Rintodestrant is an orally bioavailable selective estrogen receptor degrader (SERD) developed by G1 Therapeutics for the treatment of estrogen receptor-positive (ER+) breast cancer. Structurally inspired by the 6-OH-benzothiophene scaffold used in arzoxifene and raloxifene, rintodestrant selectively binds to the estrogen receptor and inhibits ER signaling, demonstrating efficacy in endocrine-resistant tumors.[1]
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Other names | G1T48 |
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Formula | C26H19FO5S |
Molar mass | 462.49 g·mol−1 |
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A phase I clinical trial evaluated rintodestrant as monotherapy and in combination with the CDK4/6 inhibitor palbociclib in patients with ER+/HER2- advanced breast cancer.[2]
References
edit- ^ Gheysen M, Punie K, Wildiers H, Neven P (November 2024). "Oral SERDs changing the scenery in hormone receptor positive breast cancer, a comprehensive review". Cancer Treatment Reviews. 130: 102825. doi:10.1016/j.ctrv.2024.102825. PMID 39293125.
- ^ Clinical trial number NCT03455270 for "G1T48, an Oral SERD, Alone and in Combination With Palbociclib in ER-Positive, HER2-Negative Advanced Breast Cancer" at ClinicalTrials.gov