On March 15, 2023 Elevation Oncology, Inc. (Nasdaq: ELEV), an innovative oncology company focused on the discovery and development of selective cancer therapies to treat patients across a range of solid tumors with significant unmet medical needs, reported that preclinical proof-of-concept data for EO-3021 will be highlighted in an oral presentation at the New Drugs on the Horizon special session at the American Association for Cancer Research (AACR) (Free AACR Whitepaper) Annual Meeting 2023, being held April 14-19, 2023 in Orlando, Florida (Press release, Elevation Oncology, MAR 15, 2023, View Source;utm_medium=rss&utm_campaign=elevation-oncology-to-present-at-the-american-association-of-cancer-research-aacr-annual-meeting-2023 [SID1234628647]). A poster highlighting the preclinical data for EO-3021, a potential best-in-class antibody-drug conjugate (ADC) designed to target Claudin 18.2, will also be presented at the conference.

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"The oral presentation at this year’s AACR (Free AACR Whitepaper) New Drugs on the Horizon session is an exciting opportunity for Elevation Oncology to showcase preclinical data for EO-3021 as a potential best-in-class ADC targeting solid tumors expressing Claudin 18.2.," said David Dornan, Chief Scientific Officer of Elevation Oncology. "In addition, we look forward to presenting the preclinical data in more detail in a poster session at AACR (Free AACR Whitepaper) and remain on track to initiate a U.S. Phase 1 clinical trial evaluating EO-3021 during the second half of 2023."

Elevation Oncology will also present two posters on NRG1 fusions, including updated data from the Phase 2 CRESTONE study evaluating seribantumab in patients with solid tumors harboring NRG1 fusions. Elevation Oncology announced in January 2023 that it has paused enrollment in the Phase 2 CRESTONE study and further investment in seribantumab, pending entering a partnership.

Details of presentations at AACR (Free AACR Whitepaper) 2023 are as follows:

Title: EO-3021: An antibody drug conjugate targeting CLDN18.2 expressing cancers
Presentation: Oral Presentation by David Dornan, Chief Scientific Officer, Elevation Oncology
Session Type: Drug Development Track: Special Session – New Drugs on the Horizon Session: Part 3
Data and Time: Monday, April 17, 2023, 10:15AM-11:45AM ET

Title: Therapeutic potential of EO-3021/SYSA1801, a Claudin18.2 antibody-drug conjugate, for the treatment of CLDN18.2-expressing cancers
Authors: Mo Dan, et al.
Session Type: Poster Presentation
Session: Experimental and Molecular Therapeutics – Growth Factor Receptors as Therapeutic Targets
Abstract Number: 6300
Data and Time: Wednesday, April 19, 2023, 9:00AM-12:00PM ET

Title: Identification of NRG1 fusions in patients with solid tumors: Analysis from a real-world community oncology network
Authors: Emma G. Sturgill, et al.
Session Type: Poster Presentation
Session: Clinical Research Excluding Trials – Analyses Using Clinical and Genomic Databases
Abstract Number: 921
Data and Time: Sunday, April 16, 2023, 1:30PM-5:00PM ET

Title: CRESTONE: A Phase 2 study of seribantumab in adult patients with neuregulin-1 (NRG1) fusion positive locally advanced or metastatic solid tumors
Authors: Tejas Patil, et al.
Session Type: Poster Presentation
Session: Phase II Clinical Trials 2
Abstract Number: CT229
Data and Time: Tuesday, April 18, 2023, 9:00AM-12:30PM ET

On March 14, 2023 Erasca, Inc. (Nasdaq: ERAS), a clinical-stage precision oncology company singularly focused on discovering, developing, and commercializing therapies for patients with RAS/MAPK pathway-driven cancers, reported the company will present a poster presentation at the upcoming American Association for Cancer Research (AACR) (Free AACR Whitepaper) Annual Meeting, taking place April 14-19, 2023, in Orlando, Florida (Press release, Erasca, MAR 14, 2023, View Source [SID1234639360]).

