DDInter1026 DDInter1658
Larotrectinib is an orally administered inhibitor of tropomyosin receptor kinase (Trk), a receptor tyrosine kinase activated by neurotrophins which is mutated in a variety of cancer cell types and plays an important role in tumor cell growth and survival. Upon administration, larotrectinib binds to Trk, thereby preventing neurotrophin-Trk interaction and Trk activation, which results in both the induction of cellular apoptosis and the inhibition of cell growth in tumors that overexpress Trk. Larotrectinib was granted accelerated approval by the FDA in November 2018 for the treatment of Trk-positive solid tumors. It was notable for being the second tissue-agnostic chemotherapy ever approved by the FDA.
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.
Larotrectinib {u} may cause a minor interaction that can limit clinical effects when taken with {v} Sibutramine
Larotrectinib {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Lefamulin
Larotrectinib {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Calaspargase pegol
Larotrectinib {u} may lead to a major life threatening interaction when taken with {v} Pimozide
Larotrectinib may cause a minor interaction that can limit clinical effects when taken with Sibutramine
Larotrectinib may cause a moderate interaction that could exacerbate diseases when taken with Lefamulin
Larotrectinib may cause a moderate interaction that could exacerbate diseases when taken with Calaspargase pegol
Larotrectinib may lead to a major life threatening interaction when taken with Pimozide