Rintodestrant

Last updated

Rintodestrant
Rintodestrant.svg
Clinical data
Other namesG1T48
Identifiers
  • (E)-3-[4-[2-(4-fluoro-2,6-dimethyl-benzoyl)-6-hydroxy-benzothiophen-3-yl]oxyphenyl]prop-2-enoic acid
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
ChEMBL
Chemical and physical data
Formula C26H19FO5S
Molar mass 462.49 g·mol−1
3D model (JSmol)
  • 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=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 (G1T48) is an orally bioavailable selective estrogen receptor degrader (SERD) discovered in Greg Thatcher's lab at UIC [1] and developed by G1 Therapeutics for the treatment of estrogen receptor-positive (ER+) breast cancer [2] . 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. [3]

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. [4]

References

  1. ↑ Xiong R, Zhao J, Gutgesell LM, Wang Y, Lee S, Karumudi B, et al. (23 February 2017). "Novel Selective Estrogen Receptor Downregulators (SERDs) Developed against Treatment-Resistant Breast Cancer". Journal of medicinal chemistry. 60 (4): 1325–1342. doi:10.1021/acs.jmedchem.6b01355. PMID   28117994.
  2. ↑ Andreano KJ, Wardell SE, Baker JG, Desautels TK, Baldi R, Chao CA, et al. (April 2020). "G1T48, an oral selective estrogen receptor degrader, and the CDK4/6 inhibitor lerociclib inhibit tumor growth in animal models of endocrine-resistant breast cancer". Breast cancer research and treatment. 180 (3): 635–646. doi:10.1007/s10549-020-05575-9. PMID   32130619.
  3. ↑ 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.
  4. ↑ 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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