On March 26, 2025 Sapience Therapeutics, Inc., a clinical-stage biotechnology company focused on the discovery and development of peptide therapeutics to address oncogenic and immune dysregulation that drive cancer, reported four poster presentations at the American Association for Cancer Research (AACR) (Free AACR Whitepaper) Annual Meeting 2025, taking place April 25-30, 2025, in Chicago, Illinois (Press release, Sapience Therapeutics, MAR 26, 2025, View Source [SID1234651492]). Sapience will present non-clinical results from both of its clinical programs, lucicebtide (formerly known as ST101), a first-in-class antagonist of C/EBPβ, and ST316, a first-in-class antagonist of β-catenin and its co-activator, BCL9, as well as results from its preclinical Fra1 antagonist peptide (FraAP) program, a first-in-class antagonist of the activator protein 1 (AP-1) complex.

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"We are thrilled to be presenting a compendium of non-clinical data supportive of our clinical and preclinical SPEARs programs, including lucicebtide, ST316, and our FraAP program, at the upcoming AACR (Free AACR Whitepaper) Annual Meeting," said Jim Rotolo, Ph.D., Sapience’s Chief Scientific Officer. "Results from our lucicebtide and ST316 studies further elucidate their respective mechanisms of action and highlight their potential for combination strategies. Additionally, preclinical data demonstrate the potential of our FraAP program to induce anti-cancer activity by targeting the AP-1 complex, particularly in head and neck squamous cell carcinoma."

Poster Presentation Details and Abstract Highlights:

Title: "The clinical C/EBPβ antagonist peptide lucicebtide synergizes with molecularly targeted therapies in GBM"
Session Title: Targeted Therapies and Combinations 1
Location: Poster Section 34
Abstract Number: 839
Date and Time: Sunday, April 27, 2025, 2:00 pm – 5:00 pm CDT
Abstract Summary:

In non-clinical studies, the mechanism of lucicebtide, which has previously demonstrated antitumor activity via direct cell death and immune activation within the tumor microenvironment, enabled a synthetic lethal effect with molecularly targeted therapeutics, such as EGFR inhibitors, that are typically not effective when used as monotherapies for the treatment of glioblastoma (GBM). Transcriptional analysis utilizing GBM genetics and signatures of C/EBPβ activity were performed to identify potential target populations likely to benefit from lucicebtide combinations.
Title: "FraAP, a peptide antagonist against the activator protein 1 transcription factor complex, demonstrates cancer cell cytotoxicity and reduced invasion in vitro and tumor regression in vivo in HNSCC models"
Session Title: Gene Regulation and Transcription Factors 2
Location: Poster Section 10
Abstract Number: 1415
Date and Time: Monday, April 28, 2025, 9:00 am – 12:00 pm CDT
Abstract Summary:

FraAP selectively binds to and inhibits key oncogenic drivers of the AP-1 transcription factor complex, resulting in the suppression of AP-1 driven pathways required for cancer cell cycle progression, proliferation, and invasion and promotes apoptosis in preclinical studies. Further, in a head and neck squamous cell carcinoma (HNSCC) xenograft model, administration of FraAP results in significant tumor growth inhibition, further demonstrating the anti-cancer potential of targeting the AP-1 complex.
Title: "An ex vivo organoid study to identify biomarkers of sensitivity to ST316, a clinical-stage β-catenin antagonist peptide"
Session Title: Biomarkers and Molecular Targets for Prevention
Location: Poster Section 43
Abstract Number: 2361
Date and Time: Monday, April 28, 2025, 9:00 am – 12:00 pm CDT
Abstract Summary:

Analysis of 60 patient-derived tumor organoids revealed that tumors with TP53 WT and mutations in the MAPK pathway significantly correlate with sensitivity to ST316, a β-catenin antagonist peptide. Further, in non-clinical models, combining ST316 with encorafenib, a BRAF inhibitor, showed synergistic effects in BRAFV600E-mutant colorectal cancer (CRC) organoids, demonstrating a promising combination approach in this poor prognosis and underserved patient population. Across studies, findings support rational combinations of ST316 with clinically relevant MAPK inhibitors.
Title: "Reprogramming of MDSCs by ST316, a clinical peptide antagonist of β-Catenin/BCL9, enhances anti-tumor immuno- and chemotherapy"
Session Title: Modifiers of Tumor Microenvironment
Location: Poster Section 30
Abstract Number: 3275
Date and Time: Monday, April 28, 2025, 2:00 pm – 5:00 pm CDT
Abstract Summary:

