Rintodestrant

Rintodestrant
Clinical data
Other names	G1T48
Identifiers
	IUPAC name (E)-3-[4-[2-(4-fluoro-2,6-dimethyl-benzoyl)-6-hydroxy-benzothiophen-3-yl]oxyphenyl]prop-2-enoic acid;
CAS Number	2088518-51-6;
PubChem CID	129205616;
ChemSpider	76743881;
UNII	W3Y784Y0ES;
KEGG	D11736;
ChEMBL	ChEMBL4059888;
Chemical and physical data
Formula	C26H19FO5S
Molar mass	462.49 g·mol−1
3D model (JSmol)	Interactive image;
	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;
	InChI InChI=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+; Key: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.^[2]

References

^ 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

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[Gheysen_2024-1] 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.

[2] 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

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