LX-039 / WuXi AppTec, Luoxin Pharma - LARVOL DELTA

Results from a first-in-human phase Ia/b study of LX-039, an oral selective estrogen receptor (ER) degrader (SERD), in postmenopausal patients with ER+, HER2- advanced breast cancer (ABC) (ESMO 2023) - P1 | "All pts received prior endocrine therapy (range: 1-7 lines, 56.8% fulvestrant) and/or CDK4.6i(40.9%), chemotherapy(54.5%) in the advanced setting. Conclusions LX-039 was well tolerated with preliminary anti-tumor activity in ER+, HER2- ABC. RP2D was determined at 600 mg QD and a phase II trial is being planned."

Clinical • Metastases • P1 data • Breast Cancer • HER2 Breast Cancer • Hormone Receptor Breast Cancer • Oncology • Solid Tumor • CDK4 • ER • HER-2

Luoxin Pharmaceutical's LX-039 (Innovative Anti-Tumor Drug): Phase I Clinical Study Data Presented at ESMO 2023 (PRNewswire) - P1 | N=44 | NCT04097756 | Sponsor: Shandong Luoxin Pharmaceutical Group Stock Co., Ltd | "Maximum tolerated dose (MTD) was not reached in this study. Most adverse events are graded as mild to moderate (grade 1-2). The exposure of LX-039 increased along with the dose escalation, and no obvious accumulation after multiple doses. Inhibition of the ER pathway is observed in all subjects participating in the PD exploration. Four subjects achieved partial response, with an objective response rate of 10.8% and a clinical benefit rate at 24 weeks of 40%. LX-039 demonstrates good tolerability and PK/PD properties in ER+ and HER2- advanced breast cancer and shows preliminary anti-tumor activity. These encouraging results suggest that LX-039 holds great potential for further development. Consequently, a phase II study is under planning."

P1 data • Breast Cancer • Estrogen Receptor Positive Breast Cancer • HER2 Negative Breast Cancer • Oncology • Solid Tumor

A Phase I Study of LX-039 Tablets (clinicaltrials.gov) - P1 | N=44 | Completed | Sponsor: Shandong Luoxin Pharmaceutical Group Stock Co., Ltd. | Enrolling by invitation ➔ Completed | N=68 ➔ 44 | Trial completion date: Jul 2023 ➔ Feb 2023

Enrollment change • Metastases • Trial completion • Trial completion date • Breast Cancer • HER2 Breast Cancer • Hormone Receptor Breast Cancer • Hormone Receptor Positive Breast Cancer • Oncology • Solid Tumor • ER • HER-2

Discovery and preclinical profile of LX-039, a novel indole-based oral selective estrogen receptor degrader (SERD). (PubMed, Bioorg Med Chem Lett) - P1 | "We report herein its profound anti-tumor activity, desirable ER antagonistic characteristics combined with favorable pharmacokinetic and preliminary safety properties. LX-039 is currently in clinical trial (NCT04097756)."

Journal • Preclinical • Breast Cancer • Estrogen Receptor Positive Breast Cancer • Hormone Receptor Positive Breast Cancer • Oncology • Solid Tumor • ER

A Phase I Study of LX-039 Tablets (clinicaltrials.gov) - P1; N=68; Enrolling by invitation; Sponsor: Shandong Luoxin Pharmaceutical Group Stock Co., Ltd.; Not yet recruiting ➔ Enrolling by invitation; Initiation date: Sep 2019 ➔ Jan 2020

Clinical • Enrollment open • Trial initiation date • ER • HER-2

A Phase I Study of LX-039 Tablets (clinicaltrials.gov) - P1; N=68; Not yet recruiting; Sponsor: Shandong Luoxin Pharmaceutical Group Stock Co., Ltd.

Clinical • New P1 trial