giredestrant

11/03/2023 - "Results warrant further evaluation of giredestrant in randomized trials in early- and late-stage ER+ breast cancer."
11/29/2023 - "Optimizing Early-Stage Clinical Pharmacology Evaluation to Accelerate Clinical Development of Giredestrant in Advanced Breast Cancer."
11/29/2023 - "This phase Ia/Ib dose-escalation/-expansion study (NCT03332797) evaluated the safety, pharmacokinetics, pharmacodynamics, and preliminary antitumor activity of giredestrant in estrogen receptor-positive HER2-negative locally advanced/metastatic breast cancer. "
01/01/2023 - "We report the primary and final analyses of the coopERA Breast Cancer study, designed to test whether giredestrant, a highly potent, non-steroidal, oral SERD, would show a stronger anti-proliferative effect than anastrozole after 2 weeks for oestrogen receptor-positive, HER2-negative, untreated early breast cancer. "
03/01/2023 - "Giredestrant is a promising small-molecule therapeutic agent under development by Genentech to treat patients with estrogen receptor-positive breast cancer. "

08/01/2023 - "This study aimed to develop physiologically-based pharmacokinetic/pharmacodynamic (PBPK-PD) models to characterize the relationships between oral exposure of GDC-9545 and GDC-0927 and tumor regression in HCI-013 tumor-bearing mice, and to translate these PK-PD relationships to a projected human efficacious dose by integrating clinical PK data. "
11/03/2023 - "Clinical benefit was observed in all cohorts (48.6% of patients in the single-agent cohort and 81.3% in the giredestrant +palbociclib ±LHRH agonist cohort), with no clear dose relationship, including in patients with ESR1-mutated tumors. "
09/21/2022 - "In addition, giredestrant demonstrated activity against a molecularly characterized ESR1 mutant tumor from a patient enrolled in a phase 1 clinical trial. "

01/01/2023 - "At the final analysis (data cutoff Nov 24, 2021), the most common grade 3-4 adverse events were neutropenia (29 [26%] of 112 in the giredestrant plus palbociclib group vs 29 [27%] of 109 in the anastrozole plus palbociclib group) and decreased neutrophil count (17 [15%] vs 16 [15%]). "

01/01/2023 - "One patient died due to an adverse event in the giredestrant plus palbociclib group (myocardial infarction). "

09/21/2022 - "Giredestrant reverses progesterone hypersensitivity driven by estrogen receptor mutations in breast cancer."