Tag: NSCLC

Mavelertinib is a Selective and Irreversible EGFR TKI

Mutant EGFRs are one of the major drivers of non-small-cell lung cancer (NSCLC). While reversible first-generation EGFR inhibitors are initially an effective treatment. However, a drug-resistant gatekeeper T790M mutation accounts for ∼50% of disease progression in patients with first-generation agents. Irreversible second-generation EGFR inhibitors are more potent against the...

CAY10404 is a Highly Selective COX-2 Inhibitor

Clooxygenase (COX) is an enzyme responsible for the formation of prostaglandins from arachidonic acid, including thromboxanes and prostaglandins. Specifically, it is a member of the animal heme peroxidase family, also known as prostaglandin G/H synthase. Besides, cyclooxygenase-2 is a candidate gene for lung injury induced by mechanical ventilation. COX-2...

JX06 is a Potent, Selective and Covalent Inhibitor of PDK

Pyruvate dehydrogenase kinase (PDK) is a kinase that can be inactivated by the use of ATP phosphorylation of pyruvate dehydrogenase. Specifically, PDK is relevant to the regulation of the pyruvate dehydrogenase complex with pyruvate dehydrogenase as the first component. Besides, PDK acts as a molecular switch to reduce mitochondrial...

ONO-7475 is a Selective and Orally Active AXL/Mer Inhibitor

EGFR tyrosine kinase inhibitors (EGFR-TKIs) are efficient for the treatment of non-small cell lung cancer (NSCLC) harboring EGFR mutations. However, most EGFR-positive NSCLC patients exhibit resistance to EGFR-TKIs after sometimes. The 3rd generation EGFR-TKI Osimertinib shows efficacy for overcoming EGFR T790M mutation-positive NSCLC. Anexelekto (AXL) belongs to the TAM...

TP3011 is a Potent Topoisomerase-1 Inhibitor with Anti-tumor Effect

Topoisomerases are proteins that cut the DNA backbone. Especially, topoisomerases let the cut ends twist past each other to a more relaxed configuration. Moreover, topoisomerases reseal the phosphodiester bonds in the backbone to again form an intact double helix. DNA topoisomerases I and II present in cells acts through...

AMG-510 is a First-in-Class, Orally Active, and Selective KRAS G12C Inhibitor

The KRAS oncoprotein is a GTPase and an essential mediator of intracellular signaling pathways. They are involved in tumor cell growth and survival. Somatic, activating mutations in KRAS are a hallmark of cancer. Furthermore, they prevent the association of GTPase-activating proteins, thus stabilizing effector binding and enhancing KRAS signaling....