Results reveal a novel role for Wnt/β-catenin signaling in myeloid-derived suppressor cell (MDSC) biology, a key mediator of immune-suppression, whereby antagonism of β-catenin with ST316 leads to suppression of MDSC expansion. In combination studies, ST316 significantly enhances the anti-tumor efficacy of anti-PD-1 immunotherapy and standard-of-care chemotherapies for advanced CRC such as FOLFIRI. While anti-PD-1 and FOLFIRI alone each resulted in expansion of immunosuppressive MDSCs, combination with ST316 prevented this expansion. These data suggest that therapeutically targeting the β-catenin/BCL9 interaction may be an effective strategy to enhance both chemotherapy and immunotherapy in Wnt-driven tumors that respond poorly to monotherapy.
More information can be found on the AACR (Free AACR Whitepaper) Annual Meeting 2025 website.

About Lucicebtide (formerly known as ST101)
Lucicebtide, a first-in-class antagonist of C/EBPβ, has completed the main portion of a Phase 2 dose expansion study in recurrent GBM (rGBM) (NCT04478279). An ongoing window-of-opportunity sub-study is evaluating lucicebtide in combination with radiation and temozolomide in patients with newly diagnosed GBM (ndGBM) and as a monotherapy in patients with rGBM, with patients receiving ST101 before and after surgical resection in both cohorts. ST101 has been granted Fast Track designation for rGBM from the U.S. Food and Drug Administration (U.S. FDA) and orphan designations for glioma from the U.S. FDA and the European Commission.

About ST316
ST316 is a first-in-class antagonist of the interaction between β-catenin and its co-activator, BCL9, a complex responsible for driving oncogene expression and immune exclusion in multiple cancers where aberrant Wnt/β-catenin pathway signaling is observed. ST316 exposure in cancer cells prevents BCL9-driven nuclear localization of β-catenin and formation of the enhanceosome protein complex. Disruption of this interaction selectively suppresses the transcription of oncogenic Wnt target genes that regulate proliferation, migration, invasion and the metastatic potential of tumor cells, as well as genes that regulate the immunosuppression of the tumor microenvironment. ST316 creates a pro-immune tumor microenvironment and in preclinical models has shown to be synergistic with checkpoint inhibition. Due to its selectivity and downstream modulation of the Wnt/β-catenin pathway, ST316 presents an opportunity to safely and effectively target Wnt/β-catenin driven pathologies without the toxicities previously seen with other Wnt pathway agents.

ST316-101 (NCT05848739) is a first-in-human, open-label, Phase 1-2 Dose Escalation and Expansion study designed to determine the safety, tolerability, PK, PD and early efficacy of ST316. The Phase 1 Dose Escalation portion of the study tested various dose levels of ST316 in patients with select advanced solid tumors that are known to harbor abnormalities of the Wnt/β-catenin signaling pathway, including colorectal cancer (CRC). ST316 is currently being tested in the Phase 2 portion of the study in CRC patients in combination with relevant standards of care and in multiple lines of treatment. The U.S. Food and Drug Administration (U.S. FDA) has granted Orphan Drug Designation to ST316 for the treatment of familial adenomatous polyposis (FAP).

On March 26, 2025 Hoth Therapeutics, Inc. (NASDAQ: HOTH), a biopharmaceutical company focused on developing first-in-class therapies for allergic and inflammatory diseases, reported two major developments in the ongoing advancement of its proprietary antisense oligonucleotide (ASO) cancer fighting drug candidate, HT-KIT (Press release, Hoth Therapeutics, MAR 26, 2025, View Source [SID1234651491]).

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The Company has filed amended claims with the U.S. Patent and Trademark Office for its lead ASO technology targeting MS4A6A and FcεRIβ—genes implicated in allergic inflammation and mast cell-related diseases. These refined claims enhance intellectual property protection for HT-KIT and further position it as a novel therapeutic platform with broad clinical potential, including use in treating conditions such as anaphylaxis, mastocytosis, and allergic asthma.

