PI3K Inhibitor Pipeline Insight 2025

DelveInsight’s, “PI3K Inhibitor Pipeline Insight, 2025” report provides comprehensive insights about 20+ companies and 25+ pipeline drugs in PI3K Inhibitor  pipeline landscape. It covers the PI3K Inhibitor pipeline drug profiles, including PI3K Inhibitor clinical and nonclinical stage products. It also covers the PI3K Inhibitor therapeutics assessment by product type, stage, PI3K Inhibitor route of administration, and PI3K Inhibitor molecule type. It further highlights the inactive PI3K Inhibitor pipeline products in this space.  

 

Geography Covered

• Global coverage

 

PI3K Inhibitor Understanding

Phosphoinositide 3-kinases (PI3Ks) are a family of enzymes involved in key cellular functions such as growth, proliferation, metabolism, and survival. The PI3K/AKT/mTOR signaling pathway is frequently activated in many types of cancer, often due to genetic mutations, particularly in the PIK3CA gene. This has made PI3Ks attractive targets for cancer therapy, and several inhibitors have been developed to block this pathway and suppress tumor growth.

 

PI3K inhibitors are broadly categorized into pan-PI3K inhibitors (targeting multiple isoforms) and isoform-specific inhibitors (targeting a specific PI3K subtype, such as α, β, γ, or δ). Different isoforms play distinct roles in cancer biology. For example, PI3K-α is commonly associated with solid tumors, especially in breast cancer and endometrial cancer, while PI3K-δ and -γ are more active in hematologic malignancies. The therapeutic intent behind selective inhibition is to maximize efficacy while minimizing side effects.

 

One of the most notable PI3K inhibitors is Alpelisib (brand name Piqray), which selectively inhibits PI3K-α. It was approved for the treatment of HR-positive, HER2-negative, PIK3CA-mutated advanced breast cancer in combination with fulvestrant. Clinical trials have shown that Alpelisib significantly improves progression-free survival in patients with PIK3CA mutations. However, common side effects include hyperglycemia, rash, and gastrointestinal issues, which require close monitoring and management.

 

In hematologic cancers, several PI3K inhibitors have been approved, including Idelalisib (Zydelig), Duvelisib (Copiktra), and Copanlisib (Aliqopa). These drugs target the PI3K-δ and/or -γ isoforms and are used in conditions like chronic lymphocytic leukemia (CLL) and follicular lymphoma. While effective, these drugs have been associated with serious toxicities such as immune-mediated adverse events and increased risk of infections, which have led to warnings and, in some cases, withdrawal of indications or halted trials.

 

The development of PI3K inhibitors has faced challenges due to toxicity concerns and limited overall survival benefits in broader cancer populations. In 2022, the U.S. FDA raised concerns about this drug class, recommending tighter regulatory standards and more robust trial designs for future approvals. These actions reflect a broader shift toward balancing efficacy with long-term safety in targeted cancer therapies.

 

Looking ahead, the future of PI3K inhibitors may lie in precision oncology—using biomarkers to identify patients most likely to benefit, and in combining them with other targeted therapies or immunotherapies. Efforts are ongoing to develop next-generation PI3K inhibitors with improved selectivity and reduced toxicity, offering renewed hope for effective, patient-tailored cancer treatments.

 

“PI3K Inhibitor Pipeline Insight, 2025" report by DelveInsight outlays comprehensive insights of present scenario and growth prospects across the mechanism of action. A detailed picture of the PI3K Inhibitor pipeline landscape is provided which includes the disease overview and PI3K Inhibitor treatment guidelines. The assessment part of the report embraces, in depth PI3K Inhibitor commercial assessment and clinical assessment of the PI3K Inhibitor pipeline products under development. In the report, detailed description of the drug is given which includes mechanism of action of the drug, PI3K Inhibitor clinical trials, NDA approvals (if any), and product development activities comprising the technology, PI3K Inhibitor collaborations, licensing, mergers and acquisition, funding, designations and other product related details.

 

PI3K Inhibitors Pipeline Report Highlights

• The PI3K Inhibitor companies and academics are working to assess challenges and seek opportunities that could influence PI3K Inhibitor R&D. The therapies under development are focused on novel approaches to treat/improve PI3K Inhibitor. 

 

PI3K Inhibitor Emerging Drugs Chapters

This segment of the PI3K Inhibitor report encloses its detailed analysis of various drugs in different stages of clinical development, including phase II, I, preclinical and Discovery. It also helps to understand clinical trial details, expressive pharmacological action, agreements and collaborations, and the latest news and press releases.

 

PI3K Inhibitor Emerging Drugs

• Gedatolisib: Celcuity

Gedatolisib is a dual inhibitor of PI3K and mTOR, targeting all class I isoforms of PI3K and mTORC1 and mTORC2. This unique mechanism of action distinguishes it from other inhibitors that target PI3K or mTOR alone. Gedatolisib aims to address drug resistance and potential resistance mechanisms that can occur with isoform-specific inhibitors. The drug has shown promising results in clinical trials, demonstrating manageable toxicity and potential efficacy in combination therapies for hormone receptor–positive, HER2-negative metastatic breast cancer patients who progressed after CDK4/6 inhibitor treatment. Currently, the drug is in Phase III stage of its clinical trial for the treatment of Breast cancer.

