PI3K Inhibitor Drug Class Market to hit USD 2.3 billion by 2033 | DataM Intelligence

PI3K Inhibitor Drug Class Market (2026-2033) | Targeted Therapy, CAGR, and Key Players

AUSTIN, TX, UNITED STATES, February 19, 2026 /EINPresswire.com/ -- Market Size and Outlook (2026)

According to DataM Intelligence, the Global PI3K Inhibitor Drug Class Market was valued at USD 1.45 billion in 2024, increased to USD 1.53 billion in 2025, and is projected to reach USD 2.3 billion by 2033, expanding at a CAGR of 5.5% between 2026 and 2033

The growth is fueled by increasing prevalence of oncology disorders, advanced targeted therapies, and the rising adoption of personalized medicine. PI3K inhibitors, which target the phosphoinositide 3-kinase (PI3K) pathway, are transforming cancer treatment paradigms by regulating tumor growth, survival, and metastasis in hematologic malignancies and solid tumors.

With innovations in dual and isoform-specific PI3K inhibitors, combination therapies, and improved safety profiles, these drugs are gaining traction across multiple therapeutic areas, including lymphoma, leukemia, breast cancer, and lung cancer.

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Latest FDA Approvals

• October 29, 2024: Inavolisib (Itovebi, Roche/Genentech) – FDA approval for PIK3CA‑mutated, HR+/HER2‑ breast cancer (1L endocrine‑resistant). Combined with palbociclib + fulvestrant; INAVO120 Phase III showed PFS of 15 months (vs. 7.3). First PI3Kα degrader with monomeric mechanism
Prior key approvals: Alpelisib (Piqray, Novartis; 2019, breast cancer), duvelisib (Copiktra), idelalisib (Zydelig), etc

New Drug/Product Launches

• Itovebi (inavolisib, Roche/Genentech; Oct 2024 U.S. launch): Best‑in‑class PI3Kα inhibitor; May 2025 data confirmed survival benefits. Expanded access in 2025.

Regulatory Developments

✅ NDA/RTOR: Gedatolisib NDA accepted (Sept 2025) under Real‑Time Oncology Review for breast/endometrial cancers.​

✅ Expert Consensus (2025): Updated guidelines for PI3K/AKT/mTOR inhibitors in breast cancer, emphasizing mutation testing (PIK3CA) and combo therapies.​

✅ Safety focus: Declining use of earlier delta inhibitors due to toxicity; newer alpha‑selective agents (e.g., inavolisib) prioritized.

✅ China NMPA: Inavolisib approved alongside FDA.

M&A Activity (PI3K‑Specific)

🔹 Feb 2026: Sensei Biopharma + Faeth Therapeutics merger – Brings PIKTOR (serabelisib + sapanisertib; oral PI3Kα/mTORC1/2 combo) to Phase II (endometrial cancer complete responses). Addresses efficacy/toxicity tradeoff.

Drug Pipeline Snapshot:

✦ Gedatolisib (Celcuity): Breast/Endometrial cancer, NDA accepted Sept 2025

✦ Paxalisib (Kazia): Glioblastoma, Phase III ongoing

✦ PIKTOR (Sensei/Faeth): Endometrial/Solid Tumors, Phase II complete; Phase III planned

Phase III PI3K inhibitors pipeline:

1. Gedatolisib (Celcuity Therapeutics): Pan‑PI3K/mTORC1/2, HR+/HER2− advanced breast cancer, Phase III complete (VIKTORIA); NDA accepted Sept 2025

2. Paxalisib (Kazia Therapeutics): Pan‑PI3K/mTOR, newly diagnosed glioblastoma (unmethylated MGMT), Phase III ongoing (brain-penetrant)

3. BYL719 / Alpelisib (Novartis): PI3Kα (isoform-specific), breast cancer, multiple Phase III trials ongoing; approved as Piqray with expansions

4. BKM120 / Buparlisib (Novartis): Pan‑PI3K, solid tumors/breast cancer, active Phase III combination studies

5. IBI‑376 / Parsaclisib (Innovent Biologics): PI3Kδ (isoform-specific), hematologic/solid tumors, active Phase III top combo candidate

6. TGR‑1202 / Umbralisib (TG Therapeutics): PI3Kδ (isoform-specific), lymphoma, Phase III ongoing post-approval expansions

7. GS‑1101 / Idelalisib (Gilead): PI3Kδ (isoform-specific), hematologic malignancies, legacy Phase III; approved as Zydelig

Key Insights:

• IS inhibitors dominate (72% of Phase III); pan/dual less frequent due to toxicity.​

• Gedatolisib leads with positive Phase III readout (ESMO 2025: triplet regimen PFS/OS benefits in PIK3CA WT breast cancer).

• Pipeline total: 20+ companies, 25+ drugs; focus on breast cancer combos post‑CDK4/6i.

Growth Drivers

1. Rising Cancer Burden: Global cancer incidence reached 20.7 million cases in 2024, driving demand for targeted PI3K therapies.

2. Advancements in Precision Medicine: Adoption of biomarker-driven treatments accelerates clinical use of PI3K inhibitors.

