Vipergen Establishes Research Partnership with Bayer to Discover Novel Compoundsfor Pharmaceuticals and More Sustainable Crop Protection Solutions

On December 21, 2021 Vipergen, a leading provider of small-molecule drug discovery services based on DNA-encoded library (DEL) technologies, reported the signing of a multi-target research agreement with Bayer to discover novel small-molecule lead compounds for development of pharmaceuticals and more sustainable crop protection solutions (Press release, Bayer, DEC 21, 2021, View Source [SID1234597558]). Under the terms of the agreement, Vipergen will apply its new in-living-cell DNA-encoded library (DEL) screening platform to discover novel small-molecule compounds that bind to selected Bayer protein targets. Bayer will select potential drug and crop protection development candidates based on the hits generated by Vipergen’s technology. Bayer will retain exclusive rights to globally commercialize all products resulting from the collaboration. Financial details of the partnership were not disclosed.

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Vipergen’s Cellular Binder Trap Enrichment (cBTE) technology is the first and only platform for screening DNA-encoded small-molecule libraries inside living cells. The technology is designed to accelerate and improve the success rate for discovering novel, high-quality small molecules against protein targets of interest, including challenging targets that are difficult to express and purify in an active form.

"We are looking forward to the partnership with Vipergen and to building on its new technology for screening DNA-encoded libraries under physiologically relevant conditions of living cells for the development of new products in health and agriculture," said Monika Lessl, SVP and Head of Corporate R&D and Social Innovation at Bayer.

"We are very pleased to partner with Bayer, a life sciences leader in human health and agriculture," said Nils Hansen, PhD, Chief Executive Officer of Vipergen. "We look forward to applying our Cellular Binder Trap Enrichment technology to screen DNA-encoded libraries in living cells to support the development of new drugs and sustainable crop-protection solutions."

Aptamer Science “Development of proprietary ApDC linker technology”

On December 21, 2021 Aptamer Science, a company specializing in aptamer platforms, reported that it has completed the development of its own linker technology to be applied to an aptamer-based drug delivery platform (Aptamer Drug conjugate (ApDC)) and has applied for domestic and PCT patents (Press release, Aptamer Sciences, DEC 21, 2021, View Source;idx=271 [SID1234641628]).

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The linker technology developed this time is a dendrimer-type molecular structure that can load multiple payloads, and the number of loaded payloads can be adjusted depending on the number of branched branches.

The junction site with the aptamer is also designed to enable a click reaction mediated by a simple thiol group, which can further improve ApDC production and pharmacological efficacy.

ApDC technology, due to the nature of the aptamer structure, had to limit the drug loading location to the end, which also limited the number of drugs.

The company explains that through the development of this technology, the drug-aptamer ratio (DApR) can be increased by loading the desired amount of drug into ApDC.

An Aptamer Science official said, "In the case of antibody-drug conjugate (ADC) technology, aggregation occurs due to increased hydrophobicity when introducing multiple payloads, which has a significant impact on manufacturing and stability.

"In order to solve this problem, when introducing a hydrophilic group such as PEG, there was a difficulty in making the manufacturing process complicated," he said. "Because the aptamer material itself shows high hydrophilicity,

"It is possible to manufacture stable ApDC with a high drug loading rate using a simple linker without introducing additional functional groups."

The developed branched linker-payload technology is being applied to various ApDCs being developed by the company, such as CD25 and Trop2.

In addition, we plan to introduce it in the development of follow-up technologies, such as targeting immunostimulants (STING, TLR7/8) and targeting delivery of therapeutic radionuclides.

ADC, in which global big pharma companies are investing recently, is emerging as a technical limitation due to side effects such as interstitial lung disease (ILD) and complex manufacturing processes.

ApDC’s advantages over ADC include high cancer tissue penetration, low side effects, and high stability.

