KAT6 Inhibitors Market Size, Target Population, Competitive Landscape, and Market Forecast - 2040

Key Highlights:

• New chemically induced proximity approaches are presented, offering opportunities for unique target selectivity profiles and tissue-specific targeting of KATs.
• Molecular changes in KATs most commonly occur in paralogous enzymatic subunits of KAT enzyme complexes (EP300/CREBBP, KAT6A/KAT6B) and result in altered stoichiometric levels of active enzymatic forms incorporated in complexes.
• New KAT inhibitors are more drug-like and gain high selectivity across the KAT family by exploiting amino acid differences in BRDs or catalytic (HAT) domains.
• KAT6A is over-expressed in a variety of tumor types, including breast cancer, prostate cancer, ovarian cancer, cervical cancer, lung cancer, colon and rectal cancer, and medulloblastoma.
• As per the secondary search, In breast cancer, KAT6A was found to be amplified in 12-15% of tumors as part of the 8p11-12 amplicon, and is associated with poor outcomes for primary breast cancer patients, mostly of luminal subtype. In ER+ breast cancer models, KAT6A inhibition was shown to directly repress ESR1 transcription and arrest cell growth.
• KAT6A shows variable amplification and overexpression across cancers. In breast cancer, it is amplified as in about 11-15% of cases, with amplification seen in roughly 9.4% of triple-negative breast cancers (TNBC). In ovarian cancer, genomic amplification occurs in around 6% of cases, while high KAT6A protein expression is observed in nearly 75%. These findings highlight KAT6A as a recurrently dysregulated oncogenic driver in multiple tumor types.
• There are currently no approved KAT6 inhibitors, highlighting both the challenges in development and the limited awareness of this target. However, the presence of several emerging candidates in early and preclinical stages reflects growing interest in this mechanism for cancer treatment.
• Emerging drugs in the early phase are PF-07248144 (Pfizer), MEN2312 (Stemline Therapeutics), OP-3136 (Olema Pharmaceuticals), among others, while some in the preclinical phase include IST-477 (Isosterix), among others.
• In April 2025, Olema Pharmaceuticals announced preclinical data demonstrating the anti-tumor activity of OP-3136 in prostate, ovarian, and non-small cell lung cancer (NSCLC) models. These findings were presented in a late-breaking poster session at the American Association for Cancer Research (AACR) Annual Meeting.
• In January 2025, Menarini and Insilico signed a second licensing deal for an AI-discovered oncology drug, worth up to USD 550 million, following their 2024 KAT6 inhibitor partnership.
• Given the current limitations in the pipeline, it is crucial to prioritize the development of drugs in this class, as they show significant promise in treating metastatic breast cancer, non-small cell lung cancer (NSCLC), and castration-resistant prostate cancer (CRPC), highlighting the need for dedicated efforts in this area.

DelveInsight's "KAT6 Inhibitors - Target Population, Competitive Landscape, and Market Forecast - 2040" report delivers an in-depth understanding of the KAT6 inhibitors, historical and Competitive Landscape as well as the KAT6 inhibitors market trends in the United States, EU4 (Germany, France, Italy, and Spain) and the United Kingdom, and Japan.

The KAT6 inhibitors market report provides current treatment practices, emerging drugs, market share of individual therapies, and current and forecasted 7MM KAT6 inhibitors market size from 2020 to 2040. The report also covers current KAT6 inhibitors treatment practices/algorithms and unmet medical needs to curate the best opportunities and assess the market's potential.

Geography Covered:

• The United States
• EU4 (Germany, France, Italy, and Spain) and the United Kingdom
• Japan

Study Period: 2020-2040

Study Period 2020-2040

Forecast Period 2025-2040

Geographies Covered US, EU4 (Germany, France, Italy, and Spain) the UK, and Japan

KAT6 Inhibitors Epidemiology Segmented by:

• Total cases of selected indications for KAT6 Inhibitors
• Total Eligible Patient Pool of Selected Indications
• Total treated cases in the selected indication for KAT6 Inhibitors

KAT6 Inhibitors Key Companies * Pfizer

• Stemline Therapeutics
• Olema Pharmaceuticals, and others

KAT6 Inhibitors Key Therapies * PF-07248144

• MEN2312
• OP-3136, and others

KAT6 Inhibitors Market Segmentation Segmented by:

