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Imlonstrant is a substance under investigation that acts as a selective estrogen receptor modulator (SERM) and is specifically designed to treat advanced breast cancer, particularly hormone receptor-positive (HR+) and human epidermal growth factor 2 (HER2-)-negative breast cancer.However, a significant proportion of patients develop resistance to these drugs over time, often due to mutations in the estrogen receptor 1 (ESR1) gene or through adaptive cellular mechanisms that keep ER receptor signaling active.To overcome the obstacle of resistance to hormone therapy, new therapeutic approaches such as selective estrogen receptor lysates (SERLs) have been developed.
Imlonstrant is a substance under investigation that acts as a selective estrogen receptor modulator (SERM) and is specifically designed to treat advanced breast cancer, particularly hormone receptor-positive (HR+) and human epidermal growth factor 2 (HER2−)-negative breast cancer.
Breast cancer is a polymorphic disease characterized by the uncontrolled proliferation of epithelial cells within breast tissue. HER2-positive breast cancer accounts for approximately 70% of all breast cancer cases and is highly dependent on estrogen receptor (ER) signaling. Estrogen stimulates tumor growth by binding to ER receptors, which in turn activates genes responsible for cell development and retention.
Hormone therapy is the cornerstone of management for HER2-positive breast cancer and includes drugs such as aromatase inhibitors and selective estrogen receptor modulators (SERMs). However, a significant proportion of patients develop resistance to these drugs over time, often due to mutations in the estrogen receptor 1 (ESR1) gene or through adaptive cellular mechanisms that keep ER receptor signaling active.
To overcome the obstacle of resistance to hormone therapy, new therapeutic approaches such as selective estrogen receptor lysates (SERLs) have been developed. These molecules, including imlonstrant, work by binding to the estrogen receptor and accelerating its breakdown, thereby inhibiting the growth of ER-dependent tumors and offering a promising treatment option for refractory and advanced forms of the disease.
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