On October 9, 2024 Zai Lab Limited (NASDAQ: ZLAB; HKEX: 9688; "Zai Lab") reported that data from a Phase 1 study of ZL-1310, the Company’s investigational antibody-drug conjugate (ADC), will be presented during a plenary session at the EORTC-NCI-AACR (Free EORTC-NCI-AACR Whitepaper) Symposium (ENA) 2024 taking place October 23-25, in Barcelona, Spain (Press release, Zai Laboratory, OCT 9, 2024, View Source [SID1234647122]). The preliminary results from the ongoing, open-label, multicenter clinical trial (NCT06179069) will address the potential of ZL-1310 as a novel treatment for small cell lung cancer (SCLC).

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DLL3 is overexpressed in many neuroendocrine tumors, including SCLC, and is typically associated with poor clinical outcomes. ZL-1310 comprises a humanized anti-DLL3 antibody and a novel camptothecin derivative as its payload. The compound was designed with a novel linker-payload platform called TMALIN, which leverages the tumor microenvironment to overcome challenges associated with first-generation ADC therapies.

"New therapies that reduce off-target toxicity and increase anti-tumor effectiveness are critically needed to improve treatment options for many cancer patients, including SCLC and other tumors of neuroendocrine origin," said Rafael G. Amado, M.D., President, Head of Global Research and Development, Zai Lab. "ZL-1310 is an example of our company’s commitment to progressing a differentiated global oncology pipeline that will help fill these types of treatment gaps and provide meaningful benefit to patients. We look forward to sharing preliminary results from the Phase 1 study of this exciting next-generation ADC at ENA 2024."

Details regarding the ZL-1310 oral presentation at ENA 2024 are as follows:

Title: Preliminary Results from a Phase 1a/1b, Open-Label, Multicenter Study of ZL-1310, a DLL3-targeted ADC, to Evaluate the Safety, Tolerability, and Pharmacokinetics in Subjects with Small Cell Lung Cancer
Abstract Number: ENA24-0345
Presenter: Alex Spira, MD, PhD, FACP, FASCO, Virginia Cancer Specialists, Fairfax, VA
Presentation Date and Time: Thursday, October 24, 2024, 11:12 a.m. – 11:24 a.m. CET (presentation), 11:24 a.m. – 11:30 a.m. CET (Q&A)
Location: Centre de Convencions Internacional de Barcelona (CCIB), Room 111 and 112

On October 9, 2024 BullFrog AI Holdings, Inc. (NASDAQ: BFRG; BFRGW) ("BullFrog AI" or the "Company"), a technology-enabled drug development company using artificial intelligence (AI) and machine learning to enable the successful development of pharmaceuticals and biologics, reported the publication of new research in the peer-reviewed journal Cell Reports supporting the potential of BullFrog AI’s drug candidate, BF-114 (SPTBN1 siRNA), in treating a range of liver diseases, including metabolic dysfunction-associated steatotic liver disease (MASLD), metabolic dysfunction-associated steatohepatitis (MASH), and hepatocellular carcinoma (HCC) (Press release, Bullfrog AI, OCT 9, 2024, View Source [SID1234647105]). The research was generated in a study led by Lopa Mishra, MD, professor of medicine, Merinoff Endowed Chair and co-director of the Institute for Bioelectronic Medicine at Feinstein Institutes for Medical Research at Northwell Health, Cold Spring Harbor Laboratory.

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"This research strengthens the scientific foundation for BF-114 and its potential role in addressing complex liver diseases," said Vin Singh, CEO of BullFrog AI. "Dr. Mishra’s work offers compelling evidence that our approach could change the treatment landscape for these metabolic disorders."

Dr. Mishra’s research demonstrates that β2-spectrin, a protein encoded by the SPTBN1 gene, mediates the effects of environmental factors that drive the progression of MASH. By reducing β2-spectrin levels, BF-114 has been shown to halt the progression of MASLD and MASH in animal models, while also reducing liver damage.

These findings strengthen and extend previously published data from Dr. Mishra’s laboratory that support BullFrog AI’s development of BF-114 for the treatment of obesity and liver diseases.

BullFrog AI plans to leverage its proprietary AI-driven platform to analyze single-cell data from animal models and human patients. This analysis will provide additional mechanistic understanding of the effects of SPTBN1 silencing in obesity and liver disease. The insights gained are expected to inform the continued development of BF-114 and may potentially reveal additional therapeutic applications.

BullFrog AI is also pleased to welcome Dr. Mishra to its Scientific Advisory Board. Dr. Mishra will provide guidance as the Company advances its BF-114 program. Dr. Mishra received her MBBS from the University of London and completed fellowships in Medicine and Gastroenterology at Royal Northern/Whittington Hospital (London), Mount Sinai Medical Center, and Johns Hopkins Hospital. With over 100 peer-reviewed publications relevant to the field and an H-Index of 66, her expertise will be instrumental in guiding the continued development of BF-114.