• Therapies
• Indications

KAT6 Inhibitors Market Analysis * KOL Views

• SWOT Analysis
• Analyst Views
• Reimbursement
• Unmet needs

KAT6 Inhibitors Disease Understanding and Treatment Algorithm

KAT6 Inhibitors Overview

Lysine acetyltransferases (KATs) are epigenetic enzymes that regulate gene expression by modifying histone proteins, and have emerged as important targets in cancer therapy due to their frequent dysregulation through mutations, amplifications, or chromosomal translocations. Among them, KAT6A and KAT6B members of the MYST family play a pivotal role in acetylating histone H3 at lysine 23 (H3K23), facilitating chromatin remodeling and transcriptional activation. These enzymes operate as part of a tetrameric complex with chromatin-associated proteins like BRPF1, ING4/5, and EAF6, and are essential for biological processes such as embryonic development, cellular senescence, hematopoietic stem cell maintenance, and gene transcription. In cancer, KAT6A/B alterations can lead to widespread changes in histone acetylation and gene expression, including the activation of oncogenes or repression of tumor suppressor genes. Additionally, they act as coactivators for oncogenic transcription factors, further contributing to tumor progression. Given their central role in cancer biology, KAT6A and KAT6B are being actively explored as therapeutic targets, with several small-molecule inhibitors under development that specifically block their enzymatic or bromodomain functions.

KAT6 Inhibitors Patient Pool

The KAT6 Inhibitors epidemiology chapter in the report provides historical as well as forecasted epidemiology segmented as total cases of selected indications for KAT6 Inhibitors, total eligible patient pool of selected indications, total treated cases in selected indications for KAT6 Inhibitors in the 7MM covering the United States, EU4 (Germany, France, Italy, and Spain), and the United Kingdom, and Japan from 2020 to 2040.

• The total incident cases of breast cancer in the 7MM comprised around 670,000 cases in 2024.
• Among 7MM, the US accounts for the highest number of incident cases of HR+/HER2- breast cancer, with approximately 211,580 in 2024.
• In the US, the maximum number of HR+/HER2- breast cancer patients lies in the age group of 60-79 years.
• In 2024, the estimated prevalent cases of CRPC in the US were around 53,000.
• Around 43% of all metastatic prostate cancer cases are attributed for metastatic CRPC.
• In Japan, incident cases of NSCLC are approximately 121,910 in 2024.

KAT6 Inhibitors Drug Chapters

The drug chapter segment of the KAT6 report encloses a detailed analysis of KAT6 early-stage (Phase I) pipeline drugs. It also helps to understand the KAT6's clinical trial details, expressive pharmacological action, agreements and collaborations, approval and patent details, advantages and disadvantages of each included drug, and the latest news and press releases.

KAT6 Inhibitors Emerging Drugs

PF-07248144: Pfizer

PF-07248144 is a selective catalytic inhibitor of KAT6, a histone lysine acetyltransferase. It is currently in Phase I of the development for the treatment of advanced or metastatic ER+ HER2- breast cancer, CRPC, and NSCLC.

In April 2025, at the American Society of Clinical Oncology (ASCO) Annual Meeting, Pfizer presented a rapid oral session featuring dose-optimization results from its ongoing Phase I trial of PF-07248144 in patients with ER+/HER2- metastatic breast cancer. These results supported the recommended dosing for PF-07248144 paving the way for a pivotal trial of KAT6i plus fulvestrant in second-line and later ER+/HER2- metastatic breast cancer, set to begin in the second half of 2025.

MEN2312: Stemline Therapeutics (Menarini Group)

MEN2312 is a potent and selective orally bioavailable KAT6A/B inhibitor. MEN2312 blocks the estrogen receptor at the transcriptional level, giving it the potential to overcome resistance to endocrine therapies due to mutation or ligand-independent constitutive activation of the estrogen receptor. MEN2312 is being investigated as a single agent and in combination with SoC in metastatic breast cancer ER+/HER- patients.

In January 2024, Stemline Therapeutics, a wholly-owned subsidiary of the Menarini Group, along with Insilico Medicine, announced that they have entered into an exclusive licensing agreement granted Stemline the global rights to develop and commercialize a novel, small molecule KAT6A inhibitor designed using Insilico's AI platform, as a potential treatment for hormone sensitive cancers and other oncology indications.

