PI3K Inhibitors Clinical Trials Analysis 2025: Pipeline Analysis, Competitive Landscape, Emerging Therapies, Companies, and Future Outlook by DelveInsight

PI3K Inhibitors Clinical Trials

DelveInsight’s ‘PI3K Inhibitors Pipeline Insight 2025’ report provides comprehensive global coverage of pipeline PI3K inhibitors in various stages of clinical development, major pharmaceutical companies are working to advance the pipeline space and future growth potential of the PI3K inhibitors pipeline domain.

PI3K inhibitors are primarily used in the treatment of various cancers, including breast cancer, lymphoma, and leukemia. With the global burden of cancer expected to rise due to factors like aging populations and lifestyle changes, chemotherapy’s limitations impacting patient adherence led to a transition from traditional chemotherapy to targeted therapies in cancer treatment. With growing demand for targeted therapies, competitive dynamics within the pharmaceutical industry, coupled with favorable regulatory environments and efforts to improve healthcare infrastructure and access, there will likely be a growing demand for effective cancer treatments, including PI3K inhibitors.

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Key Takeaways from the PI3K Inhibitors Pipeline Report

• DelveInsight’s PI3K inhibitors pipeline report depicts a robust space with 20+ active players working to develop 25+ pipeline PI3K inhibitors.
• Key PI3K inhibitors companies such as TG Therapeutics, Pfizer, Relay Therapeutics, Curis, AUM Biosciences, Onconova Therapeutics, Kazia Therapeutics, Rhizen Pharmaceuticals, The Menarini Group, Inflection Biosciences, Totus Medicines, Hoffman-La-Roche, BeiGene, HUTCHMED, Nanjing Zenshine Pharmaceuticals, ARTham Therapeutics, Scorpion Therapeutics, Sumitomo Pharma America, BridgeBio Pharma, Novartis, Haihe Biopharma, Faeth Therapeutics, Shanghai Yingli Pharmaceutical, Chia Tai Tianqing Pharmaceutical Group Co., Ltd., GlaxoSmithKline, and others are evaluating new PI3K Inhibitors drugs to improve the treatment landscape.
• Promising pipeline PI3K inhibitors such as Umbralisib, Gedatolisib, RLY 2608, Fimepinostat, AUM 302, Rigosertib, Paxalisib, Tenalisib, MEN1611, IBL-202, TOS-358, Inavolisib, BGB-10188, Amdizalisib, ZX-4081, ART 001, STX 478, TP 3654, BBO 10203, BYL719, CYH33, Serabelisib, Linperlisib, TQ-B3525, GSK2636771, and others are under different phases of PI3K inhibitors clinical trials.
• In October 2025, Ensem Therapeutics, Inc. (ENSEM) today announced the U.S. Food and Drug Administration (FDA) granted Fast Track designation to its clinical stage pan mutant-specific allosteric PI3Kα inhibitor and degrader, ETX-636, for the treatment of adult patients with PIK3CA-mutant, hormone receptor positive (HR+)/human epidermal growth factor negative (HER2-) advanced breast cancer.
• In August 2025, Celcuity Inc. (Nasdaq: CELC), a clinical-stage biotechnology company pursuing development of targeted therapies for oncology, today announced the U.S. Food and Drug Administration (“FDA”) agreed to accept its New Drug Application (“NDA”) for gedatolisib in HR+/HER2- advanced breast cancer (“ABC”) for review under the Real-Time Oncology Review (“RTOR”) program, which facilitates earlier submission of topline efficacy and safety results, prior to the submission of the complete application, to support an earlier start to the FDA’s evaluation of the application. Celcuity is expected to initiate in September a rolling submission to the FDA of its NDA for gedatolisib, based on topline data from the PIK3CA wild-type cohort of the Phase 3 VIKTORIA-1 clinical trial. Completion of the NDA submission is targeted for the fourth quarter of 2025.
• In February 2025, Kazia executed an agreement to evaluate paxalisib in the next-Generation aGile Genomically Guided Glioma platform (5G) study. The 5G study is an academic trial conducted by the Drug Development Unit – Investigator Initiated Team and sponsored by the Institute of Cancer Research, London and fully funded by Cancer Research UK and the Australian charity, Minderoo Foundation. Every patient in this study will have their genome sequenced, enabling researchers to target their treatment with greater precision. Patients with PI3k/mTOR related mutations will be enrolled to receive paxalisib once a day.
• In March 2024, BeiGene, Ltd. announced the presentation of emerging oncology pipeline data at the American Association for Cancer Research (AACR) Annual Meeting April 5-10 in San Diego. BeiGene has nine abstracts scheduled for poster presentations at AACR. An additional clinical presentation includes the first data from a Phase Ia dose escalation study of BGB-10188, a phosphatidylinositol 3 kinase delta (PI3Kδ) inhibitor, plus tislelizumab in patients with solid tumors.
• In December 2023, Genentech a member of the Roche Group announced positive results from the Phase III INAVO120 study of the investigational therapy, inavolisib, in combination with palbociclib (Ibrance) and fulvestrant as a potential first-line treatment option for people with PIK3CA-mutated, hormone receptor (HR)-positive, HER2-negative, endocrine-resistant, locally advanced or metastatic breast cancer.
• In October 2023, the FDA had granted permission to proceed with clinical investigations of Roginolisib in the United States, according to iOnctura. It is currently being developed for patients with solid and hematologic malignancies, including uveal melanoma. Roginolisib is the first novel allosteric modulator of PI3K and utilizes a unique binding mode that when combined with high selectivity for PI3K. It is expected to improve safety and tolerability relative to that of earlier generation inhibitors.
• In July 2023, the FDA granted fast track designation to paxalisib plus radiotherapy as a treatment for solid tumor brain metastases with PI3K pathway mutations.
• In May 2023, Scorpion Therapeutics announced that the first patient has been dosed in a Phase I/II first-in-human dose escalation and expansion clinical trial evaluating STX-478, Scorpion’s highly differentiated, allosteric and central nervous-system (“CNS”) penetrant inhibitor of mutant phosphoinositide-3-kinase alpha (“PI3Kα”), for the treatment of HR+/HER2- breast cancer and other solid tumors.
• In April 2023, Totus Medicines presented four posters at the American Association for Cancer Research (AACR) Annual Meeting, regarding its lead program, TOS-358, the first highly specific, covalent PI3Kα inhibitor.

