Antennova to Present Latest Data of ATN-037 in a Mini Oral Presentation at ESMO Congress 2024

On September 8, 2024 Antennova, a clinical-stage biotech company focused on oncology reported that it will present the latest data of CD73 small molecule inhibitor ATN-037 in a Mini Oral presentation at the 2024 European Society of Medical Oncology (ESMO) (Free ESMO Whitepaper) Congress (ESMO Congress 2024), taking place from September 13th to September 17th at the Fira Barcelona Gran Via in Barcelona, Spain (Press release, Antennova, SEP 8, 2024, View Source [SID1234646411]).

Schedule your 30 min Free 1stOncology Demo!
Discover why more than 1,500 members use 1stOncology™ to excel in:

Early/Late Stage Pipeline Development - Target Scouting - Clinical Biomarkers - Indication Selection & Expansion - BD&L Contacts - Conference Reports - Combinatorial Drug Settings - Companion Diagnostics - Drug Repositioning - First-in-class Analysis - Competitive Analysis - Deals & Licensing

                  Schedule Your 30 min Free Demo!

Details of the Presentation:

ATN-037 (also known as ATG-037, CD73 Oral Small Molecule Inhibitor)

Title: A First-In-Human Phase I/Ib study of ATG-037 Monotherapy and Combination Therapy with Pembrolizumab in Patients with Advanced Solid Tumours – STAMINA-01

Abstract: 6067

Presentation Number: 997MO

Date: September 16, 2024

Time:

10:50 AM – 10:55 AM (Central European Summer Time)

4:50 AM – 4:55 AM (US Eastern Time)

ATN-037 is a highly potent oral small molecule inhibitor of CD73. The STAMINA-01 Phase I/II study is investigating the safety, pharmacokinetics and optimal dose of ATN-037 as a monotherapy or in combination with Merck’s anti-PD-1 therapy KEYTRUDA (pembrolizumab) in patients with refractory/relapsed solid tumors. Antennova has initiated the dose optimization and dose expansion portion of the Phase II STAMINA trial of ATN-037 in Australia and plans to initiate the study in China at the end of October 2024.

As of February 29, 2024, 32 patients have been enrolled, receiving doses ranging from 20mg BID to 600mg BID. 20 of these patients who acquired checkpoint inhibitor (CPI) resistance were treated with combination therapy.
Efficacy data showed that in the 32 patients in the monotherapy group who were all evaluable, 14 achieved stable disease (SD) with a 43.8% disease control rate (DCR). In the 15 evaluable patients among the 20 patients in the combination therapy group, 3 patients (2 with melanoma and 1 with NSCLC) achieved confirmed partial response (PR) and 1 patient with non-small cell lung cancer (NSCLC) achieved unconfirmed PR with an overall response rate (ORR) of 20.0%. Additionally, 9 patients achieved SD, contributing to a 65.0% DCR.

40.6% of patients on monotherapy and 25.0% on combination therapy reported treatment-related adverse events (TRAEs). Only one patient receiving combination therapy experienced a dose-limiting toxicity grade 3 rash, while all other TRAEs were grades 1-2.
The updated results as of July 26, 2024 will be presented in the Mini Oral Session of ESMO (Free ESMO Whitepaper) Congress 2024, scheduled on September 16.
KEYTRUDA is a registered trademark of Merck Sharp & Dohme LLC, a subsidiary of Merk & Co., Inc., Rahway, NJ, USA.

Ascentage Pharma to Present Updated Data of Olverembatinib in Patients with SDH-Deficient GIST during a Mini Oral Presentation at the 2024 ESMO Congress

On September 8, 2024 Ascentage Pharma (6855.HK), a global biopharmaceutical company engaged in discovering, developing and commercializing both first-in-class and best-in-class therapies for malignancies, reported that it will present the latest clinical data of olverembatinib (HQP1351), the company’s novel drug candidate, in patients with succinate dehydrogenase- (SDH-) deficient gastrointestinal stromal tumor (GIST), in a Mini Oral at the 2024 European Society of Medical Oncology (ESMO) (Free ESMO Whitepaper) Congress (Press release, Ascentage Pharma, SEP 8, 2024, View Source;ascentage-pharma-to-present-updated-data-of-olverembatinib-in-patients-with-sdh-deficient-gist-during-a-mini-oral-presentation-at-the-2024-esmo-congress-302241379.html [SID1234646410]).

