PVTX-321 / SK Bio - LARVOL DELTA

Discovery and characterization of PVTX-321, an estrogen receptor heterobifunctional degrader (AACR 2024) - "Moreover, PVTX-321 achieves tumor regression as an oral agent at 10 mg/kg in MCF-7 mouse xenograft model. Furthermore, PVTX-321 possesses excellent in vitro and in vivo safety profiles and warrants further development for the treatment of ER+/HER2- breast cancer."

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 • ER • HER-2

Discovery and Characterization of PVTX-321 as a Potent and Orally Bioavailable Estrogen Receptor Degrader for ER+/HER2- Breast Cancer. (PubMed, J Med Chem) - "It demonstrates favorable oral bioavailability, dose-dependent ERα degradation in vivo and induces tumor regression at 10 mg/kg (QD) in MCF-7 xenografts. With minimal CYP inhibition and a strong preclinical safety profile, PVTX-321 is a promising candidate for advancing ER+/HER2- breast cancer treatment."

Journal • Breast Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • HER2 Positive Breast Cancer • Hormone Receptor Breast Cancer • Oncology • Solid Tumor • CRBN • ER • HER-2

Proteovant Therapeutics to Present Preclinical Data from Estrogen Receptor and IKZF2 Protein Degrader Programs (GlobeNewswire) - "Proteovant Therapeutics...announced it will present data on PVTX-321, an estrogen receptor degrader, at the Protein Degradation & Targeting Undruggables Congress USA, March 15-16 in Boston and on PVTX-405, an IKZF2 molecular glue, at the Targeted Protein Degradation Europe Conference, March 28-30 in London....'PVTX-321, our degrader targeting the estrogen receptor, is highly potent and demonstrates impressive, dose dependent tumor growth inhibition and shrinkage in preclinical models. In addition, PVTX-405 has best-in-class potential with robust IKZF2 degradation in vivo'."

Preclinical • Oncology