PI3K Inhibitors Market & Clinical Trials Outlook: Evaluating 25+ Drug Candidates Across 20+ Active Companies by DelveInsight

PI3K Inhibitors Pipeline

DelveInsight’s “PI3K Inhibitors Pipeline Insight” delivers an extensive global assessment of PI3K inhibitors currently under clinical development across various stages. The report highlights how major pharmaceutical and biotechnology companies are actively strengthening this therapeutic domain, underscoring its long-term growth prospects and innovation potential.

PI3K inhibitors are predominantly utilized in oncology, particularly for conditions such as breast cancer, lymphoma, and leukemia. As cancer incidence continues to rise worldwide—driven by aging populations, environmental factors, and lifestyle changes—the limitations of conventional chemotherapy, including toxicity and reduced patient compliance, have accelerated the shift toward targeted therapies. Growing demand for precision oncology, combined with competitive industry dynamics, supportive regulatory policies, and expanding healthcare access, is expected to fuel sustained demand for effective targeted agents such as PI3K inhibitors.

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Key Highlights from the PI3K Inhibitors Pipeline Report

• DelveInsight’s analysis reveals a dynamic and competitive PI3K inhibitors landscape, with more than 20 active companies collectively developing over 25 pipeline candidates.
• Major developers including TG Therapeutics, Pfizer, Relay Therapeutics, Curis, AUM Biosciences, Onconova Therapeutics, Kazia Therapeutics, Rhizen Pharmaceuticals, The Menarini Group, Inflection Biosciences, Totus Medicines, 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 actively advancing novel PI3K inhibitor therapies aimed at improving cancer treatment outcomes.
• High-potential pipeline assets 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 being evaluated across multiple phases of clinical development.
• In October 2025, Ensem Therapeutics, Inc. announced that the U.S. FDA granted Fast Track designation to ETX-636, a clinical-stage, mutant-selective allosteric PI3Kα inhibitor and degrader, for the treatment of adult patients with PIK3CA-mutant, hormone receptor–positive (HR+), HER2-negative advanced breast cancer.
• In August 2025, Celcuity Inc. disclosed that the FDA accepted its New Drug Application (NDA) for gedatolisib in HR+/HER2- advanced breast cancer under the Real-Time Oncology Review (RTOR) pathway. This program allows earlier submission of key efficacy and safety data to expedite regulatory review. Celcuity planned to initiate a rolling NDA submission in September 2025, based on topline results from the Phase III VIKTORIA-1 trial, with full submission expected by Q4 2025.
• In February 2025, Kazia entered into an agreement to assess paxalisib within the next-generation aGile Genomically Guided Glioma (5G) study. This investigator-initiated academic trial, sponsored by the Institute of Cancer Research in London and funded by Cancer Research UK and the Minderoo Foundation, employs comprehensive genomic sequencing to enable precision treatment selection. Patients harboring PI3K/mTOR pathway alterations are eligible to receive once-daily paxalisib.
• In March 2024, BeiGene announced the presentation of new oncology pipeline data at the AACR Annual Meeting held in San Diego. The company scheduled nine poster presentations, including first-in-human data from a Phase Ia dose-escalation study of BGB-10188, a PI3Kδ inhibitor, in combination with tislelizumab for solid tumors.
• In December 2023, Genentech (a Roche Group company) reported positive Phase III results from the INAVO120 study evaluating inavolisib in combination with palbociclib and fulvestrant as a potential first-line therapy for patients with PIK3CA-mutated, HR-positive, HER2-negative, endocrine-resistant advanced or metastatic breast cancer.
• In October 2023, iOnctura announced that the FDA cleared clinical trials of roginolisib in the United States. The drug is being developed for both solid and hematologic malignancies, including uveal melanoma. Roginolisib is a first-in-class allosteric PI3K modulator with a novel binding mechanism designed to enhance selectivity, safety, and tolerability compared with earlier-generation inhibitors.
• In July 2023, the FDA granted Fast Track designation to paxalisib combined with radiotherapy for the treatment of solid tumor brain metastases associated with PI3K pathway mutations.
• In May 2023, Scorpion Therapeutics announced dosing of the first patient in a Phase I/II clinical trial evaluating STX-478, an allosteric, CNS-penetrant inhibitor of mutant PI3Kα, for HR+/HER2- breast cancer and other solid tumors.
• In April 2023, Totus Medicines presented four posters at the AACR Annual Meeting highlighting its lead candidate, TOS-358, the first highly selective covalent PI3Kα inhibitor.

