4-hydroxyandrostenedione (4-OHA), known as Formestane (Lentaron), is the first steroidal aromatase inhibitor (AI) used in clinical practice. It was introduced in the early 1990s as a second-generation AI. However, its intramuscular administration method limited its widespread use due to glucuronidation issues. Despite being withdrawn from the market, clinical trials have shown its effectiveness in treating breast cancer relapse. To address its limitations, a new formulation of 4-OHA cream was developed for topical application on the mammary gland.
Research has shown that 4-OHA cream can effectively regress mammary tumors in rats. Clinical trials with the cream demonstrated similar antitumor effects to 4-OHA injections. The cream was found to inhibit the proliferation of breast cancer cells and arrest the cell cycle, indicating its potential as a treatment for breast cancer.
Common side effects of Formestane include hot flashes and joint pain/stiffness. These side effects are a result of reduced estrogen levels induced by Formestane and can impact patient comfort and quality of life. It is important for patients to communicate any side effects to their healthcare providers for proper management.
[1] Lanyang Gao. “The transdermal cream of Formestane anti-breast cancer by controlling PI3K-Akt pathway and the tumor immune microenvironment.” Frontiers in Immunology 14 (2023): 1041525.
[2] What are the side effects of Formestane? (patsnap.com) https://synapse.patsnap.com/article/what-are-the-side-effects-of-formestane