DDInter448 DDInter1658
Crizotinib is a tyrosine kinase receptor inhibitor used for the treatment of anaplastic lymphoma kinase (ALK) or ROS1-positive non-small cell lung cancer (NSCLC) tumors, as well as ALK-positive anaplastic large cell lymphoma (ALCL) and inflammatory myofibroblastic tumor (IMT). By targeting the echinoderm microtubule-associated protein-like 4 (EML4)-ALK fusion protein, crizotinib offers robust effectiveness in treating NSCLC in patients with this type of rearrangement. Crizotinib was the first-in-class drug used to treat ALK-positive tumors. Second- and third-generation ALK-tyrosine kinase-inhibitors have overcome many of the pharmacodynamic and genetic resistance mechanisms crizotinib is prone to. Crizotinib was approved by the FDA in 2011, and its use is accompanied by FDA-approved tests used
Selpercatinib is a kinase inhibitor with enhanced specificity for RET tyrosine kinase receptors (RTKs) over other RTK classes.[A202055, A202052, L13604] Enhanced RET (Rearranged during transfection) oncogene expression is a hallmark of many cancers. Although multikinase inhibitors, including [cabozantinib], [ponatinib], [sorafenib], [sunitinib], and [vandetanib], have shown efficacy in RET-driven cancers, their lack of specificity is generally associated with substantial toxicity. Selpercatinib (LOXO-292) and pralsetinib (BLU-667) represent the first generation of specific RET RTK inhibitors for the treatment of RET-driven cancers.[A202049, A202055, A202052, L13604] Although selpercatinib is currently still under investigation in clinical trial NCT04211337, it was granted accelerated FDA approval on May 8, 2020, for specific RET-driven cancer indications. It is currently marketed under the brand name RETEVMO™ by Loxo Oncology Inc. Selpercatinib is also approved by the European Commission.
Crizotinib {u} (Compound) treats {v} (Disease) lung cancer
Crizotinib {u} (Compound) binds {v} (Gene) MET
Crizotinib {u} (Compound) upregulates {v} (Gene) COL11A1
Crizotinib {u} (Compound) is included by {v} (Pharmacologic Class) Organic Cation Transporter 2 Inhibitors
Crizotinib {u} (Compound) downregulates {v} (Gene) WDR77
Crizotinib {u} (Compound) causes {v} (Side Effect) Dizziness postural
Crizotinib {u} may cause a minor interaction that can limit clinical effects when taken with {v} Modafinil
Crizotinib {u} may cause a minor interaction that can limit clinical effects when taken with {v} Fedratinib
Crizotinib {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Enfortumab vedotin
Crizotinib {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Gefitinib
Crizotinib (Compound) treats lung cancer (Disease)
Crizotinib (Compound) binds MET (Gene)
Crizotinib (Compound) upregulates COL11A1 (Gene)
Crizotinib (Compound) is included by Organic Cation Transporter 2 Inhibitors (Pharmacologic Class)
Crizotinib (Compound) downregulates WDR77 (Gene)
Crizotinib (Compound) causes Dizziness postural (Side Effect)
Crizotinib may cause a minor interaction that can limit clinical effects when taken with Modafinil
Crizotinib may cause a minor interaction that can limit clinical effects when taken with Fedratinib
Crizotinib may cause a moderate interaction that could exacerbate diseases when taken with Enfortumab vedotin
Crizotinib may cause a moderate interaction that could exacerbate diseases when taken with Gefitinib