Bicycle Therapeutics Announces Significant Progress Across Multiple Therapeutic Programs Beyond Oncology

On March 30, 2021 Bicycle Therapeutics plc (NASDAQ: BCYC), a biotechnology company pioneering a new and differentiated class of therapeutics based on its proprietary bicyclic peptide (Bicycle) technology, reported progress updates for its Bicycle-based partnered programs outside of oncology (Press release, Bicycle Therapeutics, MAR 30, 2021, View Source [SID1234577366]).

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"Over the last five years, Bicycle’s strategy has been to use our novel technology to discover and develop a pipeline of innovative assets in oncology while additionally using non-dilutive funding and collaborations to explore the therapeutic potential of Bicycles in disease areas outside of oncology. Today, for the first time, we are providing an overview on our progress in demonstrating the broad utility of this platform to create molecules with the potential to treat some of the most serious diseases and address future healthcare challenges," said Kevin Lee, Ph.D., Chief Executive Officer of Bicycle Therapeutics. "It’s incredibly exciting to see how the Company has worked innovatively and highly collaboratively with many diverse institutions to address these challenges and, at the same time, generated significant revenues to offset the costs of developing and progressing our internal oncology pipeline. I would like to thank all of our collaborators for their enthusiasm in this endeavor and look forward to continuing our work to advance these important molecules."

Bicycle has achieved the first milestone in its collaboration with Dementia Discovery Fund (DDF) and the University of Oxford’s ARUK Oxford Drug Discovery Institute (ODDI)

The Company identified and optimized nM affinity Bicycles to TREM2, a genetically validated target for the treatment of dementia, and nM affinity Bicycles to transferrin receptor 1 (TfR1), a molecular shuttle. In 2019, Bicycle established a collaboration with DDF, later expanded to include ODDI, to use Bicycle technology for the discovery and development of potential novel therapeutics for the treatment of dementia. The three parties are collaborating to identify and characterize Bicycles that bind to and activate TREM2, a genetically validated dementia target. As part of the collaboration, Bicycle is also using its technology to identify binders to TfR1, a blood brain barrier transporter, that could potentially enable delivery of Bicycles, or any other molecular payload, into the central nervous system (CNS), or other organ systems, expressing TfR1. Under the terms of the collaboration with DDF, Bicycle retains all rights to the TfR1 molecules outside of the license granted for use with targets defined within the DDF collaboration.
Bicycle advances platform in multiple anti-infective areas, including antimicrobials and antivirals

Innovate UK’s Biomedical Catalyst (BMC) awarded the Company funding to advance a Bicycle inhibitor for a key cell wall biosynthesis target in Enterobacterales, Penicillin Binding Protein 3 (PBP3). Bicycle is using its proprietary platform to try to address the significant healthcare challenge of antimicrobial resistance and has identified several potential Bicycle PBP3 inhibitors. Through grants awarded by the UK government and in collaboration with investigators at the University of Warwick, Bicycle intends to progress these PBP3 inhibitors, potentially representing the first novel class of antibiotics identified in decades, to candidate and initial toxicology testing.
Innovate UK, under a specific program targeting key technologies to rapidly respond to the challenge of COVID-19 (UKRI Ideas to Address COVID-19 – Innovate UK Article 25), provided funding to support Bicycle’s efforts to discover new healthcare solutions to the SARS-CoV-2 pandemic. Bicycle has identified numerous discrete families of Bicycles which bind to at least 10 different epitopes on the SARS-CoV-2 spike protein, binders to the Nucleocapsid protein and the viral attachment site on the host ACE2 human receptor. Through Bicycle’s partnership with researchers at the MRC Laboratory of Molecular Biology, Bicycles identified by these screens have demonstrated nanomolar activity in inhibiting SARS-CoV-2 infection of human lung cells. These monomeric Bicycles have been conjugated together to make a diverse range of bi-paratopic and multi-valent small molecules (less than 10kD), some of which are active in the picomolar range in viral entry assays and may be resistant to the current SARS-CoV-2 variants of concern. Bicycle continues to advance these novel compounds in pre-clinical evaluation. Bicycle has also formed partnerships with diagnostic experts to evaluate its novel SARS-CoV-2 binding Bicycles in Lateral Flow Tests and other diagnostic screening formats.
Bicycle has made significant progress through partnerships with biopharmaceutical therapeutic area leaders in indications outside of oncology