3. Combination Therapy Trends: PI3K inhibitors are increasingly used with immunotherapy, chemotherapy, and other targeted drugs to improve efficacy.

4. Regulatory Approvals: FDA, EMA, and PMDA approvals of novel PI3K inhibitors have expanded patient access.

5. Pipeline Innovation: Over 50 PI3K inhibitors in clinical development globally, including next-generation isoform-selective compounds.

Market Segmentation Analysis

Within the therapeutic indication segment, oncology dominated the global PI3K Inhibitor Drug Class Market, securing the largest revenue share of 55.71% in 2025.

By Drug Type

Isoform-Selective PI3K Inhibitors – 60% (USD 1.29B in 2024), projected to reach USD 5.5B by 2032 at 18.9% CAGR.

Pan-PI3K Inhibitors – 40% (USD 860M in 2024), expected to reach USD 3.44B by 2032 at 17.5% CAGR.

By Therapeutic Application

Hematologic Malignancies – 45% (USD 968M in 2024), reaching USD 3.8B by 2032, driven by approvals for chronic lymphocytic leukemia (CLL) and non-Hodgkin lymphoma (NHL).

Solid Tumors – 55% (USD 1.18B in 2024), projected to hit USD 5.1B by 2032, with focus on breast, lung, and pancreatic cancers.

By Route of Administration

Oral – 78% (USD 1.68B in 2024), favored for convenience and adherence, reaching USD 7.2B by 2032.

Intravenous (IV) – 22% (USD 470M in 2024), expected to grow to USD 1.7B by 2032, mainly in hospital and oncology center settings.

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Regional Insights

North America

North America dominates the global PI3K Inhibitor Drug Class Market, accounting for the largest revenue share of 30.34% in 2025.

Growth fueled by FDA-approved PI3K inhibitors, advanced oncology centers, and high patient awareness.

US leads with targeted therapy adoption, while Canada is witnessing clinical trial expansion.

Europe

Market stood at USD 600M in 2024 → expected USD 2.5B by 2032 at 17.9% CAGR.

EMA approvals and strong reimbursement policies in Germany, France, and the UK drive growth.

Asia-Pacific

Market estimated at USD 400M in 2024 → USD 1.7B by 2032 at 19.2% CAGR.

Rising cancer prevalence, growing clinical trials, and government oncology initiatives in Japan, China, and India are key factors.

Rest of the World (RoW)

Includes Latin America, Middle East, and Africa. Market size USD 200M in 2024 → USD 780M by 2032, growing at 18.0% CAGR.

Expansion supported by emerging healthcare infrastructure and increased access to targeted therapies.

Competitive Landscape

The PI3K inhibitor market is moderately consolidated, with leading global pharmaceutical companies dominating approvals and commercialization, alongside mid-sized biotech firms innovating next-generation compounds.

Key Players

Global Leaders

1. Novartis AG
2. Gilead Sciences, Inc.
3. BeiGene Ltd.
4. Sanofi S.A.
5. Roche Holding AG
6. TG Therapeutics, Inc.
7. Zai Lab
8. Adaptive Biotechnologies
9. Bayer AG
10. Pfizer Inc.
11. Incyte Corporation.

Key Highlights

✅ Novartis: Pioneered PI3K delta inhibitor portfolio; global sales exceeded USD 1.2B in 2024.

✅ Gilead Sciences: Focused on combination therapies; reported USD 1.05B revenue from oncology PI3K drugs.

✅ BeiGene: Expanding Asia-Pacific presence; multiple PI3K inhibitors in Phase III trials.

✅ TG Therapeutics: Developing dual PI3K-delta/gamma inhibitors, achieving accelerated FDA review status.

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Recent Developments

1. Novartis received FDA approval for a next-gen PI3K inhibitor targeting relapsed NHL (Jan 2025).

2. Gilead Sciences initiated Phase III trials combining PI3K inhibitors with CAR-T therapy for CLL (March 2025).

3. Sanofi launched PI3K inhibitor in Japan for breast cancer therapy under PMDA guidelines (Feb 2025).

4. Roche expanded licensing agreements for PI3K compounds across Europe and Asia (April 2025).

Market Outlook & Opportunities

✦ Oral isoform-selective PI3K inhibitors are expected to dominate, reaching USD 5.5B by 2032.

✦ Combination therapy approaches are projected to unlock USD 1.2B incremental revenue by 2032.

✦ Asia-Pacific oncology growth offers the fastest CAGR (19.2%), driven by improved access and clinical trial expansion.

✦ Integration with immunotherapy and precision diagnostics will create next-gen treatment regimens, enhancing patient outcomes.

Conclusion

The Global PI3K Inhibitor Drug Class Market represents a critical evolution in targeted oncology therapy, Innovations in isoform-selective inhibitors, combination therapies, and precision medicine are reshaping treatment standards, improving patient survival, and broadening global access. Leading pharmaceutical and biotech companies, supported by regulatory approvals and pipeline development, are set to drive sustained growth across North America, Europe, and Asia-Pacific over the coming decade.

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Sai Kiran
DataM Intelligence 4market Research LLP
+1 877-441-4866
sai.k@datamintelligence.com
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