Schedule your 30 min Free 1stOncology Demo!
Discover why more than 1,500 members use 1stOncology™ to excel in:

Early/Late Stage Pipeline Development - Target Scouting - Clinical Biomarkers - Indication Selection & Expansion - BD&L Contacts - Conference Reports - Combinatorial Drug Settings - Companion Diagnostics - Drug Repositioning - First-in-class Analysis - Competitive Analysis - Deals & Licensing

                  Schedule Your 30 min Free Demo!

As one of the world’s leading and most influential oncology congresses, the ESMO (Free ESMO Whitepaper) Congress showcases the latest results in some of the most cutting-edge cancer research from around the world. This year, the ESMO (Free ESMO Whitepaper) Congress will be held from September 13 to 17 in Barcelona, Spain.

"We are pleased to have this opportunity to showcase olverembatinib’s therapeutic potential for the treatment of SDH-deficient GIST," said Dr. Yifan Zhai, Chief Medical Officer of Ascentage Pharma. "As a third-generation TKI developed in house by Ascentage Pharma, olverembatinib was recently cleared by the China CDE to enter a registrational Phase III study in patients with SDH-deficient GIST. We will expeditiously advance this clinical development program in efforts to bring more treatment options to patients around the world."

Details of the Mini Oral presentation at this year’s ESMO (Free ESMO Whitepaper) Congress are as follows:

Updated efficacy results of olverembatinib (HQP1351) in patients with succinate dehydrogenase (SDH)-deficient gastrointestinal stromal tumors (GIST) and potential mechanisms of action (MOA)

Format: Mini oral
Presentation#: 1722MO
Category: Sarcoma
Date & Time: Friday September 13, 2024, 16:30 – 16:35 CEST
Speaker: Haibo Qiu, MD, PhD, Sun Yat-sen University Cancer Center

Eisai to Present E7386, co-created by PRISM BioLab and Eisai, at the ESMO (European Society for Medical Oncology) Annual Meeting

On September 8, 2024 PRISM BioLab, Co. Ltd. ("PRISM"), a leading discovery and development biotechnology company designing small molecule inhibitors of protein-protein interaction (PPI) targets, reported that the interim analysis of a combination study of E7386(*1), created through collaboration research with Eisai Co., Ltd. ("Eisai"), and Lenvatinib mesylate ( "lenvatinib") (*2) will be presented by Eisai at the European Society for Medical Oncology (ESMO) (Free ESMO Whitepaper) Congress 2024, held in Barcelona, Spain from September 13 to 17, 2024 (Press release, Eisai, SEP 8, 2024, View Source [SID1234646409]). The abstract of the study has been released today.

Schedule your 30 min Free 1stOncology Demo!
Discover why more than 1,500 members use 1stOncology™ to excel in:

Early/Late Stage Pipeline Development - Target Scouting - Clinical Biomarkers - Indication Selection & Expansion - BD&L Contacts - Conference Reports - Combinatorial Drug Settings - Companion Diagnostics - Drug Repositioning - First-in-class Analysis - Competitive Analysis - Deals & Licensing

                  Schedule Your 30 min Free Demo!

To determine the recommended dose of E7386 in combination with Lenvatinib in the open-label Phase Ib study(NCT0400879(*3)), expansion cohort of advanced endometrial cancer patients progressed following platinum-based chemotherapy and anti-PD-(L)1 immunotherapy have been implemented by Eisai. By data cutoff (Mar 7, 2024) in 16 patients, 31% (5 patients) showed the confirmed partial response (decrease of tumor size > 30%), and 31% (5 patients) showed the stable disease (tumor size -30% to +20%).

These results confirmed promising preliminary antitumor activity of E7386 + Lenvatinib with a manageable safety profile. To complete the study, enrollment to the expansion part is ongoing.