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The abstract will be available on the AACR (Free AACR Whitepaper) meeting website. The poster will be available online at Erasca.com/science/presentations following the presentation.

Poster Presentation Details

Abstract CT184 – Preliminary dose escalation results of ERAS-601 in combination with cetuximab in FLAGSHP-1: A Phase 1 study of ERAS-601, a potent and selective SHP2 inhibitor, in patients with previously treated advanced or metastatic solid tumors
Date/Time: Tuesday, April 18, 2023, 9:00 AM – 12:30 PM ET
Session: First-in-Human Phase I Clinical Trials 2
Presenter: Dr. Meredith McKean, Sarah Cannon Research Institute at Tennessee Oncology
Location: Orange County Convention Center, Poster Section 45, Poster Board 16

On March 14, 2023 Exscientia plc (Nasdaq: EXAI) reported two new wholly-owned precision oncology development candidates, EXS74539 (‘539), an LSD1 inhibitor, and EXS73565 (‘565), a MALT1 protease inhibitor (Press release, Exscientia, MAR 14, 2023, View Source [SID1234635630]). These compounds have been precision designed to improve the potential for patient benefit and solve complex design issues that may limit the probability of success of other compounds in development. IND-enabling studies are underway and the Company expects to provide an update on clinical development plans leveraging Exscientia’s personalised medicine platform in the second half of 2023.

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Both molecules were funded through a 2019 collaboration with Celgene, which was acquired by Bristol Myers Squibb, and each molecule met the criteria for which BMS could exercise its option. Bristol Myers Squibb’s options to the candidates have now lapsed and Exscientia maintains all worldwide rights to both compounds. In 2021, an agreement was signed to expand the collaboration to include additional programmes in oncology and immunology. These programmes are currently in active development.

"Building off of our success with the CDK7, A2A and PKC-theta programmes, these candidates clearly show how our AI-driven precision design platform can solve challenging target profiles in a more efficient way than traditional drug discovery," said Professor Andrew Hopkins, D.Phil., founder and Chief Executive Officer of Exscientia. "Both ‘539 and ‘565 met the primary nonclinical design goals for potency, selectivity, dosing and safety. In addition, these molecules also have the potential for meaningful patient selection strategies to optimise clinical design. We are excited about the promise these compounds hold in a broad range of haematologic and solid tumours."

First potent, selective, reversible and brain-penetrant LSD1 inhibitor: EXS74539 (‘539) is a differentiated lysine demethylase 1 (LSD1) inhibitor with potential in both haematology and oncology. LSD1 demethylates histones which play a critical role in regulating the expression of genes which suppress differentiation and drive the proliferation and survival of a number of tumour types. To date, other LSD1 inhibitors in development have failed to achieve the combination of appropriate pharmacokinetics, good brain penetrance and a reversible mechanism of action. Exscientia’s candidate, ‘539, achieves a design objective of suitable CNS penetration to target brain metastases, which are prevalent in certain cancer subtypes. Additionally, in vivo studies of ‘539 have shown favourable activity in small cell lung cancer (SCLC) xenograft models, with dose dependent inhibition of tumour growth. Studies have also shown a favourable absorption, distribution, metabolism, and excretion (ADME) profile, with a shorter predicted human half-life than some LSD1 inhibitors currently in clinical trials. No safety concerns have been observed in preclinical studies conducted to date. Exscientia will present data on the discovery and development of ‘539 at an upcoming scientific conference in the first half of 2023.