In parallel, Hoth has initiated a GLP-compliant 4-week intravenous toxicity study with a 14-day recovery period in C57BL/6 mice. This preclinical study, conducted in partnership with OnTargetx R&D Inc. and ITR Laboratories, is designed to evaluate the safety profile of HT-KIT in support of upcoming regulatory filings. The study will include multiple dose groups, detailed pathology assessments, and pharmacokinetic profiling.

"These strategic milestones mark significant momentum for HT-KIT as we move toward clinical readiness, "said Robb Knie, CEO of Hoth Therapeutics. "The strengthened patent position and robust preclinical package will be instrumental as we explore partnerships and advance our discussions with regulators."

Next Steps in Development

Hoth Therapeutics is committed to advancing HT-KIT toward clinical evaluation. The company is currently conducting additional preclinical studies to further validate HT-KIT’s efficacy and safety profile, with plans to initiate regulatory discussions for first-in-human trials.

On March 26, 2025 Antengene Corporation Limited ("Antengene", SEHK: 6996.HK), a leading innovative, commercial-stage global biopharmaceutical company dedicated to discovering, developing and commercializing first-in-class and/or best-in-class medicines for hematologic malignancies and solid tumors, reported that it will release results from four preclinical studies in poster presentations at the 2025 American Association for Cancer Research (AACR) (Free AACR Whitepaper) Annual Meeting (AACR 2025), taking place from April 25th to 30th at the McCormick Place Convention Center, Chicago, the United States (Press release, Antengene, MAR 26, 2025, View Source [SID1234651490]). These four posters will feature Antengene’s four highly differentiated and high-potential programs, including ATG-201 (CD19 x CD3 TCE) and ATG-042 (MTAPnull-selective PRMT5 Inhibitor), which are poised to enter clinical development in the second half of 2025; ATG-110 (LY6G6D x CD3 TCE), which was developed on the AnTenGagerTM TCE 2.0 platform for the treatment of microsatellite stable colorectal cancer; and a companion diagnostic antibody developed to assess CD24 expression and guide clinical studies of CD24-targeted therapies.

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Details of the Poster Presentation:
ATG-201 (CD19 x CD3 T cell engager)
Title: ATG-201, a novel T-cell engager (TCE) effectively depletes B cells with reduced risk of CRS for the treatment of B cell malignancies and B cell related autoimmune diseases
Abstract Number: 7326
Session Category: Immunology
Session Title: T Cell Engagers and Novel Antibody-Based Therapies
Date: April 30, 2025
Time: 9:00 AM – 12:00 PM (Central Time)
10:00 PM, April 30, 2025 – 1:00 AM, May 1, 2025 (Beijing Time)
Location: Poster Section 40

Introduction: By depleting autoreactive B cells, CD19-targeted CAR-T have shown early yet promising efficacy in treating patients with B cell-driven autoimmune diseases. However, the clinical application of TCE continues to be greatly hindered by the unfavorable pharmacokinetics and toxicity associated with cytokine release syndrome. To overcome these limitations, Antengene developed ATG-201, a "2+1" CD19 x CD3 TCE, which was evaluated in a series of in vitro studies for binding affinity, T cell dependent cytotoxicity (TDCC) cytokine release, and drug developability. The in vivo anti-lymphoma efficacy and pharmacodynamic effect were evaluated in Raji xenograft model. The tissue resident B cell depletion was assessed in CD34+ hematopoietic stem cells humanized mice. Pharmacokinetic parameters of ATG-201 were evaluated in normal Balb/c mice.
Results: Compared to benchmark TCEs, ATG-201 demonstrated stronger naïve B cell depletion activity with much lower cytokine release in vitro. ATG-201 showed potent anti-lymphoma activity in PBMC-humanized subcutaneous Raji xenograft model with significant augment of infiltrated CD8+ T cells in tumor microenvironment and limited proinflammatory cytokines detected in plasma. Single dose ATG-201 completely and deeply depleted B cells in blood, bone marrow and spleen of CD34+ cells humanized mice. ATG-201 demonstrated potent efficacy in mouse systemic lupus erythematosus model, inhibiting the lymph node swelling and auto-antibody producing.
Conclusions: ATG-201 demonstrated CD19-dependent CD3 binding and activation, inducing effective B cell depletion in vitro and in vivo with low cytokine release, which provides potential for the treatment of B cell malignancies and B cell related autoimmune diseases. ATG-201 is poised to enter clinical development in the second half of 2025.
ATG-042 (MTAPnull-selective PRMT5 Inhibitor)
Title: Preclinical characterization of ATG-042, a novel MTAPnull-selective PRMT5 inhibitor
Abstract Number: 4230
Session Category: Experimental and Molecular Therapeutics
Session Title: HDAC and Methyltransferase Inhibitors
Date: April 29, 2025
Time: 9:00 AM – 12:00 PM (Central Time)
10:00 PM, April 29, 2025 – 1:00 AM, April 30, 2025 (Beijing Time)
Location: Poster Section 16

