HP568 / Hinova Pharma - LARVOL DELTA

PROteolysis TArgeting Chimera (PROTAC) Estrogen Receptor Degraders for Treatment of Estrogen Receptor-Positive Advanced Breast Cancer. (PubMed, Target Oncol) - "Preclinical data demonstrate increased tumor growth inhibition with vepdegestrant alone or in combination with CDK4/6 inhibitors compared with the selective ER degrader fulvestrant. In a first-in-human phase 1/2 clinical study, vepdegestrant administered orally as monotherapy or in combination with palbociclib showed promising clinical activity and a favorable safety profile in patients with heavily pretreated ER+/HER2- advanced breast cancer. Several other PROTAC ER degraders (AC699, ERD-3111, ERD-4001, and HP568) are in early development and have demonstrated activity in preclinical breast cancer models, with some recently entering clinical trials. The data highlight the potential for PROTAC ER degraders to be a new backbone therapy in breast cancer."

Journal • Review • Breast Cancer • Estrogen Receptor Positive Breast Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • HER2 Positive Breast Cancer • Hormone Receptor Breast Cancer • Hormone Receptor Positive Breast Cancer • Oncology • Solid Tumor • Targeted Protein Degradation • ER • HER-2

HP568, a highly potent and orally bioavailable ER PROTAC for breast cancer treatment, currently undergoing phase 1/2 clinical studies (AACR 2025) - P1/2 | "In direct efficacy comparisons with ARV-471, HP568 shows superior, dose-dependent tumor growth inhibition (TGI) of 90%-123%, well correlated with drug exposure and pharmacodynamic biomarkers. Importantly, in models resistant to fulvestrant, including MCF-7 ERα D538G and Y537S cell-derived CDX mice, it demonstrates significant dose-dependent TGI (29%-115%) while maintaining favorable safety profiles...The Phase 1 dose escalation part of the study is assessing safety, pharmacokinetics, pharmacodynamics, preliminary antitumor activity, and potential efficacy biomarkers. The Phase 2 expansion will evaluate HP568 both as a monotherapy and in combination with a CDK4/6 inhibitor.HP568 structure will not be disclosed."

Clinical • Late-breaking abstract • P1/2 data • Breast Cancer • HER2 Breast Cancer • HER2 Positive Breast Cancer • Hormone Receptor Breast Cancer • Oncology • Solid Tumor • ER • HER-2

Hinova Pharmaceuticals Receives FDA Proceed Authorization for its IND Application for HP568, an Orally Bioavailable Chimeric Degrader Targeting ER for ER+/HER2- Advanced Breast Cancer Treatment (Hinova Pharma Press Release) - "Hinova Pharmaceuticals Inc...announced that the US Food and Drug Administration (FDA) has cleared the company’s investigational new drug application (IND) for HP568, an investigational drug targeting Estrogen Receptor (ER) for the treatment of ER-positive (ER+) and human epidermal growth factor receptor 2-negative (HER2-) advanced breast cancer."

IND • Estrogen Receptor Positive Breast Cancer • HER2 Negative Breast Cancer

A Phase I/II Trial to Evaluate Oral HP568 Tablets in Patients with ER+/HER2 Advanced Breast Cancer (clinicaltrials.gov) - P1/2 | N=204 | Not yet recruiting | Sponsor: Hinova Pharmaceuticals Inc.

New P1/2 trial • Breast Cancer • HER2 Breast Cancer • Hormone Receptor Breast Cancer • Oncology • Solid Tumor

The first subject has been enrolled in the Phase I/II clinical trial of HP568 tablets, an oral PROTAC drug developed by Haichuang Pharmaceuticals, for the treatment of ER+/HER2- advanced breast cancer in China [Google translation] (Sina Corp) - "Recently, the first subject was enrolled in the clinical trial...of HP568 tablets independently developed by Haichuang Pharmaceutical Co., Ltd. (hereinafter referred to as 'the Company') for the treatment of estrogen receptor (ER)-positive and human epidermal growth factor receptor 2 (HER2)-negative advanced breast cancer (ER+/HER2-advanced breast cancer)."

Enrollment open • Estrogen Receptor Positive Breast Cancer • HER2 Negative Breast Cancer

’Haichuang Pharmaceutical’s oral PROTAC drug HP568 tablets for the treatment of ER+/HER2- advanced breast cancer clinical trial application approved by the US FDA’ [Google translation] (Hinova Pharma Press Release) - "Recently, Haichuang Pharmaceutical Co., Ltd...received a Study May Proceed Notification from the U.S. Food and Drug Administration...The clinical trial application of HP568 tablets independently developed by the company for the treatment of estrogen receptor (ER) positive and human epidermal growth factor receptor 2 (HER2) negative advanced breast cancer (ER+/HER2-advanced breast cancer) was officially approved by the FDA."

IND • Estrogen Receptor Positive Breast Cancer • HER2 Negative Breast Cancer

Haichuang Pharmaceuticals: HP568 tablets for the treatment of ER+/HER2- advanced breast cancer approved for clinical trials [Google translation] (163.com) - "Haichuang Pharmaceutical...announced on the evening of October 15 that the company received the 'Notice of Approval for Drug Clinical Trial' approved and issued by the Drug Review Center of the National Medical Products Administration, agreeing to conduct clinical trials of HP568 tablets for the treatment of estrogen receptor (ER)-positive and human epidermal growth factor receptor 2 (HER2)-negative advanced breast cancer (ER+/HER2-advanced breast cancer)."

New trial • Breast Cancer • Estrogen Receptor Positive Breast Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • Oncology • Solid Tumor

Identification of the highly potent and orally available ER-targeting PROTAC degrader HP568 for the treatment of breast cancer (AACR 2024) - "HP568 is under the preclinical development and has the potential to be the best-in-class ER-targeting degrader. HP568 structure will not be disclosed."

Late-breaking abstract • Breast Cancer • Hormone Receptor Breast Cancer • Oncology • Solid Tumor • ER