DDInter648 DDInter1658
Entrectinib is a tropomyosin receptor tyrosine kinase (TRK) TRKA, TRKB, TRKC, proto-oncogene tyrosine-protein kinase ROS1, and anaplastic lymphoma kinase (ALK) inhibitor. It was approved by the FDA in August 2019 for use in the treatment of ROS1-positive metastatic non-small cell lung cancer and NTRK gene fusion positive solid tumors. Entrectinib's approved use is meant as a last line of therapy due to its accelerated approval based on early trial data. This therapy offers benefit over similar ALK inhibitors such as [alectinib], [ceritinib], and [lorlatinib] due to a wider range of targets.
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.
Entrectinib {u} may cause a minor interaction that can limit clinical effects when taken with {v} Sulfamethoxazole
Entrectinib {u} may cause a minor interaction that can limit clinical effects when taken with {v} Darolutamide
Entrectinib {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Norethisterone
Entrectinib {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Oliceridine
Entrectinib {u} may lead to a major life threatening interaction when taken with {v} Disopyramide
Entrectinib {u} may lead to a major life threatening interaction when taken with {v} Macimorelin
Entrectinib may cause a minor interaction that can limit clinical effects when taken with Sulfamethoxazole
Entrectinib may cause a minor interaction that can limit clinical effects when taken with Darolutamide
Entrectinib may cause a moderate interaction that could exacerbate diseases when taken with Norethisterone
Entrectinib may cause a moderate interaction that could exacerbate diseases when taken with Oliceridine
Entrectinib may lead to a major life threatening interaction when taken with Disopyramide
Entrectinib may lead to a major life threatening interaction when taken with Macimorelin