Introduction: Targeting the PRMT5-MTA complex has become a promising strategy for treating MTAPnull cancer in a synthetically lethal manner, avoiding on-target off-tumor hematological toxicity when using first-generation, non-selective PRMT5 inhibitors. Herein, Antengene developed ATG-042, a novel MTAPnull-selective PRMT5 small molecule inhibitor with good brain penetration. In this study, the in vitro activity and MTAP selectivity of ATG-042 were profiled using HCT116 MTAP wild type (wt) cells, HCT116 MTAP knock out (ko) cells and multiple endogenous MTAPnull cell lines. The in vivo efficacy was tested in cell derived xenograft (CDX) mouse models with HCT116 MTAP wt cells, HCT116 MTAP ko cells, LU99 cells (MTAPnull) and U87MG-luc (MTAPnull). The pharmacokinetic and toxicological properties were assessed with corresponding assay methods.
Results: ATG-042 showed excellent anti-proliferative activities on multiple endogenous MTAPnull cell lines with IC50 values between 10nM and 100nM. ATG-042 demonstrated high permeability, good metabolic stability, and low risk of drug-drug interaction. In vivo PK study shows that ATG-042 is well absorbed, with a dose-dependent increase in plasma distribution and high oral bioavailability in mice, SD rats and beagle dogs. Furthermore, ATG-042 is brain-penetrable (B/P ratio=51% in mice; KPuubrain=0.73 in rats). ATG-042 showed robust in vivo efficacy in both subcutaneous CDX models (HCT116 -MTAP ko, LU99) and orthotopic CDX model (U87MG-luc) as a single agent. In addition, ATG-042 also exhibited potential synergy in combination with other drugs for antitumor therapy.
Conclusions: ATG-042 is an oral MTAPnull-selective PRMT5 inhibitor with potent efficacy against MTAPnull tumor. It also demonstrated good tolerability and brain penetrability. ATG-042 is poised to enter clinical development in the second half of 2025.
ATG-110 (LY6G6D x CD3 T cell engager)
Title: ATG-110, a novel "2+1" LY6G6D-targeted T-cell engager (TCE) for the treatment of MSS colorectal cancer
Abstract Number: 3509
Session Category: Immunology
Session Title: T Cell Engagers
Date: April 28, 2025
Time: 2:00 PM – 5:00 PM (Central Time)
3:00 AM – 6:00 AM, April 29, 2025 (Beijing Time)
Location: Poster Section 38

