Indications
Certican is a kinase inhibitor indicated for the treatment of: Postmenopausal women with advanced hormone receptor-positive, HER2- negative breast cancer in combination with exemestane after failure of treatment with letrozole or anastrozole. Adults with progressive neuroendocrine tumors of pancreatic origin (PNET) and adults with progressive, well-differentiated, non-functional neuroendocrine tumors (NET) of gastrointestinal (GI) or lung origin that are unresectable, locally advanced or metastatic. ... Read moreCertican is a kinase inhibitor indicated for the treatment of: Postmenopausal women with advanced hormone receptor-positive, HER2- negative breast cancer in combination with exemestane after failure of treatment with letrozole or anastrozole. Adults with progressive neuroendocrine tumors of pancreatic origin (PNET) and adults with progressive, well-differentiated, non-functional neuroendocrine tumors (NET) of gastrointestinal (GI) or lung origin that are unresectable, locally advanced or metastatic. Adults with advanced renal cell carcinoma (RCC) after failure of treatment with sunitinib or sorafenib. Adults with renal angiomyolipoma and tuberous sclerosis complex (TSC), not requiring immediate surgery. Certican are kinase inhibitors indicated for the treatment of adult and pediatric patients aged 1 year and older with TSC who have subependymal giant cell astrocytoma (SEGA) that requires therapeutic intervention but cannot be curatively resected.Certican is a kinase inhibitor indicated for the adjunctive treatment of adult and pediatric patients aged 2 years and older with TSC- associated partial-onset seizures.
⚠️ Always consult a registered physician before taking any medicine.
Pharmacology
Everolimus inhibits mammalian target of rapamycin (mTOR), a serine-threonine kinase acting downstream of the PI3K/AKT pathway. The mTOR pathway is dysregulated in several human cancers and in tuberous sclerosis complex (TSC). Everolimus binds to an intracellular protein, FKBP-12, forming a complex that inhibits mTOR complex 1 (mTORC1) and thereby suppresses mTOR kinase activity. Everolimus reduced the activity of S6 ribosomal protein kinase (S6K1) and eukaryotic initiation factor 4E-binding protein (4E-BP1), both downstream effectors of mTOR involved in protein synthesis. S6K1 is a substrate of mTORC1 and phosphorylates the activation domain 1 of the estrogen receptor, resulting in ligand-independent activation of the receptor. In addition, everolimus inhibited the expression of hypoxia-inducible factor (e.g., HIF-1) and reduced the expression of vascular endothelial growth factor (VEGF). Inhibition of mTOR by everolimus has been shown, in in vitro and/or in vivo studies, to reduce cell proliferation, angiogenesis, and glucose uptake.
Constitutive activation of the PI3K/Akt/mTOR pathway can contribute to endocrine resistance in breast cancer. In vitro studies show that estrogen-dependent and HER2-positive breast cancer cells are sensitive to the inhibitory effects of everolimus, and that combining everolimus with Akt, HER2, or aromatase inhibitors enhances its anti-tumor activity in a synergistic manner.
Pregnancy & Breastfeeding
Everolimus may harm a developing baby, based on findings from animal studies and how the drug works. A few case reports describe its use during human pregnancy, but there are too few to say how it affects the risk of birth defects or miscarriage. It is not known whether everolimus or its breakdown products pass into breast milk, or what effect it might have on a nursing infant or on milk supply.
⚠️ Talk to your doctor before taking any medicine during pregnancy or while breastfeeding.
Dosage Reference
⚠️ Reference ranges from official sources only. Consult your doctor for personalized dosing.
Side Effects & Interactions
Side Effects
No side-effect data recorded yet.