II trial of the c-Met inhibitor tepotinib in advanced lung adenocarcinoma with MET exon 14 skipping mutations
PK Paik 20541N/AN/A
TitleLead AuthorAbstract #Presentation Date / Time (CDT)Location
M3814 (DNA-PK)
Poster Session
Solid Tumors
A multicenter phase I trial of the DNA-dependent protein kinase (DNA-PK) inhibitor M3814 in patients with solid tumors
M van Bussel2556June 5
8:00-11:30
Hall A
Publication
Solid Tumors
A phase Ia/Ib trial of the DNA-dependent protein kinase inhibitor (DNA-PKi) M3814 in combination with radiotherapy in patients with advanced solid tumors
B Van Trieste14048N/AN/A
TitleLead AuthorAbstract #Presentation Date / Time (CDT)Location
M7583 (BTKi)
Publication
B Cell Malignancies
Phase I/II, first in human trial of the Bruton’s tyrosine kinase inhibitor (BTKi) M7583 in patients with B cell malignancies
S Rulee14101N/AN/A

About Avelumab
Avelumab is a human antibody specific for a protein called PD-L1, or programmed death ligand-1. Avelumab is designed to potentially engage both the adaptive and innate immune systems. By binding to PD-L1, avelumab is thought to prevent tumor cells from using PD-L1 for protection against white blood cells, such as T-cells, exposing them to anti-tumor responses. Avelumab has been shown to induce antibody-dependent cell-mediated cytotoxicity (ADCC) in vitro. In November 2014, Merck KGaA, Darmstadt, Germany, and Pfizer announced a strategic alliance to co-develop and co-commercialize avelumab.

***Indications
The U.S. Food and Drug Administration (FDA) granted accelerated approval for avelumab (BAVENCIO«) for the treatment of (i) metastatic Merkel cell carcinoma (mMCC) in adults and pediatric patients 12 years and older and (ii) patients with locally advanced or metastatic urothelial carcinoma (UC) who have disease progression during or following platinum-containing chemotherapy, or who have disease progression within 12 months of neoadjuvant or adjuvant treatment with platinum-containing chemotherapy. Continued approval for these indications may be contingent upon verification and description of clinical benefit in confirmatory trials. Avelumab is not approved for any indication in any market outside the U.S.

Important Safety Information
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 avelumab include fatigue, musculoskeletal pain, diarrhea, nausea, infusion-related reaction, peripheral edema, decreased appetite/hypophagia, urinary tract infection and rash.

For full prescribing information and medication guide for BAVENCIO, please see www.BAVENCIO.com.

About Erbitux« (cetuximab)
Erbitux« 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 90 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, KGaA, Darmstadt, Germany 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 inhibitor of DNA-dependent protein kinase (DNA-PK). DNA-PK is a key enzyme for non-homologous end-joining (NEHJ), the most important DNA double strand break repair pathway (DSB), and could potentially enhance the efficacy of many commonly used DNA-damaging agents such as radiotherapy and chemotherapy. M3814 complements Merck, KGaA, Darmstadt, Germany’s extensive DNA damage response (DDR) portfolio and is currently in Phase I studies.

About M7824
M7824, anti-PD-L1/TGF-▀ trap, is an investigational potentially first-in-class bi-functional immunotherapy designed to simultaneously block two immuno-inhibitory pathways (PD-L1 and transforming growth factor beta) that are commonly used by cancer cells to evade the immune system. The aim of this investigational drug is to control tumor growth by restoring and enhancing anti-tumor immune responses. M7824 is currently in Phase I studies for solid tumors.

About Tepotinib
Tepotinib (also known as 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 correlate with aggressive tumor behavior and poor clinical prognosis. Tepotinib is currently under evaluation in Phase I/II trials.
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