DDInter704 DDInter1352
Everolimus is a derivative of Rapamycin (sirolimus), and works similarly to Rapamycin as an mTOR (mammalian target of rapamycin) inhibitor. It is currently used as an immunosuppressant to prevent rejection of organ transplants. In a similar fashion to other mTOR inhibitors Everolimus' effect is solely on the mTORC1 protein and not on the mTORC2 protein.
Osimertinib is an oral, third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) drug developed by AstraZeneca Pharmaceuticals.[A7926,L43453] Its use is indicated for the treatment of metastatic non-small cell lung cancer (NSCLC) in cases where tumour EGFR expression is positive for the T790M mutation as detected by FDA-approved testing and which has progressed following therapy with a first-generation EGFR tyrosine kinase inhibitor. Approximately 10% of patients with NSCLC have a rapid and clinically effective response to EGFR-TKIs due to the presence of specific activating EGFR mutations within the tumour cells. More specifically, deletions around the LREA motif in exon 19 and exon 21 L858R point mutations are correlated with response to therapy. Development of third-generation EGFR-TKIs, such as osimertinib, has been in response to altered tumour resistance patterns following treatment and toxic side effects that impact patient quality of life. Treatment with first-generation EGFR-TKIs (gefitinib and erlotinib) has been associated with the development of resistance through activating mutations in the EGFR gene. Second-generation EGFR-TKIs (afatinib and dacomitinib) were then developed to be more potent inhibitors, although their use is associated with increased toxicity through nonspecific targeting of wild-type EGFR. In contrast, third-generation inhibitors are specific for the gate-keeper T790M mutations which increases ATP binding activity to EGFR and result in poor prognosis for late-stage disease. Furthermore, osimertinib has been shown to spare wild-type EGFR during therapy, thereby reducing non-specific binding and limiting toxicity.[A7926,A7927,A7931]
Everolimus {u} (Compound) resembles {v} (Compound) Sirolimus
Sirolimus {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Osimertinib
Everolimus {u} (Compound) binds {v} (Gene) CYP3A4
CYP3A4 {u} (Gene) is bound by {v} (Compound) Bortezomib
Bortezomib {u} may cause a minor interaction that can limit clinical effects when taken with {v} Osimertinib
Everolimus {u} (Compound) resembles {v} (Compound) Sirolimus
Sirolimus {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Lidocaine
Lidocaine {u} may cause a minor interaction that can limit clinical effects when taken with {v} Osimertinib
Everolimus {u} (Compound) downregulates {v} (Gene) PSMB5
PSMB5 {u} (Gene) is bound by {v} (Compound) Bortezomib
Bortezomib {u} may cause a minor interaction that can limit clinical effects when taken with {v} Osimertinib
Everolimus {u} (Compound) resembles {v} (Compound) Sirolimus
Sirolimus {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Ivacaftor
Ivacaftor {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Osimertinib
Everolimus {u} (Compound) upregulates {v} (Gene) HMOX1
HMOX1 {u} (Gene) is upregulated by {v} (Compound) Bortezomib
Bortezomib {u} may cause a minor interaction that can limit clinical effects when taken with {v} Osimertinib
Everolimus {u} (Compound) resembles {v} (Compound) Sirolimus
Sirolimus {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Vinorelbine
Vinorelbine {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Osimertinib
Everolimus {u} (Compound) upregulates {v} (Gene) HMOX1
HMOX1 {u} (Gene) is upregulated by {v} (Compound) Formoterol
Formoterol {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Osimertinib
Everolimus {u} (Compound) binds {v} (Gene) CYP3A4
CYP3A4 {u} (Gene) is bound by {v} (Compound) Ivacaftor
Ivacaftor {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Osimertinib
Everolimus {u} (Compound) resembles {v} (Compound) Sirolimus
Sirolimus {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Tazemetostat
Tazemetostat {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Osimertinib
Everolimus (Compound) resembles Sirolimus (Compound) and Sirolimus may cause a moderate interaction that could exacerbate diseases when taken with Osimertinib
Everolimus (Compound) binds CYP3A4 (Gene) and CYP3A4 (Gene) is bound by Bortezomib (Compound) and Bortezomib may cause a minor interaction that can limit clinical effects when taken with Osimertinib
Everolimus (Compound) resembles Sirolimus (Compound) and Sirolimus may cause a moderate interaction that could exacerbate diseases when taken with Lidocaine and Lidocaine may cause a minor interaction that can limit clinical effects when taken with Osimertinib
Everolimus (Compound) downregulates PSMB5 (Gene) and PSMB5 (Gene) is bound by Bortezomib (Compound) and Bortezomib may cause a minor interaction that can limit clinical effects when taken with Osimertinib
Everolimus (Compound) resembles Sirolimus (Compound) and Sirolimus may cause a moderate interaction that could exacerbate diseases when taken with Ivacaftor and Ivacaftor may cause a moderate interaction that could exacerbate diseases when taken with Osimertinib
Everolimus (Compound) upregulates HMOX1 (Gene) and HMOX1 (Gene) is upregulated by Bortezomib (Compound) and Bortezomib may cause a minor interaction that can limit clinical effects when taken with Osimertinib
Everolimus (Compound) resembles Sirolimus (Compound) and Sirolimus may cause a moderate interaction that could exacerbate diseases when taken with Vinorelbine and Vinorelbine may cause a moderate interaction that could exacerbate diseases when taken with Osimertinib
Everolimus (Compound) upregulates HMOX1 (Gene) and HMOX1 (Gene) is upregulated by Formoterol (Compound) and Formoterol may cause a moderate interaction that could exacerbate diseases when taken with Osimertinib
Everolimus (Compound) binds CYP3A4 (Gene) and CYP3A4 (Gene) is bound by Ivacaftor (Compound) and Ivacaftor may cause a moderate interaction that could exacerbate diseases when taken with Osimertinib
Everolimus (Compound) resembles Sirolimus (Compound) and Sirolimus may cause a moderate interaction that could exacerbate diseases when taken with Tazemetostat and Tazemetostat may cause a moderate interaction that could exacerbate diseases when taken with Osimertinib