On January 13, 2021 Taiho Pharmaceutical Co, Ltd., (hereinafter Taiho) reported that it and Astex Pharmaceuticals (UK), (hereinafter Astex), both Otsuka group companies, have granted an exclusive license under their joint, small-molecule drug discovery program targeting SHP2 to Merck & Co., Inc., Kenilworth, NJ, USA, known as MSD outside the United States and Canada (hereinafter MSD) through a subsidiary (Press release, Taiho, JAN 13, 2021, View Source [SID1234573914]).

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An option for MSD to acquire the exclusive license to the Astex-Taiho SHP2 program was included as part of the strategic oncology collaboration between MSD, Astex and Taiho, announced in January 2020. The collaboration focuses on the discovery and development of small molecule inhibitors against several drug targets, including the KRAS oncogene, which are currently being investigated for the treatment of cancer.

SHP2, a dephosphorylating enzyme, is a signaling molecule which regulates various cellular processes including cell proliferation and differentiation, and acts as a regulator in the activation of the RAS signaling pathway such as KRAS.*1

"We are delighted to have extended the breadth of our strategic oncology collaboration with MSD to encompass assets from the joint Astex-Taiho SHP2 program", said Teruhiro Utsugi, Ph.D., managing director at Taiho. "This will allow for a number of important drug-drug combinations to be explored as potential new treatment modalities for patients."

In exchange for providing MSD with an exclusive global license to their small molecule SHP2 inhibitor candidates, Taiho and Astex will receive an option-exercise fee payment and will be eligible to receive further undisclosed payments contingent upon the achievement of clinical, regulatory and sales milestones for SHP2 products, as well as tiered royalties on sales. MSD will be solely responsible for funding all further research and development and will be responsible for commercialization of SHP2 products globally. Taiho has retained co-commercialization rights in Japan and an option to promote SHP2 products in specific areas of Southeast Asia.

"We are pleased with the discovery research progress and collaboration with Taiho and Astex as we seek to develop new small molecule candidates for the treatment of cancer," said Nick Haining, vice president, Discovery Oncology and Immunology, MSD Research Laboratories. "We look forward to working more extensively with Taiho and Astex on the SHP2 pathway and accelerating this promising research which has the potential to impact a number of cancer types."

Harren Jhoti, Ph.D., president and CEO of Astex Pharmaceuticals (UK), commented,

"Together with our Taiho colleagues, we are delighted to extend our strategic alliance with MSD to include assets from our joint SHP2 program that have been generated using our leading fragment-based drug discovery approach."

On January 13, 2021 Astellas Pharma Inc. (TSE: 4503, President and CEO: Kenji Yasukawa, Ph.D., "Astellas" ) reported that it has entered into a research collaboration for molecular targeted radiotherapies with Actinium Pharmaceuticals, Inc. (NYSE AMERICAN: ATNM, Chief Executive Officer and Chairman of the Board: Sandesh Seth, "Actinium") (Press release, Astellas, JAN 13, 2021, View Source [SID1234573913]). This collaboration is a component of Astellas’ initiative to develop "theranostics" as part of its Rx+ business1.

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Theranostics is a combined term of "therapeutics" and "diagnostics", defined as a treatment protocol or concept in which healthcare professionals assess lesion sites and simultaneously determine the appropriate treatment for each patient2. Through utilization of a diagnostic agent developed in parallel with a therapeutic agent that shares the same target, it may be possible to identify patients in advance who would benefit from the treatment. This approach may help healthcare professionals provide more efficient and effective treatment.

In this collaboration, the potential therapeutic effect will be assessed by combining certain targeted oncology drugs that were discovered by Astellas based on its drug discovery capabilities cultivated thus far with Actinium’s nuclear medicine technology which utilizes an alpha particle-emitting radioisotope3 (Actinium-225). Astellas is already conducting pre-clinical trials of the diagnostic agents on the target　molecule．When a promising therapeutic drug candidate is identified in the course of this collaboration, clinical trials for the theranostics may be initiated.

Through its Rx+ business, Astellas aims to realize a society where people can live in their own way, both physically and mentally through scientifically based on scientific evidence. Astellas aims to optimize therapeutic approach by improving diagnostic and surgical accuracy and maximize patient outcomes. The development of theranostics that integrates diagnostics and therapeutics is part of this effort.

