Merck Highlights Novel Mechanisms with the Potential to Transform Standards of Care in Several Cancers, MS, and Lupus

Merck, a leading science and technology company, today provided an overview of its innovative pipeline with a focus on five mid- to late-stage assets with first-in-class and/or best-in-class potential at its R&D Update Call.

“At Merck we are working to translate our extensive expertise and deep knowledge in key tumors and neurological and immunological diseases with a goal to change treatment paradigms and improve patient outcomes,” said Danny Bar-Zohar, Global Head of Development for the Healthcare business of Merck. “With evobrutinib, xevinapant, and berzosertib, we have the opportunity to be not only first-in-class, but potential game-changers in how we treat MS, head & neck cancer and small cell lung cancer going forward.”

Advancing Assets with Transformational Potential
Evobrutinib (BTK inhibitor) – A pioneering development program with a new mechanism of action (MoA) for the treatment of patients with relapsing multiple sclerosis (RMS) that has the potential to change the standard of care.

• Oral, central nervous system (CNS)-penetrant, covalent Bruton’s tyrosine kinase inhibitor (BTKi) in development for RMS.
• MoA combines potent B-cell inhibition to target acute inflammation (associated with relapses) with a central effect on microglia that aims to reduce chronic inflammation (associated with disease progression).
• Comprehensive Phase II clinical data support best-in-class potential.
• Evobrutinib is the first BTKi to have completed enrollment of the Phase III clinical trial program for relapsing multiple sclerosis, with data readout expected in Q4 2023.

Xevinapant (IAP antagonist) – As a potent oral antagonist of Inhibitor of Apoptosis Proteins (IAP) and the only IAP antagonist in late-stage development, xevinapant builds on our market-leading expertise in squamous cell carcinoma of the head and neck (SCCHN), aimed at maximizing the chances of a cure in locally advanced disease setting.

• Ongoing Phase III TrilynX study for previously untreated unresectable locally advanced (LA) SCCHN in combination with platinum-based chemoradiotherapy.
• Second global Phase III study to be initiated in the first half of 2022 to evaluate xevinapant in patients with cisplatin-ineligible LA SCCHN.
• 5-year update of OS data from Phase II study anticipated in 2022.
• First launch expected in 2025.

Berzosertib (ATR inhibitor) – The lead candidate in our DNA Damage Response (DDR) inhibitor portfolio and the first ATR inhibitor with positive randomized clinical trial in any tumor type, seeks to exploit the synergistic effect of combining ATR inhibition with topoisomerase I inhibitors

• Multiple mid-stage clinical trials in small cell lung cancer (SCLC) build on positive Phase II study results, with the goal of establishing a new standard of care in second-line SCLC.
• Study planned for indication expansion in ovarian cancer and potentially in refractory GI cancers.

M1231 (MUC1/EGFR bi-specific ADC) – The first bi-specific ADC (antibody-drug conjugate) from our pipeline that aims to optimize targeting of cancer cells and overcome remaining safety limitations of conventional ADCs.

• M1231 delivers a cytotoxic payload to tumor cells expressing both MUC1 and EGFR and has a highly controlled drug-antibody ratio, which is anticipated to increase tumor specificity, selectivity, and efficacy.
• Phase I clinical study to characterize the safety and preliminary activity is well underway, and efficacy expansions into late-stage non-small cell lung cancer and esophageal squamous cell carcinoma are expected to begin in 2022.

Enpatoran (TLR7/8 inhibitor) – Oral therapythat aims to overcomelimitations of available lupus therapies by providing selective inhibition of lupus-relevant disease drivers, which may increase efficacy while preserving immunity against infections.

• Highly specific potential first-in-class immune modulator blocking the activation of Toll-like receptor (TLR)7 and TLR8, known to be activated in lupus.
• Initiation of Phase II studies in systemic lupus erythematosus (SLE) / cutaneous lupus erythematosus (CLE) in the first half of 2022.

Advancing the broader pipeline and portfolio
Merck will initiate 11 new studies in 2022 across the early- and late-stage pipeline, including a Phase III confirmatory study with tepotinib in EGFRm MET amplification in NSCLC, five proof-of-concept studies including trials of M1774, an oral ATR inhibitor being evaluated as both a monotherapy and in combination with PARP inhibitors; the JAVELIN Bladder Medley umbrella study in the first-line urothelial carcinoma, combining avelumab with novel investigational agents including our anti-TIGIT M6223 and Nektar Therapeutics’ interleukin-15 (IL-15) receptor agonist, NKTR-255, in the maintenance setting; two first-in-human studiesinvolving M9140, a next-generation ADC based on an internally developed linker-payload technology; and M1069, our dual adenosine receptor antagonist.

“Our rapidly progressing pipeline of in-house–discovered and partnered assets with first-in-class potential demonstrate the deep expertise and collaborative mindset of our R&D organization,” said Joern-Peter Halle, Global Head of Research for the Healthcare business of Merck. “We expect exciting new entries and substantial advances of our early- and late-stage pipeline in the next few years.”

To access the presentation and a recording, please visit the Company’s website at https://www.merckgroup.com/en/investors/events-and-presentations.html.

Merck’s Commitment to Cancer
Merck is a science-led organization dedicated to delivering transformative medicines with the goal of making a meaningful difference in the lives of people affected by cancer. Our oncology research efforts aim to leverage our synergistic portfolio in oncogenic pathways, immuno-oncology, and DNA Damage Response (DDR) to tackle challenging tumor types in gastrointestinal, genitourinary, and thoracic cancers. Our curiosity drives our pursuit of treatments for even the most complex cancers, as we work to illuminate a path to scientific breakthroughs that transform patient outcomes. Learn more at https://www.merckgrouponcology.com.

Merck in Neurology and Immunology
Merck has a long-standing legacy in neurology and immunology, with significant R&D and commercial experience in multiple sclerosis (MS). The company`s current MS portfolio includes two products for the treatment of relapsing MS – Rebif® (interferon beta-1a) and MAVENCLAD® (cladribine tablets). Merck aims to improve the lives of patients by addressing areas of unmet medical needs. In addition to Merck`s commitment to MS, the company also has a pipeline focusing on discovering new therapies that have the potential in other neuroinflammatory and immune-mediated diseases, including systemic lupus erythematosus (SLE).

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About Merck
Merck, a leading science and technology company, operates across healthcare, life science and electronics. Around 58,000 employees work to make a positive difference to millions of people’s lives every day by creating more joyful and sustainable ways to live. From advancing gene editing technologies and discovering unique ways to treat the most challenging diseases to enabling the intelligence of devices – the company is everywhere. In 2020, Merck generated sales of € 17.5 billion in 66 countries.

Scientific exploration and responsible entrepreneurship have been key to Merck’s technological and scientific advances. This is how Merck has thrived since its founding in 1668. The founding family remains the majority owner of the publicly listed company. Merck holds the global rights to the Merck name and brand. The only exceptions are the United States and Canada, where the business sectors of Merck operate as EMD Serono in healthcare, MilliporeSigma in life science, and EMD Electronics.

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