Temozolomide

Glioblastoma is the most common malignant primary brain tumor in adults, with a five-year survival rate of less than 5%, and there has been a long-term lack of treatment regimens with high efficacy and low toxicity in clinical practice. As a second-generation imidazotetrazine alkylating agent, temozolomide can penetrate the blood-brain barrier, induce apoptosis by methylating the guanine sites of tumor cell DNA, and is currently the first-line reference drug for glioma chemotherapy. Its indications cover newly diagnosed glioblastoma multiforme (concurrent chemoradiotherapy and adjuvant therapy), glioblastoma multiforme or anaplastic astrocytoma that relapses or progresses after conventional treatment. Meanwhile, it is also recommended by guidelines for the treatment of pediatric glioma, brain metastasis of melanoma and other conditions, and is an indispensable core drug in the field of central nervous system tumor treatment.

At present, the global market size of temozolomide is stable at around US$1.2 billion, while the annual sales in the Chinese market exceed RMB 3 billion, with a compound annual growth rate maintained at 6% to 8%. With the improvement of the popularity of glioma diagnosis and treatment and the expansion of combination therapy regimens, the market demand still has room for steady growth. In terms of competitive landscape, the original research product accounts for more than 60% of the global market share, while the domestic market presents a situation where original research drugs and generic drugs coexist. Generic preparations from more than 15 enterprises have passed the consistency evaluation. The implementation of volume-based procurement has driven a significant drop in the price of preparations, and has also driven the continuous release of demand for upstream API. At present, a number of domestic enterprises have the capacity for large-scale production of temozolomide API.

The original research enterprise of temozolomide is Merck Sharp & Dohme, and the original brand name is Temodar®. The core compound patent of temozolomide expired in the United States in 2014, and the compound patent in China expired in 2013. The main dosage forms approved for the original research product are capsules, with specifications including 5mg, 20mg, 100mg, 140mg, 180mg and 250mg, and the specification of the injection is 100mg. Both the original capsules and injections are included in the *Catalogue of Reference Preparations for Chemical Drugs* issued by the NMPA, and are also listed in the FDA Reference Preparations Catalogue. At present, there are more than 20 domestic registration numbers of temozolomide API, most of which are in status A (approved for use in marketed preparations). Multiple domestic manufacturers have obtained marketing approval for temozolomide capsules and temozolomide for injection. (Data as of June 2025, please refer to the official website of CDE for the latest information)

CATO can provide a full set of impurity reference standards for temozolomide API. Most of the products are available from stock. For in-stock products, orders placed before 16:00 can be shipped on the same day. All products meet the requirements of multiple regulatory systems such as Chinese Pharmacopoeia and FDA, and can fully meet various compliance needs of pharmaceutical enterprises in the stages of R&D, quality research and mass production.