Potent and selective MALT1 protease inhibitor with potential safety differentiation: EXS73565 (‘565) is a mucosa-associated lymphoid tissue lymphoma translocation protein 1 (MALT1) protease inhibitor with potential applications in haematology. MALT1 is a protease crucial for activation of the NF-κB pathway which supports the uncontrolled proliferation of malignant T- and B-cells in haematological cancers. Exscientia’s precision design approach was able to optimise the safety profile for agents targeting MALT1 whilst also generating potency and selectivity. Scaffolds of other MALT1 inhibitors in the clinic significantly inhibit UGT1A1, an enzyme involved in the metabolism of bilirubin, often leading to dose-limiting toxicities in the clinic. In vivo studies of ‘565 have shown anti-tumour activity in mouse models and favourable pharmacokinetics both as monotherapy and in combination with ibrutinib. Toxicology studies have shown that ‘565 has an acceptable therapeutic index, with the ability to maintain high levels of potency, selectivity and safety benchmarks while avoiding meaningful inhibition of UGT1A1, which can lead to hyperbilirubinemia.

"With three existing clinical programmes already in the pipeline, we feel very confident we will meet our goal of four clinical stage compounds in 2024," said Prof. Hopkins. "Our vision is to change the way drug design, discovery and development is done, as we have shown in our first eight drug candidates. Over the course of 2023, we expect to provide more details on these programmes as well as on our broader internal and partnered pipeline."

On March 14, 2023 Defence Therapeutics Inc. ("Defence" or the "Company"), reported that it has signed a Collaboration Agreement with Orano Support SAS on behalf of Orano SA ("Orano"), a world-renowned multinational company, headquartered in Chatillon, France, to develop the next generation of radio-immunoconjugates for radio-immunotherapy using Defence’s intracellular targeting technology (Press release, Defence Therapeutics, MAR 14, 2023, View Source [SID1234635131]).

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The novel concept is to develop new targeted radiotherapies by combining the ability of biological molecules (e.g. an antibody) to target cancer cells with the use of radioactive elements as a means to destroy them, in combination with Defence’s intracellular targeting technology to increase the efficacy.

Under the Agreement, Defence will develop the first radio-immuno-conjugates therapy based on Auger electron emitter by combining Defence’s intracellular targeting expertise and radiochemistry expertise provided by Orano. Auger electron emitter radionuclide, such as Indium111 will be used. This type of radioactive element needs to be very close to DNA for inducing DNA Damage and cell death. Defence’s intracellular targeting technology could be the ultimate solution to improve the therapeutic efficacity of Auger electron radionuclide. The best results should lead to an optimize product from which a GLP tox studies will then be planned accordingly.

With existing antibody-conjugate drugs, a clinical issue with radio-immuno-conjugates to improve is their low intracellular drug delivery to cancer cells, which may cause resistance and recurrence. With the radio-immuno-conjugates using Auger emitters such as 111In is that their efficacies are dependent to their proximity to the DNA. Combining Defence’s AccumTM technology to the radioimmuno-conjugate is expected to amplify the therapeutic index of the drug while minimizing side effects observed in patients undergoing the therapy. Defence’s AccumTM platform has been developed and tested in vitro and in vivo in animals to enhance the intranuclear drug delivery on multiple FDA approved antibody-conjugates or new conjugates under development.

"We have a long-standing knowledge and experience working and developing our AccumTM platform technology, including in the antibody-conjugate therapeutics field, and we definitely believe that Orano, with its international expertise, represents a strong collaborator for the development of the next generation of radio-immuno-conjugates using Defence’s intracellular targeting technology to increase the efficacy in targeting tumoral cancer cells" said Sebastien Plouffe, Chief Executive Officer of Defence Therapeutics. "We look forward to the continued advancement of our AccumTM-expanding pipeline," he added.

According to The Insight Partners, the Radiopharmaceuticals Market is projected to reach US$ 13.818 billion by 2028 from US$ 7.55 billion in 2021; it is expected to grow at a CAGR of 9.0% during 2021–2028. And the global cancer immunotherapy market is expected to reach USD 196.45 billion by 2030, registering CAGR of 7.2% during the forecast period, according to a report by Grand View Research, Inc.

Verastem has filed a 10-K – Annual report [Section 13 and 15(d), not S-K Item 405] with the U.S. Securities and Exchange Commission .

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