Dr. Mishra commented, "I am excited to join BullFrog AI’s Scientific Advisory Board and continue our work in targeting SPTBN1. The combination of BullFrog AI’s approach to drug development and the promising results we’ve seen with BF-114 provides a strong foundation for the continued exploration of its potential in treating obesity and liver diseases. I look forward to contributing to the advancement of BF-114 and exploring its multiple therapeutic possibilities."

On October 9, 2024 Exscientia plc (Nasdaq: EXAI) reported three abstracts to be presented at the 36th EORTC-NCI-AACR (Free EORTC-NCI-AACR Whitepaper) (ENA) Symposium 2024 from October 23-25, in Barcelona, Spain (Press release, Exscientia, OCT 9, 2024, View Source [SID1234647123]).

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"As our precision-designed LSD1 and MALT1 inhibitors continue to progress towards the clinic, we are excited to share new preclinical data from both programmes," said David Hallett, Ph.D., interim Chief Executive Officer and Chief Scientific Officer of Exscientia. "These posters, as well as an additional focus on our assay development, highlight the potential of our platform to design best-in-class molecules with improved properties. As our state-of-the-art automation facility continues to ramp up in scale, we look forward to further accelerating the design and development of future molecules."

The ENA posters will be available on the Exscientia website from their time of presentation.

Poster Presentations
Title: Combining next-generation BTK and MALT1 inhibitors to enhance efficacy and therapeutic utility in B-cell malignancies
Session Title: Combination therapies
Catalog Number: 218
Poster Board Number: PB206
Date/Time: Thursday, October 24 / 9:00 a.m. – 5:30 p.m. CEST

EXS73565 (‘565) is a potent, selective allosteric MALT1 inhibitor designed to have an improved safety profile, with clinical studies expected to start in early 2025
Combining MALT1 inhibitors, such as ‘565, with BTK inhibitors has the potential to provide enhanced efficacy in B-cell malignancies, by greater inhibition of pathogenic nuclear factor-kappa B (NF-kB) signalling and addressing BTK-resistance mechanisms
Exscientia researchers combined ‘565 with the BTK inhibitor zanubrutinib and observed deeper, more durable efficacy responses in xenograft models of B-cell malignancies, with long-lasting tumour eradication seen for activated B-cell-like diffuse large B-cell lymphoma (ABC-DLBCL)
Studies also confirmed target pathway biology engagement, with ‘565 alone and in combination with zanubrutinib inhibiting NF-kB target gene expression in in vivo models
Overall, the selective profiles of ‘565 and zanubrutinib may maximise the therapeutic index of MALT1 and BTK inhibition in combination, providing scope for enhanced efficacy for patients with B-cell malignancies
Title: In vivo pharmacokinetics, pharmacodynamics and anti-tumour efficacy of EXS74539: A novel, reversible LSD1 inhibitor for acute myeloid leukaemia
Session Title: Epigenetic modulators (HDAC bromodomain modulators, EZH2)
Catalog Number: 250
Poster Board Number: PB238
Date/Time: Thursday, October 24 / 9:00 a.m. – 5:30 p.m. CEST

‘539 is a novel, potent, selective and reversible LSD1 inhibitor, with a highly differentiated profile and designed to be brain penetrant, expected to enter the clinic in early 2025
The poster highlights that by combining ex vivo perturbation of primary human acute myeloid lymphoma (AML) samples with ‘539 and omics profiling, 12 potential pharmacodynamic (PD) biomarker gene candidates were identified that correlate with LSD1 inhibitor activity
Upregulation of the identified biomarker gene candidates was confirmed in an in vivo AML xenograft model post ‘539 treatment
Treatment of the in vivo model with the reversible inhibitor ‘539 resulted in limited platelet level effects, highlighting how ‘539 was designed to maximise target engagement while limiting thrombocytopenia
Title: Xcellomics: Powering rapid translation of HTS outputs to AI-driven drug discovery programmes
Session Title: Functional genomics
Catalog Number: 414
Poster Board Number: PB402
Date/Time: Friday, October 25 / 9:00 a.m. – 3:00 p.m. CEST

Xcellomics is a collaboration between Exscientia and The Centre for Medicines Discovery at the University of Oxford, used to rapidly translate the results of cell-based, high-throughput screens into transformative oncology therapies
The collaboration has successfully identified and validated novel essential regulators of a key oncogenic pathway
Automated assay development and chemical hit ID performed by Exscientia rapidly pushed these novel therapeutic targets into drug discovery programmes

On October 9, 2024 Olema Pharmaceuticals, Inc. ("Olema" or "Olema Oncology", Nasdaq: OLMA), a clinical-stage biopharmaceutical company focused on the discovery, development, and commercialization of targeted therapies for women’s cancers, reported that it will be presenting multiple posters during the 36th EORTC-NCI-AACR (Free EORTC-NCI-AACR Whitepaper) Symposium on Molecular Targets and Cancer Therapeutics (ENA 2024) taking place October 23-25, 2024, in Barcelona, Spain (Press release, Olema Oncology, OCT 9, 2024, View Source [SID1234649115]).