(*1) E7386

E7386 is an orally available small molecule CBP/ β-catenin inhibitor that inhibits protein-protein interactions between the transcription factor CBP and β-catenin, and regulates the Wnt signaling. E7386 achieved clinical POC (Proof of concept) in October 2021 and following clinical studies are ongoing including phase I for solid tumors as monotherapy, Phase Ib for solid tumors in combination with tyrosine kinase inhibitor Lenvatinib, Phase Ib/II for solid tumors in combination with pembrolizumab, the anti-PD-1 antibody from Merck & Co., Inc., Rahway, NJ, USA.

(*2) Lenvatinib

Lenvatinib is a multi-kinase inhibitor, discovered by Eisai and being co-developed and co-commercialized under a collaboration agreement with Merck & Co., Inc., Rahway, NJ, USA, which inhibits vascular endothelial growth factor receptors (VEGFRs),VEGFR1, VEGR2, VEGFR3 and fibroblast growth factor receptors (FGFRs), FGFR1, FGFR2, FGFR3, FGFR4, and other receptor tyrosine kinases, PDGFR-alpha, KIT, RET. Lenvatinib have been approved for thyroid cancer, hepatocellular carcinoma, thymic caner and renal cell carcinoma (in combination with Everolimus or pembrolizumab, the anti-PD-1 antibody from Merck & Co., Inc., Rahway, NJ, USA.). Lenvatinib is also approved for endometrium cancer in combination with pembrolizumab

(*3) NCT04008797

NCT04008797 is an open-label Phase Ib study of E7386 in combination with other anticancer drug, Lenvatinib for the patients with solid tumors. The study has been implemented by Eisai in Japan, Korea, Taiwan, US, and France determine the safety and the recommended phase 2 dose (RP2D) and also to see the pharmacokinetics and efficacy of E7386 + Lenvatinib. Enrolment of each cohort of hepatic, colon, endometrial cancers are ongoing.

Perioperative Ivonescimab (PD-1/VEGF) for NSCLC Demonstrated Clinically Significant Phase II Results, Presented in Oral Session at WCLC 2024

On September 8, 2024 Akeso (9926. HK) reported that its internally developed PD-1/VEGF bispecific antibody ivonescimab showed clinically significant results from a Phase II study, either as a monotherapy or in combination with chemotherapy, for the perioperative treatment of resectable non-small cell lung cancer (NSCLC) at the 25th World Conference on Lung Cancer (WCLC) (Press release, Akeso Biopharma, SEP 8, 2024, View Source [SID1234646408]). This marks ivonescimab’s third oral presentation at an international conference in 2024. Professor Zhao Xiaoliang from Tianjin Medical University Cancer Hospital delivered an oral presentation at WCLC, sharing China’s advancements in innovative cancer immunotherapies with global experts.

Schedule your 30 min Free 1stOncology Demo!
Discover why more than 1,500 members use 1stOncology™ to excel in:

Early/Late Stage Pipeline Development - Target Scouting - Clinical Biomarkers - Indication Selection & Expansion - BD&L Contacts - Conference Reports - Combinatorial Drug Settings - Companion Diagnostics - Drug Repositioning - First-in-class Analysis - Competitive Analysis - Deals & Licensing

                  Schedule Your 30 min Free Demo!

As of February 2024, the AK112-205 study enrolled 60 patients, with 78.3% in stage III and 90% in N+ stage (Among N+ stage patients, 70% are in N2 stage). Of these, 49 underwent surgery (all R0 resections). The study results demonstrated that perioperative ivonescimab monotherapy or combined with chemotherapy for resectable NSCLC demonstrated high rates of pathological complete response (pCR) and major pathological response (MPR) in this phase II study.

Compared with ivonescimab monotherapy, rates of MPR and pCR in ivonescimab combined with chemotherapy were numerically higher, and across tumor stage and PD-L1 expression subgroups.

Ivonescimab + chemotherapy cohort: pCR rate was 43.6%, MPR rate was 71.8%. 69.2% of patients are with residual viable tumor (RVT) < 5%.
As of Aug, 2024, 55 patients in this cohort completed surgery, pCR and MPR rates were improved to 52.7% and 72.7%, respectively. For squamous NSCLC, pCR and MPR rates were 63.6% and 84.1%, respectively.
Ivonescimab monotherapy cohort: pCR rate was 30.0%, MPR rate was 60.0%.
Event-Free Survival (EFS) is not mature yet. Related studies have point to a strong correlation between pCR and EFS.

