Nilotinib,Markets and News,API,Nilotinib hydrochloride monohydrate,923288-90-8,ANQING CHICO PHARMACEUTICAL
Abstract
Nilotinib hydrochloride monohydrate (CAS No. 923288-90-8) is a second‐generation Bcr-Abl tyrosine kinase inhibitor primarily used in the treatment of Philadelphia chromosome–positive chronic myelogenous leukemia (CML). First approved by the U.S. Food and Drug Administration (FDA) in 2007. nilotinib was developed by Novartis (marketed as Tasigna) as an evolution from earlier therapies to overcome imatinib resistance. Over its nearly two decades on the market, nilotinib has faced evolving competitive dynamics—including a growing presence of generic formulations—which have influenced its global sales and market share. This paper summarizes nilotinib’s chemical and pharmacological characteristics, outlines its clinical development history and regulatory milestones, examines its market evolution and competitive challenges, and speculates on the annual global sales over 2020–2024. Insights are drawn from established chemical databases and recent market research publications.
Keywords
Nilotinib hydrochloride monohydrate; Tasigna; Bcr-Abl inhibitor; chronic myelogenous leukemia; FDA approval 2007; global sales; market competition; generics.
1. Introduction
Nilotinib hydrochloride monohydrate is an orally bioavailable, selective Bcr-Abl tyrosine kinase inhibitor developed to treat patients with Philadelphia chromosome–positive CML who are resistant or intolerant to earlier therapies such as imatinib. Since its FDA approval in 2007. it has emerged as a critical option in targeted cancer therapy, offering enhanced potency and activity against both wild-type and mutated forms of the Bcr-Abl fusion protein. Over the years, nilotinib has become a cornerstone therapy in the management of CML. However, as patents expire and generic competitors enter the market, the commercial landscape for nilotinib is evolving.
2. Chemical Properties and Mechanism of Action
Nilotinib hydrochloride monohydrate is a crystalline solid with the following key attributes:
CAS Number: 923288-90-8
Chemical Formula: C??H??ClF?N?O?
Molecular Weight: Approximately 584 g/mol
Melting Point: 198–201 °C
Physical Appearance: Off-white to pale beige powder
Solubility: Slightly soluble in aqueous acidic media and DMSO, with improved solubility upon gentle heating
SMILES:
O.Cl.CC1=CN(C=N1)C1=CC(NC(=O)C2=CC=C(C)C(NC3=NC=CC(=N3)C3=CC=CN=C3)=C2)=CC(=C1)C(F)(F)F
Mechanistically, nilotinib binds to and stabilizes the inactive conformation of the Bcr-Abl fusion protein’s kinase domain, thereby inhibiting its constitutive activity. This inhibition interrupts downstream signaling pathways that are essential for the proliferation and survival of leukemic cells, rendering nilotinib effective in controlling the progression of CML.
3. Clinical and Regulatory Milestones
3.1. Original Research and Development
Nilotinib was developed as a response to resistance issues encountered with imatinib therapy. Research led by Novartis demonstrated that nilotinib is 10–30 times more potent than imatinib against Bcr-Abl kinase and effective against many imatinib-resistant mutations. Early-phase clinical trials established nilotinib’s safety and efficacy, forming the basis for its accelerated development.
3.2. Approval Timeline and Market Introduction
Initial FDA Approval: 2007 for the treatment of Ph+ CML in patients resistant or intolerant to prior therapies.
Subsequent Indications: In 2012. nilotinib received approval for the treatment of newly diagnosed adult patients with Ph+ CML in the chronic phase.
Time on the Market: As of 2025. nilotinib has been available for clinical use for approximately 18 years.
4. Market Performance and Competitive Landscape
4.1. Global Sales and Speculative Forecast
According to recent market research reports, the global nilotinib market size was valued at around USD 1.3 billion in 2023. In the face of increasing generic competition, revenue growth for the branded product (Tasigna) has been gradually declining. Based on market trends and expert judgment, the following speculative global annual sales estimates for nilotinib are provided:
2020: USD 1.42 billion
2021: USD 1.40 billion
2022: USD 1.37 billion
2023: USD 1.33 billion
2024: USD 1.30 billion
These modest decreases reflect the penetration of generics as patents erode the pricing power of the originator product while overall patient numbers remain steady.
4.2. Market Competition and Generics
Nilotinib’s primary market competitor has been its own branded version (Tasigna by Novartis) alongside a growing number of generic versions. As patents expire and local regulatory bodies approve generics—for example, in India, where domestic manufacturers capture over 60% of the CML therapy market—the branded product faces intense pricing pressure. Reports indicate that generic nilotinib formulations in various regions are now offered at significantly lower prices, which affects overall revenue for the innovator. In markets such as North America and Europe, where healthcare systems push for cost-effective treatments, formulary shifts have been observed.
4.3. Other Related News and Trends
Recent developments in the field include:
Expanded Clinical Applications: Ongoing research is evaluating nilotinib’s potential benefits beyond CML—for example, in neurodegenerative diseases such as Parkinson’s disease. Preliminary data from Phase II studies have reported improvements in motor function, although these findings are yet to gain regulatory approval.
Strategic Collaborations: Novartis has been active in forging partnerships aimed at sustaining its portfolio through lifecycle management—developing new formulations and fixed-dose combinations.
Regulatory Shifts: Regional variations in approval processes and reimbursement policies continue to shape nilotinib’s commercial performance. For instance, price negotiations in emerging markets have resulted in significant discounting, while stringent regulatory pathways in North America maintain higher prices but slower market growth.
5. Conclusion
Nilotinib hydrochloride monohydrate has established itself as a pivotal therapy in the management of Ph+ CML since its introduction in 2007. Its superior potency over imatinib and expanded indications have secured its place in oncology practice. However, as the product matures on the market, rising competition from generics has started to erode sales margins gradually. The speculative sales forecast for 2020–2024 indicates modest but steady declines in global sales values, reflecting both market saturation and cost-containment trends among healthcare providers. Despite these challenges, ongoing research into new therapeutic applications and strategic partnerships may offer avenues for renewed growth and market diversification.
6. References
Nilotinib Hydrochloride Monohydrate | PubChem, PubChem, retrieved April 2025.
Nilotinib Hydrochloride Monohydrate | ChemicalBook, ChemicalBook, retrieved April 2025.
Nilotinib HCl hydrate | Sigma-Aldrich, Sigma-Aldrich product page, retrieved April 2025.
Wikipedia – Nilotinib, available at: https://en.wikipedia.org/wiki/Nilotinib (accessed April 2025).
Nilotinib Market Size, Growth, Key Trends to 2033 – DataIntelo,DataIntelo, retrieved April 2025.
Nilotinib Hydrochloride Market – PW Consulting, PW Consulting, retrieved April 2025.
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Nilotinib hydrochloride monohydrate,923288-90-8
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