DDInter1678 DDInter1658
Sirolimus, also known as rapamycin, is a macrocyclic lactone antibiotic produced by bacteria _Streptomyces hygroscopicus_, which was isolated from the soil of the Vai Atari region of Rapa Nui (Easter Island). It was first isolated and identified as an antifungal agent with potent anticandida activity; however, after its potent antitumor and immunosuppressive activities were later discovered, it was extensively investigated as an immunosuppressive and antitumour agent. Its primary mechanism of action is the inhibition of the mammalian target of rapamycin (mTOR), which is a serine/threonine-specific protein kinase that regulates cell growth, proliferation, and survival. mTOR is an important therapeutic target for various diseases, as it was shown to regulate longevity and maintain normal glucose homeostasis. Targeting mTOR received more attention especially in cancer, as mTOR signalling pathways are constitutively activated in
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.
Sirolimus {u} (Compound) resembles {v} (Compound) Pimecrolimus
Sirolimus {u} (Compound) binds {v} (Gene) ABCB1
Sirolimus {u} (Compound) upregulates {v} (Gene) WDR13
Sirolimus {u} (Compound) is included by {v} (Pharmacologic Class) Decreased Immunologic Activity
Sirolimus {u} (Compound) downregulates {v} (Gene) IMP3
Sirolimus {u} (Compound) causes {v} (Side Effect) Aspartate aminotransferase increased
Sirolimus {u} may cause a minor interaction that can limit clinical effects when taken with {v} Zinc sulfate
Sirolimus {u} may cause a minor interaction that can limit clinical effects when taken with {v} Vitamin E
Sirolimus {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Lansoprazole
Sirolimus {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Brigatinib
Sirolimus (Compound) resembles Pimecrolimus (Compound)
Sirolimus (Compound) binds ABCB1 (Gene)
Sirolimus (Compound) upregulates WDR13 (Gene)
Sirolimus (Compound) is included by Decreased Immunologic Activity (Pharmacologic Class)
Sirolimus (Compound) downregulates IMP3 (Gene)
Sirolimus (Compound) causes Aspartate aminotransferase increased (Side Effect)
Sirolimus may cause a minor interaction that can limit clinical effects when taken with Zinc sulfate
Sirolimus may cause a minor interaction that can limit clinical effects when taken with Vitamin E
Sirolimus may cause a moderate interaction that could exacerbate diseases when taken with Lansoprazole
Sirolimus may cause a moderate interaction that could exacerbate diseases when taken with Brigatinib