Category: Targeted therapy

Regorafenib, a potent oral multi-kinase inhibitor, leverages a distinct and multi-pronged approach to inhibit cancer progression by targeting multiple signaling pathways critical for tumor growth, angiogenesis, and metastasis. Unlike traditional cytotoxic chemotherapy, its unique mechanism of action focuses on blocking specific proteins, providing a targeted therapeutic effect.

Afatinib is a second-generation tyrosine kinase inhibitor approved for specific non-small cell lung cancer (NSCLC) types. A key to its effectiveness lies in understanding **what is the mechanism of action of afatinib**—its irreversible inhibitory activity against multiple ErbB receptor family targets.

In 2020, selumetinib received FDA approval as the first effective treatment for children with neurofibromatosis type 1 (NF1) and inoperable plexiform neurofibromas (PNs). But beyond its clinical success, a critical question remains: **how does selumetinib work** at a molecular level to produce these therapeutic effects?

Affecting 3–4% of non-small cell lung cancer (NSCLC) patients, MET exon 14 skipping alterations are a specific therapeutic target. Understanding **what is the mechanism of action of tepotinib** is key to appreciating how this targeted therapy addresses such mutations by selectively inhibiting the MET tyrosine kinase receptor. This dual-action inhibitor not only controls tumor growth by blocking the MET signaling pathway but also combats multidrug resistance.

In recent clinical trials, the targeted drug trastuzumab deruxtecan (Enhertu) demonstrated a 72% improvement in progression-free survival for certain patients with HER2-positive metastatic breast cancer compared to a different therapy. This innovative medication, which incorporates the chemotherapy payload **Deruxtecan**, represents a significant advancement in oncology by selectively delivering potent treatment directly to cancer cells.

According to the American Cancer Society, about half of all melanomas have changes in the BRAF gene. A BRAF inhibitor is a targeted cancer drug that blocks the activity of the mutated BRAF protein, helping to stop cancer cells from growing and dividing uncontrollably.

Sorafenib, a multikinase inhibitor also known by the brand name Nexavar®, was one of the first targeted therapies to demonstrate a significant survival benefit in patients with advanced hepatocellular carcinoma. This oral medication is primarily used to treat three distinct types of advanced cancer: liver, kidney, and a specific type of thyroid carcinoma.

Zanubrutinib, sold under the brand name Brukinsa, is a highly selective inhibitor of Bruton's tyrosine kinase (BTK) that has been shown to offer superior efficacy and cardiac safety compared to first-generation BTK inhibitors in clinical trials. This targeted oral therapy addresses the core signaling pathways that drive the growth of malignant B-cells, representing a major advancement in the treatment of certain blood cancers. Understanding **what is the mechanism of Brukinsa** provides crucial insight into how this precision medicine combats cancer at a molecular level.