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Details of the ENA 2024 poster presentations are:

Title: Combining palazestrant, a CERAN, and everolimus, an mTOR inhibitor, enhances tumor suppression in ER+/HER2- breast cancer models
Poster/Abstract: 211
Session: Poster Session 300, Exhibition Hall
Date/Time: Thursday, October 24, 2024, from 09:00 to 17:30 CEST

Title: Combining palazestrant, a CERAN, and capivasertib, a pan-AKT inhibitor, enhances tumor suppression in ER+/HER2- breast cancer models
Poster/Abstract: 212
Session: Poster Session 300, Exhibition Hall
Date/Time: Thursday, October 24, 2024, from 09:00 to 17:30 CEST

Title: Combining OP-3136, a KAT6 inhibitor, with endocrine therapy and CDK4/6 inhibitor enhances anti-tumor activity in ER+/HER2- breast cancer models
Poster/Abstract: 230
Session: Poster Session 300, Exhibition Hall
Date/Time: Thursday, October 24, 2024, from 09:00 to 17:30 CEST

Additional information, including abstracts for these presentations, can be found on the ENA website. Copies of the posters will be made available on the Publications page of Olema’s website in alignment with the Symposium’s embargo policy.

About Palazestrant (OP-1250)
Palazestrant (OP-1250) is a novel, orally-available small molecule with dual activity as both a complete estrogen receptor (ER) antagonist (CERAN) and selective ER degrader (SERD). It is currently being investigated in patients with recurrent, locally advanced or metastatic ER-positive (ER+), human epidermal growth factor receptor 2-negative (HER2-) breast cancer. In clinical studies, palazestrant completely blocks ER-driven transcriptional activity in both wild-type and mutant forms of metastatic ER+ breast cancer and has demonstrated anti-tumor efficacy along with attractive pharmacokinetics and exposure, favorable tolerability, CNS penetration, and combinability with CDK4/6 inhibitors. Palazestrant has been granted U.S. Food and Drug Administration (FDA) Fast Track designation for the treatment of ER+/HER2- metastatic breast cancer that has progressed following one or more lines of endocrine therapy with at least one line given in combination with a CDK4/6 inhibitor. It is being evaluated both as a single agent in an ongoing Phase 3 clinical trial, OPERA-01, and in Phase 1/2 combination studies with CDK4/6 inhibitors (palbociclib and ribociclib), a PI3Ka inhibitor (alpelisib), and an mTOR inhibitor (everolimus). For more information on OPERA-01, please visit www.opera01study.com.

On October 9, 2024 Can-Fite BioPharma Ltd. (NYSE American: CANF) (TASE: CANF), a biotechnology company advancing a pipeline of proprietary small molecule drugs that address oncological and inflammatory diseases, reported the Company’s oncology drug candidate, Namodenoson, has been granted Orphan Drug Designation by the U.S. Food and Drug Administration (FDA) for the indication of pancreatic cancer, one of the most aggressive malignancies (Press release, Can-Fite BioPharma, OCT 9, 2024, View Source [SID1234647106]). The designation as an orphan drug will provide among others, potential for market exclusivity for seven years after approval and several and regulatory advantages (View Source)

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Can-Fite is now completing all the preparatory work for a Phase II study in patients with pancreatic cancer. The study will be a multicenter open-label trial in patients with advanced pancreatic adenocarcinoma whose disease has progressed on at least 1st-line therapy. The trial will evaluate the safety, clinical activity, and pharmacokinetics (PK) of Namodenoson in this patient population. All patients will receive oral Namodenoson 25 mg, administered twice daily for consecutive 28-day cycles. Patients will be evaluated regularly for safety. Approximately 20 evaluable patients will be enrolled. The primary objective of this trial is to characterize the safety profile of Namodenoson, and the secondary objective is to evaluate the clinical activity as determined by the Objective Response Rate (ORR) using Response Evaluation Criteria in Solid Tumors (RECIST 1.1), Progression-Free Survival (PFS), Disease Control Rate (DCR), Duration of Response (DoR), and Overall Survival (OS).

"We are advancing our plans to start our Phase 2 study in pancreatic cancer and aim to commence the study by the end of year; we are thrilled that the FDA has granted Orphan Drug Status," stated Can-Fite CEO Motti Farbstein".

About Namodenoson

Namodenoson is a small orally bioavailable drug that binds with high affinity and selectivity to the A3 adenosine receptor (A3AR), on the surface of liver and pancreatic cancer cells. Namodenoson, induces apoptosis of these cancer cell types. Namodenoson was evaluated in Phase II liver cancer trials for two indications, as a second line treatment for hepatocellular carcinoma, and as a treatment for non-alcoholic fatty liver disease (NAFLD) and non-alcoholic steatohepatitis (NASH). A3AR is highly expressed in diseased cells whereas low expression is found in normal cells. This differential effect accounts for the excellent safety profile of the drug.