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PI3K Inhibitors Overview

Phosphoinositide 3-kinase (PI3K) inhibitors are a class of targeted therapeutic agents that have garnered significant attention in the field of cancer research and treatment. The PI3K pathway plays a crucial role in regulating cell growth, survival, proliferation, and metabolism, making it an attractive target for cancer therapy. Aberrant activation of the PI3K pathway is a common occurrence in many types of cancers, contributing to tumor development, progression, and resistance to conventional therapies.

PI3K inhibitors work by blocking the activity of one or more isoforms of PI3K enzymes. There are four main isoforms of PI3K: class I and class II. Class IA PI3Ks are the most frequently implicated in cancer, particularly the p110α subunit encoded by the PIK3CA gene. By inhibiting PI3K, these inhibitors aim to disrupt the signaling cascade downstream of PI3K, which includes the well-known protein kinase AKT and the mammalian target of rapamycin pathway. This signaling network regulates various cellular processes, including cell growth, survival, metabolism, and angiogenesis.

PI3K inhibitors have shown promising results in preclinical studies and clinical trials, particularly in cancers where the PI3K pathway is hyperactive due to genetic mutations. However, challenges remain, including drug resistance, off-target effects, and the need for patient stratification based on molecular markers. Combination therapies, such as combining PI3K inhibitors with other targeted agents or immune checkpoint inhibitors, are being explored to enhance their efficacy and overcome resistance.

