Liposomal Formulation of the CDK9 PROTAC THAL-SNS-032 Enhances the Antitumor activity in Breast Cancer

Liposomal Formulation of the CDK9 PROTAC THAL-SNS-032 Enhances the Antitumor activity in Breast Cancer

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Thrilled to announce our latest work in Biomedicine & Pharmacotherapy (July 12, 2025): “Liposomal formulation of the CDK9 PROTAC THAL‑SNS‑032 enhances the antitumor activity in breast cancer cell lines.”

In this study, we tackled a key hurdle in PROTAC therapeutics—bioavailability and off‑target toxicity—by converting THAL‑SNS‑032, a potent CDK9‑targeting PROTAC, into three lipid‑based nano‑formulations: solid lipid nanoparticles (SLN‑THAL), cholesterol‑free liposomes (LIP‑THAL), and cholesterol‑loaded liposomes (cLIP‑THAL). Of these, cLIP‑THAL stood out for stability, controlled release, and impressive in vitro efficacy against breast cancer cell lines. Importantly, it maintained anticancer potency comparable to free PROTACs while showing reduced toxicity in non‑cancerous cells.

By encapsulating THAL‑SNS‑032 in nanocarriers, we improved pharmacological properties and safety, paving the way for next‑gen nanomedicine applications of PROTACs in oncology. This could mark a significant step toward targeted, safer therapies for breast cancer