Moderna’s mRNA-4157: A breakthrough in melanoma treatment and the road ahead for patent protection

Moderna and Merck join forces to advance mRNA therapeutics in cancer treatment

SOPHIA ANTIPOLIS, France – March 03, 2023 │mRNA therapeutics against cancer are an area of strong R&D activity, especially since the efficient use of mRNA vaccines to fight the SARS-CoV-2 pandemic. On the other hand, although the number of clinical trials is increasing, there is still no approved mRNA vaccine for cancer. However, Moderna could become the first in the pharmaceutical industry to offer this type of therapy. Indeed, in February 2021, mRNA-4157/V940, an investigational personalized mRNA cancer vaccine (developed by Moderna), in combination with KEYTRUDA (Merck’s anti-PD-1 therapy), was granted Breakthrough Therapy Designation by the U.S. Food and Drug Administration (FDA) for the adjuvant treatment of patients with high-risk melanoma following complete resection. Breakthrough Therapy designation is a process designed to expedite the development and review of drugs that are intended to treat a serious condition, and preliminary clinical evidence indicates that the drug may demonstrate substantial improvement over available therapy on a clinically significant endpoint(s). For six years, the two companies have combined their expertise in mRNA and immuno-oncology. In October 2020, the companies finally announced that they will share costs and any profits equally under this worldwide collaboration.

Results from the phase 2b trial: Moderna’s vaccine shows promise in high-risk melanoma patients

The FDA granted Breakthrough Therapy Designation based on positive data from the Phase 2b KEYNOTE-942/mRNA-4157-P201 trial (NCT03897881). Indeed, the data showed a reduction in the risk of disease recurrence or death with Moderna’s vaccine. KEYNOTE-942 is an ongoing randomized, open-label Phase 2b trial that enrolled 157 patients with stage III/IV melanoma. Following complete surgical resection, patients were randomized to receive mRNA-4157/V940 (9 total doses of mRNA-4157) and KEYTRUDA (200 mg every 3 weeks up to 18 cycles) versus KEYTRUDA alone for approximately one year until disease recurrence or unacceptable toxicity. The primary endpoint is recurrence-free survival, and secondary endpoints include distant metastasis-free survival and safety. In December 2020, the companies revealed their first results. Data demonstrated a statistically significant and clinically meaningful improvement in the primary endpoint of recurrence-free survival. Adjuvant treatment with mRNA-4157/V940 in combination with KEYTRUDA reduced the risk of recurrence or death by 44% compared with KEYTRUDA alone. These data provide the first evidence that mRNA-4157 can improve on the rates of recurrence-free survival achieved by PD-1 blockade in resected high-risk melanoma. These findings also provide the first randomized evidence that a personalized neoantigen approach may be beneficial in melanoma. A Phase 3 study will be initiated in melanoma patients in 2023.