Astellas has already reflected the impact from this collaboration in its financial forecast of the current fiscal year ending March 31, 2021.

On January 12, 2021 PharmEnable reported that the company has entered a new partnership with Sosei Heptares (Press release, PharmEnable, JAN 12, 2021, View Source [SID1234641050]). This collaboration will drive a novel drug discovery programme against a challenging G protein-coupled receptor (GPCR) target, which is associated with neurological disease.

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Sosei Heptares is an international biopharmaceutical group, focused on the discovery and early development of new medicines originating from their world-leading GPCR-targeted StaR technology and structure-based drug design platform capabilities.

Miles Congreve, Chief Scientific Officer of Sosei Heptares, said: "We have been very impressed with PharmEnable’s technology and approach, which we believe to be highly complementary to our own, offering important synergies for drug discovery on challenging GPCR targets. We are excited to apply these technologies on a peptidergic GPCR target that has proved particularly difficult to drug. We have so far assembled a wealth of structural and ligand-binding information on the target and created several promising molecules but have yet to identify compounds with sufficiently desirable neurological drug-like properties to advance into preclinical studies. Combining our respective technologies and expertise may be the key that unlocks this target and enables the identification of higher quality molecules to progress into preclinical development."

Dr Hannah Sore, Founder and CEO of PharmEnable, commented: "We are excited to partner with Sosei Heptares on this challenging and complex GPCR target. We have proven the strength of our platform in tapping unexplored parts of the chemical universe to find novel and specific hits for currently undruggable targets. Combining our platform with the technology and structural insights developed by Sosei Heptares should enable us to generate several potential hits, and to establish our pipeline of candidate molecules for the treatment of challenging diseases.".

The collaboration will enhance innovation and development of the next generation of small molecule drugs against the particularly difficult GPCR target. PharmEnable is excited to begin this collaborative project and look forward to working closely with Sosei Heptares.

On January 12, 2021 Almac Sciences, a member of the Almac Group, reported that it has secured £2million of support from Invest Northern Ireland (INI) to accelerate a programme of enzyme research (Press release, Almac, JAN 12, 2021, View Source [SID1234575424]).

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Almac Sciences had previously established a cutting-edge biotechnology platform for enzyme chemistry and biology through two successfully completed rounds of R&D investment supported by Invest NI. This investment in R&D, awarded by INI and supported by the European Regional Development Fund, will further develop the program to establish IN Silico Informed metaGenomic Harvesting Technology (INSIGHT), a platform built from multi-disciplinary research bringing together computational, metagenomics, biology and chemistry methodologies.

Routes of synthesis for most drugs are amenable to biocatalytic intervention. The INSIGHT project aims to improve the enzyme discovery process to allow more robust enzymes to supersede multi-step chemical routes currently used to produce pharmaceutical intermediates and products.

The unique project involves the development of an enzyme identification platform based around the exploitation of Almac’s existing metagenomic data mining using enzyme modelling / engineered lead diversity screening married with the company’s strength on industrial focus. This combination approach has never been developed to accelerate enzyme discovery and their subsequent application in the past and is a significant research and development programme.

This new technology will bring significant benefit to, not only Almac, but also to the wider pharmaceutical industry as it will offer simpler, lower cost and less polluting enzymatic processes. Specifically, INSIGHT will deliver new, best-in-class metagenomics, computational and engineering platforms for the pharmaceutical, biotechnology, life sciences and fine chemicals sectors.

Dr Stefan Mix, Almac Sciences’ Head of Biocatalysis, will lead a team of experts to complete the project and deliver the foundations for future commercialisation. The INSIGHT project will span six work packages which will run over 36 months once recruitment has been secured.

Professor Tom Moody, VP Technology Development and Commercialisation, Almac Sciences and Arran Chemical Company commented: "This project, and the related INI support, will be vital to ensure we can achieve our aspiration of becoming a global leader in biotechnology. The ambitious project will bring together each of the critical elements to accelerate enzyme identification and discovery and will de-risk the enzyme development pipelines for Almac. As a result of this unique project there will be both major academic and commercial benefits, providing significant growth opportunity for the NI Bio-economy and the wider economy."

