borestrant (ZB716) / Zenopharm, EnhancedBio - LARVOL DELTA

Analysis of the Main Directions in the Development of Mono and Combination Pharmacotherapy Acting on Hormonal Signaling Pathways of Breast Cancer According to the FDA Databases and Clinicaltrials.gov. (PubMed, Curr Med Chem) - "It is evident that traditional endocrine treatments play a pivotal role in the management of HR+ BC. However, the emergence of resistance necessitates the development of novel therapeutic strategies. These strategies should be based on pharmacokinetics, further investigation of the molecular signaling pathways of BC, such as new SERMs, SERDs, PROTACs, as well as new drug groups, like SERCAs, CERANs, SHERPAs. Combination therapy represents the most promising avenue for BC treatment. While PROTAC combination with new monotherapeutic agents for BC treatment has yet to be investigated, we believe that such combinations have the potential to make the treatment more selective, effective, and personalised in the future."

Journal • Breast Cancer • Endocrine Cancer • Hormone Receptor Breast Cancer • Oncology • Solid Tumor • Targeted Protein Degradation • CDK4

Design and synthesis of a novel ZB716-d6 as a stable isotopically labeled internal standard. (PubMed, Synth Commun) - "This procedure is very practicable and gives the final compound in good yield (19% total yield) and high purity (D, >99%, chemical purity 98%). At present, ZB716-d6 has been successfully used as an internal standard in clinical bioanalysis."

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

Fulvestrant-3-Boronic Acid (ZB716) Demonstrates Oral Bioavailability and Favorable Pharmacokinetic Profile in Preclinical ADME Studies. (PubMed, Pharmaceuticals (Basel)) - "In human liver microsomes, ZB716 demonstrated relatively low inhibition of CYP1A2, 2C8, 2C9, 2C19, 2D6, and 3A4 (when testosterone was used as the substrate), and no inhibition of CYP2B6 and 3A4 (when midazolam was used as the substrate). In assays for enzyme activity, ZB716 induced CYP1A2, 2B6, and 3A4 in a concentration-dependent manner. Single-dose and repeated-dose pharmacokinetic studies in rats and dogs showed oral bioavailability, dose-proportional drug exposure, and drug accumulation as measured by maximum concentration and area under the concentration-time curve (AUC)."

Journal • PK/PD data • Preclinical • Breast Cancer • Hormone Receptor Breast Cancer • Oncology • Solid Tumor • ER

ER+/HER2- Locally Advanced or Metastatic Breast Cancer (ENZENO Study) (clinicaltrials.gov) - P1/2; N=106; Recruiting; Sponsor: EnhancedBio USA Inc.; Not yet recruiting ➔ Recruiting; Initiation date: Feb 2021 ➔ May 2021

Clinical • Combination therapy • Enrollment open • Monotherapy • Trial initiation date • Breast Cancer • Estrogen Receptor Positive Breast Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • Hormone Receptor Breast Cancer • Hormone Receptor Positive Breast Cancer • Oncology • Solid Tumor • ER

ER+/HER2- Advanced or Metastatic Breast Cancer (ENZENO Study) (clinicaltrials.gov) - P1/2; N=106; Not yet recruiting; Sponsor: EnhancedBio USA Inc.

Clinical • Combination therapy • Monotherapy • New P1/2 trial • Breast Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • Hormone Receptor Breast Cancer • Hormone Receptor Positive Breast Cancer • Oncology • Solid Tumor • ER