mRNA-4157: a mRNA-based personalized cancer vaccine

The KEYNOTE-942/mRNA-4157-P201 trial results from the collaboration of two companies, but above all from the combination of two different therapies. First, Merck has developed KEYTRUDA (pembrolizumab), which received its first approval for treating advanced melanoma patients with BRAF mutations in 2014. There are currently more than 1,600 trials studying pembrolizumab across a wide variety of cancers and treatment settings. Pembrolizumab is a humanized monoclonal antibody that blocks the interaction between anti-programmed death receptor-1 (PD-1) and its ligands, PD-L1 and PD-L2, thereby activating T lymphocytes, which may affect both tumor cells and healthy cells. In the phase 2 clinical study KEYNOTE-942/mRNA-4157, pembrolizumab is administered as a 200 mg dose via a 30-minute intravenous infusion once every 21 days for up to 18 cycles (approximately one year). Then, Moderna has developed mRNA-4157, a mRNA-based personalized cancer vaccine, which is described in a patent family (WO2020/097291). A personalized cancer vaccine is directed against a personalized antigen, a tumor-specific antigen, also referred to as a neoantigen, that is present in a tumor of an individual, but not expressed or expressed at low levels in normal non-cancerous tissue of the individual. The antigen may or may not be present in tumors of other individuals. The cancer vaccine composition developed by Moderna comprises mRNA(s) that encode 34 peptide epitopes, 29 of which are MHC class I epitopes and 5 of which are MHC class II or MHC class I and II epitopes. These peptide epitopes are chosen between personalized cancer antigens (3 to 20 peptide epitopes) and cancer hotspot antigens (KRAS G12 mutation or KRAS G13 mutation, or both mutations). The peptide epitopes are in the form of a concatemeric cancer antigen, and a linker is used between peptides to reduce or eliminate pseudoepitope formation. It is important that the junction not be an immunogenic peptide that could produce an immune response. The mRNA is then encapsulated in lipid nanoparticles (LNP). The personalized cancer antigens are selected based on a next-generation sequencing analysis (NGS), e.g. whole exome sequencing (WES), of the human subject’s DNA from a tumor sample, relative to DNA from a blood sample, which serves as the germline (un-mutated) reference. Results from the blood sample are also used to determine the subject’s HLA-type using an NGS-based approach. Finally, regarding the method of administration described in the clinical trial part of the patent family, the mRNA vaccines are administered as 1 mg doses via intramuscular injection once every 21 days for 9 doses.

Moderna’s patent application for mRNA-4157: examining novelty, inventive step and patentability

In November 2019, Moderna filed an international patent application for “RNA cancer vaccines” (WO2020/097291) which was extended to EP/US/JP/CA/AU/MA. All patent applications are currently pending, but information is available for the European patent application (EP3876947). A third party has filed several documents, one of which being a patent document from BioNTech in collaboration with TRON in 2012 (Individualized vaccines for cancer, WO2012/159754). Additionally, there are 7 non-patent literatures, 4 of which have at least one BioNTech member among the authors. The European Patent Office then published an international preliminary report on patentability disclosing some claims that were not novel and did not satisfy the requirements for novelty, as well as other claims that did not involve an inventive step. Thus, the applicant modified their claims before examination. Shortly afterwards, the European search opinion was published. Reviewers noted that the third-party observations submitted during the international phase cast doubt on the patentability of the invention. Even though some claims appear to be novel, others do not, so Moderna’s EP patent is unlikely to be granted. The claims should be further amended to meet the requirements.

Moderna’s mRNA-4157: a step towards the first mRNA cancer vaccine

Moderna is known for its key role in the development of mRNA vaccine against Covid-19, but it is also a key player in mRNA cancer therapeutics (details in mRNA Cancer Therapies Patent Landscape 2022). Indeed, the company owns 38 patent families in this area, and 66% of its live patents are pending applications. The company’s portfolio is focused on RNA modification and stabilization, as well as on mRNA-encoded immunomodulators and antigens. Moreover, currently, Moderna’s mRNA cancer therapy pipeline has 3 cancer vaccines and 2 intratumoral immune-oncology therapies. Among them, only its personalized cancer vaccine mRNA-4157 is in clinical phase 2b (efficacy and side effects). This vaccine could not only be Moderna’s first vaccine against cancer but it could also be the first mRNA cancer vaccine provided to a certain category of cancer patients, showing the importance of the patent family WO2020/097291. The granting of these patent applications in the US and Europe will be a strategic step for Moderna in the protection of these new therapeutic approaches. However, with the third-party observations submitted in the European procedure, the modifications of the claims that Moderna will have to make and the potential oppositions that can be filed after the granting of this patent application, the road will still be long for Moderna to obtain a solid protection for its melanoma vaccine.

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About the author
Fabienne Massa, PhD., works for Knowmade in the field of Biotechnology and Life Sciences. She holds a PhD in Molecular and Cellular Biology from the IPMC (Sophia Antipolis, France). She also holds a Master of Business Management from IAE (Nice, France) and she previously worked in the pharmaceutical industry.

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