Rintodestrant Explained

Cas Number:2088518-51-6
Pubchem:129205616
Chemspiderid:76743881
Unii:W3Y784Y0ES
Kegg:D11736
Chembl:4059888
Synonyms:G1T48
Iupac Name:(E)-3-[4-[2-(4-fluoro-2,6-dimethyl-benzoyl)-6-hydroxy-benzothiophen-3-yl]oxyphenyl]prop-2-enoic acid
C:26
H:19
F:1
O:5
S:1
Smiles:CC1=CC(=CC(=C1C(=O)C2=C(C3=C(S2)C=C(C=C3)O)OC4=CC=C(C=C4)/C=C/C(=O)O)C)F
Stdinchi:InChI=1S/C26H19FO5S/c1-14-11-17(27)12-15(2)23(14)24(31)26-25(20-9-6-18(28)13-21(20)33-26)32-19-7-3-16(4-8-19)5-10-22(29)30/h3-13,28H,1-2H3,(H,29,30)/b10-5+
Stdinchikey:KOAITBOFZOEDOC-BJMVGYQFSA-N

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]

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.

Notes and References

  1. Gheysen M, Punie K, Wildiers H, Neven P . Oral SERDs changing the scenery in hormone receptor positive breast cancer, a comprehensive review . Cancer Treatment Reviews . 130 . 102825 . November 2024 . 39293125 . 10.1016/j.ctrv.2024.102825 . free .