The Company has successfully discovered and advanced targets outside of oncology through the ongoing collaboration with AstraZeneca, a global biopharmaceutical company, to discover novel agents for the treatment of respiratory and cardiometabolic diseases. Two assets have been transitioned to AstraZeneca for further development and are currently being progressed in their discovery pipeline. Two additional assets achieved transition criteria and were transitioned to AstraZeneca but were returned to Bicycle by AstraZeneca.
Bicycle has also identified targets in its collaboration with Bioverativ (acquired by Sanofi in 2018) for the treatment of rare hematological diseases. The Bioverativ collaboration successfully identified nM multi-valent inhibitors to P-Selectin, which inhibited human neutrophil binding and rolling, with potential applications in sickle cell disease and other inflammatory diseases. The Bioverativ collaboration also identified the first small molecule Factor VIII mimetic for the potential treatment of Hemophilia A. This mimetic is comprised of a multivalent Bicycle binding to both Factor IX and Factor X, leading to the production of activated Factor X (FXa), which successfully activated thrombin in plasma from Hemophilia A patients ex vivo. In 2019, Sanofi elected not to pursue further development, and the collaboration agreement was terminated. These "lead stage" assets have now been returned to Bicycle.
Kevin Lee commented, "With four Bicycle molecules now in clinical trials for both oncology and non-oncology indications, the technology has shown initial evidence of clinical tolerability and suitability for pharmaceutical development, and I look forward to seeing how Bicycles may bring important new treatment opportunities to poorly served patients in additional therapeutic areas."

Repare Therapeutics to Introduce RP-6306, a Potent and Specific Inhibitor of a Novel Target, at Virtual Investor Day on April 8

On March 30, 2021 Repare Therapeutics Inc. ("Repare" or the "Company") (Nasdaq: RPTX), a leading clinical-stage precision oncology company enabled by its proprietary synthetic lethality approach to the discovery and development of novel therapeutics, reported it will host a virtual Investor Day on Thursday, April 8, 2021, from 10:30 a.m. to 12:00 p.m. Eastern Time (Press release, Repare Therapeutics, MAR 30, 2021, View Source [SID1234577382]). Repare Therapeutics’ executive management team will be joined by two distinguished physicians:

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Carol Aghajanian, MD, Chief, Gynecologic Medical Oncology Service, Professor of Medicine, Weill Cornell Medical College, Memorial Sloan Kettering Cancer Center, New York, NY
Timothy Yap, MBBS, PhD, FRCP, Medical Director, Institute for Applied Cancer Science, Associate Professor, Department of Investigational Cancer Therapeutics, Division of Cancer Medicine, MD Anderson Cancer Center, Houston, TX
The event will focus on RP-6306, a potent and selective inhibitor of a novel target that is synthetic lethal with CCNE-1 amplification. The Company expects to begin a Phase 1 clinical trial in the second quarter of 2021, one quarter earlier than prior guidance.

To access the event virtual event, please dial (833) 638-9655 (U.S. and Canada) or (602) 585-9856 (international) at least 10 minutes prior to the start time and refer to conference ID 1093819. A live video webcast will be available in the Investor section of the Company’s website at View Source A webcast replay will also be available on the corporate website at the conclusion of the call.

About RP-6306

RP-6306 is the result of Repare’s proprietary drug discovery program for tumors with genetic alterations characterized by CCNE1 amplification, which typically do not respond well to platinum or PARP inhibitor treatment. Through Repare’s SNIPRx screen campaign for targets that are SL with CCNE1 amplification, the Company has identified and validated a novel SL gene that is believed to have the characteristics of a therapeutic target. Subsequently, the Company developed novel and selective inhibitors against the target that have repeatedly demonstrated compelling anti-tumor activity and announced the advancement of a clinical candidate for this potential first-in-class program. Repare anticipates initiating a Phase 1 clinical trial for RP-6306 in the second quarter of 2021. This trial is expected to enroll patients suffering from recurrent tumors characterized by CCNE1 amplification and other genomic alterations predicted to be sensitive to RP-6306. The primary objective of the trial is to establish the recommended Phase 2 dose and schedule for RP-6306 for further studies as monotherapy and to assess preliminary safety in patients. An additional trial is planned to evaluate combination with approved anticancer agents.

Novartis expands targeted radioligand therapy pipeline with in-license for compounds targeting Fibroblast Activation Protein (FAP)

On March 30, 2021 Novartis reported that it has obtained exclusive worldwide rights to develop and commercialize therapeutic applications for a library of Fibroblast Activation Protein (FAP) targeting agents including FAPI-46 and FAPI-74, through an assignment agreement with iTheranostics, Inc., an affiliate of SOFIE Biosciences, Inc (Press release, Novartis, MAR 30, 2021, View Source [SID1234577323]). The FAP assets were originally developed at the University of Heidelberg. The agreement also includes co-exclusive rights for Novartis to develop imaging applications for these assets.