Introduction: Colorectal cancer (CRC) is one of the most common cancers worldwide and requires more effective and safer therapies to improve the poor survival outcome, particularly in patients with microsatellite stable (MSS) colorectal cancer, who exhibit primary resistance to immune checkpoint inhibitors and lack effective treatment options. T cell engagers have shown encouraging efficacy in treating hematological malignancies, while exhibiting suboptimal clinical efficacies in solid tumors. The risk of cytokine release syndrome (CRS) remains as a significant challenge clinically. ATG-110 is a novel "2+1" LY6G6D x CD3 TCE developed by Antengene. In this study, ATG-110 was evaluated in a series of preclinical in vitro studies for binding affinity, T cell activation and cytokine release, T cell dependent cytotoxicity (TDCC), and drug developability. The in vivo anti-tumor efficacy was evaluated in PBMC-humanized immunodeficient NDG mice engrafted with LY6G6Dmedium-expression HT55 or LY6G6Dvery low-expression SW480 MSS CRC cells.
Results: ATG-110 binds to LY6G6D-positive cell lines, including LY6G6D-overexpression 293T, HT55, LS1034, with the nanomolar grade EC50. The CD3 binding site of ATG-110 is concealed by the LY6G6D Fab arm before binding to LY6G6D, due to the steric hindrance. Therefore, ATG-110 demonstrated limited binding capability to CD3+ cells before LY6G6D crosslinking. It activates T cells and induces cytokine release only in the presence of LY6G6D+ cells. In vitro, ATG-110 resulted in potent T cell dependent cytotoxicity with single-digit pM IC50 values on HT55 and SW480 cells. ATG-110 also showed potent anti-tumor activity in PBMC-humanized SW480 xenograft model and exhibited complete response (CR) in PBMC-humanized HT55 xenograft model. Furthermore, ATG-110 also demonstrated good drug developability.
Conclusions: ATG-110 demonstrated LY6G6D-dependent CD3 binding and activation with low risk of CRS. It showed powerful in vitro and in vivo anti-tumor efficacy against colorectal cancer, which warrants further clinical evaluation.
ATG1144 (CD24 CDx Antibody)
Title: Development of a diagnostic antibody for CD24 targeted therapy
Abstract Number: 671
Session Category: Clinical Research
Session Title: Diagnostic Biomarkers 2
Date: April 27, 2025
Time: 2:00 PM – 5:00 PM (Central Time)
3:00 AM – 6:00 AM, April 28, 2025 (Beijing Time)
Location: Poster Section 29

Introduction: CD24 has emerged as a promising therapeutic target for anti-cancer treatment. Several clinical trials are being conducted to evaluate the safety and efficacy of CD24-targeted therapies. Here, Antengene developed and characterized an anti-CD24 diagnostic antibody to enhance the screening and selection of patients based on CD24 expression. In this study, the authors described the discovery of the diagnostic antibody, and the evaluation of accuracy, sensitivity (selectivity), specificity, and assay precision of the antibody.
Results: Monoclonal antibody clone ATG1144 binds to the hCD24 core peptide in ELISA with an EC50 of 0.06 nM. Distinct membrane staining on human normal esophageal tissue FFPE specimens can also be observed with IHC staining using ATG1144. For accuracy assessment, six CDX and twenty human specimens, comprising both positive and negative specimens (including solid tumors and B-cell non-Hodgkin lymphomas), were validated. Samples exhibiting high, medium, and low CD24 expression levels were evaluated for sensitivity and specificity, and the interpreted results aligned with the reference outcomes. FFPE tissues from three distinct patients were evaluated for assay precision assessment. The TMA IHC staining result revealed that 50-80% of patients with lung, breast, bladder, ovarian, or liver cancer have CD24 expression on tumor cell surface with low expression in the para-cancerous normal tissue.
Conclusions: ATG1144 specifically binds to human CD24 with high sensitivity as demonstrated by IHC staining. The development and validation of the method have been finalized using Leica Bond III platforms. These data suggest a potential diagnostic use of ATG1144 for identifying CD24+ patients.

On March 26, 2025 Innovent Biologics, Inc. (Innovent) (HKEX: 01801), a world-class biopharmaceutical company that develops, manufactures and commercializes high-quality medicines for the treatment of cancer, cardiovascular and metabolic, autoimmune, ophthalmology and other major diseases, reported its 2024 annual results, including major business updates, financial performance and the strategy and outlook for 2025 and beyond (Press release, Innovent Biologics, MAR 26, 2025, View Source [SID1234651489]).

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Dr. Michael Yu, Founder, Chairman and CEO of Innovent, stated: "2024 marked a year of historic milestones—Innovent’s Non-IFRS net profit and EBITDA both turned positive for the first time, underscoring our strategic excellence and execution as a pioneer in sustainable biopharmaceutical operations. Meanwhile, we achieved record revenue, expanded our robust product portfolio to 15 approved products and delivered all late-stage development milestones to secure sustained growth momentum. We are also advancing breakthrough innovations in our early-stage pipeline for global opportunities while strengthening both global and local partnerships to accelerate innovation and growth.

With a clear strategy outlined above and a strong track record of execution, we are laying a solid foundation to enter a new phase of growth and global innovation. In the coming years, we aim to achieve RMB20bn product revenue in 2027 and advance five pipeline assets to the global MRCT Phase 3 stage by 2030. Through these efforts, we will evolve into a premier global biopharmaceutical company, delivering long-term value for patients, employees, shareholders and society."

