Small Molecule Targeted Cancer Therapy Market Report 2025

The small molecule targeted cancer therapy market size has grown strongly in recent years. It will grow from $78.07 billion in 2024 to $85.35 billion in 2025 at a compound annual growth rate (CAGR) of 9.3%. The growth during the historic period was driven by an improved understanding of cancer biology, rising approvals of inhibitors, increasing cancer prevalence, early adoption of personalized medicine, and expansion of oncology clinical trials.

The small molecule targeted cancer therapy market size is expected to see strong growth in the next few years. It will grow to $120.35 billion in 2029 at a compound annual growth rate (CAGR) of 9%. The growth during the forecast period is fueled by growing demand for precision oncology, rising investment in next generation inhibitors, increasing healthcare expenditure in emerging markets, greater demand for these therapies, and expanding strategic collaborations. The primary trends in the forecast period include a focus on tumor agnostic therapies, development of allosteric modulators, adoption of artificial intelligence in drug discovery, increased use of oral targeted therapies, and a shift towards combination treatment strategies.

The increasing demand for personalized medicine is expected to drive growth in the small molecule targeted therapy market. Personalized medicine is a medical approach that customizes the prevention, diagnosis, and treatment of diseases based on the unique characteristics of each patient. The rising demand for personalized medicine stems from the growing need for targeted therapies that enhance treatment effectiveness and reduce side effects. Small molecule targeted therapy plays a significant role in meeting this demand by providing treatments that are more specific, improving patient responses, minimizing adverse effects, and offering therapies tailored to an individual’s genetic and molecular makeup. In February 2024, the Personalized Medicine Coalition reported that in 2023, the FDA approved 16 new personalized treatments for rare disease patients, a significant increase from the six approvals in 2022. This growing demand is driving the expansion of the small molecule targeted therapy market.

Leading companies in the small molecule targeted cancer therapy market are focusing on innovations such as structure-based drug design to create highly selective inhibitors targeting specific oncogenic mutations. This method leverages the 3D structure of a target protein to design small molecules that bind precisely, improving drug effectiveness while reducing side effects. For example, in December 2022, Mirati Therapeutics, a US-based oncology firm, announced the FDA approval of KRAZATI (adagrasib) as a targeted therapy for adult patients with KRAS G12C-mutated advanced or metastatic non-small cell lung cancer (NSCLC) who had received at least one prior systemic therapy. This approval offers a new treatment option for patients with this difficult-to-treat mutation, addressing a major unmet need. KRAZATI works by selectively inhibiting the KRAS G12C mutant protein, which is involved in the proliferation and survival of cancer cells.

In May 2023, Gilead Sciences, a US-based biopharmaceutical company, acquired XinThera Inc. for an undisclosed amount. This acquisition aims to enhance Gilead’s oncology and inflammation pipeline by incorporating XinThera’s small molecule inhibitors targeting PARP1 and MK2, thus expanding its precision medicine portfolio. XinThera is a biotechnology company focused on developing small molecule therapies for oncology and immunology.

Major players in the small molecule targeted cancer therapy market are Johnson & Johnson Services Inc., F. Hoffmann-La Roche Ltd., Merck & Co. Inc., Pfizer Inc., AbbVie Inc., Bayer AG, Sanofi S.A., Novartis International AG, AstraZeneca plc, Bristol-Myers Squibb Company, GlaxoSmithKline plc (GSK), Eli Lilly and Company, Takeda Pharmaceutical Company Limited, Amgen Inc., Gilead Sciences Inc., Boehringer Ingelheim International GmbH, Astellas Pharma Inc., Daiichi Sankyo Company Limited, Eisai Co. Ltd., and Ipsen Biopharmaceuticals Inc.

North America was the largest region in the small molecule targeted cancer therapy market in 2024. Asia-Pacific is expected to be the fastest-growing region in the forecast period. The regions covered in small molecule targeted cancer therapy report are Asia-Pacific, Western Europe, Eastern Europe, North America, South America, Middle East and Africa. The countries covered in the small molecule targeted cancer therapy market report are Australia, Brazil, China, France, Germany, India, Indonesia, Japan, Russia, South Korea, UK, USA, Canada, Italy, Spain.

Note that the outlook for this market is being affected by rapid changes in trade relations and tariffs globally. The report will be updated prior to delivery to reflect the latest status, including revised forecasts and quantified impact analysis. The report’s Recommendations and Conclusions sections will be updated to give strategies for entities dealing with the fast-moving international environment.

The sudden escalation of U.S. tariffs and the consequent trade frictions in spring 2025 are severely impacting the pharmaceutical companies contend with tariffs on APIs, glass vials, and lab equipment inputs with few alternative sources. Generic drug makers, operating on razor-thin margins, are especially vulnerable, with some reducing production of low-profit medicines. Biotech firms face delays in clinical trials due to tariff-related shortages of specialized reagents. In response, the industry is expanding API production in India and Europe, increasing inventory stockpiles, and pushing for trade exemptions for essential medicines.

Small molecule targeted cancer therapy is a form of cancer treatment that uses low-molecular-weight compounds to specifically target cancer cell proteins or pathways, inhibiting tumor growth while minimizing harm to healthy cells. Its goal is to provide precise, effective, and personalized treatment options that enhance patient outcomes and reduce the side effects associated with conventional chemotherapy.

The primary therapy types of small molecule targeted cancer therapy include tyrosine kinase inhibitors, proteasome inhibitors, histone deacetylase inhibitors, PARP inhibitors, CDK inhibitors, BCL-2 inhibitors, mTOR inhibitors, and others. Tyrosine kinase inhibitors are targeted compounds designed to block specific enzymes involved in cancer cell growth and proliferation, offering precise therapeutic effects with reduced systemic toxicity. These therapies are applied across cancer types such as lung cancer, breast cancer, colorectal cancer, leukemia, prostate cancer, and others. They are administered via oral or intravenous routes, distributed through hospital pharmacies, retail pharmacies, online pharmacies, and direct sales, and serve key end users including hospitals, specialty clinics, research institutes, and others.

The small molecule targeted cancer therapy market research report is one of a series of new reports that provides small molecule targeted cancer therapy market statistics, including the small molecule targeted cancer therapy industry global market size, regional shares, competitors with the small molecule targeted cancer therapy market share, detailed small molecule targeted cancer therapy market segments, market trends, and opportunities, and any further data you may need to thrive in the small molecule targeted cancer therapy industry. This small molecule targeted cancer therapy market research report delivers a complete perspective of everything you need, with an in-depth analysis of the current and future scenarios of the industry.

The small molecule targeted cancer therapy market consists of sales of novel agents, venetoclax, imatinib, olaparib, niraparib. Values in this market are ‘factory gate’ values, meaning the value of goods sold by the manufacturers or creators of the drugs, whether to other entities (including downstream manufacturers, wholesalers, distributors, and retailers) or directly to end customers. The value of goods in this market also includes related services provided by the creators of these therapies.

The market value is defined as the revenues that enterprises gain from the sale of goods and/or services within the specified market and geography through sales, grants, or donations in terms of the currency (in USD unless otherwise specified).

The revenues for a specified geography are consumption values that are revenues generated by organizations in the specified geography within the market, irrespective of where they are produced. It does not include revenues from resales along the supply chain, either further along the supply chain or as part of other products.

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