DDInter462 DDInter1658
Dabrafenib mesylate (Tafinlar) is a reversible ATP-competitive kinase inhibitor and targets the MAPK pathway. It was approved on May 29, 2013, for the treatment of melanoma with V600E or V6000K mutation. It was also used for metastatic non-small cell lung cancer with the same mutation. In May 2018, Tafinlar (dabrafenib), in combination with Mekinist (), was approved to treat anaplastic thyroid cancer caused by an abnormal BRAF V600E gene.
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.
Dabrafenib {u} (Compound) binds {v} (Gene) SLCO1B3
Dabrafenib {u} (Compound) upregulates {v} (Gene) PSAT1
Dabrafenib {u} (Compound) is included by {v} (Pharmacologic Class) Organic Anion Transporter 3 Inhibitors
Dabrafenib {u} (Compound) downregulates {v} (Gene) LIG1
Dabrafenib {u} (Compound) causes {v} (Side Effect) Abdominal pain
Dabrafenib {u} may cause a minor interaction that can limit clinical effects when taken with {v} Bortezomib
Dabrafenib {u} may cause a minor interaction that can limit clinical effects when taken with {v} Fostemsavir
Dabrafenib {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Nilotinib
Dabrafenib {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Darolutamide
Dabrafenib {u} may lead to a major life threatening interaction when taken with {v} Levacetylmethadol
Dabrafenib (Compound) binds SLCO1B3 (Gene)
Dabrafenib (Compound) upregulates PSAT1 (Gene)
Dabrafenib (Compound) is included by Organic Anion Transporter 3 Inhibitors (Pharmacologic Class)
Dabrafenib (Compound) downregulates LIG1 (Gene)
Dabrafenib (Compound) causes Abdominal pain (Side Effect)
Dabrafenib may cause a minor interaction that can limit clinical effects when taken with Bortezomib
Dabrafenib may cause a minor interaction that can limit clinical effects when taken with Fostemsavir
Dabrafenib may cause a moderate interaction that could exacerbate diseases when taken with Nilotinib
Dabrafenib may cause a moderate interaction that could exacerbate diseases when taken with Darolutamide
Dabrafenib may lead to a major life threatening interaction when taken with Levacetylmethadol