Pioneering profitability with RMB20bn sales target in 2027

First-ever Non-IFRS Positive Profit and EBITDA*
Non-IFRS profit was RMB331.6 million and Non-IFRS EBITDA was RMB411.6 million
The gross profit margin was 84.9%, a year-over-year increase of 2.1 percentage points
The S,G&A expenses ratio was 50.9%, a year-over-year decrease of 7.1 percentage points
R&D expenses were RMB2,499.8million; Cash and short-term financial assets were RMB10,221.1 million, or approximately over USD1.4 billion, providing a solid foundation to our long-term ambitions
Revenue reached new height with solidified oncology leadership
Total revenue reached RMB9,421.9 million, growing by 51.8% year-over-year.
Product sales revenue reached RMB8,227.9 million, growing by 43.6% year-over-year.
Expansion of oncology product portfolio with new indications and broader NRDL coverage and patient access
Building CVM commercialization as another core capability
* Note: The financial numbers mentioned above, unless stated, were based on non-IFRS measure. Detailed disclosure can be found at the Company’s 2024 annual results announcement.

Six new product launches in 2025 with growth momentum anticipated
Three additional approved precision therapies to strengthen lung and hematological cancer franchises:
Dovbleron (taletrectinib) : Potentially best-in-class ROS1 inhibitor
Limertinib: Third-generation EGFR TKI
Jaypirca(pirtobrutinib) : First non-covalent BTK inhibitor launched in China
Build chronic disease as another growth engine:
SINTBILO (tafolecimab injection): First PCSK-9 inhibitor successfully included in the NRDL
SYCUME (Teprotumumab N01 injection): First approved anti-IGF-1R monoclonal antibody, ending a 70-year drought of no new treatment options for thyroid eye disease in China；new studies for front-line treatment and inactive thyroid eye disease in plan
Mazdutide (GCG/GLP-1) : Global first GCG/GLP-1 dual receptor agonist, with two NDAs under NMPA review — first NDA for weight management in obese or overweight populations and second NDA for glycemic control of T2D adults. In addition, new Phase 3 studies are in plan for adolescent obesity, obstructive sleep apnea (OSA) and obesity with metabolic dysfunction-associated fatty liver disease (MAFLD, head-to-head with semaglutide 2.4mg). New clinical studies are also in plan for metabolic dysfunction-associated steatohepatitis (MASH), heart failure with preserved ejection fraction (HFpEF), and higher dose of mazdutide for obesity.
Picankibart (IL-23p19): Potentially best-in-class YTE IL-23p19 monoclonal antibody, with an NDA for moderate-to-severe plaque psoriasis under NMPA review. New studies for psoriasis with prior inadequate response to IL-17, adolescent psoriasis, and psoriatic arthritis(PsA) in plan.
2027 RMB20bn sales target with clear growth trajectory
With ever-growing innovative pipeline, sustainable growth is anticipated to continue even beyond 2027
Embarking on a new era of global innovation

Innovent Academy powers core technology platforms
Robust High-potential Pipeline Targeting 5 Assets in MRCT Phase 3 by 2030
Encouraging data readouts of key pipeline in support of next-step pivotal development
IBI363 (PD-1/IL-2α-bias): Unleashing potential as a next-generation IO therapy with global first-in-class design
Promising Phase 1 results reported in NSCLC, CRC and melanoma, aiming to address some of the most challenge cancer types including IO-failed, PD-L1 low expression and cold tumors;
Two Fast-track Designations from U.S. FDA for IO-treated melanoma and IO-treated squamous NSCLC;
First pivotal clinical trial has been initiated, in head-to-head comparison with pembrolizumab in IO-naïve mucosal and acral melanoma.
IBI343 (CLDN18.2 ADC): Novel Site-specific TOPO1i CLDN18.2 ADC
First MRCT Phase 3 of GC has been initiated in China and Japan
MRCT Phase 1 of PDAC is underway in China and U.S.
NMPA CDE Breakthrough Therapy Designation (BTD) and FDA Fast-track Designation (FTD) granted.
Nearly 10 next-generation programs aiming for global development
Oncology: IBI3009 (DLL3 ADC), IBI3001 (EGFR/B7H3 ADC), and IBI3020 (CEACAM5 dual-payload ADC)
CVM: IBI3016（AGT siRNA）, IBI3032（GLP-1 oral）, IBI3012 (GGG Antibody-peptide conjugate, APC), IBI3030（GGG-PCSK9 APC）
Autoimmune: IBI356 (OX40L) and IBI3002 (IL-4Rα/TSLP)
Hybrid models to accelerate innovation
IBI3009 (DLL3 ADC): global rights granted to Roche, to benefit SCLC patients worldwide
Research innovation showcased at medical conferences, including:
AACR, ASCO (Free ASCO Whitepaper), ESMO (Free ESMO Whitepaper) GI, ESMO (Free ESMO Whitepaper) plenary, ESMO (Free ESMO Whitepaper), WCLC, SITC (Free SITC Whitepaper), ESMO (Free ESMO Whitepaper) Asia for oncology pipeline innovation
ADA, APAO, ICE, CSE for general biomedicine pipeline material progress
Facilities and manufacturing capacity adhering to high-quality standards