The safety profile was manageable. There were no TRAEs that led to cancelled or delayed surgery or wound healing complications.

About Ivonescimab

Ivonescimab is a novel global first-in-class PD-1/VEGF bi-specific immunotherapy drug internally developed by Akeso. Ivonescimab has been approved in China for treating EGFR mutated locally advanced or metastatic non-squamous NSCLC patients who have progressed after EGFR TKI treatment. It is the world’s first approved bispecific antibody with a "cancer immunotherapy + anti-angiogenesis" synergistic mechanism.

Akeso out-licensed Summit Therapeutics exclusive rights to ivonescimab for the development and commercialization in certain territories including United States, Canada, Europe, Japan, Latin America, Africa and the Middle East. Ivonescimab is known as AK112 within Akeso and SMT112 in the territories licensed to Summit.

Currently, a Phase III study of ivonescimab monotherapy versus pembrolizumab monotherapy as first-line treatment for PD-L1+ NSCLC has met its primary endpoint of progression-free survival (PFS) in an interim analysis, achieving a decisive positive outcome. Based on this study, a supplemental New Drug Application (sNDA) for ivonescimab monotherapy as first-line treatment for PD-L1+ NSCLC has been submitted and granted priority review. Additionally, a Phase III clinical study of ivonescimab combined with chemotherapy versus tislelizumab combined with chemotherapy as first-line treatment for squamous NSCLC is ongoing. The HARMONi study, an international multicenter Phase III clinical study led by Akeso’s partner Summit, is investigating ivonescimab combined with chemotherapy for EGFR-mutated, locally advanced or metastatic nsq-NSCLC that has progressed after third-generation EGFR-TKI therapy. Another international multicenter Phase III study is comparing ivonescimab combined with chemotherapy to pembrolizumab combined with chemotherapy as first-line treatment for squamous NSCLC.

Furthermore, 3 new Phase III clinical studies are either initiated or about to start, including ivonescimab combined with AK117 (CD47) as first-line treatment for PD-L1 positive squamous cell carcinoma of the head and neck (vs. pembrolizumab), ivonescimab combined regimen as first-line treatment for cholangiocarcinoma (vs. durvalumab combined regimen), and ivonescimab combined regimen as first-line treatment for pancreatic cancer. Overall, ivonescimab is engaged in over 25 clinical trials across 17 indications, including lung cancer, pancreatic cancer, breast cancer, hepatocellular carcinoma, and colorectal cancer, through both monotherapy and combination therapy approaches.

Novel computational pathology-based TROP2 biomarker for datopotamab deruxtecan was predictive of clinical outcomes in patients with non-small cell lung cancer in TROPION-Lung01 Phase III trial

On September 8, 2024 r Astrazeneca reported results from an exploratory analysis of the TROPION-Lung01 Phase III trial showed TROP2 as measured by it’s proprietary computational pathology platform, quantitative continuous scoring (QCS), was predictive of clinical outcomes in patients with advanced or metastatic non-small cell lung cancer (NSCLC) who were treated with datopotamab deruxtecan (Dato-DXd) (Press release, AstraZeneca, SEP 8, 2024, View Source [SID1234646406]). In patients with TROP2-QCS biomarker positive tumours, datopotamab deruxtecan demonstrated a meaningfully greater magnitude of efficacy versus docetaxel than in the overall trial population.

Schedule your 30 min Free 1stOncology Demo!
Discover why more than 1,500 members use 1stOncology™ to excel in:

Early/Late Stage Pipeline Development - Target Scouting - Clinical Biomarkers - Indication Selection & Expansion - BD&L Contacts - Conference Reports - Combinatorial Drug Settings - Companion Diagnostics - Drug Repositioning - First-in-class Analysis - Competitive Analysis - Deals & Licensing

                  Schedule Your 30 min Free Demo!

These results will be featured in a Presidential Symposium (PL02.11) at the IASLC 2024 World Conference on Lung Cancer (WCLC) hosted by the International Association for the Study of Lung Cancer.