Emerging Drugs

Product Company RoA Phase Indication

PF-07248144 Pfizer Oral I Advanced or metastatic ER+ HER2- breast cancer, CRPC, and NSCLC

MEN2312 Stemline Therapeutics Oral I Advanced breast cancer

OP-3136 Olema Pharmaceuticals Oral I Advanced or metastatic ER+ HER2- breast cancer, CRPC, and NSCLC

Preclinical Drugs

Drugs Mechanism Company Status

BG-75202 KAT6A/B inhibitor BeOne Phase I to start by 2025

IDE251 KAT6/7 inhibitor Ideaya Biosciences US IND filing planned in 2025

HLX97-069 KAT6A/B inhibitor Shanghai Henlius (Fosun) IND filing planned in 2025

HW321005 KAT6A/6B inhibitor Humanwell Healthcare Preclinical poster at AACR 2025

QLS1304 KAT6A/B inhibitor Qilu Pharmaceutical Preclinical poster at AACR 2025

IST-477 KAT6A inhibitor Isosterix Preclinical poster at AACR 2024

KAT6 Inhibitors Market Outlook

The market outlook for KAT6 inhibitors is gaining momentum, driven by growing interest in epigenetic targets and the recognition of KAT6A/B as key regulators in cancer progression. These enzymes are frequently dysregulated in various malignancies, making them attractive candidates for targeted therapy. KAT6 inhibitors are being explored primarily for their ability to modulate oncogenic gene expression, induce cellular senescence, and suppress tumor growth, especially in cancers with aberrant acetylation profiles. While still in the early stages of clinical development, the pipeline for KAT6 inhibitors is beginning to take shape. Some notable candidates in development include PF-07248144 (Pfizer), MEN2312 (Stemline Therapeutics), and OP-3136 (Olema Pharmaceuticals), all of which are progressing through early clinical stages. These agents reflect the industry's growing investment in targeting lysine acetyltransferases for precision oncology.

Despite the therapeutic promise, the current KAT6 pipeline remains relatively limited, with only a few compounds advancing to human trials. This underscores the need for continued research and innovation to expand and validate the potential of this drug class. Several biopharmaceutical companies are actively investing in this space, signaling a shift in focus toward epigenetic modulation as a viable and potentially transformative cancer treatment strategy. Overall, KAT6 inhibitors represent an emerging and exciting area of oncology drug development, with strong scientific rationale and early data supporting their use across multiple cancer types. With further clinical progress and strategic partnerships, this class has the potential to reshape the future of targeted cancer therapy.

KAT6 Inhibitor Drugs Uptake

This section focuses on the uptake rate of potential emerging KAT6 inhibitors expected to be launched in the market during 2025-2040.

KAT6 Inhibitors Pipeline Development Activities

The report provides insights into different therapeutic candidates in the early stages. It also analyzes key players involved in developing targeted therapeutics.

The presence of numerous drugs under different stages is expected to generate immense opportunities for the KAT6 inhibitors market growth over the forecasted period.

Pipeline Development Activities

The report covers information on collaborations, acquisitions and mergers, licensing, and patent details for KAT6 inhibitor therapies.

KOL Views

To keep up with current and future market trends, we take Industry Experts' opinions working in the domain through primary research to fill the data gaps and validate our secondary research. Industry experts were contacted for insights on KAT6 inhibitors' evolving treatment landscape, patient reliance on conventional therapies, patient therapy switching acceptability, drug uptake, along challenges related to accessibility.

DelveInsight's analysts connected with 10+ KOLs to gather insights; however, interviews were conducted with 5+ KOLs in the 7MM. Centers such as Johns Hopkins Sidney Kimmel Cancer Center and others.

Their opinion helps understand and validate current and emerging therapy treatment patterns or KAT6 inhibitors market trends. This will support the clients in potential upcoming novel treatments by identifying the overall scenario of the market and the unmet needs.

KOL Views

"Drug discovery around KAT enzymes has advanced high-quality small-molecule inhibitors which are currently being used as chemical tools to further study KAT function in cancer. Preclinical evidence highlights important differences in the biological outcome depending on the mode of target inhibition."

