Regor Therapeutics Announces First-in-Human Dosing of RGT-419B, a Next-Generation Oral CDK2/4/6 Inhibitor, in Phase 1 Clinical Trial

On April 8, 2022, Regor Therapeutics, a clinical-stage biotechnology company, announced that the first patient has been dosed in the Phase I clinical trial of its self-developed next-generation small molecule targeted anti-tumor inhibitor RGT-419B.

RGT-419B is a new generation of small molecule oral CDK2/4/6 inhibitor with an optimized kinase activity profile. RGT-419B is expected to be used in combination with endocrine therapy for the treatment of advanced or metastatic hormone receptor-positive (HR+), human epidermal growth factor receptor 2-negative (HER2-) breast cancer.Breast CancerPre-/post-menopausal women. This trial is a Phase I, non-randomized, open-label, first-in-human clinical study exploring the oral dose escalation of RGT-419B in hormone receptor-positive, HER-2 receptor-negative advanced or metastatic breast cancer patients under single-agent or combination endocrine therapy conditions. The study officially launched in March 2022 and completed the first patient dosing in the United States.

Preclinical studies have found that RGT-419B completely inhibits tumor cell proliferation in CDK4/6 inhibitor-resistant ER+ breast cancer cell models. Meanwhile, preclinical data indicate that the inhibitory effect of RGT-419B on tumor cells is further enhanced when combined with selective estrogen receptor degraders (SERD) or PI3K inhibitors.BioValley bioon）