Welcoming the investment, Kevin Holland, CEO of Invest NI said: "Almac has long been one of Northern Ireland’s most successful companies within our thriving life & health sciences sector and has worked hard to build an impressive global reputation for ground-breaking work in the global pharmaceutical industry. It recognises the benefits of investing in cutting edge R&D and is making this new investment to build upon the foundations from previous R&D and capital investment over the last number of years.

"Invest NI has developed a strong collaborative partnership with Almac over the years, offering support for job creation and highly successful R&D projects. Our £2million ERDF funded offer of support for this new investment will further cement the company’s world-renowned reputation and enable it to expand its biocatalysis capability creating a new, greener and more cost-effective solution to industry. The development of this new technology enhances Northern Ireland’s global reputation in the field."

Invest NI’s R&D support is part financed by the European Regional Development Fund under the EU investment for Growth and Jobs Programme 2014-2020.

On January 12, 2021 Eisai Co., Ltd. (Headquarters: Tokyo, CEO: Haruo Naito, "Eisai") reported that presentations on a series of abstracts highlighting updates on its in-house discovered lenvatinib mesylate (product name: LENVIMA, the orally available kinase inhibitor, "lenvatinib") will be given at the Gastrointestinal Cancers Symposium Virtual Meeting, from January 15 to 17, 2021 (Press release, Eisai, JAN 12, 2021, View Source [SID1234574984]).

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At this symposium, regarding the lenvatinib monotherapy, the real-world effectiveness among unresectable hepatocellular carcinoma (HCC) patients treated in United States clinical practices (Abstract No: 273), as well as the results of a post hoc analysis of patients with unresectable HCC who progressed to the Child-Pugh B stage in the Phase 3 REFLECT study (Abstract No: 298), will be presented.

In addition, the data to be presented regarding the combination therapy of lenvatinib plus pembrolizumab (product name: KEYTRUDA), the anti-PD-1 therapy from Merck & Co., Inc., Kenilworth, N.J., U.S.A. (known as MSD outside the United States and Canada), are results from the biliary tract cancer cohort (Abstract No: 321), the colorectal cancer cohort (Abstract No: 94), and the gastric cancer cohort (Abstract No: 230) of the basket-type Phase 2 LEAP-005 clinical study for 6 types of previously treated advanced solid tumors.

In March 2018, Eisai and Merck & Co., Inc., Kenilworth, N.J., U.S.A., through an affiliate, entered into a strategic collaboration for the worldwide co-development and co-commercialization of lenvatinib.

Eisai positions oncology as a key therapeutic area, and is aiming to discover revolutionary new medicines with the potential to cure cancer. Eisai will continue to create innovation in the development of new drugs based on cutting-edge cancer research, as it seeks to contribute further to addressing the diverse needs of, and increasing the benefits provided to, patients with cancer, their families, and healthcare providers.

This release discusses investigational compounds and investigational uses for FDA-approved products. It is not intended to convey conclusions about efficacy and safety. There is no guarantee that any investigational compounds or investigational uses of FDA-approved products will successfully complete clinical development or gain FDA approval.

The full list of Eisai presentations are below.

Product / Compound
Abstract No. Title / Scheduled Date and Time (local time: Eastern Standard Time)
Lenvatinib 273

Real-world effectiveness of lenvatinib monotherapy among unresectable hepatocellular carcinoma patients treated in United States clinical practices
January 15 (Fri)

Lenvatinib 298

Post hoc analysis in patients (pts) with unresectable hepatocellular carcinoma (uHCC) who progressed to Child-Pugh B (CPB) liver function in the phase 3 REFLECT study of lenvatinib (LEN)
January 15 (Fri)

Lenvatinib + pembrolizumab 321

Lenvatinib plus pembrolizumab for patients with previously treated biliary tract cancers in the multicohort phase 2 LEAP-005 study
January 15 (Fri)

Lenvatinib + pembrolizumab 94

LEAP-005: A phase 2, multicohort study of lenvatinib plus pembrolizumab in patients with previously treated selected solid tumors: results from the colorectal cancer cohort
January 15 (Fri)

Lenvatinib + pembrolizumab 230

LEAP-005: A phase 2 multicohort study of lenvatinib plus pembrolizumab in patients with previously treated selected solid tumors: results from the gastric cancer cohort
January 16 (Sat), 4:30 PM-5:15 PM　(Accepted in poster highlight session)