KAT6 Inhibitor Market Qualitative Analysis

We perform Qualitative and market Intelligence analysis using various approaches, such as SWOT analysis. In the SWOT analysis, strengths, weaknesses, opportunities, and threats in terms of gaps in disease diagnosis, patient awareness, physician acceptability, competitive landscape, cost-effectiveness, and geographical accessibility of therapies are provided.

Market Access and Reimbursement

Reimbursement may be referred to as the negotiation of a price between a manufacturer and a payer that allows the manufacturer access to the market. It is provided to reduce the high costs and make the essential drugs affordable. Health technology assessment (HTA) plays an important role in reimbursement decision-making and recommending the use of a drug. These recommendations vary widely throughout the seven major markets, even for the same drug.

In the US healthcare system, both Public and Private health insurance coverage are included. Also, Medicare and Medicaid are the largest government-funded programs in the US. The major healthcare programs, including Medicare, Medicaid, the Children's Health Insurance Program (CHIP), and the state and federal health insurance marketplaces, are overseen by the Centers for Medicare & Medicaid Services (CMS). Other than these, Pharmacy Benefit Managers (PBMs) and third-party organizations that provide services and educational programs to aid patients are also present.

The report further provides detailed insights on the country-wise accessibility and reimbursement scenarios, cost-effectiveness scenario of approved therapies, programs making accessibility easier and out-of-pocket costs more affordable, insights on patients insured under federal or state government prescription drug programs, etc.

Scope of the Report:

• The report covers a segment of key events, an executive summary, and a descriptive overview of the KAT6 inhibitor, explaining its mechanism and emerging therapies.
• Comprehensive insight into the Competitive Landscape, and forecasts, the future growth potential of treatment rate, drug uptake, and drug information have been provided.
• Additionally, an all-inclusive account of the current and emerging therapies and the elaborate profiles of early-stage and prominent therapies will impact the current landscape.
• A detailed review of the KAT6 inhibitor market, historical and forecasted market size, market share by therapies, detailed assumptions, and rationale behind our approach is included in the report, covering the 7MM drug outreach.
• The report provides an edge while developing business strategies, by understanding trends, through SWOT analysis, expert insights/KOL views, and treatment preferences that help shape and drive the 7MM KAT6 inhibitor market.

KAT6 Inhibitors Report Insights

• KAT6 Inhibitor Targeted Patient Pool
• Therapeutic Approaches
• KAT6 Inhibitor Pipeline Analysis
• KAT6 Inhibitor Market Size and Trends
• Existing and future Market Opportunity

KAT6 Inhibitor Report Key Strengths

• Fifteen years Forecast
• The 7MM Coverage
• Key Cross Competition
• Drugs Uptake and Key Market Forecast Assumptions

KAT6 Inhibitor Report Assessment

• Current Treatment Practices
• Unmet Needs
• Analyst Views
• Pipeline Product Profiles
• Market Attractiveness
• Qualitative Analysis (SWOT Analysis)

Key Questions:

• What was the KAT6 inhibitor total market size, the market size by therapies, market share (%) distribution, and what would it look like in 2040? What are the contributing factors for this growth?
• Which drug is going to be the largest contributor in 2040?
• What are the risks, burdens, and unmet needs of treatment with KAT6 inhibitors? What will be the growth opportunities across the 7MM for the patient population of KAT6 inhibitors?
• What are the key factors hampering the growth of the KAT6 inhibitor market?
• What are the indications for which recent novel therapies and technologies have been developed to overcome the limitations of existing treatments?
• What key designations have been granted to the therapies for KAT6 inhibitors?
• Patient acceptability in terms of preferred therapy options as per real-world scenarios?

Reasons to buy:

• The report will help develop business strategies by understanding the latest trends and changing dynamics driving the KAT6 inhibitor Market.
• Understand the existing market opportunities in varying geographies and the growth potential over the coming years.
• Distribution of historical and current patient share based on real-world prescription data along with reported sales of approved products in the US, EU4 (Germany, France, Italy, and Spain) and the United Kingdom, and Japan.
• Identifying strong upcoming players in the market will help devise strategies to help get ahead of competitors.
• To understand Key Opinion Leaders' perspectives around the accessibility, acceptability, and compliance-related challenges of existing treatment to overcome barriers in the future.
• Detailed insights on the unmet needs of the existing market so that the upcoming players can strengthen their development and launch strategy.