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PI3K Inhibitors Competitive Landscape

A snapshot of the Pipeline PI3K Inhibitors Drugs mentioned in the report:

Learn more about the emerging PI3K inhibitors @ PI3K Inhibitors Clinical Trials and FDA Approvals

PI3K Inhibitor Emerging Drugs Summary

Gedatolisib (Celcuity):

A dual PI3K/mTOR inhibitor targeting all class I PI3K isoforms and both mTORC1/2 complexes. Its broad inhibition helps overcome resistance seen with isoform-specific agents. Gedatolisib has shown promising efficacy and manageable toxicity in combination therapies for hormone receptor–positive, HER2-negative metastatic breast cancer patients who progressed after CDK4/6 inhibitors. It is currently in Phase III trials for breast cancer.

TBO-309 (ThromBio):

A potent, selective PI3Kβ inhibitor that prevents platelet activation and aggregation while minimizing bleeding risk. Unlike conventional antiplatelets, it offers a wide therapeutic window and can be safely combined with other anticoagulants. Proof-of-concept and Phase I studies confirmed its efficacy and safety in reducing arterial thrombosis. It is in Phase II development for ischemic stroke and tandem occlusion.

TL117 (Suzhou Teligene):

An oral PI3K inhibitor with potential antitumor activity. By blocking the PI3K/Akt pathway, it inhibits tumor cell growth and survival, addressing resistance linked to PI3K dysregulation. TL117 is currently in Phase I/II trials for head and neck squamous cell carcinoma.

Scope of the PI3K Inhibitors Pipeline Report

• Coverage: Global
• Therapeutic Assessment By Product Type: Mono, Combination, Mono/Combination
• Therapeutic Assessment By Clinical Stages: Discovery, Pre-clinical, Phase I, Phase II, Phase III
• Therapeutics Assessment By Route of Administration: Infusion, Intradermal, Intramuscular, Intranasal, Oral, Parenteral, Subcutaneous, Topical
• Therapeutics Assessment By Molecule Type: Gene therapies, Small molecule, Vaccines, Polymers, Peptides, Monoclonal antibodies
• Key PI3K Inhibitors Companies: TG Therapeutics, Pfizer, Relay Therapeutics, Curis, AUM Biosciences, Onconova Therapeutics, Kazia Therapeutics, Rhizen Pharmaceuticals, The Menarini Group, Inflection Biosciences, Totus Medicines, Hoffman-La-Roche, BeiGene, HUTCHMED, Nanjing Zenshine Pharmaceuticals, ARTham Therapeutics, Scorpion Therapeutics, Sumitomo Pharma America, BridgeBio Pharma, Novartis, Haihe Biopharma, Faeth Therapeutics, Shanghai Yingli Pharmaceutical, Chia Tai Tianqing Pharmaceutical Group Co., Ltd., GlaxoSmithKline, and others
• Key PI3K Inhibitors Pipeline Therapies: Umbralisib, Gedatolisib, RLY 2608, Fimepinostat, AUM 302, Rigosertib, Paxalisib, Tenalisib, MEN1611, IBL-202, TOS-358, Inavolisib, BGB-10188, Amdizalisib, ZX-4081, ART 001, STX 478, TP 3654, BBO 10203, BYL719, CYH33, Serabelisib, Linperlisib, TQ-B3525, GSK2636771, and others

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Table of Contents

1. PI3K Inhibitors Pipeline Report Introduction

2. PI3K Inhibitors Pipeline Report Executive Summary

3. PI3K Inhibitors Pipeline: Overview

4. Analytical Perspective In-depth Commercial Assessment

5. PI3K Inhibitors Clinical Trial Therapeutics

6. PI3K Inhibitors Pipeline: Late-Stage Products (Pre-registration)

7. PI3K Inhibitors Pipeline: Late-Stage Products (Phase III)

8. PI3K Inhibitors Pipeline: Mid-Stage Products (Phase II)

9. PI3K Inhibitors Pipeline: Early-Stage Products (Phase I)

10. PI3K Inhibitors Pipeline Therapeutics Assessment

11. Inactive Products in the PI3K Inhibitors Pipeline

12. Company-University Collaborations (Licensing/Partnering) Analysis

13. Key Companies

14. Key Products in the PI3K Inhibitors Pipeline

15. Unmet Needs

16. Market Drivers and Barriers

17. Future Perspectives and Conclusion

18. Analyst Views

About DelveInsight

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