TROP2 is a protein broadly expressed in NSCLC on the surface of and inside tumour cells.1,2 When assessed using conventional immunohistochemistry (IHC)-based pathology, TROP2 expression has not been predictive of patient responses to TROP2-directed antibody drug conjugates (ADC).3,4 QCS is a fully supervised computational pathology platform, developed by AstraZeneca, that analyses digitised images of patient tissue samples and precisely quantifies targets, like TROP2, on and inside a tumour cell.

Datopotamab deruxtecan is a specifically engineered TROP2-directed DXd ADC discovered by Daiichi Sankyo and being jointly developed by AstraZeneca and Daiichi Sankyo.

In this analysis, QCS was used to analyse tissue samples collected from patients in TROPION-Lung01. This produced a normalised membrane ratio for each tumour cell in each sample. Patients’ tumours were considered TROP2-QCS biomarker positive if the majority (≥75%) of tumour cells exhibited a ratio below a predetermined value (≤0.56), indicating a greater proportion of TROP2 in the cytoplasm.

The analysis showed a greater proportion of patients with nonsquamous NSCLC were considered TROP2-QCS biomarker positive than those with squamous NSCLC (66% versus 44%, respectively). The threshold for biomarker positivity was optimised for progression-free survival (PFS) in the subgroup of patients with nonsquamous NSCLC without actionable genomic alterations because it represents a population with significant unmet medical need and without actionable biomarkers.

In patients with TROP2-QCS biomarker positive tumours (60% of the biomarker evaluable population including patients with nonsquamous and squamous NSCLC), datopotamab deruxtecan reduced the risk of disease progression or death by 43% versus docetaxel (median PFS of 6.9 versus 4.1 months; hazard ratio [HR] 0.57; 95% confidence interval [CI] 0.41-0.79).

By comparison, in the primary analysis of the overall trial population, datopotamab deruxtecan reduced the risk of disease progression or death by 25% versus docetaxel (PFS of 4.4 versus 3.7 months; HR 0.75; 95% CI 0.62-0.91; p=0.004) as presented at the 2023 European Society for Medical Oncology Congress.5

In the subgroup of patients with nonsquamous NSCLC without actionable genomic alterations and with TROP2-QCS biomarker positive tumours, datopotamab deruxtecan reduced the risk of disease progression or death by 48% (PFS of 7.2 versus 4.1 months; HR 0.52; 95% CI 0.35-0.78).

Marina Garassino, MD, The University of Chicago, Professor of Medicine and investigator in the trial, said: "TROP2 is broadly expressed on solid tumour cells, including non-small cell lung cancer, but it has yet to be established as a predictive biomarker for any TROP2-directed antibody drug conjugate. We have shown with this analysis that the more precise quantitative measurement of TROP2 on and inside tumour cells, enabled by AstraZeneca’s computational pathology platform, can identify which patients with non-small cell lung cancer are most likely to benefit from treatment with datopotamab deruxtecan."

Susan Galbraith, Executive Vice President, Oncology R&D, AstraZeneca, said: "This analysis demonstrates the power of our computational pathology platform to discover new predictive biomarkers and substantially improve patient selection for datopotamab deruxtecan. It also has great potential to help more precisely select patients across our broader antibody drug conjugate portfolio. ​We are excited to extend our collaboration with Roche Tissue Diagnostics with the aim of validating this exploratory approach for TROP2, developing the companion diagnostic and bringing it to the clinic as quickly as possible."

Ken Takeshita, MD, Global Head, R&D, Daiichi Sankyo, said: "The results from the QCS analysis support the potential of TROP2, as measured by quantitative continuous scoring, as a predictive biomarker for datopotamab deruxtecan and begin to answer the question of why certain patients with non-small cell lung cancer respond better to treatment. These insights are critical to advancing our understanding of how we can more precisely identify patients with non-small cell lung cancer who may benefit from treatment with our TROP2-directed antibody drug conjugate."

In the biomarker evaluable population, no new safety concerns were identified and rates of Grade 3 or higher treatment-related adverse events (TRAE) were similar regardless of TROP2 status. In patients with TROP2-QCS biomarker positive tumours, Grade 3 or higher TRAEs occurred in 30% and 46% of patients in the datopotamab deruxtecan and docetaxel arms, respectively. The most common Grade 3 or higher TRAEs were stomatitis (7%, 3%) and ocular surface events (3%, 0%). Grade 3 or higher adjudicated drug-related interstitial lung disease events occurred in 3% and 1% of patients in the datopotamab deruxtecan and docetaxel arms, respectively.

