azd-5153 + ptc-209

AZD-5153 + PTC-209 is a **combination of two small molecule inhibitors** targeting dysregulated epigenetic modifiers. AZD-5153 is a reversible, bivalent inhibitor of the bromodomain and extraterminal domain family protein **BRD4**, developed to disrupt oncogenic transcriptional programs, notably MYC, by binding to both BRD4 bromodomains. PTC-209 is a selective inhibitor of the **Polycomb repressive complex 2 (PRC2)** component **Bmi-1**, which regulates stem cell renewal and cancer cell proliferation. This combination exhibits **synergistic antiproliferative and cytostatic effects** in preclinical models, notably in **autosomal dominant polycystic kidney disease (ADPKD) patient-derived cells** and **3D polycystic kidney disease cyst models**, as well as in various cancers. The mechanism involves dual targeting of two distinct epigenetic regulators, potentially overcoming resistance and exerting more robust tumor suppression[1][3][7]. AZD-5153 was developed by **AstraZeneca**, while PTC-209 was developed by **PTC Therapeutics**.

Other names

azd-5153 plus ptc-209azd5153 plus ptc-209azd 5153 plus ptc-209azd-5153 + ptc-209 combination