DDInter704 DDInter107
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.
Apalutamide is a potent androgen receptor (AR) antagonist that selectively binds to the ligand-binding domain of AR and blocks AR nuclear translocation or binding to androgen response elements . It has been used in trials studying the treatment of Prostate Cancer, Hepatic Impairment, Prostatic Neoplasms, Castration-Resistant Prostate Cancer, and Prostatic Neoplasms, Castration-Resistant, among others. Exerting an antitumor action, apalutamide blocking the effect of androgens that promote tumor growth. It targets the AR ligand-binding domain and prevents AR nuclear translocation, DNA binding, and transcription of AR gene targets in prostate tumors . In mice bearing human CRPC xenograft models, apalutamide treatment produced tumor regressions in a dose-dependent manner that was more effective than that of or . Unlike bicalutamide, apalutamide antagonized AR-mediated signaling in AR overexpressing human CRPC cell lines . Androgen-deprivation therapy, or hormone therapy, can be used as part of maintenance therapy for patients with non-metastatic prostate cancer. Although most patients achieve therapeutic responses at the initial hormone therapy, many patients progress to non-metastatic castration-resistant (resistance to hormone therapy) prostate cancer which is the second-most common cause of cancer-related deaths in American males . Castration-resistant prostate cancer is often incurable, which poses significant clinical challenges for patients. Approximately 10 to 20 % of prostate cancer cases are castration-resistant, and up to 16% of these patients show no evidence of cancer metastasis at the time of castration-resistant diagnosis . Higher prostate-specific antigen (PSA) and shorter PSA doubling time (PSA DT) are associated with a higher risk for metastases and death . In a phase-2 multicenter open-label study, 89% of patients with non-metastatic, castration-resistant prostate cancer had ≥50% PSA decline at week 12 of apalutamide treatment . In a randomized trial, the median metastasis-free survival for patients taking apalutamide was 40.5 months compared to 16.2 months for patients taking a placebo . Apalutamide displayed good tolerability and safety profile in clinical studies. Apalutamide was approved in February 2018 by the FDA as Erleada for the treatment of patients with non-metastatic prostate cancer that is resistant to treatment with hormone therapy (castration-resistant). It is available as oral tablets. Apalutamide is the first FDA-approved treatment for non-metastatic, castration-resistant prostate cancer .
Everolimus {u} (Compound) resembles {v} (Compound) Sirolimus
Sirolimus {u} may lead to a major life threatening interaction when taken with {v} Apalutamide
Everolimus {u} (Compound) binds {v} (Gene) CYP3A4
CYP3A4 {u} (Gene) is bound by {v} (Compound) Eplerenone
Eplerenone {u} may cause a minor interaction that can limit clinical effects when taken with {v} Apalutamide
Everolimus {u} (Compound) resembles {v} (Compound) Sirolimus
Sirolimus {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Eplerenone
Eplerenone {u} may cause a minor interaction that can limit clinical effects when taken with {v} Apalutamide
Everolimus {u} (Compound) downregulates {v} (Gene) TOPBP1
TOPBP1 {u} (Gene) is downregulated by {v} (Compound) Eplerenone
Eplerenone {u} may cause a minor interaction that can limit clinical effects when taken with {v} Apalutamide
Everolimus {u} (Compound) causes {v} (Side Effect) Upper respiratory tract infection
Upper respiratory tract infection {u} (Side Effect) is caused by {v} (Compound) Eplerenone
Eplerenone {u} may cause a minor interaction that can limit clinical effects when taken with {v} Apalutamide
Everolimus {u} (Compound) downregulates {v} (Gene) TOPBP1
TOPBP1 {u} (Gene) is downregulated by {v} (Compound) Trametinib
Trametinib {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Apalutamide
Everolimus {u} (Compound) resembles {v} (Compound) Sirolimus
Sirolimus {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Alfentanil
Alfentanil {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Apalutamide
Everolimus {u} (Compound) resembles {v} (Compound) Sirolimus
Sirolimus {u} may lead to a major life threatening interaction when taken with {v} Fluconazole
Fluconazole {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Apalutamide
Everolimus {u} (Compound) causes {v} (Side Effect) Gastrooesophageal reflux disease
Gastrooesophageal reflux disease {u} (Side Effect) is caused by {v} (Compound) Clomipramine
Clomipramine {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Apalutamide
Everolimus {u} (Compound) binds {v} (Gene) CYP3A4
CYP3A4 {u} (Gene) is bound by {v} (Compound) Alfentanil
Alfentanil {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Apalutamide
Everolimus (Compound) resembles Sirolimus (Compound) and Sirolimus may lead to a major life threatening interaction when taken with Apalutamide
Everolimus (Compound) binds CYP3A4 (Gene) and CYP3A4 (Gene) is bound by Eplerenone (Compound) and Eplerenone may cause a minor interaction that can limit clinical effects when taken with Apalutamide
Everolimus (Compound) resembles Sirolimus (Compound) and Sirolimus may cause a moderate interaction that could exacerbate diseases when taken with Eplerenone and Eplerenone may cause a minor interaction that can limit clinical effects when taken with Apalutamide
Everolimus (Compound) downregulates TOPBP1 (Gene) and TOPBP1 (Gene) is downregulated by Eplerenone (Compound) and Eplerenone may cause a minor interaction that can limit clinical effects when taken with Apalutamide
Everolimus (Compound) causes Upper respiratory tract infection (Side Effect) and Upper respiratory tract infection (Side Effect) is caused by Eplerenone (Compound) and Eplerenone may cause a minor interaction that can limit clinical effects when taken with Apalutamide
Everolimus (Compound) downregulates TOPBP1 (Gene) and TOPBP1 (Gene) is downregulated by Trametinib (Compound) and Trametinib may cause a moderate interaction that could exacerbate diseases when taken with Apalutamide
Everolimus (Compound) resembles Sirolimus (Compound) and Sirolimus may cause a moderate interaction that could exacerbate diseases when taken with Alfentanil and Alfentanil may cause a moderate interaction that could exacerbate diseases when taken with Apalutamide
Everolimus (Compound) resembles Sirolimus (Compound) and Sirolimus may lead to a major life threatening interaction when taken with Fluconazole and Fluconazole may cause a moderate interaction that could exacerbate diseases when taken with Apalutamide
Everolimus (Compound) causes Gastrooesophageal reflux disease (Side Effect) and Gastrooesophageal reflux disease (Side Effect) is caused by Clomipramine (Compound) and Clomipramine may cause a moderate interaction that could exacerbate diseases when taken with Apalutamide
Everolimus (Compound) binds CYP3A4 (Gene) and CYP3A4 (Gene) is bound by Alfentanil (Compound) and Alfentanil may cause a moderate interaction that could exacerbate diseases when taken with Apalutamide