Shanghai R&D Center (medical) is newly operational in August 2024
Building U.S. lab in San Francisco
First manufacturing site: 60,000L antibody production capacity and ADC production lines in operation
Second manufacturing site: first phase of 80,000L completed construction
Committed to responsible business practices and enhancing ESG management practices

Innovent has been graded ‘AAA’ rating in MSCI ESG rankings, positioning us at the forefront of the biotechnology industry.
We recently launched our ESG website to further strengthen commitment to sustainability, corporate responsibility and ethical business conduct.
We initiated the "Warmth Stations" program to support frontline urban workers (e.g., sanitation workers, delivery personnel), by providing rest areas and essential supplies. Additionally, we launched the third annual "Children’s Book Donation" campaign, bringing hope and support to underprivileged children through book donations.
We have supported over 200,000 patients through our dedicated patient assistance programs, with drug donations totaling RMB 3.6 billion.
Our commitment to medical philanthropy has been recognized through prestigious awards, including the "Medical Philanthropy Promoter" title and designation as a "China Philanthropic Enterprise".
We were recognized on the "2024 China’s Most Attractive Employers List," with a workforce of 7,000 employees.

On March 26, 2025 IDEAYA Biosciences, Inc. (Nasdaq: IDYA), a leading precision medicine oncology company, reported the publication of abstracts for an oral presentation in the New Drugs on the Horizon series, and three poster presentations on IDE275 (GSK959) at the American Association for Cancer Research (AACR) (Free AACR Whitepaper) Annual Meeting, taking place April 25-30, 2025, in Chicago, Illinois (Press release, Ideaya Biosciences, MAR 26, 2025, View Source [SID1234651488]). IDE275 (GSK959), a potential best-in-class Werner Helicase (WRN) inhibitor, has demonstrated selective preclinical efficacy in the high microsatellite instability (MSI-H) solid tumor setting, and is advancing in a Phase 1 dose escalation trial in partnership with GSK.

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"IDE275 (GSK959) has a potential best-in-class profile and the preclinical data to be presented at AACR (Free AACR Whitepaper) 2025 with GSK highlights the molecule’s selectivity to treat MSI-H solid tumors and potential to be developed clinically as both a monotherapy agent and in combination with PD1," said Yujiro S. Hata, President and Chief Executive Officer, IDEAYA Biosciences. "MSI-H represents a meaningful biomarker-defined population with double-digit percent prevalence observed in multiple solid tumor types, including endometrial, colorectal, and gastric cancers. By binding uniquely to the helicase domain of WRN, IDE275 (GSK959) delivers potent and selective inhibition across MSI-H models," said Michael White, Ph.D., Chief Scientific Officer, IDEAYA Biosciences.

IDE275 (GSK959) was discovered through a collaboration between IDEAYA and GSK. Preclinical studies have demonstrated IDE275’s (GSK959) potential as a best-in-class WRN inhibitor, inducing single-agent tumor regressions in MSI-H patient-derived xenograft (PDX) and cell line-derived xenograft (CDX) models for endometrial, colorectal, and gastric cancers. Notably, MSI-H prevalence in these cancers has been reported at approximately 31%, 20%, and 19%, respectively, underscoring the significant patient population that could benefit from this therapeutic approach.