Go to article: Aptamer Science "Development of proprietary ApDC linker technology"

Aligos Therapeutics to Present at the 40th Annual J.P. Morgan Healthcare Conference

On December 21, 2021 Aligos Therapeutics, Inc. (Nasdaq: ALGS), a clinical stage biopharmaceutical company focused on developing novel therapeutics to address unmet medical needs in viral and liver diseases, reported that Lawrence M. Blatt, Ph.D., MBA, Chairman and CEO of Aligos, will present at the 40th Annual J.P. Morgan Healthcare Conference on Wednesday, January 12, 2022 at 5:15 pm ET (Press release, Aligos Therapeutics, DEC 21, 2021, View Source/news-releases/news-release-details/aligos-therapeutics-present-40th-annual-jp-morgan-healthcare" target="_blank" title="View Source/news-releases/news-release-details/aligos-therapeutics-present-40th-annual-jp-morgan-healthcare" rel="nofollow">View Source [SID1234597519]). Both the presentation and the Q&A session will be held virtually.

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An audio webcast of the presentation will be available through the Aligos investor section of the website. View Source

The Aligos management team will also participate in investor 1×1 meetings during the conference. Please contact your J.P. Morgan Healthcare representative to schedule virtual one-on-one meetings with Aligos during the conference. For more information about the 40th Annual J.P. Morgan Healthcare Conference, please refer to the Conference Website.

Propanc Biopharma Demonstrates Significant Effects of Proenzyme Therapy on the Tumor Microenvironment

On December 21, 2021 Propanc Biopharma, Inc. (OTCQB: PPCB) ("Propanc" or the "Company"), a biopharmaceutical company developing novel cancer treatments for patients suffering from recurring and metastatic cancer, reported that Ms. Belen Toledo MSc., from the laboratory of Professor Macarena Perán Ph.D., at the University of Jaén, Spain, recently completed an important experimental thesis on the effects of proenzyme therapy and the impact on the tumor microenvironment, which is key to the development, invasion, metastatic spread, and recurrence of solid tumors (Press release, Propanc, DEC 21, 2021, View Source [SID1234597536]). Ms. Toledo also reconfirmed proenzymes kill cancer stem cells (CSCs). This research is part of the "Proenzymes Optimization Project 1" (POP1) Joint Research and Drug Discovery Program at the Universities of Jaén and Granada, Spain, designed to produce synthetic recombinant, commercial scale quantities of the two proenzymes, trypsinogen and chymotrypsinogen.

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The encouraging results demonstrates that proenzymes have a specific effect on tumor cells and CSCs, but also effects other tumor elements in the tumor microenvironment. However, the most significant conclusion from Ms. Toledo is that the proenzymes also caused a reversal of the malignant tumor phenotype, which was, "most unexpected, very exciting and powerfully conclusive." The process that causes a reversal of the tumor phenotype is called differentiation, which is fundamentally how proenzymes exert anti-tumor, anti-cancer and anti-metastatic effects. Therefore, proenzyme treatment, also known as differentiation therapy, exerts these effects on malignant cells, but leaves healthy cells alone.

"The tumor microenvironment displays certain characteristics common to all solid tumors. Proenzymes normalize this tumor microenvironment," said Dr. Julian Kenyon Mb., ChB., M.D., Propanc’s Chief Scientific Officer. "Therefore, the process of cell differentiation induced by the proenzymes will be applicable to all cancers from solid tumors, as well as sarcomas. This is truly a remarkable finding and may be the key to unlocking the uncontrolled spread of malignant tumors, the main cause of patient death for cancer sufferers. As a result of these findings, I believe there is an urgency in advancing our lead product candidate, PRP, into clinical trials."

The POP1 program is designed to produce a backup clinical compound to the Company’s lead product candidate, PRP. The objective is to produce large quantities of trypsinogen and chymotrypsinogen for commercial use that exhibits minimal variation between lots and without sourcing the proenzymes from animals. Propanc is undertaking the challenging research project in collaboration with the Universities of Jaén and Granada, led by research scientists Mr. Aitor González MSc. and Ms. Toledo, supported by Profs. Perán and Juan Antonio Marchal, M.D., representing the Universities respectively, and Dr. Kenyon.