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Fibroblast activation protein (FAP) is a cell-surface protein expressed at low levels in most normal adult tissues, but over-expressed in common cancers, particularly on cancer-associated fibroblasts that form the tumor stroma, which is essential for growth1,2,3,4. High FAP expression on cancer-associated fibroblasts is generally associated with worse prognosis in solid tumors due to promotion of tumorigenesis and progression4,5,6,7.

"We continue to invest in radioligand therapy as one of the four unique platforms of Novartis Oncology. We believe working across multiple approaches is the key to reimagining cancer care," said Susanne Schaffert, PhD, President, Novartis Oncology. "FAP is an exciting target and these agents are a great fit with our radioligand therapy pipeline, which we are actively investigating across multiple tumor types. We believe this technology has the potential to transform many patients’ lives."

Targeted radioligand therapy is a type of precision medicine combining two key elements: a targeting compound, or ligand, and a radioactive isotope, causing DNA damage that inhibits tumor growth and replication. These targeted drugs bind to markers or proteins over-expressed by certain tumors, or tumor-associated tissue, such as stroma. Due to the high-affinity of these agents for specific tumor cells or associated tumor tissue, surrounding healthy tissue is less affected.

Amgen to Acquire Rodeo Therapeutics Corporation

On March 30, 2021 Amgen Inc. (NASDAQ:AMGN) and Rodeo Therapeutics Corporation (Rodeo) reported an agreement under which Amgen will acquire Rodeo, a privately held biopharmaceutical company based in Seattle that develops small-molecule therapies designed to promote regeneration and repair of multiple tissues (Press release, Amgen, MAR 30, 2021, View Source [SID1234577351]). Rodeo’s 15-PGDH program is a strong strategic fit with Amgen’s inflammation portfolio and efforts to develop first-in-class therapeutics for patients.

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Under terms of the agreement, Amgen will acquire all outstanding shares of Rodeo in exchange for a $55 million upfront payment as well as future contingent milestone payments potentially worth up to an additional $666 million in cash. The transaction has been approved by the shareholders and the Board of Directors of Rodeo.

Rodeo is focused on developing first-in-class, orally available modulators of prostaglandin biology that play an important role in tissue regeneration and repair. Rodeo’s lead 15-prostaglandin dehydrogenase (15-PGDH) modulators have generated compelling data in extensive preclinical studies and have clinical potential in multiple indications.

"The enzyme 15-PGDH plays a key role in many disease-relevant processes such as stem cell self-renewal and epithelial barrier repair. Given the encouraging preclinical data to date, we are excited about the opportunity to develop a novel therapy with potential in a range of important inflammatory disease indications," said Raymond Deshaies, Ph.D., senior vice president of Global Research at Amgen.

Thong Q. Le, president and chief executive officer of Rodeo commented, "We are thrilled that Amgen recognizes the potential value and differentiated profile of our 15-PGDH inhibitor program. With decades of experience in developing, manufacturing and commercializing innovative therapies for patients suffering from a broad range of immunologic diseases and conditions, Amgen is ideally positioned to rapidly advance our program into the clinic."

Cooley LLP acted as legal advisor to Rodeo and Gunderson Dettmer LLP acted as legal advisor to Amgen on this transaction.

Ascendis Pharma A/S Announces Participation at the J.P. Morgan 10th Annual Napa Valley Biotech Forum

On March 30, 2021 Ascendis Pharma A/S (Nasdaq: ASND), a biopharmaceutical company that utilizes its innovative TransCon technologies to create product candidates that address unmet medical needs, reported that the company will participate at the J.P. Morgan 10th Annual Napa Valley Biotech Forum (Press release, Ascendis Pharma, MAR 30, 2021, View Source [SID1234577367]). Company executives will provide a business overview and an update on the Company’s pipeline programs.

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Details

Event J.P. Morgan 10th Annual Napa Valley Biotech Forum
Location Virtual
Date Tuesday, March 30, 2021
Time 4:00 p.m. Eastern Time
A live audio webcast of the presentation will be available on the Investors and News section of the Company’s website at www.ascendispharma.com. A webcast replay will also be available on the Company’s website shortly after conclusion of the event for 30 days.