 

• TBO-309: ThromBio

TBO-309 is a novel antiplatelet compound with truly remarkable properties. TBO-309 is a potent, selective and ATP competitive PI3K [beta] inhibitor which reduces platelet activation adhesion/aggregation particularly under conditions of disturbed blood flow and promotes platelet disaggregation. By targeting PI3K [beta], TBO-309 specifically inhibits thrombosis whilst minimizing the impact on normal hemostasis. A key point of differentiation between TBO-309 and currently approved antiplatelets is its wide therapeutic window. When combined with existing anti-clotting therapies, it does not cause a major increase in bleeding. This has been confirmed in several proof-of-concept studies in both animal models and two Phase I human clinical trials. In a broad range of preclinical animal models, and in two Phase I human clinical trials studies have demonstrated that TBO-309 (AZD6482) can inhibit arterial thrombus formation in a dose-dependent manner, without causing a major increase in bleeding and TBO-309 can be safely and effectively combined with other antithrombotic agents without causing a major increase in bleeding. Currently, the drug is in Phase II Stage of its clinical development for the treatment of Ischemic Stroke and Tandem Occlusion.

 

• TL117: Suzhou Teligene

TL117 is an orally bioavailable Phosphatidylinositol 3-Kinase (PI3K) inhibitor, with potential antineoplastic activity. Upon oral administration, PI3K inhibitor TL117 specifically inhibits the activity of PI3K, and prevents the activation of the PI3K/Akt (protein kinase B)-mediated signaling pathway. This may result in the inhibition of both tumor cell growth and survival in PI3K-overexpressing tumor cells. Activation of the PI3K signaling pathway is frequently associated with tumorigenesis. Dysregulated PI3K signaling may contribute to tumor resistance to a variety of antineoplastic agents. Currently, the drug is in Phase I/II Stage of its clinical development for the treatment of Head and Neck Squamous Cell Carcinoma.

Further product details are provided in the report……..

 

PI3K Inhibitors Therapeutic Assessment

This segment of the report provides insights about the different PI3K Inhibitor drugs segregated based on following parameters that define the scope of the report, such as:

 

Major PI3K Inhibitor Companies 

There are approx. 20+ key PI3K Inhibitor companies which are developing the therapies for PI3K Inhibitor. The companies which have their PI3K Inhibitor drug candidates in the most advanced stage, i.e. Phase III include, Celcuity.

 

PI3K Inhibitor Phases

DelveInsight’s report covers around 25+ products under different phases of clinical development like

• Late stage products (Phase III)
• Mid-stage products (Phase II)
• Early-stage product (Phase I) along with the details of 
• Pre-clinical and Discovery stage candidates
• Discontinued & Inactive candidates

 

PI3K Inhibitors Route of Administration

PI3K Inhibitor pipeline report provides the therapeutic assessment of the pipeline drugs by the Route of Administration. Products have been categorized under various ROAs such as 

• Intra-articular
• Intraocular
• Intrathecal 
• Intravenous
• Oral
• Parenteral
• Subcutaneous
• Topical
• Transdermal

 

PI3K Inhibitors Molecule Type

Products have been categorized under various Molecule types such as

• Oligonucleotide
• Peptide
• Small molecule

 

PI3K Inhibitors Product Type

Drugs have been categorized under various product types like Mono, Combination and Mono/Combination.

 

PI3K Inhibitors Pipeline Development Activities 

The PI3K Inhibitor pipeline report provides insights into different therapeutic candidates in phase II, I, preclinical and discovery stage. It also analyses PI3K Inhibitor therapeutic drugs key players involved in developing key drugs. 

 

Pipeline Development Activities

The report covers the detailed information of collaborations, acquisition and merger, licensing along with a thorough therapeutic assessment of emerging PI3K Inhibitor drugs.

 

PI3K Inhibitor Report Insights

• PI3K Inhibitor  Pipeline Analysis
• Therapeutic Assessment
• Unmet Needs
• Impact of PI3K Inhibitor Drugs

 

PI3K Inhibitor Report Assessment

• Pipeline Product Profiles
• PI3K Inhibitor Therapeutic Assessment
• Pipeline Assessment
• Inactive drugs assessment
• Unmet Needs

 

Key Questions

Current Treatment Scenario and Emerging Therapies:

• How many PI3K Inhibitor companies are developing PI3K Inhibitor drugs?
• How many PI3K Inhibitor drugs are developed by each company?
• How many emerging PI3K Inhibitor drugs are in mid-stage, and late-stage of development for the treatment of PI3K Inhibitor?
• What are the key collaborations (Industry–Industry, Industry–Academia), Mergers and acquisitions, licensing activities related to the PI3K Inhibitor therapeutics? 
• What are the recent trends, drug types and novel technologies developed to overcome the limitation of existing therapies? 
• What are the PI3K Inhibitor clinical trials going on for PI3K Inhibitor and their status?
• What are the key designations that have been granted to the emerging PI3K Inhibitor drugs?

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