CSTONE ANNOUNCED NEW DRUG APPROVAL OF CEJEMLY® (SUGEMALIMAB) IN CHINA TO POTENTIALLY RESHAPE THE LANDSCAPE OF IMMUNO-ONCOLOGY THERAPY IN LUNG CANCER

On December 21, 2021 CStone Pharmaceuticals (the "Company" or "CStone") reported that the National Medical Products Administration ("NMPA") of China has approved the new drug application ("NDA") of anti-PD-L1 monoclonal antibody Cejemly (sugemalimab) in combination with chemotherapy for treatment-naïve metastatic (stage IV) non-small cell lung cancer ("non-small cell lung caner" or "NSCLC") patients (Press release, CStone Pharmaceauticals, DEC 21, 2021, View Source [SID1234597560]).

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Key Highlights

Anti-PD-L1 monoclonal antibody Cejemly approved in combination with pemetrexed and carboplatin as first-line treatment of patients with metastatic nonsquamous NSCLC, with no EGFR or ALK genomic tumor aberrations; and in combination with paclitaxel and carboplatin as first-line treatment of patients with metastatic squamous NSCLC.
It is the first anti-PD-L1 plus chemotherapy approved for the first-line treatment of metastatic non-squamous and squamous NSCLC patients worldwide.
The NDA of Cejemly in stage III NSCLC is under regulatory review, and the product has the potential to provide an anti-PD-L1 monoclonal antibody option for both stage III and stage IV non-small cell lung cancer patents in the future.
Cejemly is CStone’s third new drug approval in China in 2021, following two first-in-class precision medicines GAVRETO and AYVAKIT.
Globally, the incidence of lung cancer continues to rise, and it is still the leading cause of cancer death worldwide, with huge unmet medical needs. According to statistics, there were 2.21 million new lung cancer cases worldwide in 2020. NSCLC accounts for about 85% of all lung cancer cases, and about 66% of patients are diagnosed with stage III/IV NSCLC. According to IQVIA’s Global Oncology Trends, the size of global oncology drug market is estimated to reach US$269 billion by 2025, of which immuno-oncology drugs will contribute about 20%.

Dr. Frank Jiang, Chairman and CEO of CStone, said: "Cejemly is our third approved new drug in China this year. This further demonstrates CStone’s ability and track record in developing and commercializing high-quality new drugs. As a drug supported by China’s national science innovation program, Cejemly is a globally leading anti-PD-L1 monoclonal antibody. We will work closely with Pfizer to leverage resources and advantages of both sides to accelerate commercialization so that more Chinese patients can benefit from this innovative therapy soon."

Professor Caicun Zhou, Principal Investigator of the GEMSTONE-302 registrational phase III clinical study of Cejemly and Director of the Department of Oncology, Shanghai Pulmonary Hospital, said, "The latest data show that Cejemly plus chemotherapy further prolonged progression-free survival ("PFS") of treatment-naïve patients with stage IV NSCLC. Compared with chemotherapy alone, Cejemly plus chemotherapy demonstrated durable survival benefits with lower toxicity and immunogenicity risks. With a unique dual mechanism of action, Cejemly mobilizes both T cells and macrophages to destroy tumor cells. Therefore, Cejemly is expected to reshape the landscape of lung cancer treatment."

Dr. Jason Yang, Chief Medical Officer of CStone, said, "We are thrilled that Cejemly has been approved in Mainland China. It took only four years for Cejemly to obtain the first NDA approval in lung cancer from the initiation of the phase I clinical trial in humans. It comprehensively showcased CStone’s robust clinical strategy, innovative trial design and rapid execution, while once again demonstrating the ‘CStone Speed’. We will continue to work with our partner to pursue regulatory discussions for Cejemly on the NDAs of stage III and stage IV NSCLC with regulators in multiple countries and regions, including the U.S. Food and Drug Administration, and bring this innovative immunotherapy to more lung cancer patients soon. We will also continue to advance the registrational studies of Cejemly in esophageal squamous cell carcinoma, gastric cancer, relapsed/refractory extranodal natural killer/T-cell lymphoma, to benefit more cancer patients."