AstraZeneca and Roche Tissue Diagnostics collaborate to co-develop and commercialise the TROP2-QCS biomarker companion diagnostic

AstraZeneca and Roche Tissue Diagnostics are extending their existing collaboration to co-develop a novel companion diagnostic incorporating AstraZeneca’s proprietary computational pathology platform, QCS, which will be deployed within Roche’s navify Digital Pathology image management system.

Jill German, Head, Roche Tissue Diagnostics, said: "Our collaboration with AstraZeneca continues to push the boundaries of traditional cancer diagnostics. By developing an innovative Al tool that goes beyond human capabilities, the solution will be able to help determine which cancer patients are most likely to benefit from targeted therapies, potentially improving patient care."

Under this expanded collaboration, Roche Tissue Diagnostics and AstraZeneca will co-develop and commercialise a novel companion diagnostic in Roche’s navify Digital Pathology platform, based on the QCS computational pathology platform, to aid pathologists in interpreting an investigational VENTANA TROP2 assay.

As the leading provider of pathology lab solutions, Roche Tissue Diagnostics is delivering an end-to-end digital pathology workflow from tissue staining to producing high-quality digital images that can be reliably assessed using automated clinical image analysis algorithms.

Notes

Advanced non-small cell lung cancer
Nearly 2.5 million lung cancer cases were diagnosed globally in 2022.6 NSCLC is the most common type of lung cancer, accounting for about 80% of cases.7 Approximately 75% and 25% of NSCLC tumours are of nonsquamous or squamous histology, respectively.8 While immunotherapy and targeted therapies have improved outcomes in the 1st-line metastatic setting, most patients eventually experience disease progression and receive chemotherapy.9-11 For decades, chemotherapy has been the last treatment available for patients with advanced NSCLC, despite limited effectiveness and known side effects.9-11

TROP2 is a protein broadly expressed in the majority of NSCLC tumours.1 There is currently no TROP2-directed ADC approved for the treatment of lung cancer.12,13

TROPION-Lung01
TROPION-Lung01 is a global, randomised, multicentre, open-label Phase III trial evaluating the efficacy and safety of datopotamab deruxtecan (6.0mg/kg) versus docetaxel (75mg/m2) in adult patients with locally advanced or metastatic NSCLC with and without actionable genomic alterations who require systemic therapy following prior treatment. Patients with actionable genomic alterations were previously treated with platinum-based chemotherapy and an approved targeted therapy. Patients without known actionable genomic alterations were previously treated, concurrently or sequentially, with platinum-based chemotherapy and a PD-1 or PD-L1 inhibitor.

The dual primary endpoints of TROPION-Lung01 are PFS as assessed by blinded independent central review (BICR) and OS. Key secondary endpoints include investigator-assessed PFS, objective response rate, duration of response, time to response, disease control rate as assessed by both BICR and investigator, and safety.

TROPION-Lung01 enrolled approximately 600 patients in Asia, Europe, North America, Oceania and South America. For more information visit ClinicalTrials.gov.

Datopotamab deruxtecan (Dato-DXd)
Datopotamab deruxtecan (Dato-DXd) is an investigational TROP2-directed ADC. Designed using Daiichi Sankyo’s proprietary DXd ADC Technology, datopotamab deruxtecan is one of six DXd ADCs in the oncology pipeline of Daiichi Sankyo, and one of the most advanced programmes in AstraZeneca’s ADC scientific platform. Datopotamab deruxtecan is comprised of a humanised anti-TROP2 IgG1 monoclonal antibody, developed in collaboration with Sapporo Medical University, attached to a number of topoisomerase I inhibitor payloads (an exatecan derivative, DXd) via tetrapeptide-based cleavable linkers.

A comprehensive global clinical development programme is underway with more than 20 trials evaluating the efficacy and safety of datopotamab deruxtecan across multiple cancers, including NSCLC, triple-negative breast cancer and HR-positive, HER2-negative breast cancer. The programme includes seven Phase III trials in lung cancer and five Phase III trials in breast cancer evaluating datopotamab deruxtecan as a monotherapy and in combination with other anticancer treatments in various settings.