As part of the collaboration, GSK is responsible for 80% of global research and development costs for IDE275 (GSK959), and IDEAYA is responsible for 20% of such costs. GSK holds a global, exclusive license to develop and commercialize IDE275 (GSK959). IDEAYA has the potential to earn a $10.0 million milestone payment upon initiation of Phase 1 clinical dose expansion. Additionally, IDEAYA is eligible to receive up to $465 million in future late-stage development and regulatory milestone payments. Upon commercialization, IDEAYA will be eligible to receive up to $475.0 million of commercial milestones, 50% of U.S. net profits and tiered royalties on global non-U.S. net sales of the IDE275 (GSK959) – ranging from high single-digit to sub-teen double-digit percentages, subject to certain customary reductions.

At AACR (Free AACR Whitepaper) 2025, IDEAYA will have 8 total presentations across 3 clinical and 2 pre-clinical programs. There will be 4 IDEAYA/GSK presentations of IDE275 (GSK959) and 4 additional presentations across the IDE397/MAT2A, IDE161/PARG, PRMT5, and KAT6/7 programs.

Details for the oral presentation are as follows:
Presenter: Dr. Yanhua Rao, GSK
Title: An innovative and reversible WRN helicase inhibitor, GSK4418959 (IDE275), emerges as a promising clinical candidate for MSI-H cancers
Session: New Drugs on the Horizon Session, Part 3 (DDT003)
Date and Time: Monday, April 28, 2025 at 10:40am CDT
Location: Room S406 (Vista Ballroom) – McCormick Place South (Level 4)

Poster presentation details are below:
Author: Rao, Y. et al.
Title: Patient selection, target engagement and pharmacodynamic markers of WRN inhibitor GSK4418959 (IDE275)
Poster Number: 6393/30
Session Title: Pharmacokinetics and Pharmacodynamics of Cancer Therapeutics
Date and Time: Tuesday, April 29, 2025 at 9:00am – 12:00pm CDT

Author: Lee, Y. et al.
Title: Preclinical Characterization of GSK4418959 (IDE275): A Potent, Selective, and Highly Efficacious WRN Inhibitor for MSI-H Tumors Across Multiple Cancer Types
Poster Number: 2913/20
Session Title: DNA Damage Response and Modulation of DNA Repair 1
Date and Time: Monday, April 28, 2025 at 2:00pm – 5:00pm CDT

Author: Taygerly, P. et al.
Title: Discovery of GSK4418959 (IDE275): A novel, non-covalent, reversible Werner Helicase inhibitor and a new potential therapeutic for the treatment of MSI-H cancers
Poster Number: 5750/50
Session Title: Drug Design, Synthesis, & Disposition
Date and Time: Tuesday, April 29, 2025 at 2:00pm CDT

Author: Gupta, M. et al.
Title: Dual KAT6/7 inhibition disrupts epigenetic programs that promote tumor evolution and adaptive drug resistance
Poster Number: 442/3
Session Title: Epigenetic Targets
Date and Time: Sunday, April 27, 2025 at 2:00pm – 5:00pm CDT

Author: Maskey, R. et al.
Title: PARG inhibition provokes a DNA damage-dependent innate immune reaction that enhances ICI-driven anti-tumor immunity
Poster Number: 2899/6
Session Title: DNA Damage Response and Modulation of DNA Repair 1
Date and Time: Monday, April 28, 2025 at 2:00pm – 5:00pm CDT

Author: Garbett, D. et al.
Title: The allosteric MAT2A inhibitor IDE397 uniquely exploits metabolic liabilities associated with MTAP deletion to perturb DNA replication and repair
Poster Number: 4268/25
Session Title: New and Emerging Cancer Drug Targets
Date and Time: Tuesday, April 29, 2025 at 9:00am – 12:00pm CDT

Author: Aubi, O. et al.
Title: The impact of metabolite kinetics on dysregulation of essential enzymes in cancers with MTAP deficiencies
Poster Number: 4504/15
Session Title: Proteomic Biomarkers and Therapeutics
Date and Time: Tuesday, April 29, 2025 at 9:00am – 12:00pm CDT

The oral presentation and posters will be available online at View Source following the presentations.