The NMPA approval is based on the positive data of GEMSTONE-302 study, a multi-center, randomized, double-blind, phase III study that evaluated the efficacy and safety of Cejemly or placebo in combination with chemotherapy in first-line stage IV NSCLC patients. Compared with placebo plus chemotherapy, Cejemly plus chemotherapy lowered the risk of disease progression or death by 52%, significantly prolonged the patients’ PFS and an encouraging trend in overall survival ("OS") was observed. The clinical benefit was irrespective of NSCLC pathologies and PD-L1 expression levels. Cejemly has a well-tolerated safety profile, and no new safety signals were found.

Apart from the approved indication, the NMPA accepted the NDA of Cejemly as consolidation therapy in patients with unresectable stage III NSCLC without disease progression after concurrent or sequential chemoradiotherapy in September 2021. The product has the potential to become an anti-PD-L1 monoclonal antibody approved to cover stage III and stage IV NSCLC in all-comer settings.

About Cejemly (sugemalimab)

The potential best-in-class anti-PD-L1 monoclonal antibody Cejemly (sugemalimab) is an investigational anti-PD-L1 monoclonal antibody discovered by CStone. Authorized by the U.S.-based Ligand Corporation, Cejemly is developed by the OmniRat transgenic animal platform, which can generate fully human antibodies in one stop. As a fully human, full-length anti-PD-L1 monoclonal antibody, Cejemly mirrors the natural G-type immunoglobulin 4 (IgG4) human antibody, which reduces the risk of immunogenicity and potential toxicities in patients, a unique advantage over similar drugs.

Currently, the China NMPA has approved the potential best-in-class anti-PD-L1 monoclonal antibody Cejemly in combination with chemotherapy for the treatment of treatment-naïve patients with stage IV NSCLC. In addition, Cejemly is being investigated in a number of ongoing clinical trials, including one Phase II registrational study for lymphoma and four Phase III registrational studies in stage III NSCLC, stage IV NSCLC, gastric cancer, and esophageal cancer, respectively.

CStone formed a strategic collaboration agreement with Pfizer that includes the development and commercialization of Cejemly in mainland China, and a framework to bring additional oncology assets to the Greater China market.

About the GEMSTONE-302 Study

The GEMSTONE-302 study (ClinicalTrials.gov registration number: NCT03789604; drug clinical trial registration number: CTR20181452) is a randomized, double-blind Phase III study, designed to evaluate the efficacy and safety of anti-PD-L1 monoclonal antibody Cejemly combined with chemotherapy as the first-line treatment in treatment-naïve patients with stage IV NSCLC vs. placebo combined with chemotherapy. The primary endpoint of the study was investigator-assessed PFS. Secondary endpoints included OS, BICR-assessed PFS and safety, etc.

In August 2020, the GEMSTONE-302 study met its primary endpoint of significantly prolonged PFS, with the risk of disease progression or death reduced by 50% with Cejemly combined with chemotherapy compared to placebo combined with chemotherapy, as assessed by iDMC at the planned interim analysis. Specific study data were presented in a Proffered Paper Oral Presentation (Late-Breaking Abstract) at the ESMO (Free ESMO Whitepaper) Asia 2020.

In July 2021, the final analysis of PFS from the GEMSTONE-302 study showed that Cejemly in combination with chemotherapy demonstrated further improvement in PFS and the risk of disease progression or death was reduced by 52%, together with a trend of OS benefits. Data were presented in a Mini Oral Presentation (Late-Breaking Abstract) at the IASLC 2021 World Conference on Lung Cancer.