DDInter1628 DDInter107
Ruxolitinib, formerly known as INCB018424 or INC424, is an anticancer drug and a Janus kinase (JAK) inhibitor. It is a potent and selective inhibitor of JAK1 and JAK2, which are tyrosine kinases involved in cytokine signalling and hematopoiesis. Myeloproliferative neoplasms, such as myelofibrosis and polycythemia vera, are often characterized by aberrant activation of the JAK-STAT pathway, leading to abnormal blood cell counts and thrombotic complications. By inhibiting JAK1 and JAK2, ruxolitinib works to block the dysregulated cell signalling pathways and prevents abnormal blood cell proliferation. Due to a large number of patients with myeloproliferative neoplasms who have JAK2 mutations, ruxolitinib was the first ATP-competitive inhibitor of JAK1 and JAK2 ever developed. Rux
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 .
Ruxolitinib {u} (Compound) treats {v} (Disease) hematologic cancer
hematologic cancer {u} (Disease) is treated by {v} (Compound) Nilotinib
Nilotinib {u} may lead to a major life threatening interaction when taken with {v} Apalutamide
Ruxolitinib {u} (Compound) binds {v} (Gene) PLK3
PLK3 {u} (Gene) is upregulated by {v} (Compound) Irinotecan
Irinotecan {u} may lead to a major life threatening interaction when taken with {v} Apalutamide
Ruxolitinib {u} (Compound) treats {v} (Disease) hematologic cancer
hematologic cancer {u} (Disease) is treated by {v} (Compound) Lenalidomide
Lenalidomide {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Apalutamide
Ruxolitinib {u} (Compound) binds {v} (Gene) BMP2K
BMP2K {u} (Gene) is bound by {v} (Compound) Sunitinib
Sunitinib {u} may lead to a major life threatening interaction when taken with {v} Apalutamide
Ruxolitinib {u} (Compound) binds {v} (Gene) PLK3
PLK3 {u} (Gene) is upregulated by {v} (Compound) Teniposide
Teniposide {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Apalutamide
Ruxolitinib {u} (Compound) binds {v} (Gene) MKNK2
MKNK2 {u} (Gene) is bound by {v} (Compound) Sorafenib
Sorafenib {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Apalutamide
Ruxolitinib {u} (Compound) binds {v} (Gene) IRAK1
IRAK1 {u} (Gene) is downregulated by {v} (Compound) Digoxin
Digoxin {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Apalutamide
Ruxolitinib {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
Ruxolitinib {u} (Compound) binds {v} (Gene) ROCK1
ROCK1 {u} (Gene) is downregulated by {v} (Compound) Irinotecan
Irinotecan {u} may lead to a major life threatening interaction when taken with {v} Apalutamide
Ruxolitinib {u} (Compound) upregulates {v} (Gene) FOXJ3
FOXJ3 {u} (Gene) is upregulated by {v} (Compound) Digoxin
Digoxin {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Apalutamide
Ruxolitinib (Compound) treats hematologic cancer (Disease) and hematologic cancer (Disease) is treated by Nilotinib (Compound) and Nilotinib may lead to a major life threatening interaction when taken with Apalutamide
Ruxolitinib (Compound) binds PLK3 (Gene) and PLK3 (Gene) is upregulated by Irinotecan (Compound) and Irinotecan may lead to a major life threatening interaction when taken with Apalutamide
Ruxolitinib (Compound) treats hematologic cancer (Disease) and hematologic cancer (Disease) is treated by Lenalidomide (Compound) and Lenalidomide may cause a moderate interaction that could exacerbate diseases when taken with Apalutamide
Ruxolitinib (Compound) binds BMP2K (Gene) and BMP2K (Gene) is bound by Sunitinib (Compound) and Sunitinib may lead to a major life threatening interaction when taken with Apalutamide
Ruxolitinib (Compound) binds PLK3 (Gene) and PLK3 (Gene) is upregulated by Teniposide (Compound) and Teniposide may cause a moderate interaction that could exacerbate diseases when taken with Apalutamide
Ruxolitinib (Compound) binds MKNK2 (Gene) and MKNK2 (Gene) is bound by Sorafenib (Compound) and Sorafenib may cause a moderate interaction that could exacerbate diseases when taken with Apalutamide
Ruxolitinib (Compound) binds IRAK1 (Gene) and IRAK1 (Gene) is downregulated by Digoxin (Compound) and Digoxin may cause a moderate interaction that could exacerbate diseases when taken with Apalutamide
Ruxolitinib (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
Ruxolitinib (Compound) binds ROCK1 (Gene) and ROCK1 (Gene) is downregulated by Irinotecan (Compound) and Irinotecan may lead to a major life threatening interaction when taken with Apalutamide
Ruxolitinib (Compound) upregulates FOXJ3 (Gene) and FOXJ3 (Gene) is upregulated by Digoxin (Compound) and Digoxin may cause a moderate interaction that could exacerbate diseases when taken with Apalutamide