BI 2536 + pemetrexed

BI 2536 + pemetrexed is a combination therapy consisting of BI 2536, a potent and highly selective small molecule inhibitor of polo-like kinase 1 (Plk1), and pemetrexed, an approved antifolate chemotherapeutic agent. Plk1 is a key regulator of mitotic progression, making its inhibition a targeted approach for cancer therapy. Pemetrexed inhibits multiple enzymes involved in folate metabolism and DNA synthesis. This combination has been investigated primarily in patients with relapsed or advanced non-small-cell lung cancer (NSCLC). Clinical studies have shown that the combination has an acceptable safety profile, with the most common adverse events being fatigue, nausea, rash, and neutropenia. The recommended dose from phase I trials was established as BI 2536 at 200 mg combined with standard-dose pemetrexed (500 mg/m²) every three weeks[1][3]. The antitumor activity observed supports further investigation of Plk inhibitors in oncology[1][3].