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PI3K Inhibitors: Therapeutic Overview

Phosphoinositide 3-kinase (PI3K) inhibitors represent a critical class of targeted therapies that have gained substantial traction in oncology research and drug development. The PI3K signaling pathway plays a central role in regulating cellular growth, proliferation, survival, metabolism, and angiogenesis, making it a compelling therapeutic target in cancer.

Dysregulation or hyperactivation of the PI3K pathway—often driven by genetic mutations such as PIK3CA alterations—is frequently observed across multiple tumor types and contributes to disease progression, therapeutic resistance, and poor clinical outcomes.

PI3K inhibitors exert their effects by suppressing the activity of one or more PI3K enzyme isoforms. Among the four PI3K classes, Class IA PI3Ks—particularly the p110α catalytic subunit—are most commonly implicated in oncogenesis. Inhibition of PI3K disrupts downstream signaling through AKT and mTOR pathways, ultimately impairing tumor cell growth, survival, and metabolic adaptation.

While PI3K inhibitors have demonstrated encouraging efficacy in both preclinical and clinical settings, challenges such as resistance mechanisms, off-target toxicities, and the need for biomarker-driven patient selection remain. To address these limitations, combination strategies involving PI3K inhibitors with other targeted agents or immunotherapies are actively being explored.

Learn more about PI3K-targeted therapies through the @ PI3K Inhibitors Competitive Landscape

PI3K Inhibitors Competitive Landscape

• Umbralisib: TG Therapeutics
• Rigosertib: Onconova Therapeutics
• Fimepinostat: Curis
• BGB-10188: BeiGene

Emerging PI3K Inhibitors: Drug ProfilesGedatolisib (Celcuity)

Gedatolisib is a dual PI3K/mTOR inhibitor that targets all Class I PI3K isoforms as well as mTORC1 and mTORC2. Its broad mechanism helps overcome resistance associated with isoform-selective inhibitors. The drug has demonstrated favorable efficacy and tolerability in combination regimens for HR+/HER2- metastatic breast cancer patients following CDK4/6 inhibitor therapy and is currently in Phase III clinical development.

TBO-309 (ThromBio)

TBO-309 is a selective PI3Kβ inhibitor designed to reduce platelet activation and thrombosis risk while maintaining a wide therapeutic window. Unlike traditional antiplatelet agents, it minimizes bleeding risk and supports combination use with anticoagulants. The drug has progressed through proof-of-concept and Phase I studies and is now in Phase II trials for ischemic stroke.

TL117 (Suzhou Teligene)

TL117 is an orally administered PI3K inhibitor with potential antitumor activity through blockade of the PI3K/AKT signaling pathway. By targeting PI3K-driven resistance mechanisms, TL117 is being evaluated in Phase I/II trials for head and neck squamous cell carcinoma.

Explore additional pipeline and regulatory insights via PI3K Inhibitors Clinical Trials and FDA Approvals

Scope of the PI3K Inhibitors Pipeline Report

• Geographic Coverage: Global
• Therapeutic Classification: Monotherapy, combination therapy, mono/combination
• Development Stages: Discovery, preclinical, Phase I, Phase II, Phase III
• Routes of Administration: Oral, intravenous, intramuscular, subcutaneous, intradermal, intranasal, topical, parenteral, infusion
• Molecule Types: Small molecules, monoclonal antibodies, peptides, gene therapies, vaccines, polymers
• Key Companies: TG Therapeutics, Pfizer, Relay Therapeutics, Curis, AUM Biosciences, Onconova Therapeutics, Kazia Therapeutics, Rhizen Pharmaceuticals, The Menarini Group, Inflection Biosciences, Totus Medicines, 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 Pipeline Drugs: 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

Access in-depth insights on emerging PI3K inhibitors @ PI3K Inhibitors Drugs in Pipeline

Table of Contents

1. PI3K Inhibitors Pipeline Report – Introduction
2. Executive Summary
3. PI3K Inhibitors Pipeline Overview
4. In-depth Analytical and Commercial Assessment
5. Clinical Trial Therapeutics Analysis
6. Late-Stage Pipeline Products (Pre-registration)
7. Late-Stage Pipeline Products (Phase III)
8. Mid-Stage Pipeline Products (Phase II)
9. Early-Stage Pipeline Products (Phase I)
10. Therapeutics Assessment Framework
11. Inactive and Discontinued Pipeline Assets
12. Company–Academia Collaborations and Licensing Analysis
13. Key Market Players
14. Leading Pipeline Products
15. Unmet Medical Needs
16. Market Drivers and Challenges
17. Future Outlook and Conclusions
18. Analyst Perspectives

About DelveInsight

DelveInsight is a leading Life Science market research and business consulting company recognized for its off-the-shelf syndicated market research reports and customized solutions to firms in the healthcare sector.

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