copanlisib + refametinib

Copanlisib + refametinib is an investigational combination therapy consisting of two targeted small molecule inhibitors developed by Bayer. Copanlisib is an intravenous, pan-class I phosphoinositide 3-kinase (PI3K) inhibitor with predominant activity against the PI3K-alpha and PI3K-delta isoforms, while refametinib (BAY 86-9766) is a highly selective, orally administered allosteric inhibitor of MEK1/2. The combination has demonstrated synergistic antitumor activity in preclinical models and was evaluated in a phase Ib clinical trial for patients with advanced solid tumors, including colorectal cancer, non-small cell lung cancer, and biliary tract cancers. The primary objectives were to assess safety, tolerability, maximum tolerated dose (MTD), recommended phase II doses (RP2D), pharmacokinetics, and preliminary antitumor efficacy. The most common adverse events included diarrhea, nausea, rash, and fatigue; the best observed response was stable disease[1][2][3].