PI3K inhibitors - Pipeline Insight, 2025

DelveInsight’s, “PI3K inhibitors- Pipeline Insight, 2025” report provides comprehensive insights about 100+ companies and 100+ pipeline drugs based on PI3K inhibitors pipeline landscape. It covers the pipeline drug profiles, including clinical and nonclinical stage products. It also covers the therapeutics assessment by product type, stage, route of administration, and molecule type. It further highlights the inactive pipeline products in this space.

Geography Covered

• Global coverage

PI3K inhibitors Understanding

PI3K inhibitors: Overview

Phosphatidylinositol-3 kinases (PI3Ks) are lipid kinases that phosphorylate signaling lipid PIP2 to PIP3. PIP3 molecules recruit proteins bearing PIP3-binding pleckstrin homology (PH) domains such as Akt in the PI3K/Akt/mTOR signaling pathway to the plasma membrane. The PI3K pathway is among the most frequently activated in human cancers, impacting almost 50% of the malignancies. Class IA isoforms PI3Kα, β and δ are particularly strongly associated with cancer.Activating mutations in the PIK3CA gene, which encodes the p110α catalytic subunit of PI3Kα and suppressing mutations of tumor suppressor PTEN5,6 (a lipid phosphatase that dephosphorylates PIP3, thus opposes PI3Kα action) are the second and third most frequently mutated in cancer, making PI3Kα a vastly important target for drug discovery

PI3K inhibitors Emerging Drugs Chapters

This segment of the PI3K inhibitors report encloses its detailed analysis of various drugs in different stages of clinical development, including phase III, 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 inhibitors Emerging Drugs

• Umbralisib: TG Therapeutics

Umbralisib (TGR-1202) is an oral, once daily, dual inhibitor of PI3K delta and CK1 epsilon. Umbralisib has nanomolar potency to the delta isoform of PI3K and high selectivity over the alpha, beta, and gamma PI3K isoforms. Umbralisib also uniquely inhibits casein kinase 1 epsilon (CK1 epsilon), which may have both direct anti-cancer effects and may also modulate T-cell activity associated with immune-mediated adverse events seen with previous PI3K inhibitors. Currently, umbralisib is being evaluated in Phase IIb and Phase III trials in patients with NHL and CLL.

• Gedatolisib: Pfizer

Gedatolisib (PF-05212384) is an experimental drug for treatment of cancer in development by Pfizer. It works by targeting PI3K/mTOR. The Phase II clinical trials of gedatolisib for treatment of endometrial cancer and colorectal cancer were terminated early due to enrollment issues. It is currently in phase II stage of development.

• Parsaclisib: Incyte Corporation

Parsaclisib is a potent, highly selective, next-generation PI3Kδ inhibitor that is not associated with clinically meaningful transaminitis. It is in phase II stage of development.

• YH 25248: Yuhan

YH 25248 is an oral selective phosphatidylinositol 3-kinase (PI3K) delta inhibitor, being developed by Yuhan, for the treatment of cancer.

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

PI3K inhibitors: Therapeutic Assessment

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

• Major Players in PI3K inhibitors

There are approx. 100+ key companies which are developing the therapies based on PI3K inhibitors. The companies which have their drug candidate based on PI3K inhibitors in the most advanced stage, i.e. phase II/III include TG Therapeutics and others

• Phases

DelveInsight’s report covers around 100+ products under different phases of clinical development like

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

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

• Infusion
• Intradermal
• Intramuscular
• Intranasal
• Oral
• Parenteral
• Subcutaneous
• Topical.
• Molecule Type

Products have been categorized under various Molecule types such as

• Gene therapies
• Small molecule
• Vaccines
• Polymers
• Peptides
• Monoclonal antibodies
• Product Type

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

PI3K inhibitors: Pipeline Development Activities

The report provides insights into different therapeutic candidates in phase III, II, I, preclinical and discovery stage. It also analyses PI3K inhibitors 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 inhibitors drugs.

Report Highlights

• The companies and academics are working to assess challenges and seek opportunities that could influence PI3K inhibitors R&D. The therapies under development are focused on novel approaches to treat/improve the disease condition.
• In May 2019, Onconova to receive USD 4 Million upfront, including USD 2 Million Fee and USD 2 Million for Onconova Shares Purchased at a Premium, Plus up to USD 45.5 Million in Regulatory and Sales Milestones for Rigosertib in Greater China.
• In December 2019, Onconova Therapeutics, and Inceptua Medicines announced that they have entered into a collaboration to make available intravenous rigosertib via a Pre-approval Access Program in selected countries around the world.

PI3K inhibitors Report Insights

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

PI3K inhibitors Report Assessment

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

Key Questions

• What are the current treatment options available based on the PI3K inhibitors?
• How many companies are developing therapies by working on PI3K inhibitors?
• What are the principal therapies developed by these companies in the industry?
• How many therapies are developed by each company for PI3K inhibitors to treat disease condition?
• How many emerging therapies are in early-stage, mid-stage, and late stage of development for PI3K inhibitors?
• Out of total pipeline products, how many therapies are given as a monotherapy and in combination with other treatments?
• What are the key collaborations (Industry-Industry, Industry-Academia), Mergers and acquisitions, licensing activities related to the PI3K inhibitors therapies?
• Which are the dormant and discontinued products and the reasons for the same?
• What is the unmet need for current therapies developed based on this mechanism of action?
• What are the recent novel therapies, targets, mechanisms of action and technologies developed to overcome the limitation of existing therapies?
• What are the clinical studies going on for PI3K inhibitors and their status?
• What are the results of the clinical studies and their safety and efficacy?
• What are the key designations that have been granted for the emerging therapies for PI3K inhibitors?
• How many patents are granted and pending for the emerging therapies of PI3K inhibitors?

Key Players

• TG Therapeutics
• Pfizer
• Incyte Corporation
• Yuhan
• Inflection Biosciences/AUM Biosciences
• Onconova Therapeutics
• UCB

Key Products

• Umbralisib
• Gedatolisib
• Parsaclisib
• YH 25248
• Research programme: anti-cancer therapeutics
• Rigosertib
• Seletalisib