DDInter649 DDInter1658
Enzalutamide is an androgen receptor (AR) inhibitor for the treatment of castration-resistant prostate cancer (CRPC), both metastatic and non-metastatic. It is a second-generation antiandrogen agent that the FDA approved on August 31, 2012.[L40639, A252667] Although androgen deprivation therapy (ADT) is the first-line treatment of prostate cancer and remission can be achieved, arising resistance is inevitable, becoming castration-resistant prostate cancer. Until recently, docetaxel is the only treatment available for metastatic CRPC; however, AR inhibitors have been developed for more targeted therapy, although first-generation AR inhibitors like bicalutamide did not substantially increase the survival rate. Second-generation such as enzalutamide is more efficacious due to a higher affinity to AR and no partial agonist activity compared to bicalutamide.[A252667,A252642] Due to a favorable pharmacological profile,
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.
Enzalutamide {u} (Compound) resembles {v} (Compound) Nilutamide
Enzalutamide {u} (Compound) resembles {v} (Compound) Bicalutamide
Enzalutamide {u} (Compound) binds {v} (Gene) CYP3A4
Enzalutamide {u} (Compound) upregulates {v} (Gene) RPL39L
Enzalutamide {u} (Compound) is included by {v} (Pharmacologic Class) Cytochrome P450 3A4 Inducers
Enzalutamide {u} (Compound) causes {v} (Side Effect) Musculoskeletal pain
Enzalutamide {u} may cause a minor interaction that can limit clinical effects when taken with {v} Mirabegron
Enzalutamide {u} may cause a minor interaction that can limit clinical effects when taken with {v} Relugolix
Enzalutamide {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Teriflunomide
Enzalutamide {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Remdesivir
Enzalutamide (Compound) resembles Nilutamide (Compound)
Enzalutamide (Compound) resembles Bicalutamide (Compound)
Enzalutamide (Compound) binds CYP3A4 (Gene)
Enzalutamide (Compound) upregulates RPL39L (Gene)
Enzalutamide (Compound) is included by Cytochrome P450 3A4 Inducers (Pharmacologic Class)
Enzalutamide (Compound) causes Musculoskeletal pain (Side Effect)
Enzalutamide may cause a minor interaction that can limit clinical effects when taken with Mirabegron
Enzalutamide may cause a minor interaction that can limit clinical effects when taken with Relugolix
Enzalutamide may cause a moderate interaction that could exacerbate diseases when taken with Teriflunomide
Enzalutamide may cause a moderate interaction that could exacerbate diseases when taken with Remdesivir