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Association details:
| Biomarker: | PIK3CA H1047R |
|---|---|
| Cancer: | Hormone Receptor Positive Breast Cancer |
| Drug: | Ibrance (palbociclib) (CDK4 inhibitor, CDK6 inhibitor) + RLY-2608 (pan-mutant PIK3CA-selective inhibitor) |
| Direction: | Sensitive |
Evidence:
Source:
Title:
RLY-2608: The first allosteric mutant- and isoform-selective inhibitor of PI3Ka, is efficacious as a single agent and drives regressions in combination with standard of care therapies in PIK3CA mutant breast cancer models
Published date:
10/09/2021
Excerpt:
We performed in vitro combinations in two HR+ PIK3CA mutant cell lines (MCF7: E545K; T47D: H1047R) and observed synergy between RLY-2608 and fulvestrant or CDK4/6 inhibitors….in vivo combination efficacy with fulvestrant and CDK4/6 inhibitors (palbociclib or abemaciclib) was assessed in patient-derived xenografts harboring the PIK3CA H1047R or E545K mutation....RLY-2608 can be combined with fulvestrant and CDK4/6 inhibitors in vivo with tumor regressions observed in both cell- and patient-derived xenograft models. The preclinical profile of RLY-2608 supports the clinical development of RLY-2608 both in single agent and combination clinical trials in patients with PIK3CA mutant tumors, including HR+/PIK3CA mutant breast cancer.
