Tibolone

Menopause-related symptoms are common clinical problems that affect the quality of life of middle-aged and elderly women, and the clinical application of traditional hormone replacement regimens is often limited due to adverse reactions in the reproductive system. Tibolone belongs to the tissue-selective estrogen activity regulator. Its unique mechanism of action can produce estrogen, progestogen or weak androgen activity in different tissues. While improving postmenopausal symptoms such as hot flashes, night sweats and osteoporosis, it will not overstimulate the endometrium and breast tissues. It is mainly used for the treatment of perimenopausal syndrome caused by natural menopause and surgical menopause, and can also be used to prevent osteoporosis in postmenopausal women. It is suitable for people with menopause-related symptoms who have poor tolerance to traditional hormone therapy.

At present, the global tibolone market size is about USD 1.23 billion, with a compound annual growth rate maintained at around 4.2%. The growth momentum mainly comes from the expansion of the global female menopausal population and the increasing clinical demand for safer hormone replacement therapy. In terms of the domestic market, tibolone has been included in the National Medical Insurance Catalogue (Class B), and the annual sales volume at the terminal of public medical institutions is stable at RMB 270 million. At present, the domestic preparation market is dominated by the original research product, and the number of approved generic drugs is small. With the advancement of the consistency evaluation of generic drugs, the space for domestic substitution is gradually released.

The original research enterprise of tibolone is Organon (Netherlands, now under Merck & Co., Inc.), and the original brand name is "Livial". Its core compound patent expired globally in 2008. The main dosage form of the original marketed product is tablet, with a specification of 2.5mg. This product has been included in the *Catalogue of Chemical Reference Preparations* of China, and is also a recognized reference preparation by the FDA. In terms of domestic API registration, 3 tibolone API registration numbers of domestic enterprises have been publicized on the CDE platform, of which 2 are in the status of "A" (can be used in marketed preparations). A number of domestic manufacturers have passed the consistency evaluation of generic drugs and obtained approval for marketing of tibolone tablets. (Data as of October 2024, please refer to the official website of CDE for the latest information)

CATO provides a full set of impurity reference standards for tibolone API. Most of the products are available in stock. Stock orders paid before 16:00 can be shipped on the same day. All reference standards comply with the regulatory requirements of drug regulatory authorities of various countries such as the Chinese Pharmacopoeia and the FDA, and can fully meet the use needs of different scenarios such as API R&D, quality research and consistency evaluation.